June 2016 Juan C. Jaen, Ph. D. 650.483.6008 (cell) [email protected][email protected]PROFESSIONAL HISTORY May 2015 – Present: Co-Founder and President Chief Scientific Officer Arcus Biosciences, Inc. 3928 Point Eden Way Hayward, CA 94545 Oct. 2013 – April 2015: Co-Founder and President Head of R&D Flexus Biosciences, Inc. (Acquired by BMS for $1.25B, including $800M upfront payment) San Carlos, CA 94070 Jan. 2007 – Sept. 2013: Chief Scientific Officer & Senior Vice President of Drug Discovery ChemoCentryx, Inc. Mountain View, CA 94043 Aug. 2004 – Dec. 2006: Vice President of Chemistry Amgen Inc. South San Francisco, CA 94080 Sept. 1996 – Aug. 2004: Vice President of Chemistry (June 2000 – Aug. 2004) Director of Chemistry (Sept. 1996 – June 2000) Tularik Inc. (Acquired by Amgen in Aug 2004) South San Francisco, CA 94080 Dec. 1983 - Aug. 1996: Director, Neurodegenerative Diseases (last position held) Other positions held: Scientist, Sr. Scientist; Research Fellow Warner-Lambert/Parke-Davis (later acquired by Pfizer) Ann Arbor, MI 48105
May 2015 – Present: Co-Founder and President Chief Scientific Officer Arcus Biosciences, Inc. 3928 Point Eden Way Hayward, CA 94545 Oct. 2013 – April 2015: Co-Founder and President Head of R&D
Flexus Biosciences, Inc. (Acquired by BMS for $1.25B, including $800M upfront payment)
San Carlos, CA 94070 Jan. 2007 – Sept. 2013: Chief Scientific Officer & Senior Vice President of Drug Discovery ChemoCentryx, Inc. Mountain View, CA 94043
Aug. 2004 – Dec. 2006: Vice President of Chemistry Amgen Inc. South San Francisco, CA 94080 Sept. 1996 – Aug. 2004: Vice President of Chemistry (June 2000 – Aug. 2004) Director of Chemistry (Sept. 1996 – June 2000) Tularik Inc. (Acquired by Amgen in Aug 2004) South San Francisco, CA 94080
Dec. 1983 - Aug. 1996: Director, Neurodegenerative Diseases (last position held) Other positions held: Scientist, Sr. Scientist; Research Fellow Warner-Lambert/Parke-Davis (later acquired by Pfizer) Ann Arbor, MI 48105
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SIGNIFICANT ACCOMPLISHMENTS IN DRUG DISCOVERY
At Flexus Biosciences, I oversaw the discovery and/or development of several clinical candidates:
FLX287 (BMS-986205) (Solid & Hematological Tumors) Selective inhibitor of IDO1. Acquired by BMS in April 2015 in connection with the acquisition of Flexus Biosciences. Phase 1 trial (combination with nivolumab) initiated February 2016.
FLX925 (Acute Myeloid Leukemia)
Selective inhibitor of FLT3 (including clinically relevant primary and secondary mutations) and CDK4/6. Phase 1 trial in relapsed/refractory AML ongoing.
At ChemoCentryx, I oversaw the discovery and preclinical development of several first-in-class
clinical candidates:
Vercirnon (Traficet-EN®; CCX282; Immunology) Antagonist of the CCR9 chemokine receptor. Blocks T cell
recruitment to the inflamed intestine. Completed Phase 2 studies in Crohn’s disease and celiac disease in 2009. Licensed to GSK in 2010 (GSK1605786). Currently in Phase 3 for Crohn’s disease.
CCX168 (Immunology) Antagonist of the C5aR receptor. Blocks neutrophil recruitment to sites of inflammation, particularly in vasculitis & nephritis. Clinical evaluation initiated in late 2009. Phase 2 (ANCA renal vasculitis) ongoing. Orphan drug designation in aHUS and AARV in 2014.
CCX140 (Immunology) Antagonist of the CCR2 chemokine receptor. Blocks monocyte recruitment to sites of inflammation. Clinical evaluation initiated in 2008. Demonstrated efficacy in Phase 2 study (Type 2 diabetes) completed in 2010. Completed Phase 2 study in Diabetic Nephropathy.
CCX354 (Immunology) Antagonist of the CCR1 chemokine receptor. Blocks monocyte recruitment to sites of inflammation, particularly in Rheumatoid Arthritis. Clinical evaluation initiated in 2008. Demonstrated efficacy in Phase 2 study (Rheum. Arthritis). Licensed to GSK in 2011 (GSK2941266).
CCX025 (Immunology) 2nd-Generation antagonist of the CCR9 chemokine receptor. Blocks T cell recruitment to the inflamed intestine. Clinical evaluation initiated in 2008. Phase 1 completed in 2009. Licensed to GSK in 2010 (GSK2390533).
CCX721 (Immunology) 2nd-Generation antagonist of the CCR1 chemokine receptor. Blocks monocyte recruitment to sites of inflammation,
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particularly in Rheumatoid Arthritis. Licensed to GSK in 2011 (GSK2941609) at preclinical development stage.
CCX832 (Immunology) Antagonist of the ChemR23 receptor. Blocks recruitment of plasmacytoid dendritic cells to inflamed skin, such as in psoriasis. Phase 1 completed in 2011.
CCX872 (Immunology) 2nd-Generation CCR2 antagonist. Blocks monocyte recruitment during renal inflammation. Phase 2 ongoing against pancreatic cancer.
CCX507 (Immunology) 3rd-Generation antagonist of the CCR9 chemokine receptor. Blocks T cell recruitment to the inflamed intestine. Phase 1 completed in 2014.
At Tularik/Amgen, I directed drug design efforts and played a leading role in the discovery of several drug candidates that were first in their class to reach clinical evaluation:
T067 (Oncology) Clinical evaluation initiated in 1998; Inhibitor of microtubule polymerization, inducing apoptosis in drug-resistant cancer cells. Advanced to Phase 3 for hepatocellular carcinoma.
T607 (Oncology) Clinical evaluation initiated in 2000; Similar mechanism of action as T067, but designed to minimize entry into the CNS. Completed Phase 2 evaluation against several tumor types.
T611 (Antiviral) Clinical evaluation initiated in 2001; First inhibitor of human cytomegalovirus (CMV) DNA primase (UL70), a key enzyme involved in viral replication. Completed Phase 2.
T487 (Immunology) Clinical evaluation initiated in 2002; First antagonist of the CXCR3 receptor, a GPCR involved in the recruitment of T-cells to sites of inflammation. Completed Phase 2 (psoriasis).
T131 (Diabetes) Clinical evaluation initiated in 2002; Selective modulator of PPAR, a nuclear receptor that regulates genes involved in controlling glucose homeostasis. Large Phase 2 study successfully completed by licensee Intekrim Ltd.
T071 (Obesity) Clinical evaluation initiated in 2003. First antagonist of MCHR1, a GPCR involved in the control of appetite and energy homeostasis. Potential role in the treatment of anxiety. Phase 1 completed.
T009 (Asthma) Clinical evaluation initiated in 2003. First dual antagonist of both PGD2 receptors (involved in lung inflammation and airway constriction). Phase 1 completed.
AMG837 (Diabetes) Clinical evaluation initiated in 2006. First clinical-stage agonist of the long-chain fatty acid receptor GPR40.
At Parke-Davis/Warner-Lambert, I was directly responsible or led the efforts that resulted in the discovery of several CNS drug candidates in the early 1990s:
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CI-985 (Schizophrenia) Dopamine autoreceptor agonist controls dopamine levels in limbic areas of the brain. Improved efficacy over traditional antipsychotics without the extrapyramidal side effects.
CI-1007 (Schizophrenia) Second-generation dopamine autoreceptor agonist for the treatment of schizophrenia.
CI-1002 (Alzheimer’s) CNS-selective, reversible acetylcholinesterase inhibitor; Improves cognitive deficits, with better safety profile than earlier broad-scope cholinergic agents.
CI-1017 (Alzheimer’s) Selective muscarinic (m1) agonist. Improves cognitive deficits without the side-effects (e.g., seizures, cardiac, intestinal) of broad-scope cholinergic agents.
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EDUCATION
Ph.D. in Organic Chemistry University of Michigan, Ann Arbor, Michigan (1984) Research Advisor: Prof. Joseph P. Marino M.S. in Organic Chemistry University of Michigan, Ann Arbor, Michigan (1981) M.S. (equivalent) in Organic Chemistry Universidad Complutense, Madrid, Spain (1980)
B.S. (equivalent) in Organic Chemistry Universidad Complutense, Madrid, Spain (1979)
PROFESSIONAL ACTIVITIES
April 2016 – Present: Board of Directors LakePharma, Inc.; Belmont, CA
July 2015 – Present: Member of Scientific Advisory Board Cleave Biosciences; Burlingame, CA June 2015 – Present: Visiting Scholar; Institute of Chemical Biology (ChEM-H) Stanford University, Stanford, CA 2012 – 2013: Member of Scientific Advisory Board Nurix; San Francisco, CA
PHILANTHROPY
2015 – Present: Founder/Treasurer; Bella Charitable Foundation; Burlingame, CA Helping students from disadvantaged backgrounds obtain a college education
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PEER-REVIEWED PUBLICATIONS & BOOK CHAPTERS
1. Characterization of pharmacologic and pharmacokinetic properties of CCX168, a potent and selective orally administered complement 5a receptor inhibitor. Bekker P, Dairaghi D, Seitz L, Leleti M, Wang Y, Ertl L, Baumgart T, Shugarts S, Lohr L, Dang T, Miao S, Zeng Y, Fan P, Zhang P, Johnson D, Powers J, Jaen J, Charo I, Schall T. PLoS ONE 2016 (under review).
2. CCL2/CCR2 regulates the tumor microenvironment in HER-2/neu-driven mammary carcinomas in mice. Chen X, Wang Y, Nelson D, Tian S, Mulvey E, Conti I, Jaen J, Rollins BJ; PLoS ONE 2016 (under review).
3. Tissue proteases convert CCL23 into potent monocyte chemoattractants in chronic rhinosinusitis. Poposki JA, Keswani A, Kim JK, Klingler AI, Suh LA, Norton J, Carter RG, Peters AT, Hulse KE, Grammer LC, Tan BK, Conley DB, Jaen JC, Schall TJ, Kern RC, Kato A. J. Allergy & Clin. Immunol. 2016, 137(4):1274-1277.
4. Discovery of potent, selective, and orally bioavailable inhibitors of interleukin-1 receptor-
associate kinase-4. Wang Z, Sun D, Johnstone S, Cao Z, Gao X, Jaen JC, Liu J, Lively S, Miao S, Sudom A, Tomooka C, Walker NP, Wright M, Yan X, Ye Q, Powers JP. BioOrg. Med. Chem. 2015, 25(23): 5546-50.
5. CCR9 Antagonists in the treatment of ulcerative colitis. Bekker PJ, Ebsworth K, Walters MJ,
6. Abrogation of CC chemokine receptor 9 ameliorates collagen-induced arthritis of mice. Yokoyama W, Kohsaka H, Kaneko K, Walters M, Takayasu A, Fukuda S, Miyabe C, Miyabe Y, Love PE, Nakamoto N, Kanai T, Watanabe-Imai K, Charvat TT, Penfold ME, Jaen J, Schall TJ, Harigai M, Miyasaka N, Nanki T; Arthritis Res. Ther. 2014, 16(5): 445.
7. Inhibition of CXCR7 extends survival following irradiation of brain tumors in mice and rats. Walters MJ, Ebsworth K, Berahovich RD, Liu S-H, Al-Omran R, Kioi M, Chernikova S, Tseng D, Zhang P, Powers JP, Jaen JC, Schall TJ, Merchant M, Recht L, Brown MJM; British J. Cancer 2014, 110(5): 1179-1188.
8. Endothelial expression of CXCR7 and the regulation of systemic CXCL12 levels. Berahovich RD, Zabel BA, Lewén S, Walters MJ, Ebsworth K, Wang Y, Jaen JC, Schall TJ; Immunology 2014, 141(1): 111-122.
