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Page : 1B.I.C-3000
Chemical
Glibenclamide
5-chloro-N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-2-methoxybenzamide
Product :
name :
Development code :
Owner :
RN :
Boehringer Mannheim
Mp Bp :
Gen. Form. : C23H28ClN3O5S
10238-21-8
MW :
Producer :
Reactions :Phosgene
References :
Uses : Antidiabetic
Launching date :Priority date :
Other names :
Update :
Brand :
1966
Azuglucon (Azupharma: Germany)
Bastiverit (Bastian-Werk: Germany)
Calabren (Berk: UK)
Daonil (Hoechst: Australia, Belgium, Eire, Italy, Netherlands, Norway, South Africa, Spain, Sweden,
Switzerland, UK); (Hoechst Houde: France)
Dia-BASF (BASF Generics: Germany)
Diabeta (HMR: USA)
Dia-Eptal (Montavit: Austria)
Duraglucon-N (Durachemie: Germany)
Euglucan (Boehringer Mannheim: France)
Euglucon (Boehringer Mannheim: Australia, Austria, Belgium, Canada, Germany, Italy, Netherlands,
Norway, South Africa, Spain, Sweden, Switzerland); (Roussel: Eire, UK)
Gen-Glybe (Genpharm: Canada)
Gewaglucon (Nycomed: Austria)
Gilemal (Enzypharm: Austria)
Glucolon (Sabater: Spain)
Gli-Basan (Schonenberger: Switzerland)
Gliben (Gentili: Italy); (ct-Arzneimittel: Germany)
Glibenbeta (Betapharm: Germany)
Glibenclamid (R.A.N.-Pharm: Germany); (3M Medica: Germany); (Heumann: Germany); (Aliud Pharma:
Germany); (Basics Pharma: Germany); (Ratiopharm: Germany)
Glibenhexal (Hexal: Germany)
Gliben-Puren N (Isis Puren: Germany)
13/08/2015(C) Becker Associates 1999
Page : 2B.I.C-3000
Glibesifar (Siphar: Switzerland)
Glibetic (Teva: Israel)
Gliboral (Guidotti: Italy)
Glidanil (Montpellier: Argentina)
Glimidstada (Stada: Germany)
Glucobene (Merckle: Austria)
Glucolon (Sabater: Spain)
Gluconorm (Wolff: Germany)
Glucoremed (Lichtenstein: Germany)
Gluco-Tablinen (Sanorania: Germany)
Glucoven (Chinoin: Mexico)
Glukoreduct (Sanofi Winthrop: Germany)
Glukovital (Wolff: Germany)
Glyben (Rolab: South Africa)
Glycolande N (Synthelabo: Germany)
Glynase (Upjohn: USA)
Hemi-Daonil (Hoechst Houde: France); (Hoechst: Netherlands)
Humedia (APS: Germany)
Lisaglucon (Farmasa: Brazil)
Maninil (Berlin-Chemie: Germany)
Melix (Pharmador: South Africa); (Lagap: Switzerland)
Micronase (Upjohn: USA)
Miglucan (Boehringer Mannheim: France)
Neogluconin (Waldheim Pharmazeutika: Austria)
Normoglucon (Klinge: Austria)
Praeciglucon (Boehringer Mannheim: Germany)
Semi-Daonil (Hoechst: Austria, Eire, South Africa, Switzerland, UK)
Semi-Englucon (Boehringer Mannheim: Austria, Netherlands, Switzerland); (Hoechst: Austria)
Semi-Gliben-Puren (Isis Puren: Germany)
Market : launched
Comments :
Intermediates:I phenylacetonitrile
II 4-(chlorosulfonyl)benzeneacetonitrile
III 4-(cyanomethyl)benzenesulfonamide
IV 4-(2-aminoethyl)benzenesulfonamide
V 5-chloro-2-methoxybenzoic acid
VI 5-chloro-N-[2-[4-(aminosulfonyl)phenyl]ethyl]-2-methoxybenzamide
VII cyclohexyl isocyanate
VIII 5-chlorosalicylic acid
Reaction Sequences :
