公开(公告)号：FR2826003A1

公开(公告)日：2002-12-20

申请号：FR0107934

申请日：2001-06-18

Applicant: SERVIER LAB

Inventor： WIERZBICKI MICHEL ,  FOURQUEZ JEAN MARIE ,  LEVENS NIGEL ,  HUSSON ROBERT BERNADETTE ,  NOSJEAN OLIVIER ,  BOULANGER MICHELLE

IPC: C07D295/18 ,  A61K31/16 ,  A61K31/397 ,  A61K31/40 ,  A61K31/403 ,  A61K31/426 ,  A61K31/4453 ,  A61K31/5375 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  C07C237/14 ,  C07D205/04 ,  C07D207/18 ,  C07D207/20 ,  C07D209/02 ,  C07D209/52 ,  C07D277/04 ,  C07D277/22 ,  C07D295/185 ,  C07D207/12

Abstract: Cyclic alpha- amino gamma-hydroxy amides (I), their stereoisomers, and acid addition salts are new. Cyclic alpha- amino gamma-hydroxy amides (I), their stereoisomers, and acid addition salts are new. ring A = 4-8 membered saturated C ring that may be substituted by one or more 1-6C alkyl groups; R1 and R4 = H or 1-6C acyl; R2 and R3 = H or 1-6C alkyl; R5 and R6 = H, 1-6C alkyl, or together with the N atom form a saturated mono- or bicyclic nitrogen heterocycle having 1-3 heteroatoms (additional heteroatoms being O, N, or S) optionally substituted by one or more groups CN, COOR7, COR7, NO2, CONR8aR8b, S(O)nR9, or PO3R10aR10b; R7 = H or 1-6C alkyl; R8a and R8b = H, 1-6C alkyl or together form a N heterocycle as defined; R9 = H, 1-6C alkyl, or phenyl, biphenyl, naphthyl, or tetrahydronaphthyl all these aryl groups being optionally substituted by halogen, 1-6C alkyl or alkoxy, OH, 1-6C polyhalolalkyl, NO2, or 1 or 2 C alkylene dioxy; R10a and R10b = H or 1-6C alkyl; n = 1, 2, or 3.

公开(公告)号：FR2824825B1

公开(公告)日：2005-05-06

申请号：FR0106375

申请日：2001-05-15

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  BENOIST ALAIN ,  LEVENS NIGEL ,  NOSJEAN OLIVIER ,  HUSSON ROBERT BERNADETTE ,  BOULANGER MICHELLE

IPC: C07D295/10 ,  A61K31/40 ,  A61K31/426 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  C07D207/16 ,  C07D277/04 ,  C07D277/06 ,  C07D295/185 ,  C07K5/02 ,  C07D207/42

Abstract: Alpha amino acid derivatives (I), their optical isomers and addition salts, are new. Alpha amino acid derivatives of formula (I), their optical isomers and addition salts, are new: A = five-membered heterocycle, optionally substituted by a cyano group; Ak = 1-6C alkylene; X = single bond or phenylene; R1, R2, R4 = H or 1-6C alkyl; Y = NR4 or CH-NO2; R3 = NO2 or CN; and provided that: (i) when Y is CH-NO2, then R3 may further be 1-6C alkyl; and (ii) when A is unsubstituted, then Ak is propylene, X is a bond, Y is NH and R3 is NO2, are excluded.

公开(公告)号：FR2822826A1

公开(公告)日：2002-10-04

申请号：FR0104142

申请日：2001-03-28

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  BENOIST ALAIN ,  LEVENS NIGEL ,  NOSJEAN OLIVIER ,  HUSSON ROBERT BERNADETTE

IPC: C07D295/18 ,  A61K31/40 ,  A61K31/4178 ,  A61K31/426 ,  A61K31/5377 ,  A61K38/00 ,  A61P1/00 ,  A61P1/02 ,  A61P3/04 ,  A61P3/10 ,  A61P31/18 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07B57/00 ,  C07D207/16 ,  C07D231/04 ,  C07D233/06 ,  C07D233/48 ,  C07D277/04 ,  C07D277/06 ,  C07D277/10 ,  C07D295/22 ,  C07D403/12 ,  C07K5/062 ,  C07K5/078 ,  C07K5/087 ,  C07K5/097 ,  C07D207/08