9. C5a receptor (CD88) blockade protects against MPO-ANCA glomerulonephritis. Xiao H, Dairaghi DJ, Powers JP, Ertl L, Baumgart T, Wang Y, Seitz LC, Penfold ME, Gao L, Hu P, Lu B, Gerard NP, Gerard C, Schall TJ, Jaen JC, Falk RJ, Jennette JC; J. Am. Soc. Nephrol. 2014 25(2): 225-231.
10. Differences in CXCR7 protein expression on rat versus mouse and human splenic marginal zone
B cells. Berahovich RD, Penfold MET, Walter M, Miao Z, Jaen JC, Schall TJ; Immunol. Lett. 2013, 154(1-2): 77-79.
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11. CCR2 antagonist CCX140-B provides renal and glycemic benefits in diabetic transgenic human
CCR2 knockin mice. Sullivan T, Miao Z, Dairaghi DJ, Krasinski A, Wang Y, Zhao BN, Baumgart T, Ertl LS, Pennell A, Seitz L, Powers J, Zhao R, Ungashe S, Wei Z, Boring L, Tsou CL, Charo I, Berahovich RD, Schall TJ, Jaen JC. Am. J. Pathol.- Renal Pathol. 2013, 305(9), F1288-1297.
12. Recent advances in the discovery and development of CCR1 antagonists. Zhang P, Dairaghi D,
13. Evaluation of AMG 076, a potent and selective MCHR1 antagonist, in rodent and primate obesity models. Motani AS, Luo J, Liang L, Mihalic JT, Chen X, Li L, Tang L, Jaen JC, Chen JL, Dai K; Pharmacol. Res. Perspect. 2013, 1(1): e00003.
14. Experimental evidence for the use of CCR2 antagonists in the treatment of Type 2 diabetes. Sullivan TJ, Dairaghi DJ, Krasinski A, Miao Z, Zhao BN, Berahovich RD, Wang Y, Baumgart T, Ertl LS, Powers JP, Seitz LC, Schall TJ, Jaen JC; Metabolism 2013, 62(11), 1623-1632.
15. CCR9 inhibition does not interfere with the development of immune tolerance to oral antigens.
16. Discovery of INT131: a selective PPARy modulator that enhances insulin selectivity. Taygerly JP, McGee LR, Rubenstein SM, Houze JB, Cushing TD, Motani A, Li Y, Chen JL, Frankmoelle W, Ye G, Learned MR, Jaen J, Miao S, Timmermans PB, Thoolen M, Kearney P, Flygare J, Beckmann H, Weiszmann J, Lindstrom M, Walker N, Liu J, Biennann D, Wang Z, Hagiwara A, lida T, Aramaki H, Kilao Y, Shinkai H, Furukawa N, Nishiu J, Nakamura M; BioOrg. Med. Chem. 2013, 21(4), 979-992.
17. CCR1 antagonist CCX354-C treatment for rheumatoid arthritis. Tak PP, Balanescu A, Tseluyko, Bojin S, Drescher E, Dairaghi D, Miao S, Marchesin V, Jaen J, Schall TJ, Bekker P; Ann. Rheum. Dis., 2013; 72(3), 337-344.
18. Orally-Administered Chemokine Receptor CCR2 Antagonist CCX140-B in Type 2 Diabetes: A
Pilot Double-Blind, Randomized Clinical Trial. Hanefeld M, Schell E, Gouni-Berthold J, Melichar M, Vesela I, Johnson D, Miao S, Sullivan TJ, Jaen JC, Schall TJ, Bekker P; J. Diabetes Metab. 2012, 3(9), 1000225:1-8.
19. Diabetes and associated co-morbidities as an inflammatory syndrome. Jaen JC, Powers JP,
Sullivan TJ; Ann. Reports Med. Chem. 2012, 47, 159-175.
20. Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors. Jiao XY, Kopecky DJ, Liu JS, Liu JQ, Jaen JC, Cardozo MG, Sharma R, Walker N, Wesche H, Li S, Farrelly E, Xiao SH, Wang Z, Kayser F; BioOrg. Med. Chem. Letters, 2012, 22(19), 6212-6217.
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21. CCR1 Blockade reduces tumor burden and osteolysis in vivo in a mouse model of myeloma bone disease. Dairaghi DJ, Oyajobi B, Gupta A, McCluskey B, Miao S, Powers JP, Seitz LC, Wang Y, Zeng Y, Zhang P, Schall TJ, Jaen JC; Blood, 2012, 120(7), 1449-1457.
22. Discovery and optimization of a series of liver X receptor antagonists. Jiao XY, Kopecky DJ, Fisher B, Piper DE, Labelle M, McKendry S, Harrison M, Jones S, Jaen J, Shiau AK, Escaron P, Danao J, Chai A, Coward P, Kayser F; BioOrg. Med. Chem. Letters, 2012, 22(18), 5966-5970.
23. Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with
reduced hERG inhibition. Mihalic JT, Fan P, Chen X, Chen X, Fu Y, Motani A, Liang L, Lindstrom M, Tang L, Chen JL, Jaen J, Dai K, Li L; BioOrg. Med. Chem. Letters, 2012, 22(18), 3781-3785.
24. Discovery and optimization of benzenesulfonanilide derivatives as a novel class of 11β-HSD1
inhibitors. Rew Y, DeGraffenreid M, He X, Jaen JC, McMinn DL, Sun D, Tu H, Ursu S, Powers, Jay P; BioOrg. Med. Chem. Letters, 2012, 22(11), 3786-3790.
25. Discovery of a new binding mode for a series of liver X receptor agonists. Kopecky DJ, Jiao
XY, Fisher B, McKendry S, Labelle M, Piper DE, Coward P, Shiau AK, Escaron P, Danao J, Chai A, Jaen J, Kayser F; BioOrg. Med. Chem. Letters, 2012, 22(7), 2407-2410.
26. Characterization of CCX140-B, an orally bioavailable antagonist of the CCR2 chemokine
receptor, for the treatment of type 2 diabetes and associated co-morbidities. Sullivan TJ, Dairaghi DJ, Krasinski A, Miao Z, Wang Y, Zhao BN, Baumgart T, Berahovich R, Ertl LS, Pennell A, Seitz L, Ungashe S, Wei Z, Boring L, Tsou C, Charo IF, Bekker P, Schall TJ, Jaen JC; J. Pharmacol. Exp. Therap. 2012. DOI:10.1124/jpet.111.190918. [Epub ahead of print, 29 Feb 2012].
27. Discovery and characterization of a potent and selective antagonist of melanin-concentrating
hormone receptor 2. Chen X, Mihalic J, Fan P, Liang L, Lindstrom M, Wong S, Ye Q, Fu Y, Jaen J, Chen, J-L, Dai K, Li L; BioOrg. Med. Chem. Letters, 2012, 22(1), 363-366.
28. Discovery of a novel series of melanin-concentrating hormone receptor 1 antagonists for the
treatment of obesity. Mihalic JT, Chen X, Fan P, Chen X, Fu Y, Liang L, Reed M, Tang L, Chen JL, Jaen JC, Li L, Dai K; BioOrg. Med. Chem. Letters, 2011, 21(23), 7001-7005.
29. Advances in the discovery of C5a receptor antagonists. Powers JP, Dairaghi DJ, Jaen JC; Ann.
Reports Med. Chem. 2011, 46, 171-186.
30. The novel chemokine receptor CXCR7 regulates transendothelial migration of cancer cells. Zabel BA, Lewén S, Berahovich R, Jaen JC, Schall TJ; Mol. Cancer 2011, 10, 73.
31. Pharmacokinetic and pharmacodynamic evaluation of the novel CCR1 antagonist CCX354-C in
healthy human subjects: Implications for Phase 2 dose selection. Dairaghi D, Ertl L, Johnson D, Pennell AM, Powers JP, Miao S, Seitz L, Wang Y, Zeng Y, Zhang P, Bekker P, Schall TJ, Jaen JC; Clin. Pharmacol. Ther. 2011, 89(5), 726-734.
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32. A novel series of IKKβ inhibitors. Part II: Description of a potent and pharmacologically active
series of analogs. Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Browner MF, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Labadie SS, Labelle M, Lehel C, Lu P-P, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith M-L, Talamas FX, Tonn G, Walker KM, Walker NPC, Wesche H, Whitehead C, Wright M, Jaen JC; BioOrg. Med. Chem. Letters, 2011, 21(1), 423-426.
33. A novel series of IKKβ inhibitors. Part I: Initial SAR studies of a HTS hit. Cushing TD,
Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Jaen JC, Labadie SS, Labelle M, Lehel C, Lu P-P, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith M-L, Talamas FX, Tonn G, Walker KM, Walker NPC, Wesche H, Whitehead C, Wright M, Browner MF; BioOrg. Med. Chem. Letters, 2011, 21(1), 417-422.
34. Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent
11β-HSD1 inhibitors. Sun D; Wang Z; Caille S; DeGraffenreid M; Gonzalez-Lopez de Turiso F; Hungate R; Jaen JC; Jiang B; Julian LD; Kelly R; McMinn DL; Kaizerman J; Rew Y; Sudom A; Tu H; Ursu S; Walker N; Willcockson M; Yan X; Ye Q; Powers JP; BioOrg. Med. Chem. Letters, 2011, 21(1), 405-410.
35. The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors. Yan X, Wang Z, Sudom A,
Cardozo M, DeGraffenreid M, Di Y, Fan P, He X, Jaen JC, Labelle M, Liu J, Ma J, McMinn D, Miao S, Sun D, Tang L, Tu H, Ursu S, Walker N, Ye Q, Powers JP; BioOrg. Med. Chem. Letters, 2010, 20(23), 7071-7075.
36. CXCR7 protein is not expressed on mouse and human leukocytes. Berahovich RD, Zabel BA,
Penfold MET, Lewen S, Wang Y, Miao Z, Gan L, Pereda J, Dias J, Slukvin II, McGrath KE, Jaen JC, Schall TJ; J. Immunology, 2010, 185(9), 5130-5139.
37. CXCR7 protein expression correlates with elevated MMP-3 secretion in breast cancer cells.
Zabel BA, Miao Z, Lai NL, Wang Y, Lewen S, Berahovich RD, Jaen JC, Schall TS; Oncology Lett., 2010, 1(5), 845-847.
38. Characterization of CCX282-B, an orally bioavailable antagonist of the CCR9 chemokine
receptor and a potential treatment for inflammatory bowel disease. Walters M, Baumgart T, Bekker P, Ertl L, Jaen JC, Keshav S, Kollias G, Pennell A, Ungashe S, Wei Z, Wright K, Schall TJ; J. Pharmacol. Exp. Therap., 2010, 335(1), 61-69.
39. Elucidation of CXCR7-mediated signaling events and inhibition of CXCR4-mediated tumor cell
transendothelial migration by CXCR7 ligands. Zabel BA, Wang Y, Lewen S, Berahovich RD, Penfold MET, Zhang P, Powers J, Summers BC, Miao Z, Zhao B, Jalili A, Janowska-Wieczorek A, Jaen JC, Schall TJ; J. Immunology, 2009, 183(5), 3204-3211.
40. INT131: A selective modulator of PPARγ. Motani A, Wang Z, Weiszmann J, McGee LR, Lee
G, Liu Q, Staunton J, Fang Z, Fuentes H, Lindstrom M, Liu J, Biermann DHT, Jaen J, Walker N, Learned RM, Chen J-L, Li Y; J. Mol. Biol., 2009, 386(5, 1301-1311.
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41. Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11β-HSD1
inhibitors. Rew Y, McMinn DL, Wang Z, He X, Hungate RW, Jaen JC, Sudom A, Sun D, Tu H, Ursu S, Villemure E, Walker NP, Yan X, Ye Q, Powers JP; BioOrg. Med. Chem. Lett., 2009, 19(6), 1797-1801.
42. Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11β-
hydroxysteroid dehydrogenase type 1 (11β-HSD1). Sun D, Wang Z, Cardozo M, Choi R, DeGraffenreid M, Di Y, He X, Jaen JC, Labelle M, Liu J, Ma J, Miao S, Sudom A, Tang L, Tu H, Ursu S, Walker N, Yan X, Ye Q, Powers JP; BioOrg. Med. Chem. Lett., 2009, 19(5), 1522-1527.
43. Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11β-HSD1
inhibitors. McMinn DL, Rew Y, Sudom A, Caille S, DeGraffenreid M, He X, Hungate R, Jiang B, Jaen JC, Julian LD, Kaizerman J, Novak P, Sun D, Tu H, Ursu S, Walker NPC, Yan X, Ye Q, Wang Z, Powers JP; BioOrg. Med. Chem. Lett., 2009, 19(5), 1446-1450.
44. Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as
a novel class of ACK1 inhibitors. Kopecky DJ, Hao X, Chen Y, Fu J, Jiao XY, Jaen JC, Cardozo MG, Liu J, Wang Z, Walker NPC, Wesche H, Li S, Farrelly E, Xiao SH, Kayser F; BioOrg. Med. Chem. 2008, 18(24), 6352-6356.
45. Distinctive molecular inhibition mechanisms for selective inhibitors of human 11β-
hydroxysteroid dehydrogenase type 1. Tu H; Powers JP, Liu J, Ursu S, Sudom A, Yan X, Xu H, Meininger D, DeGraffenreid M, He X, Jaen JC, Sun D, Labelle M, Yamamoto H, Shan B, Walker NPC, Wang Z; BioOrg. Med. Chem. 2008, 16(19), 8922-8931.
46. Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11β-hydroxysteroid
dehydrogenase type 1 (11β-HSD1). Sun D, Wang Z, Di Y, Jaen JC, Labelle M, Ma J, Miao S, Sudom A, Tang L, Tomooka CS, Tu H, Ursu S, Walker N, Yan X, Ye Q, Powers JP; BioOrg. Med. Chem. Lett., 2008, 18(12), 3513-3516.
47. Discovery of novel, potent benzamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1
(11β-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model. Julian LD, Wang Z, Bostick T, Caille S, Choi R, DeGraffenreid M, Di Y, He X, Hungate RW, Jaen JC, Liu J, Monshouwer M, McMinn D, Rew Y, Sudom A, Sun D, Tu H, Ursu S, Walker N, Yan X, Ye Q, Powers JP; J. Med. Chem., 2008, 51(13), 3953-3960.
48. Discovery of potent LPA(2) (EDG4) antagonists as potential anticancer agents. Beck HP, Kohn
T, Rubenstein S, Hedberg C, Schwandner R, Hasslinger K, Dai K, Li C, Liang L, Wesche H, Frank B, An S, Wickramasinghe D, Jaen J, Medina J, Hungate R, Shen W; BioOrg. Med. Chem. Lett., 2008, 18(3), 1037-1041.
49. SAR studies on a novel series of human cytomegalovirus primase inhibitors. Chen X, Adrian J,
Cushing T, DiMaio H, Liang L, Mayorga V, Miao S, Peterson MG, Powers JP, Spector F, Sein C, Wright M, Xu D, Ye Q, Jaen J; BioOrg. Med. Chem. Lett., 2007, 17(8), 2188-2192.
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50. Discovery of a novel series of inhibitors of human cytomegalovirus primase. Cushing TD, Adrian J, Chen X, DiMaio H, Doughan B, Flygare J, Liang L, Mayorga V, Miao S, Mellon H, Peterson MG, Powers JP, Spector F, Stein C, Wright M, Xu D, Ye Q, Jaen JC; BioOrg. Med. Chem. Lett., 2006, 16(18), 4879-4883.
51. Discovery and initial SAR of inhibitors of Interleukin-1 Receptor-Associated Kinase-4 (IRAK-
4). Powers JP, Li S, Jaen JC, Liu J, Walker NPC, Wang Z, Wesche H; BioOrg. Med. Chem. Lett., 2006, 16(11), 2842-2845.
52. SAR and mode of action of novel non-nucleoside inhibitors of Hepatitis C NS5b RNA
polymerase. Powers JP, Piper DE, Li Y, Mayorga V, Anzola J, Chen JM, Jaen JC, Lee G, Liu J, Peterson MG, Tonn GR, Ye Q, Walker NPC, Wang Z; J. Med. Chem. 2006, 49(3), 1034-1046.
53. Hydrophylic, prodrug analogues of T138067 are efficacious in controlling tumor growth in vivo
and show a decreased ability to cross the blood-brain barrier. Rubenstein SM, Baichwal V, Beckmann H, Clark DL, Frankmoelle W, Roche D, Santha E, Schwender S, Thoolen M, Ye Q, Jaen JC; J. Med. Chem. 2001, 44(22), 3599-3605.
54. Monographs on (S)-1-Amino-2-hydroxymethylindoline; Brucine; (−)-(S,S)-α,α′-Dimethyl-dibenzylamine; (S)-(−)-α-Methoxy-α-(trifluoromethyl)phenylacetic Acid; (S)-α-Methyl-benzylamine; (+)-(S)-N-Methylsulfonylphenylalanyl Chloride; (S)-(+)-1-Phenyl-2-propylamine; and L-Tyrosine Hydrazide; Jaen JC. In Encyclopedia of Reagents for Organic Synthesis; Wiley&Sons: 2001.
55. CI-1017, a functionally M1-selective muscarinic agonist: design, synthesis and preclinical
pharmacology. Tecle H, Schwarz RD, Barrett SD, Callahan MJ, Caprathe BW, Davis RE, Doyle P, Emmerling M, Lauffer DJ, Mirzadegan T, Moreland DW, Lipinski W, Nelson C, Raby C, Spencer C, Spiegel K, Thomas AJ, Jaen JC; Pharm. Acta Helv. 2000, 74(2-3), 141-148.
56. Secreted Site-1 protease cleaves peptides corresponding to luminal loop of sterol regulatory
element-binding proteins. Cheng D, Espenshade PJ, Slaughter CA, Jaen JC, Brown MS, Goldstein JL; J. Biol. Chem. 1999, 274(32), 22805-22812.
57. Novel halogenated sulfonamides inhibit the growth of multidrug resistant MCF-7/ADR cancer
68. Acetylcholinesterase inhibition by fused dihydroquinazoline compounds. Jaen JC, Gregor VE, Lee C, Emmerling MR, Davis RE; BioOrg. Med. Chem. Lett. 1996, 6(6), 737-742.
69. Synthesis and biological evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease
inhibitors. Gilmore JL, Hays SJ, Caprathe BW, Lee C, Emmerling MR, Michael W, Jaen JC; BioOrg. Med. Chem. Lett. 1996, 6(6), 679-682.
70. Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling
implications and pharmacology. Pool WF, Woolf TF, Reily MD, Caprathe BW, Emmerling MR, Jaen JC; J. Med. Chem. 1996, 39(15), 3014-3018.
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71. Aryl 1-but-3-ynyl-4-phenyl-1,2,3,6-tetrahydropyridines as potential antipsychotic agents: Synthesis and Structure-Activity relationships. Glase SA, Akunne HC, Heffner TG, Jaen JC, Meltzer LT, Pugsley TA, Smith SJ, Wise LD; J. Med. Chem. 1996, 39(16), 3179-3187.
72. CI-1007, a dopamine partial agonist and potential antipsychotic agent. I. Neurochemical effects.
Pugsley TA, Davis MD, Akunne HC, Cooke LW, Whetzel SZ, MacKenzie RG, Shih YH, Van Leeuwen DH, Demattos SB, Georgic LM, Caprathe BW, Wright J, Jaen JC, Wise L, Heffner TG.; J. Pharmacol. Exp. Ther. 1995, 274(2), 898-911.
73. Mutations of aspartate 103 in the Hm2 receptor and alterations in receptor binding properties of
78. Kynurenic acid derivatives inhibit the binding of Nerve Growth Factor (NGF) to the low affinity p75 NGF receptor. Jaen JC, Laborde E, Bucsh RA, Caprathe BW, Sorenson RJ, Fergus J, Spiegel K, Dickerson MR, Davis RE; J. Med. Chem. 1995, 38(22), 4439-4445.
79. CI-1002, a combined acetylcholinesterase inhibitor and muscarinic antagonist. Emmerling MR,
Gregor VE, Callahan MJ, Schwarz RD, Scholten JD, Orr EL, Pugsley T, Moore CJ, Raby C, Myers SL, Davis RE, Jaen JC; CNS Drug Reviews 1995, 1, 27-49.
80. PD90780, a non-peptide inhibitor of Nerve Growth Factor’s binding to the p75 NGF receptor.
Spiegel K, Agrafiotis D, Caprathe B, Davis RE, Dickerson MR, Fergus JH, Hepburn TW, Marks JS, Van Dorf M, Wieland DM, Jaen JC; Biochem. Biophys. Res. Comm. 1995, 217, 488-494.
81. Recent advances in the design and characterization of muscarinic agonists and antagonists.
Jaen JC, Davis RE; Ann. Reports Med. Chem. 1994, 29, 23-32.
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82. The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents. Wright, JL, Caprathe BW, Downing DM, Glase SA, Heffner TG, Jaen JC, Johnson SJ, Kesten SR, Mackenzie RG, Meltzer LT, Pugsley TA, Smith SJ, Wise LD, Wustrow DJ; J. Med. Chem. 1994, 37(21), 3523-3533.
83. In vitro and in vivo effects of a dual inhibitor of acetylcholinesterase and muscarinic receptors,
CI-1002. Emmerling ME, Gregor VE, Schwarz RD, Scholten JD, Callahan MJ, Lee C, Moore CJ, Raby R, Lipinski WJ, Jaen JC, Davis RE. In Alzheimer Disease: Therapeutic Strategies, E. Giacobini and R. Becker, Eds. Birkhäuser Boston: 1994, 120-124.
Davis RE, Jaen JC, Lipinski W, Raby C, Spencer CJ, Tecle H. In Alzheimer Disease: Therapeutic Strategies, E. Giacobini and R. Becker, Eds. Birkhäuser Boston: 1994, 224-228.
85. Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-
amino-1-arylbutanols on dopamine and sigma receptors. Jaen JC, Caprathe BW, Pugsley TA, Wise LD, Akunne H; J. Med. Chem. 1993, 36(24), 3929-3936.
86. Characterization of muscarinic agonists in recombinant cell lines. Schwarz RD, Davis RE, Jaen
JC, Spencer CJ, Tecle H, Thomas AJ; Life Sci. 1993, 52(5-6), 465-472. 87. Assessment of mutagenic potential in a series of compounds structurally related to 2-amino-3-
93. Cholinergic agents in the treatment of Alzheimer’s Disease: Acetylcholinesterase inhibitors of current clinical interest. Jaen JC, Davis RE; Curr. Opin. Invest. Drugs 1993, 2, 363.
94. Chemical purity and mutagenicity: Case study of a drug in development. Kropko ML, Jaen JC,
Theiss JC, Wold S, Caprathe BW, Wise LD; Mutation Research 1992, 281(4), 233-238. 95. Cholinomimetics and Alzheimer's Disease. Jaen JC, Moos WH, Johnson G; Bio. Med. Chem.
Letters 1992, 2(8), 777-780. 96. (Book Chapter) Effects of PD 128483, a novel dopamine autoreceptor agonist, in preclinical
antipsychotic tests. Heffner TG, Caprathe B, Davis M, Jaen J, Meltzer L, Pugsley T, Wise L. In Novel Antipsychotic Drugs, H. Meltzer, ed., Raven Press: New York, 1992, 79-90.
97. Synthesis and dopaminergic activity of the enantiomers of 6-methyl-4,5,5a,6,7,8-
Wise LD, Heffner TG, Pugsley TA, Meltzer LT; J. Med. Chem. 1988, 31(8), 1621-1625.
105. Synthesis of the 1,2,3,4-tetrahydrobenzofuro[2,3-c]pyridine ring system. Jaen JC, Wise LD; J. Heterocyclic Chem. 1987, 24(5), 1317-1319.
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106. An efficient procedure for the mild oxidative cleavage of alkene-3-ols: Application to the preparation of 2-alkoxy-2-(3,4,5-trimethoxyphenyl)acetaldehyde. Marino JP, Jaen JC; Synth. Comm. 1983, 13(13), 1057-1066.
107. Syn-1,4-Addition of carboxylate salts to cyclic allylic epoxides mediated by cuprous chloride.
108. Stereospecific umpolung '-substitution of ketones via reactions of organocuprates with enol ethers of ,β-epoxycyclohexanones. Marino JP, Jaen JC; J. Am. Chem. Soc. 1982, 104(11), 3165-3172.