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Chemical
Glipizide
N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-5-methylpyrazinecarboxamide
Product :
name :
Development code :
Owner :
RN :
Carlo Erba
Mp Bp :
Gen. Form. : C21H27N5O4S
29094-61-9
MW :
Producer :
Reactions :Phosgene
References :Ger Offen DE 2,012,138 (1970), IT Appl. 26 Mar 1969 (Carlo Erba)
Uses : Antidiabetic
Launching date :Priority date :
Other names :
Update :
Brand :
1970
Glibenese (Pfizer: Austria, France, Germany, Netherlands, Spain, Switzerland, UK)
Glutotrol (Pfizer: USA)
Melizid (Medica: Finland)
Minibetic (Ikapharm: Israel)
Minidiab (Farmitalia Carlo Erba: Norway); (Pharmacia: Sweden); (Pharmacia & Upjohn: France)
Minodiab (Pharmacia & Upjohn: UK)
Ozidia (Pfizer: France)
Market : launched
Comments :
Intermediates:I chloroacetone
II ammonia
III 2,5-dimethylpyrazine
IV 5-methyl-2-pyrazinecarboxylic acid
V 5-methyl-2-pyrazinecarbonyl chloride
VI 4-(2-aminoethyl)benzenesulfonamide
VII N-[2-[4-(aminosulfonyl)phenyl]ethyl]-5-methylpyrazinecarboxamide
VIII cyclohexyl isocyanate
IX phenylacetonitrile
X 4-(chlorosulfonyl)benzeneacetonitrile
XI 4-(cyanomethyl)benzenesulfonamide
Reaction Sequences :
13/08/2015(C) Becker Associates 1999
Page : 5B.I.C-3000
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Chemical
Gliquidone
N-[(cyclohexylamino)carbonyl]-4-[2-(3,4-dihydro-7-methoxy-4,4-dimethyl-1,3-dioxo-2(1H)-isoquinolinyl)ethyl]benzenesulfonamide
Product :
name :
Development code :
Owner :
RN :
Boehringer Ingelheim
Mp Bp :
Gen. Form. : C27H33N3O6S
33342-05-1
MW :
Producer :
Reactions :Phosgene
References :U.S. US 4,523,023 (1985), DE Appl. 3,306,200, 23 Feb. 1983 (Haarmann & Reimer)
U.S. US 3,708,486 (1973), DE Appl. 19,19,570, 17 Apr. 1969 (Boehringer Ingelheim)
Uses : Antidiabetic
Launching date :Priority date :
Other names :
Update :
Brand :
1969
Glurenor (Guidotti: Italy)
Glurenor (Europharma: Spain)
Glurenorm (Bender: Austria); (Menarini: Belgium); (Yamanouchi: Germany); (Sanofi Winthrop: UK)
Market : launched
Comments :
Intermediates:I 1,2,3,4-tetrahydro-2,4,4-trimethylisoquinoline-1,3-dione
II 1,2,3,4-tetrahydro-2,4,4-trimethyl-7-nitroisoquinoline-1,3-dione
III 7-amino-1,2,3,4-tetrahydro-2,4,4-trimethylisoquinoline-1,3-dione
IV (3,4-dihydro-2,4,4-trimethyl-1,3-dioxo-1H-isoquinolin-7-yl)diazonium chloride
V 7-hydroxy-1,2,3,4-tetrahydro-2,4,4-trimethylisoquinoline-1,3-dione
VI 1,2,3,4-tetrahydro-7-methoxy-2,4,4-trimethylisoquinoline-1,3-dione
VII 7-methoxy-4,4-dimethyl-1H-benzo[c]pyran-1,3(4H)-dione
VIII 4-(2-aminoethyl)benzenesulfonamide
IX 4-[2-(3,4-dihydro-7-methoxy-4,4-dimethyl-1,3-dioxo-2(1H)-isoquinolinyl)ethyl]benzenesulfonamide
X cyclohexyl isocyanate
XI benzeneacetonitrile
XII 4-(cyanomethyl)benzenesulfonyl chloride
XIII 4-(cyanomethyl)benzenesulfonamide
Reaction Sequences :
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Chemical
Glisentide
N-[2-[4-[[[(cyclopentylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-2-methoxybenzamide