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PATENTS (Issued US Patents & PCT/US Publications for Pending US Applications) 1. 4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines and 4-(hexahydro-1-alkyl-3-pyridin-
yl)-2-thiazolamines having antipsychotic activity. Jaen JC, Wise LD, Tecle H, Bergmeier SC; US 4,650,805 (March 1987).
2. 4H-1-Benzopyran-4-ones and their sulfur containing analogs. Jaen JC, Wise LD; US 4,678,787
(July 1987). 3. Phenyl and heterocyclic tetrahydropyridylalkoxybenz-heterocyclic compounds as antipsychotic
agents. Caprathe BW, DeWald HA, Jaen JC, Wise LD; US 4,704,390 (November 1987). 4. 4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines and 4-(hexahydro-1-alkyl- 3-
pyridinyl)-2-thiazolamines having antipsychotic activity. Jaen JC, Wise LD, Tecle H, Bergmeier SC; US 4,739,067 (April 1988).
LD; US 4,762,843 (August 1988). 6. Phenyl and heterocyclic tetrahydropyridylalkoxybenz-heterocyclic compounds as antipsychotic
agents. Caprathe BW, DeWald HA, Jaen JC, Wise LD; US 4,803,203 (February 1989). 7. 4- or 5-(substituted piperazinyl)-2-aminothiazoles as antipsychotic agents. Caprathe BW, Jaen
JC, Wise LD; US 4,935,424 (June 1990). 8. Substituted cyclohexanols as Central Nervous System agents. Caprathe BW, Jaen JC, Smith SJ,
Wise LD; US 4,957,921 (September 1990). 9. Substituted cyclohexenes as Central Nervous System agents. Caprathe BW, Jaen JC, Smith SJ,
Wise LD; US 4,975,445 (December 1990). 10. Substituted tetrahydrobenzothiazoles as dopaminergic agents. Caprathe BW, Jaen JC, Wise
LD; US 4,988,699 (January 1991). 11. Substituted tetrahydropyridines as Central Nervous System agents. Jaen JC, Nickell D,
Reynolds D, Smith SJ, Wise LD, Wustrow D; US 5,045,550 (September 1991). 12. Substituted cyclohexanols as Central Nervous System agents. Caprathe BW, Jaen JC, Smith SJ,
Wise LD; US 5,047,406 (September 1991). 13. Substituted piperazines as Central Nervous System agents. Jaen JC, Nickell D, Reynolds D,
Smith SJ, Wise LD, Wustrow D; US 5,089,497 (February 1992). 14. Substituted tetrahydropyridines as Central Nervous System agents. Jaen JC, Nickell DG,
Reynolds DM, Smith SJ, Wise LD, Wustrow DJ; US 5,118,691 (June 1992).
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15. Substituted 1,2,3,6-tetrahydropyridines as Central Nervous System agents. Caprathe BW, Jaen JC, Wise LD; US 5,120,748 (June 1992).
16. Substituted tetrahydropyridines and their use as Central Nervous System agents. Jaen JC,
Nickell D, Reynolds D, Smith SJ, Wise LD, Wustrow D; US 5,187,280 (February 1993). 17. Substituted 1,2,3,6-tetrahydropyridines as Central Nervous System agents. Caprathe BW, Jaen
JC, Wise LD; US 5,198,443 (March 1993). 18. Substituted piperazines as Central Nervous System agents. Glase S, Jaen JC, Smith SJ, Wise
LD; US 5,270,312 (December 1993). 19. Substituted tetrahydropyridines and hydroxypiperidines as Central Nervous System agents.
Glase S, Jaen JC, Smith SJ, Wise LD; US 5,273,977 (December 1993). 20. 1,3-Substituted cyclohexenes and cycloalkanes as Central Nervous System agents. Caprathe
BW, Downing, DM, Jaen JC, Johnson SJ, Smith WJ, Wise LD, Wright J, Wustrow DJ; US 5,314,896 (May 1994).
21. Pyrazoloquinazolone derivatives as neurotrophic agents. Caprathe BW, Jaen JC; US 5,342,942
(August 1994). 22. Pyridazinoquinazolone derivatives as neurotrophic agents. Caprathe BW, Jaen JC; US
5,340,808 (August 1994). 23. Azabicyclic and azacyclic oximes and amines as cholinergic agents. Augelli-Szafran C, Barrett
S, Caprathe BW, Galan A, Jaen JC, Lauffer DJ, Moos WH, Pavia MR, Sanders K, Tecle H, Thomas AJ; US 5,346,911 (September 1994).
24. 1,3-Substituted cycloalkenes and cycloalkanes as Central Nervous System agents. Caprathe BW,
Downing, DM, Jaen JC, Johnson SJ, Smith WJ, Wise LD, Wright J, Wustrow DJ; US 5,409,931 (April 1995).
25. Substituted tetrahydropyridine and piperidine carboxylic acid as muscarinic antagonists.
Augelli-Szafran C, Jaen JC, Schwarz R, Thomas AJ; US 5,446,057 (August 1995). 26. Substituted tetrahydropyridines and hydroxypiperidines as Central Nervous System agents.
Glase S, Jaen JC, Smith SJ, Wise LD; US 5,466,698 (November 1995). 27. Stereochemically Pure Oximes with Muscarinic Activity. Bucsh RA, Jaen JC, Laborde E,
Thomas AJ; US 5,514,812 (May 1996). 28. [R-(Z)]-1-Azabicyclo[2.2.1]heptan-3-one, O-[3-(3-methoxyphenyl)-2-propynyl] oxime maleate
as a pharmaceutical agent. Ando H, Barrett S, Jaen JC, Rose S, Tecle H; US 5,534,522 (July 1996).
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29. Substituted tetrahydropyridines and hydroxypiperidines as Central Nervous System agents. Glase S, Jaen JC, Smith SJ, Wise LD; US 5,620,988 (April 1997). 30. 2-substituted-4H-3,1-benzoxazin-4-ones and benzothiazin-4-ones as inhibitors of complement
C1r protease for the treatment of inflammatory processes. Caprathe BW, Gilmore J, Hays S, Jaen JC; US 5,652,237 (July 29, 1997).
38. Thiazolidines as NS5B HCV polymerase inhibitors for therapeutic use in the treatment and prevention of hepatitis C infection. Jaen JC, Piper DE, Powers JP, Walker NPC, Li Y; WO-0177091 A2 (Published 10.18.01).
44. Pyrido[4,3-b]carbazole as G-protein coupled receptor modulators for treatment of eating
disorders. Chen X, Fan P, Jaen JC, Li L, Lizarzaburu M, Mihalic JT, Shuttleworth SJ; US Pat. Publication 03/176694A1 (Published 09.18.03) and WO-04/43958 (Published 05.27.04). Issued as US 7,125,885B2 (October 24, 2006) and US 7,253,179 (August 7, 2007).
46. Modulators of SREBP Processing. Jaen JC, Li L, Brown MS, Goldstein JL, Cheng D; US
6,649,593 B1 (November 18, 2003).
47. Thieno[3,2-c]pyridines and related compounds as anti-inflammatory agents. Burkitt SA, Cardozo MG, Cushing TD, DeGraffenreid MR, Farthing CN, Hao X, Jaen JC, Jiao XY, Kopecky DJ, Labelle M, Lively SE, McMinn DL, Rasmussen SP, Shin Y, Smith A, Smith ML; issued as US 7,635,695 (Dec 22, 2009).
48. Benzo-fused heterocycles for treatment of obesity and eating disorders. Chen X, Chen X,
Connors RV, Dai K, Fu Y, Jaen JC, Kim YJ, Li L, Lizarzaburu ME, Mihalic JT, Shuttleworth SJ; WO-06/20959A2 (published 02.23.06) and WO-06/199796A1 (published 09.07.06). Issued as US 7,572,783 (Aug 11, 2009).
49. Modulators of CXCR7. Powers J, Zhang P, Li L, Zeng Y, Chen X, Fan P, Gleason MM, Jaen
JC, McMahon JP; WO-10/054006 (published 05.14.10) and WO-10/0150831 (published 06.17.10). Issued as US 8,288,373 (Oct 16, 20123) and US 8,853,202 (Oct 7, 2014).
50. Diazole amides. Chen X, Dragoli DR, Fan P, Jaen JC, Li Y, Powers JP, Malathong V, Punna S,
Tanaka H, Zhang P. Issued as US 9,169,248 (October 27, 2015).
51. Preparation of phenylhydroxyamidine derivatives for use as immunomodulators. Jaen JC, Osipov M, Powers JP, Shunatona HP, Walker JR, Zibinsky M. WO-2015188085A1 (published Dec. 10, 2015).
52. Immunoregulatory agents. Beck HP, Jaen JC, Osipov M, et al. WO-2016/073738A2 (published
May 12, 2016).
53. Immunoregulatory agents. Beck HP, Jaen JC, Osipov M, et al. WO-2016/073770A1 (published May 12, 2016).
54. Immunoregulatory agents. Beck HP, Jaen JC, Osipov M, et al. WO-2016/073774A2 (published
May 12, 2016).
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ABSTRACTS
1. Novel small-molecule inhibitors of ecto-nucleotidase CD73: Activation of human CD8+ T cells and effects on tumor growth and immune parameters in experimental tumor models. Schindler U, Chen A, Leleti M, Debien L, Lawson K, Rosen B, Powers JP, Tan JBL, Sexton H, Park T, Young S, and Jaen JC. EORTC-NCI-AACR Molecular Targets & Cancer Therapeutics Symposium; Munich, Nov 29 – Dec 2, 2016. Abstract # xxx.
2. Small-molecule inhibitors of ecto-nucleotidase CD73 promote activation of human CD8+ T cells and have profound effects on tumor growth and immune parameters in experimental tumor models. Jaen JC, Chen A, Chiou SH, Leleti M, Lindsey E, Kalisiak J, Powers JP, Schindler U, Tan JBL, and Young S. CRI-CIMT-EATI-AACR International Cancer Immunotherapy Conference; New York, Sept 25-28, 2016. Abstract # xxx.
3. First-in-Human Study of FLX925, an Orally Administered FLT3/CDK4/CDK6 Inhibitor, in Subjects with Relapsed or Refractory Acute Myeloid Leukemia. Daver N, Knonpleva M, Khort H, Fridman J, Johnson D, Jaen J, Kantarjian H, Cortes J. American Society of Clinical Oncology (ASCO) Annual Meeting; May 29 – June 2, 2015. Abstract # TPS7098.
4. Potent and Selective Next-Generation Inhibitors of Indoleamine-2,3-Dioxygenase-1 (IDO1) for the Treatment of Cancer. Powers JP, Walters MJ, Noubade R, Young SW, Marshall L, Melom J, Park A, Shah N, Bjorck P, Fridman JS, Beck HP, Chian D, McKinnell J, Osipov M, Reilly MK, Shunatona HP, Walker JR, Zibinsky M, Jaen JC. American Association for Cancer Research, 106th Annual Meeting, Philadelphia (PA); April 18-22, 2015. Abstract # 4290. Cancer Research (2015); 75(15 Supplement):4290.
5. FLX925 (AMG 925) is a Rationally Designed FLT3, CDK4/6 Inhibitor that Retains Potency against Clinically Relevant Secondary Resistance Mutations in FLT3. Li C, Liang L, Xia Z, Li Z, Wang X, McGee LR, Newhall K, Sinclair A, Kamb A, Wickramasinghe D, Marubayashi S, Jaen JC, Fridman JS, Dai K. American Association for Cancer Research, 106th Annual Meeting, Philadelphia (PA); April 18-22, 2015. Abstract # 787. Cancer Research (2015); 75(15 Supplement):787.
6. Identification of Second-Generation Potent and Selective Inhibitors of Indoleamine-2,3-
dioxygenase-1 (IDO1) for the Treatment of Cancer. Jaen JC, Bjorck P, Fridman JS, Marshall L, Melom J, Noubade R, Osipov M, Walters MJ, Young S, Zibinsky M, Powers JP. 2nd Immunotherapy of Cancer Conference (ITOC-2), Munich (Germany); March 25-27, 2015. Eur. J. Cancer (2015); 51.
7. Potent and selective inhibitors of tryptophan catabolizing enzymes for the treatment of
cancer. Walters MJ, Noubade R, Young SW, Marshall L, Melom J, Park A, Shah N, Björck P, Fridman JS, Beck HP, Chian D, McKinnell J, Osipov M, Reilly MK, Shunatona HP, Walker JR, Zibinsky M, Jaen JC, Powers JP. Keystone Symposium on Tumor Immunology: Multidisciplinary Science Driving Combination Therapy, Banff (Canada); Feb 8-13, 2015. Abstract # 3042.
8. The relevance of differential expression of tolerogenic enzymes IDO-1, IDO-2 and TDO in commonly used mouse tumor models for testing novel therapeutics. Walters MJ, Noubade R,
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Marshall L, Kohrt HEK, Hebb J, Rajasekaran N, Powers JP, Young S, Jaen JC. 12th Cancer Immunotherapy Meeting, Mainz (Germany); May 6-8, 2014. Abstract # P171.
9. Therapeutic use of a clinical stage CCR2 inhibitor, CCX872, improves obesity associated
steatohepatitis in mice. Parker R, Walters MJ, Ertle L, Ebsworth K, Tan J, Sietz L, McMahon J, Dairaghi D, Powers J, Adams D, Jaen J, Schall T. 49th Annual Meeting of the European Association for the Study of the Liver, London (UK); April 9-13, 2014.
10. Therapeutic use of a clinical stage CCR2 inhibitor, CCX872, in obesity-associated
steatohepatitis. Parker R, Walters M, Ertl L, Ebsworth K, Tan J, McMahon J, Powers J, Adams D, Jaen J, Schall T. The Lancet (2014) 383, S78.
11. Expression of tolerogenic enzymes IDO-1, IDO-2 and TDO in commonly used mouse tumor models and impact on model selection for evaluation of immunosuppression reversal by novel therapeutics. Noubade R, Kohrt H, Marshall L, Sagiv-Barfi I, Hebb J, Chester C, Rajapaksa A, Waller E, Young S, Powers J, Jaen JC. American Association for Cancer Research, 105th Annual Meeting, San Diego (CA); April 5-9, 2014. Abstract # 3648. Cancer Research (2014); 74(19 Supplement):3648.
12. CCR6 antagonist confers protection against psoriasiform-like disease in mice by limiting the infiltration of CCR6+ leukocytes into the epidermis. Tan JBL, Ebsworth K, Berahovich R, Leleti M, Dairaghi D, Zhang P, Powers JP, Jaen J, Walters MJ, Schall TS. International Congress of Immunology, London (UK); March, 2014.
13. Efficacy of C-C Chemokine Receptor 2 (CCR2) antagonists CCX140 and CCX872 in a mouse
model of Ischemia-Reperfusion Injury. Jaen JC, Walters MJ, Miao Z, Berahovich R, Powers JP, Baumgart T, Ertl L, Bekker P, Schall TJ. 46th Annual Meeting of the American Society of Nephrology, Atlanta (GA); November 5-10, 2013.
14. A randomized, double-blind, placebo-controlled clinical trial of CCX168, an orally administered C5aR antagonist, in patients with ANCA-Associated Renal Vasculitis (CLEAR). Bruchfeld A, Schaier M, Ciechanowski K, Harper L, Jadoul M, Segelmark M, Selga D, Szombati I, Venning M, Hamilton P, Hugo C, van Daele P, Viklicky O, Jayne D, Potarca A, Jaen J, Schall T, Bekker P. 46th Annual Meeting of the American Society of Nephrology, Atlanta (GA); November 5-10, 2013.
15. Phase 2 clinical trial of orally administered CCR2 antagonist CCX140-B. Bekker P, Potarca A, Miao S, Dairaghi D, Lohr L, Seitz L, Miao Z, Powers J, Jaen J, Schall TJ. 46th Annual Meeting of the American Society of Nephrology, Atlanta (GA); November 5-10, 2013.
16. The CXCR7 Inhibitor CCX650 significantly prolongs survival in the C6 rat model of glioblastoma. Ebsworth K, Walters MJ, Ertl LS, Wang Y, Berahovich RD, McMahon J, Powers JP, Jaen JC, Schall TJ. Society for NeuroOncology Annual Conference; November 21-24, 2013.
17. Inhibition of chemokine receptors CCR1 and CCR6 as promising therapies for autoimmune
diseases such as rheumatoid arthritis and psoriasis. Dairaghi DJ, Zhang P, Leleti M,
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Berahovich R, Erlt L, Miao Z, Miao S, Seitz LC, Tan J, Walters MJ, Wang Y, Powers JP, Schall TJ, and Jaen JC, Annual Meeting of the American College of Rheumatology, San Diego (CA); October 28, 2013.
18. CCX507, an orally bioavailable 2nd generation antagonist of the chemokine receptor CCR9. Walters MJ, Ebsworth KE, Zhang P, Powers J, Dairaghi D, Ertl L, Zhao B, Wang Y, Miao S, Lohr L, Jaen JC, Bekker P, Schall TJ. United European Gastroenterology Week (UEGW 2012), Berlin (DE); October 12-16, 2013.
19. The CCR2 antagonist CCX140 improves renal function and hyperglycemia in diabetic mice expressing human CCR2. Powers JP, Sullivan TJ, Miao Z, Zhao N, Berahovich R, Ertl L, Walters MJ, Dang T, Miao S, Jaen JC, Schall TJ. 73rd American Diabetes Association Scientific Sessions, Chicago (IL); June 21-25, 2013. Abstract # 107-OR (selected for oral presentation).
20. Phase 1 clinical evaluation of the CCR2 antagonist CCX872-B. Bekker P, Charvat T, Miao S, Lohr L, Sullivan T, Miao Z, Powers J, Jaen J, Schall TJ. 73rd American Diabetes Association Scientific Sessions, Chicago (IL); June 21-25, 2013.
21. Inhibition of chemokine receptors CCR1 and CCR6 as promising therapies for rheumatoid arthritis. Jaen J, Dairaghi D, Leleti M, Powers J, Wang Y, Zhang P, Schall TJ, Bekker P. 2013 Annual European Congress of Rheumatology (EULAR), Madrid (Spain) June 12-15, 2013. Abstract # FRI0002.
22. The CCR2 antagonist CCX140 improves renal function in two types of diabetic mice expressing human CCR2. Powers J, Sullivan T, Miao Z, Berahovich R, Ertl L, Walters M, Miao S, Jaen J, Schall T. 50th European Renal Association – European Dialysis & Transplantation Association (ERA-EDTA) Congress; Istanbul (Turkey); May 18-21, 2013. Abstract # TO022 (selected for oral presentation).
23. Clinical development of CCR2 antagonists CCX140-B and CCX872-B. Bekker P, Charvat T, Miao S, Lohr L, Dairaghi D, Seitz L, Sullivan T, Miao Z, Powers J, Jaen J, Schall TJ. 50th European Renal Association – European Dialysis & Transplantation Association (ERA-EDTA) Congress; Istanbul (Turkey); May 18-21, 2013. Abstract # SO058 (selected for oral presentation).
24. CCX507, an orally bioavailable antagonist of the chemokine receptor CCR9, for the treatment of IBD. Walters MJ, Ebsworth KE, Sullivan TJ, Zhang P, Powers J, Ertl L, Bekker P, Jaen JC, Schall TJ. Digestive Diseases Week (DDW), Orlando (FL); May 18-21, 2013. Abstract # Tu1652.
25. C5aR Inhibitor on Leukocytes Exploratory ANCA Associated Renal Vasculitis (CLEAR) clinical trial with orally administered CCX168. Bruchfeld A, Schaier M, Jadoul M, Selga D, Szombati I, Venning M, Hamilton P, Ciechanowski K, Hugo C, Segelmark M, Jaen J, Schall T, Bekker P. 16th International Vasculitis & ANCA Workshop, Paris (France); April 14-16, 2013.
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26. Post-translational modification of CCL23 in chronic rhinosinusitis with nasal polyps. Keswani A, Poposki JA, Peterson S, Suh LA, Norton J, Peters AT, Grammer LC, Tan BK, Chandra RK, Conley DB, Jaen JC, Schall TJ, Kern RC, Schleimer RP, Kato A. 2013 Annual Meeting of the American Academy of Allergy, Asthma & Immunology, San Antonio (TX), February 22-26, 2013. Abstract #799.
27. CXCR7 Inhibition significantly prolongs survival in the ENU rat model of glioblastoma. Ebsworth K, Walters MJ, Ertl LS, Wang Y, Berahovich RD, Zhang P, Powers JP, Sullivan TJ, Jaen JC, Brown M, Schall TJ. 2012 Society for NeuroOncology Annual Conference, Washington (DC), November 15-18, 2012. Abstract # ET-11.
28. The CCR2 chemokine receptor antagonist CCX140 improves renal function in diabetic mice
expressing human CCR2. Sullivan T, Miao Z, Berahovich R, Powers JP, Baumgart T, Ertl L, Miao S, Schall TJ, Jaen JC. 45th Annual Meeting of the American Society of Nephrology, San Diego (CA); October 30-November 3, 2012. Abstract # SA-PO475.
29. CCR9 Inhibitors for the Treatment of IBD. Walters MJ; Ebsworth K; Sullivan TS; Wang Y;
Dairaghi D; Ma G; Jaen JC; Schall TJ. United European Gastroenterology Week (UEGW 2012), Amsterdam (NL) October 20-24, 2012. Abstract # P0871. Gut 2012, 61 (Suppl3), A287.
30. CCR2 inhibition improves renal function in diabetic BTBR ob/ob mice. Sullivan T; Miao Z; Berahovich R; Zhao N; Ertl L; Baumgart T; Krasinski A; Dang T; Miao S;; Powers JP; Jaen JC; Schall T. 48th Annual Meeting – European Association for the Study of Diabetes (EASD), Berlin (Germany); October 1-5, 2012 (selected for oral presentation).
31. CCR2 inhibition improves renal function in diabetic BKS db/db mice. Sullivan TJ, Miao Z,
Zhao N, Berahovich R, Powers JP, Ertl L, Jaen JC, Schall TJ. 72nd American Diabetes Association Scientific Sessions, Philadelphia (PA); June 8-12, 2012. Abstract # 517-P.
32. Orally-administered CCR1 antagonist CCX354-C in a Phase 2 rheumatoid arthritis study. Tak
PP, Balanescu A, Tseluyko, Bojin S, Drescher E, Dairaghi D, Miao S, Marchesin V, Jaen J, Schall TJ, Bekker P. 2012 Annual European Congress of Rheumatology (EULAR), Berlin (Germany) June 6-9, 2012. Abstract # OP0203 (selected for oral presentation). Ann. Rheum. Dis. 2012, 71 (Suppl.3): 123.
(online: http://www.abstracts2view.com/eular/view.php?nu=EULAR12L_OP0203&terms=). 33. Characterization of the novel C5aR antagonist CCX168, a potential therapeutic for ANCA-
vasculitis, rheumatoid arthritis, and other autoimmune disorders. Powers JP, Bekker PJ, Dairaghi DJ, Jennette JC, Johnson DA, Leleti M, Miao S, Seitz LC, Wang Y, Xiao H, Schall TJ, Jaen JC. 2012 Annual European Congress of Rheumatology (EULAR), Berlin (Germany) June 6-9, 2012. Abstract # OP0204 (selected for oral presentation). Ann. Rheum. Dis. 2012, 71 (Suppl.3): 124. (online: http://www.abstracts2view.com/eular/view.php?nu=EULAR12L_OP0204&terms=).
34. Expression of CXCR7, CXCR4, CXCR3 and their chemokine ligands in glioblastoma.
American Society of Clinical Oncology (ASCO) Annual Meeting; Chicago; June 1-5, 2012. Abstract # 243.
35. The CXCR7 inhibitor CCX662 prolongs survival in the ENU rat model of glioblastoma.
Ebsworth K, Walters MJ, Ertl LS, Wang Y, Zhang P, Powers JP, Sullivan TJ, Jaen JC, Brown M, Schall TJ. American Society of Clinical Oncology (ASCO) Annual Meeting; Chicago; June 1-5, 2012.