Product :
name :
Development code :
Owner :
RN :
Uriach
Mp Bp :
Gen. Form. : C22H27N3O5S
32797-92-5
MW :
Producer :
Reactions :Phosgene
References :
Uses : Antidiabetic
Launching date :Priority date :
Other names :
Update :
Brand :
1970
Staticum (Uriach: Spain)
Market : launched
Comments :
Intermediates:I phenylacetonitrile
II 4-(chlorosulfonyl)benzeneacetonitrile
III 4-(cyanomethyl)benzenesulfonamide
IV 4-(2-aminoethyl)benzenesulfonamide
V 2-methoxybenzoyl chloride
VI N-[2-[4-(aminosulfonyl)phenyl]ethyl]-2-methoxybenzamide
VII cyclopentyl isocyanate
VIII 2-methoxybenzoic acid
Reaction Sequences :
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Page : 10B.I.C-3000
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Page : 11B.I.C-3000
Chemical
Glisolamide
N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-5-methyl-3-isoxazolecarboxamide
Product :
name :
Development code :
Owner :
RN :
IFI
Mp Bp :
Gen. Form. : C20H25N4O5S
24477-37-0
MW :
Producer :
Reactions :Phosgene
References :
Uses : Antidiabetic
Launching date :Priority date :
Other names :
Update :
Brand :
1967
Diabenor (IFI: Italy)
Market : launched
Comments :
Intermediates:I acetone
II oxalic acid diethyl ester
III 2,4-dioxopentanoic acid ethyl ester
IV hydroxylamine
V 5-methyl-3-isoxazolecarboxylic acid ethyl ester
VI 5-methyl-3-isoxazolecarboxylic acid
VII 5-methyl-3-isoxazolecarbonyl chloride
VIII 4-(2-aminoethyl)benzenesulfonamide
IX N-[2-[4-(aminosulfonyl)phenyl]ethyl]-5-methyl-3-isoxazolecarboxamide
X cyclohexyl isocyanate
XI phenylacetonitrile
XII 4-(chlorosulfonyl)benzeneacetonitrile
XIII 4-(cyanomethyl)benzenesulfonamide
Reaction Sequences :
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Chemical
Glisoxepide
N-[2-[4-[[[[(hexahydro-1H-azepin-1-yl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-5-methyl -3-isoxazolecarboxamide
Product :
name :
Development code :
Owner :
RN :
Bayer
Mp Bp :
Gen. Form. : C20H27N5O5S
25046-79-1
MW :
Producer :
Reactions :
References :
Uses : Antidiabetic
Launching date :Priority date :
Other names :
Patent InformationUpdate :
Brand :
1969
Pro-Diaban (Bayer: Austria, Germany)
Market : launched
Comments :
Intermediates:I acetone
II oxalic acid diethyl ester
III 2,4-dioxopentanoic acid ethyl ester
IV hydroxylamine
V 5-methyl-3-isoxazolecarboxylic acid ethyl ester
VI 5-methyl-3-isoxazolecarboxylic acid
VII 5-methyl-3-isoxazolecarbonyl chloride
VIII 4-(2-aminoethyl)benzenesulfonamide
IX N-[2-[4-(aminosulfonyl)phenyl]ethyl]-5-methyl-3-isoxazolecarboxamide
X chloroformic acid methyl ester
XI N-[2-[4-[[(methoxycarbonyl)amino]sulfonyl]phenyl]ethyl]-5-methyl-3-isoxazolecarboxamide
XII 1-aminohexahydroazepine
XIII phenylacetonitrile
XIV 4-(chlorosulfonyl)benzeneacetonitrile
XV 4-(cyanomethyl)benzenesulfonamide
XVI epsilon-caprolactam
XVII hexahydro-1H-azepine
XVIII hexahydro-1-nitroso-1H-azepine
Reaction Sequences :
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