36. Clinical dose selection of the C5a receptor antagonist CCX168 for the Phase 2 ANCA-
associated renal vasculitis clinical trial (the CLEAR trial). Dairaghi DJ, Johnson DA, Leleti M, Miao S, Xiao H, Jennette JC, Powers JP, Seitz LC, Wang Y, Jaen JC, Schall TJ, Bekker PJ. 49th European Renal Association – European Dialysis & Transplantation Association (ERA-EDTA) Congress; Paris (France); May 24-27, 2012. Abstract # SAP251.
37. CCR2 inhibition in diabetic BKS db/db mice results in a rapid and robust improvement of renal
inflammation and renal function. Jaen JC, Sullivan TJ, Miao Z, Zhao N, Berahovich R, Powers JP, Ertl L, Schall TJ. 49th European Renal Association – European Dialysis & Transplantation Association (ERA-EDTA) Congress; Paris (France); May 24-27, 2012. Abstract # FP271.
38. Oral C5a receptor antagonist CCX168 in a Phase 2 clinical trial in ANCA associated renal
vaculitis. Bekker P, Potarca A, Dairaghi D, Miao S, Powers J, Jaen J, Schall TJ. 49th European Renal Association – European Dialysis & Transplantation Association (ERA-EDTA) Congress; Paris (France); May 24-27, 2012. Abstract # SAP304.
39. Pharmacological inhibition of C-C chemokine receptor 9 (CCR9) does not inhibit the
generation of oral tolerance. Walter MJ, Ebsworth KE, Sullivan TJ, Jaen JC, Schall TJ; Digestive Diseases Week (DDW), San Diego (CA); May 19-22, 2012. Abstract # 1296275.
40. Genetic deletion and pharmacological inhibition of chemokine receptor 9 (CCR9) result in
opposite effects on the development of oral tolerance. Walters MJ, Ebsworth KE, Sullivan TJ, Jaen JC, Schall TJ; 7th Congress of the European Crohn’s and Colitis Organization, Barcelona (Spain); February 16-18, 2012. Abstract # P032.
41. Safety and efficacy of oral Chemokine Receptor 1 antagonist CCX354-C in a Phase 2
rheumatoid arthritis study. Tak PP, Balanescu AR, Tseluyko V, Bojin S, Galatikova D, Drescher E, Szombati I, Hrycaj P, Dairaghi D, Miao S, Marchesin V, Jaen J, Bekker P, Schall TJ; Annual Meeting of the American College of Rheumatology, Chicago (IL); November 8, 2011. Late-Breaking Abstract # L5 (selected for oral presentation). Arthritis Rheum. 2011, 63(10 Suppl.).
42. Inhibition of the CCR2 chemokine receptor in diabetic mice results in a rapid and robust
improvement of renal function including albuminuria. Sullivan T, Miao Z, Zhao N, Berahovich R, Powers JP, Ertl L, Dang T, Zhao R, Liu S, Miao S, Seitz LC, Bekker P, Schall TJ, Jaen JC; 44th Annual Meeting of the American Society of Nephrology, Philadelphia (PA); November 8-13, 2011. Abstract # TH-PO537. J. Am. Soc. Nephrol. 2011, 22(Suppl.), 236A (online: http://www.asnonline.org/education_and_meetings/kidneyweek/archives/KW11Abstracts.pdf).
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43. Inhibition of the CCR2 chemokine receptor in diabetic mice results in a rapid and robust
improvement of hyperglycemia. Jaen JC, Sullivan T, Miao Z, Zhao N, Berahovich R, Ertl L, Baumgart T, Krasinski A, Greenman K, Bekker P, Powers J, Schall T; European Association for the Study of Diabetes, Lisbon, Portugal; Sept 12-16, 2011. Abstract # 894. Diabetologia 2011, 54(Suppl.1), S365.
44. Safety and efficacy of oral chemokine receptor 2 antagonist CCX140-B in a Phase 2 Type 2
diabetes mellitus study. Hanefeld M, Schell E, Gouni-Berthold I, Melichar M, Vesela I, Sullivan T, Miao S, Johnson D, Jaen J, Bekker P, Schall TJ. European Association for the Study of Diabetes, Lisbon, Portugal; Sept 12-16, 2011. Abstract # 192 (selected for oral presentation). Diabetologia 2011, 54(Suppl.1), S87.
45. Identification and optimization of (E)-1-((2-(1-methyl-1H-imidazol-5-yl) quinolin-4-yl)
methylene) semithiocarbazones as a novel series of IκB kinase β (IKKβ) inhibitors. Shin Y, Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Jaen J, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Sjogren E, Smith M:, Talamas FX, Tonn G, Walker K, Walker NPC, Wesche H, Whitehead C, Wright M, Browner M; 242nd ACS National Meeting, Denver; Aug 28 – Sept 1, 2011. Abstract # MEDI-111.
46. Novel series of IkB kinase β (IKKβ) inhibitors part II: Description of a potent and
pharmacologically active series of analogs. He X, Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Browner M, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Shin Y, Sjogren E, Smith M:, Talamas FX, Tonn G, Walker K, Walker NPC, Wesche H, Whitehead C, Wright M, Jaen JC; 242nd National Meeting – American Chemical Society, Denver; Aug 28 – Sept 1, 2011. Abstract # MEDI-112.
47. Oral chemokine receptor 2 antagonist CCX140-B shows safety and efficacy in Type 2 diabetes
mellitus. Hanefeld M, Schell E, Gouni-Berthold I, Melichar M, Vesela I, Sullivan T, Miao S, Johnson D, Jaen J, Bekker P, Schall TJ; 71st American Diabetes Association Scientific Sessions, San Diego (CA); June 24-28, 2011. Abstract #310-OR (selected for oral presentation). Diabetes 2011, 60(Suppl 1), A85.
48. CCR2 antagonism improves renal function and hyperglycemia in preclinical models of Type 2
diabetes. Sullivan T, Miao Z, Berahovich R, Zhao N, Charvat T, Powers J, Jaen JC, Schall TJ; 71st American Diabetes Association Scientific Sessions, San Diego (CA); June 24-28, 2011. Abstract # 606-P. Diabetes 2011, 60(Suppl 1), A582-A643.
49. C5a engagement of C5a receptors but not C6 is required for induction of GN by anti=MPO
IgG. Xiao H, Dairaghi D, Hu P, Powers JP, Wang Y, Ertl L, Baumgart T, Miao S, Seitz LC, Falk RJ, Schall TJ, Jaen JC, Jennette JC; 15th International Vasculitis & ANCA Workshop, Chapel Hill (NC); March 15-19, 2011. Clin. Exp. Immunol. 2011, 164(Suppl. 1), 127.
50. Synthesis and SAR of substituted 7H-pyrrolo[2,3-d]pyrimidines as ACK1 inhibitors. Xianyun J, Kopecky DJ, Liu JQ, Wang Z, Cardozo M, Farrelly E, Jaen J, Liu JS, Sharma R, Walker N,
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Wesche H, Xiao SH, Kayser F; 241st ACS National Meeting, Anaheim; March 27-31, 2011. Abstract # MEDI-255.
51. CCR1 blockade by an orally-available CCR1 antagonist reduces tumor burden and osteolysis in
vivo in a mouse model of myeloma bone disease. Oyajobi B, Dairaghi D, Gupta A, McCluskey B, Wang Y, Seitz LC, Powers JP, Miao S, Zhang P, Schall TJ, Jaen JC; American Society of Hematology National Meeting, Orlando (FL); December 5, 2010. Blood 2010, Nov 19 Suppl.
Ikeno F, Nakatani D, Otake H, Lyons JK, Sullivan T, Jaen J, Schall T, Tio F, Fearon W, Yeung AC, Fearon WF; American Heart Association National Meeting, Chicago (IL) November 17, 2010. Circulation 2010, 122, A17007.
53. Robust efficacy of C5aR antagonist CCX168 in a mouse model of ANCA glomerulonephritis.
Xiao H, Jennette JC, Dairaghi D, Powers JP, Wang Y, Ertl L, Baumgart T, Miao S, Seitz LC, Hu P, Falk RJ, Schall TJ, Jaen JC. 43rd Annual Meeting of the American Society of Nephrology, Denver (CO); November 16-21, 2010. Abstract # F-FC179 (selected for oral presentation). J. Am. Soc. Nephrol. 2010, 21(Suppl.), 40A (online: http://www.asn-online.org/education_and_meetings/kidneyweek/archives/RW10Abstracts.pdf).
54. Phase-1 Clinical Pharmacokinetic and Pharmacodynamic Evaluation of the Novel C5aR
Antagonist CCX168, a Potential Therapeutic for ANCA-Vasculitis. Dairaghi D, Johnson DA, Deshayes K, Miao S, Seitz L, Wang Y, Leleti MR, Powers JP, Bekker P, Schall TJ, Jaen JC; 43rd Annual Meeting of the American Society of Nephrology, Denver (CO); November 16-21, 2010. Abstract # SA-PO2111. J. Am. Soc. Nephrol. 2010, 21(Suppl.), 595A (online: http://www.asn-online.org/education_and_meetings/kidneyweek/archives/RW10Abstracts.pdf).
55. CCR1 antagonist CCX354-C in Phase 2 clinical development for Rheumatoid Arthritis.
Dairaghi DJ, Marchesin V, Johnson DA, Miao S, Seitz LC, Wang Y, Zhang P, Powers JP, Ho B, Bekker PJ, Jaen JC, Schall TJ; Annual Meeting of the American College of Rheumatology, Atlanta (GA); November 3, 2010. Abstract #1100. Arthritis Rheum. 2010, 62(10S), S460.
56. The human C5a receptor (hC5aR) antagonist CCX168 effectively ameliorates a mouse model
of ANCA-induced glomerulonephritis (GN) in hC5aR knock-in mice. Xiao H, Jennette JC, Dairaghi DJ, Ertl L, Baumgart T, Miao S, Powers JP, Seitz LC, Wang Y, Hu P, Falk RJ, Schall TJ, Jaen JC. Annual Meeting of the American College of Rheumatology, Atlanta (GA); November 3, 2010. Abstract # 2048. Arthritis Rheum. 2010, 62(10S), S856.
57. Phase-1 Clinical Pharmacokinetic and Pharmacodynamic Evaluation of the Novel C5aR
Antagonist CCX168, a Potential Therapeutic for ANCA-Vasculitis. Dairaghi DJ, Jaen JC, Deshayes K, Johnson DA, Leleti MR, Miao M, Powers JP, Seitz LC, Wang Y, Schall TJ, Bekker PJ. Annual Meeting of the American College of Rheumatology, Atlanta (GA); November 3, 2010. Abstract # 2032. Arthritis Rheum. 2010, 62(10S), S850.
58. One-year results from PROTECT-1 study of intestine-specific chemokine receptor antagonist
CCX282-B (Traficet-EN) in Crohn’s disease. Hetzel DJ, Keshav S, Johnson D, Jaen JC,
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Schall TJ, Bekker P; United European Gastroenterology Week (UEGW 2010), Barcelona (Spain) October 23-27, 2010. Abstract # PO946. Gut 2010, 59(Suppl.III), A297.
59. Inhibition of SDF-1/CXCR7 radiosensitizes ENU-induced glioblastomas in the rat. Tseng D,
Lartey F, Liu S-C, Kioi M, Walters M, Schall TJ, Jaen JC, Merchant M, Recht L, Brown M; 56th Annual Meeting of the Radiation Research Society, Maui (HI) September 26-29, 2010.
60. CCR2 antagonist CCX140-B in Phase 2 for type 2 diabetes. T. Sullivan, S. Miao, R.
Berahovich, N. Zhao, D. Johnson, P. Bekker, J. Jaen, T.J. Schall; European Association for the Study of Diabetes, Stockholm, Sweden; Sept 20-24, 2010. Abstract #883. Diabetologia 2010, 53(Suppl.1), S353.
61. A novel CCR1 antagonist CCX354-C for rheumatoid arthritis. Dairaghi D, Ertl L, Johnson D,
Pennell AM, Powers JP, Miao S, Seitz L, Wang Y, Zeng Y, Zhang P, Bekker P, Schall TJ, Jaen JC; 2010 Annual European Congress of Rheumatology (EULAR), Rome (Italy) June 16-19, 2010. Abstract # THU0203. Ann. Rheum. Dis. 2010, 69(3S), 214.
62. CCR2 Antagonist Inhibits Neointimal Proliferation Post Coronary Stent Deployment.
Teramoto T, Ikeno F, Otake H, Lyons JK, Sullivan T, Jaen J, Schall T, Tio F, Fearon W, Yeung AC; Amer. College Cardiol. National Meeting (ACC.10), Atlanta (GA) March 2010. Abstract #TCT-394. J. Am. Coll. Cardiol. 2010, 56(13Suppl.1), B91.
63. CCR9 inhibition in the treatment of colonic inflammation. Walters MJ, Berahovich R, Ertl L,
Ebsworth K, Baumgart T, Charvat TT, Powers JP, Punna S, Wang Y, Bekker P, Jaen JC, Schall TJ; 2009 Advances in Inflammatory Bowel Diseases; Crohn’s & Colitis Foundation’s Clinical & Research Conference, Hollywood, FL; December 3-6, 2009.
64. Structure-guided design of pan-LXR antagonists. Kayser F, Chai A, Coward P, Harrison M,
Jaen J, Jiao XY, Jones S, Kopecky D, Piper D, Shiau A; 235th National Meeting - American Chemical Society, New Orleans; April 6-10, 2008. Abstract # MEDI-239.
65. Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as
a novel class of ACK1 inhibitors. Hao X, Kopecky D, Jiao XY, Chen Y, Fu J, Jaen J, Wesche H, Xiao J, van der Horst E, Liu J, Wang Z, Cardozo M, Ma J, Miao S, Tang L, Kayser F; 235th National Meeting - American Chemical Society, New Orleans; April 6-10, 2008. Abstract # MEDI-094.
66. Discovery and biological evaluation of novel benzamide derivatives as potent 11β-HSD1
inhibitors for the treatment of type II diabetes. Julian LD, Bostick T, Caille S, Chan H, Degraffenreid M, He X, Hungate R, Jaen J, Jiang B, Kaizerman J, Liu J, McMinn D, Powers JP, Rew Y, Sudom A, Sun D, Tu H, Ursu S, Wang Z, Yan X, Ye Q; 234th National Meeting - American Chemical Society, Boston; August 19-23, 2007. Abstract # MEDI-051.
67. Discovery and optimization of arylsulfonamide as a novel class of 11β-HSD1 inhibitors. Sun
D, DeGraffenreid M, He X, Jaen J, Powers JP, Yan X, Di Y, Tu H, Ursu S, Ma J, Miao S, Tang L, Ye Q, Sudom A, Wang Z; 234th National Meeting - American Chemical Society, Boston; August 19-23, 2007. Abstract # MEDI-055.
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68. Discovery of potent EDG4 antagonists as potential anticancer agents. Beck HP, Dai K, Frank
B, Hasslinger K, Hedberg C, Hungate R, Jaen J, Kohn T, Li C, Liang L, Medina J, Rubenstein S, Schwandner R, Wang S, Wesche H; 233rd National Meeting - American Chemical Society, Chicago; March 25-29, 2007. Abstract # MEDI-135.
69. SAR study on a novel series of pyridocarbazole-based melanin concentrating hormone
receptor-1 antagonists: Discovery of T0910792, a potent, selective and orally bioavailable agent that is efficacious in obesity models. Li L, Fan P, Chen X, Mihalic J, Fu Y, Dai K, Liang L, Reed M, Wright M, Timmermans P, Chen JL, Jaen J; 231st National Meeting - American Chemical Society, Atlanta; March 26-30, 2006. Abstract # MEDI-197.
70. Discovery of viral primases as drug targets: Compound-based target elucidation, validation,
and advancement to the clinic. Powes JP, Chen X, Cushing TD, DiMaio H, Jaen JC, Liang L, Mayorga V, Miao S, Peterson MG, Spector F, Stein C, Wright M, Ye Q; 232nd National Meeting - American Chemical Society, San Francisco; September 10-14, 2006. Abstract # MEDI-272.
71. Discovery and optimization of potent ACK1 inhibitors – Part I: 4-Amino substitution is
important for potency improvement. Liu J, Sharma R, Lively S, Burkitt S, Clase A, Farthing C, Jiao XY, Kopecky D, Kayser F, Shuttleworth S, Harrison M, Faulder P, Li S, Wesche H, Mallari R, Farrelly E, Xiao SH, Liu J, Wang Z, Jaen JC; 232nd National Meeting - American Chemical Society, San Francisco; September 10-14, 2006. Abstract # MEDI-105.
72. Discovery and optimization of potent ACK1 inhibitors – Part II: Structural modification of the
furanopyrimidine core. Kopecky D, Burkitt S, Clase A, Farrelly E, Farthing C, Faulder P, Frenkel D, Harrison M, Jaen J, Jiao XY, Kayser F, Li S, Liu J, Lively S, Sharma R, Strelow A, Van der Horst E, Wang Z, Wesche H, Xiao SH; 232nd National Meeting - American Chemical Society, San Francisco; September 10-14, 2006. Abstract # MEDI-106.
73. Discovery and optimization of potent ACK1 inhibitors – Part III: Selected 4-amino substitution
affords very potent inhibitors. Lively S, Burkitt S, Cardozo M, Clase A, Farrelly E, Farthing C, Faulder P, Harrison M, Jaen J, Jiao XY, Kayser F, Kopecky D, Li S, Liu J, Mallari R, Sharma R, Strelow A, Van der Horst E, Wang Z, Wesche H, Xiao SH; 232nd National Meeting - American Chemical Society, San Francisco; September 10-14, 2006. Abstract # MEDI-107.
74. Inhibition of human cytomegalovirus replication by a series of novel non-nucleoside primase
Peterson G, Spector F, Stein C, Wright M, Ye Q; 41st ICAAC Annual Meeting, Chicago; December 16-19, 2001. Abstract # 1673.
77. Medicinal chemistry of T138067, an antimitotic agent that binds irreversibly and selectively to
ß-tubulin: Evaluation of the aniline region. Clark DL, Medina JC, Houze J, Gergely J, Rubenstein S, Shan B, Baichwal V, Jaen JC, Rosen T; 219th National Meeting - American Chemical Society, San Francisco; March 26-30, 2000. Abstract # MEDI-67.
78. Medicinal chemistry of T138067, an antimitotic agent that binds irreversibly and selectively to
ß-tubulin: Evaluation of the pentafluorophenylsulfonamide region. Medina JC, Clark DL, Houze J, Frankmoelle W, Rubenstein S, Gergely J, Shan B, Beckmann H, Baichwal V, Rosen T, Jaen JC; 219th National Meeting - American Chemical Society, San Francisco; March 26-30, 2000. Abstract # MEDI-68.
79. Cytotoxic effects of an isotype-specific ß-tubulin binding agent in multidrug resistant tumor
cells. Shan B, Medina JC, Learned RM, Frankmoelle WP, Chou TC, Santha E, Stott D, Jaen JC, Rosen T, Timmermans PBMWM, Beckmann H; American Association for Cancer Research, 90th Annual Meeting, Philadelphia; April 10-14, 1999. Abstract # 816.
80. Novel irreversible tubulin polymerization inhibitors with efficacy against MDR+ cell lines.
Medina JC, Clark DL, Shan B, Beckmann H, Learned RM, Roche D, Rosen T, Jaen JC; American Association for Cancer Research, 90th Annual Meeting, Philadelphia; April 10-14, 1999. Abstract # 4382.
81. Synthesis of potential oxidative metabolites of 1,3-dichloro-6,7,8,9,10,12-hexahydro
azepinoquinazoline. Gilmore JL, Hays SJ, Caprathe BW, Thomas AJ, Bucsh RA, Emmerling MR, Jaen JC; 216th National Meeting - American Chemical Society, Boston; August 23-27, 1998. Abstract # ORGN-477.
82. Novel sulfonamides with efficacy against multidrug resistant tumor cells. Medina, J. C.;
Beckmann, H.; Clark, D. L.; Farrell, R. P.; Frankmoelle, W.; Jaen, J. C.; Learned, M.; Narbut, M.; Rosen, T.; Shan, B.; Timmermans, P.; 216th National Meeting - American Chemical Society, Boston; August 23-27, 1998. Abstract # MEDI-216.
83. Thioflavin-T analogs as ligands for amyloid-ß. Hays SJ, Caprathe BW, Gilmore JL, Jaen JC,
Levine III, H; 3rd International Symposium on the Medicinal Chemistry of Neurodegenerative Diseases, Key Biscayne, FL; October 4-7, 1997.
84. A novel series of potent thrombin inhibitors: chemistry and SAR studies. Augelli-Szafran CE,
Bachand B, Berryman KA, Cai C, Cody WL, Edmunds JJ, Holland DR, Jaen JC, Narasimhan LS, Penvose-Yi JR, Plummer JS, Rapundalo ST, Rubin JR, Siddiqui MA, St-Denis Y, Susser A, Doherty A; 214th National Meeting - American Chemical Society, Las Vegas, NV; September 7-11, 1997. Abstract # MEDI 56.
85. Preparation of stereochemically pure oximes of CI-1017. Thomas AJ, Laborde E, Busch R,
Jaen JC; 16th International Congress of Heterocyclic Chemistry, Bozeman, MT; August 10-15, 1997.
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86. Design, synthesis and SAR of benzenesulfonamide derivatives as inhibitors of complement C1r
protease for the treatment of inflammatory processes; Cai, C; Plummer, J; Hays, S; Gilmore, J; Emmerling, M; Wang, K; Jaen, JC; 213th National Meeting - American Chemical Society, San Francisco; April 13-17, 1997. Abstract # MEDI 87.
87. Pharmacological characterization of PD 102807: an m4 selective muscarinic antagonist.
Schwarz, R; Nelson, C; Augelli-Szafran, C; Penvose, J; Jaen, JC; Wiley, J; Frey, K; Society for Neuroscience, 26th Annual Meeting, Washington D.C., November 16-21, 1996. Abstract # 500.16.
88. Benzoxazine isoquinolines as potential m4 selective muscarinic antagonists. Augelli-Szafran,
C; Moreland, D; Nelson, C; Penvose-Yi, J; Schwarz, R; Jaen, JC; Society for Neuroscience, 26th Annual Meeting, Washington D.C., November 16-21, 1996. Abstract # 500.15.
89. Pharmacological characterization of PD 102807: An m4 selective muscarinic antagonist.
Schwarz, R; Nelson, C; Augelli-Szafran, C; Penvose, J; Jaen, JC; Wiley, J; Frey, K; Seventh International Symposium on Subtypes of Muscarinic Receptors; Vienna (Virginia); November 12-15, 1996.
90. Identification and characterization of m4 selective muscarinic antagonists. Augelli-Szafran, C;
Moreland, D; Nelson, C; Penvose-Yi, J; Schwarz, R; Jaen, JC; Seventh International Symposium on Subtypes of Muscarinic Receptors; Vienna (Virginia); November 12-15, 1996.
91. Functional characterization of PD102807: a novel m4-selective muscarinic antagonist. Gross,
J; Augelli-Szafran, CE; Czeche, S; Friebe, T; Jaen, JC; Penvose-Yi, JR; Schwarz, RD; Mutschler, E; Lambrecht, G; Seventh International Symposium on Subtypes of Muscarinic Receptors; Vienna (Virginia); November 12-15, 1996.
Caprathe, B; Watson, D; Donahue, J; Michael, W; Emmerling, M; Wang, K; Jaen, JC; 212th National Meeting - American Chemical Society, Orlando; August 25-29, 1996. Abstract # MEDI 155.
93. Dihydroisoquinolines and substituted indoles in the synthesis of m4 selective muscarinic
antagonists; Penvose-Yi, JR; Augelli-Szafran, CE; Moreland, DW; Nelson, CB; Schwarz, RD; Jaen, JC; 25th National Medicinal Chemistry Symposium, The University of Michigan, Ann Arbor, MI, June 18-22, 1996.
94. Synthesis of potential oxidative metabolites of CI-1002, an acetylcholinesterase inhibitor;
Caprathe, BW; Bucsh, RA; Emmerling, MR; Gilmore, JL; Hays, SJ; Jaen, JC; Thomas, AJ; 25th National Medicinal Chemistry Symposium, The University of Michigan, Ann Arbor, MI, June 18-22, 1996. Abstract # 78.
95. Cholinesterase activities and levels of APP, sAß, and complement proteins C1q, C3, and C9 in
CSF from normal and AD patients; Doyle, PD; Carroll, RT; Jaen, JC; Kim, KS; Wisniewski,
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H; Wisniewski, T.; Emmerling, MR; Society for Neuroscience, 25th Annual Meeting, San Diego, November 1995. Abstract # 671.13.
96. Complement inhibition as a mechanism for treatment of neurodegenerative diseases. Hays SJ,
Caprathe BW, Emmerling MR, Gilmore JL, Jaen JC, Michael W, Narasimhan L, Watson D; 210th National Meeting - American Chemical Society, Chicago; August 20-24, 1995. Abstract # MEDI 248.
97. Complement Inhibition as a Mechanism for the Treatment of Neurodegenerative Diseases;
Hays SJ, Caprathe BW, Emmerling MR, Gilmore JL, Jaen JC, Michael W., Narasimhan L, Watson D; 210th National Meeting - American Chemical Society, Chicago; August 20-24, 1995. Abstract # MEDI 147.
98. Approaches to the preparation of optically active 1-Azabicyclo[2.2.1]heptan-3-one, a key
intermediate in the synthesis of PD 151832; Barrett SD, Tecle H, Thomas AJ, Caprathe BW, Lauffer DJ, JaenJC; 209th National Meeting - American Chemical Society, Anaheim; March 2-6, 1995. Abstract # MEDI 76.
Lauffer DJ, Davis RE, Mirzadegan T, Moreland DW, Schwarz RD, Thomas AJ, Raby C, Jaen JC; 6th Symposium on Subtypes of Muscarinic Receptors, Fort Lauderdale; November 9-12, 1994. Abstract published in Life Sci. 1995, 56, 1003.
100. Autoradiographic Distinction of High and Low Affinity Muscarinic Receptors by the m1-
Selective Ligand PD 150714. Frey KA, Desmond T, Augelli-Szafran CE, Jaen JC, Schwarz RD; 6th Symposium on Subtypes of Muscarinic Receptors, Fort Lauderdale; November 9-12, 1994. Abstract published in Life Sci. 1995, 56, 1036.
101. Identification and Characterization of m1 Selective Muscarinic Antagonists. Augelli-
Szafran CE, Blankley CJ, Jaen JC, Moreland DW, Nelson CB, Penvose JR, Schwarz RD, Thomas AJ; 6th Symposium on Subtypes of Muscarinic Receptors, Fort Lauderdale; November 9-12, 1994. Abstract published in Life Sci. 1995, 56, 1017.
102. Pharmacological Characterization of PD 150714: An m1 Selective Muscarinic Antagonist.
Nelson C, Augelli-Szafran CE, Callahan M, Jaen JC, Meltzer L, Penvose JR, Schwarz RD, Thomas AJ, Wiley J; 6th Symposium on Subtypes of Muscarinic Receptors, Fort Lauderdale; November 9-12, 1994. Abstract published in Life Sci. 1995, 56, 1017.
103. Pharmacological Characterization of PD 150714: An m1 Selective Muscarinic Antagonist.
Nelson C, Augelli-Szafran CE, Callahan M, Jaen JC, Meltzer L, Penvose JR, Schwarz RD, Thomas AJ, Wiley J; Society for Neuroscience, 24th Annual Meeting, Miami Beach, October 1994. Abstract # 209.2.
104. Esters of 1,4-Disubstituted Tetrahydropyridinecarboxylic Acids as Potential m1 Selective
Muscarinic Antagonists. Augelli-Szafran CE, Blankley CJ, Jaen JC, Moreland DW, Nelson C, Penvose JR, Schwarz RD; Society for Neuroscience, 24th Annual Meeting, Miami Beach, October 1994. Abstract # 209.1.
Thomas AJ, Davis RE, Jaen JC, Lauffer DJ, Mirzadegan T, Moreland DW, Raby C, Schwarz RD, Taylor MD, Tecle H; Society for Neuroscience, 24th Annual Meeting, Miami Beach, October 1994. Abstract # 209.5.
106. Pharmacology of PD 142505 and its Enantiomers. Tecle H, Davis RE, Augelli-Szafran C,
Barrett SD, Caprathe BW, Lauffer DJ, Moreland DW, Schwarz RD, Thomas AJ, Rafferty M, Raby C, Nelson C, Doyle P, Jaen JC; Society for Neuroscience, 24th Annual Meeting, Miami Beach, October 1994. Abstract # 209.6.
MJ, Davis RE, Jaen JC, Lipinski W, Raby C, Spencer CJ, Tecle H; Third International Springfield Symposium on Advances in Alzheimer Therapy; Springfield (Illinois); May 11-15, 1994.
108. The Identification of CI-1002 as a Novel Anticholinesterase and Antidementia Agent.
Gregor VE, Emmerling MR, Schwarz RD, Lee C, Pavia MR, Davis RE, Moos WH, Moore CJ, Jaen JC, Spencer CJ, Callahan MJ, Lipinski WJ, Pugsley TA; 207th National Meeting - American Chemical Society, San Diego; March 13-18, 1994. Abstract # MEDI 171.
109. Development of novel subtype selective muscarinic agonists using recombinant cell lines.
Schwarz R, Davis R, Jaen J, Tecle H, Thomas A; American College of Neuropsychopharmacology (ACNP); Honolulu; December 17, 1993.
110. Identification of PD 143188. A Novel Dopamine Autoreceptor Agonist with Antipsychotic-
like Activity. Wise LD, Caprathe BW, Downing DM, Glase SA, Heffner TG, Jaen JC, Kesten SR, Johnson SJ, Smith SJ, Smith WJ, Wright JL, Wustrow DJ; Society for Neuroscience, 23rd Annual Meeting, Washington, D.C. November 1993. Abstract # 246.1.
111. Subtype Selective Muscarinic Agonists: ‘In vitro’ Pharmacology of a series of 1-azabicyclo-
[2.2.1]heptan-3-one oximes. Davis RE, Doyle PD, Jaen JC, Lauffer DJ, Raby C, Schwarz R, Tecle H, Thomas AJ; Society for Neuroscience, 23rd Annual Meeting, Washington, D.C. November 1993. Abstract # 423.3.
112. Subtype Selective Muscarinic Agonists: ‘In vivo’ Pharmacology of a Series of 1-
Azabicyclo-[2.2.1]heptan-3-one oximes. Callahan MJ, Lipinski WJ, Jaen JC, Lauffer DJ, Tecle H, Thomas AJ, Davis RE; Society for Neuroscience, 23rd Annual Meeting, Washington, D.C. November 1993. Abstract # 423.4.
113. Site-Directed Mutagenesis of Aspartate 103 in the Hm2 Muscarinic Receptor: Effect on
Receptor Binding of arecoline oximes. Schwarz RD, Spencer CJ, Jaen JC, Mirzadegan T, Moreland D, Tecle H, Thomas A, Davis R; Society for Neuroscience, 23rd Annual Meeting, Washington, D.C. November 1993. Abstract # 726.3.
114. Identification of Potent and Selective Sigma Ligands: Design, Synthesis and Structure-
Activity Realtionship of PD 128298 Regioisomers. Tecle H, Pei Y, Jaen JC, Moos WH, Wise
Juan C. Jaen
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LD, Shih Y, Pugsley TA, Heffner TG; Society for Neuroscience, 23rd Annual Meeting, Washington, D.C. November 1993. Abstract # 475.7.
115. Synthetic Strategies in the Preparation of the Dopamine Autoreceptor Agonist PD 128483.
Jaen JC, Caprathe BW, Wise LD, Spence G, Wemple J; 8th European Symposium on Organic Chemistry, Barcelona (Spain), August 29-September 3, 1993.
SA, Heffner TG, Jaen JC, Johnson SJ, Kesten SR, Smith SJ, Smith WJ, Wise LD, Wustrow DJ; 206th National Meeting - American Chemical Society, Chicago; August 22-27, 1993. Abstract # MEDI 22.
117. 1-Azabicyclo[2.2.1heptan-3-one Oximes as Potential m1-Subtype Selective Muscarinic
Agonists. Tecle H, Jaen JC, Augelli-Szafran C, Barrett SD, Caprathe BW, Lauffer DJ, Mirzadegan T, Moos WH, Moreland DW, Pavia MR, Schwarz RD, Thomas AJ, Davis RE; 206th National Meeting - American Chemical Society, Chicago; August 22-27, 1993. Abstract # MEDI 191.
118. Aromatic Butynyl Amines. A New Class of Dopamine Autoreceptor Agonists. Smith SJ,
Wise LD, JaenJC, Glase S, Heffner TG, Pugsley TA, Meltzer LT; 206th National Meeting - American Chemical Society, Chicago; August 22-27, 1993. Abstract # MEDI 173.
119. The Syntheses of PD 143188 and its Analogues. Caprathe BW, Glase SA, Jaen JC,
Johnson SJ, Kesten SR, Smith SJ, Smith WJ, Wise LD, Wright JL, Wustrow DJ; 206th National Meeting – American Chemical Society, Chicago; August 22-27, 1993. Abstract # MEDI 171.
120. The Identification of PD 143188 as a Novel Antipsychotic Agent. Wustrow D, Wise L, Wright
J, Downing D, Caprathe BW, Jaen JC, Smith W, Johnson S, Kesten S, Glase S, Heffner T, Meltzer L, Pugsley T; Medicinal Chemistry Gordon Research Conference, New London, NH; August 2-6, 1993.
121. PD 90780: A Selective Non-Peptide Ligand for the p75 NGF Receptor. Davis RE, Dickerson
M, Fergus J, Hepburn T, Hopkins J, Levine H, Marks J, Spiegel K, Jaen JC, Moos W; Society for Neuroscience, 22nd Annual Meeting, Anaheim, CA; October 1992. Abstract # 544.4.
TG, Pugsley TA, Caprathe BW, Jaen JC, Wise LD; "Dopaminergic Systems and their Regulation", satellite meeting of the XIth International Congress of Pharmacology, Como, Italy; July 8-11, 1990.
129. Novel Dopamine Autoreceptor Agonists. I. 6-Arylpiperazinyl-2-amino-4,5,6,7-tetrahydro-
benzothiazoles. Smith SJ, Jaen JC, Wise LD, Caprathe BW, Heffner TG, Pugsley TA, Meltzer LT; 199th National Meeting – American Chemical Society, Boston, MA; April 22-27, 1990. Abstract # MEDI-95.
130. Novel Dopamine Autoreceptor Agonists. II. 6-Arylpiperazinyl-alkyl-2-amino-4,5,6,7-
tetrahydrobenzo-thiazoles. Caprathe BW, Jaen JC, Wise LD, Heffner TG, Pugsley TA, Meltzer LT; 199th National Meeting – American Chemical Society, Boston, MA; April 22-27, 1990. Abstract # MEDI-96.
131. Dopamine Autoreceptor Agonist Properties of (±)-trans-3,4,4a,10b-Tetrahydro-4-propyl-
2H,5H-[1]- benzopyrano[4,3-b]oxazin-9-ol and Enantiomers. Wise LD, DeWald HA, Heffner TG, Jaen JC, Meltzer LT, Pugsley TA; Society for Neuroscience, 19th Annual Meeting, Phoenix, AZ, November 1989. Abstract # 109.26.
132. Bacterial Mutagenicity Assessment of Structurally Related Quinoline Thiazolamine
Compounds, Potential Antipsychotic Drugs. Kropko ML, Jaen JC, Wold SA, Caprathe BW, Wise LD, Theiss JC; 5th International Conference on Environmental Mutagens, Cleveland, Ohio; July 10-15, 1989. Abstract # 307. Environmental and Molecular Mutagenesis, 1989, 14 (Suppl. 15), 107.
133. Dopamine Autoreceptor Agonist Properties of a Novel Series of 3-(4-Phenyl-1-piperazinyl)-
propoxyaromatic Compounds. Wise LD, DeWald HA, Jaen JC, Caprathe BW, Heffner TG, Pugsley TA; Society for Neuroscience, 18th Annual Meeting, Toronto, Canada; Nov. 1988. Abstract # 151.4.