Abstract: Sulfonated amino acid derivatives (I), their optical isomers and acid addition salts, are new. Sulfonated amino acid derivatives (I), their optical isomers and acid addition salts, are new. ring A = a 5 membered nitrogen heterocycle that may be substituted by cyano; R1 = H, 1-6C alkyl or acyl, prolyl, alanyl, histidylprolyl, or phenylalanylprolyl; Ak = 1-6C alkylene or heteroalkylene; X = a bond or phenylene optionally substituted by one or more groups selected from halogens, 1-6C alkyl, alkoxy or polyhaloalkyl, or OH; R2 = 1-6C alkyl (optionally substituted by one or more groups selected from aryl, 1-6C alkylsulfonyl, 3-7C cycloalkylsulfonyl, 3-7C cycloalkyl, and halogen), 3-10C cycloalkyl, or a group -NR2aR2b; R2a and R2b = H, 1-6C alkyl, or together with the N atom they form a nitrogen heterocycle; Y = -NR3, -NH-CH=N-, -C(=NH)-NH-, or -NR4-C(=NR5)-NR6-; R3 = H, 1-6C alkyl, 3-7C cycloalkyl, or aryl; R4, R5, R6 = H, 1-6C alkyl; or R4 and R6 together, or R5 and R6 together = imidazolidine or dihydrobenzimidazole in which the term nitrogen heterocycle encompasses a monocyclic saturated ring of 5 - 7 members having 1 - 3 heteroatoms at least one of which is N and others may be N, O or S, and the term 1-6c alkylene encompasses a group that may be straight or branched and one methylene group may be replaced by an atom or O or S.

公开(公告)号：FR2835523B1

公开(公告)日：2004-04-16

申请号：FR0201409

申请日：2002-02-06

Applicant: SERVIER LAB

Inventor： DASSONVILLE ALEXANDRA ,  BRETECHE ANNE ,  DUFLOS MURIEL ,  LE BAUT GUILLAUME ,  PFEIFFER BRUNO ,  RENARD PIERRE ,  LEVENS NIGEL ,  HUSSON ROBERT BERNADETTE

IPC: A61K31/122 ,  A61K31/222 ,  A61K31/4402 ,  A61P3/10 ,  C07C45/00 ,  C07C45/28 ,  C07C46/00 ,  C07C46/10 ,  C07C50/28 ,  C07C50/30 ,  C07D213/50

Abstract: Compound of formula (I): wherein: R 1 and R 2 , which may be identical or different, each represents hydrogen, acyl or alkyl, Ar represents aryl or heteroaryl, A represents a group selected from: R 4 represents hydrogen or alkyl, R 5 represents hydrogen, alkyl, aryl or heteroaryl, R 3 represents aryl, heteroaryl, dicyclopropylmethyl or benzhydryl, or A-R 3 represents an optionally substituted naphthyl group, with the exclusion of 2,5-dihydroxy-3-(4-methoxyphenyl)-6-(2-phenylethenyl)-1,4-benzoquinone, 2,5-dihydroxy-3-(4-methoxyphenyl)-6-(2-naphthyl)-1,4-benzoquinone and 2,5-dihydroxy-3-(2-naphthyl)-6-phenyl-1,4-benzoquinone. Medicinal products containing the same which are useful in the treatment of diseases associated with a deregulation of glycaemia.

公开(公告)号：FR2826003B1

公开(公告)日：2003-08-15

申请号：FR0107934

申请日：2001-06-18

Applicant: SERVIER LAB

Inventor： WIERZBICKI MICHEL ,  FOURQUEZ JEAN MARIE ,  LEVENS NIGEL ,  HUSSON ROBERT BERNADETTE ,  NOSJEAN OLIVIER ,  BOULANGER MICHELLE

IPC: C07D295/18 ,  A61K31/16 ,  A61K31/397 ,  A61K31/40 ,  A61K31/403 ,  A61K31/426 ,  A61K31/4453 ,  A61K31/5375 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  C07C237/14 ,  C07D205/04 ,  C07D207/18 ,  C07D207/20 ,  C07D209/02 ,  C07D209/52 ,  C07D277/04 ,  C07D277/22 ,  C07D295/185 ,  C07D207/12

Abstract: A compound of formula (I):wherein:represents an optionally substituted saturated carbon ring having from 4 to 8 ring members,R1 and R4, which may be identical or different, each represents hydrogen or acyl,R2 and R3, which may be identical or different, each represents hydrogen or alkyl,R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle,stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid.Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.

公开(公告)号：FR2835523A1

公开(公告)日：2003-08-08

申请号：FR0201409

申请日：2002-02-06

Applicant: SERVIER LAB

Inventor： DASSONVILLE ALEXANDRA ,  BRETECHE ANNE ,  DUFLOS MURIEL ,  LE BAUT GUILLAUME ,  PFEIFFER BRUNO ,  RENARD PIERRE ,  LEVENS NIGEL ,  HUSSON ROBERT BERNADETTE

IPC: A61K31/122 ,  A61K31/222 ,  A61K31/4402 ,  A61P3/10 ,  C07C45/00 ,  C07C45/28 ,  C07C46/00 ,  C07C46/10 ,  C07C50/28 ,  C07C50/30 ,  C07D213/50

Abstract: Compound of formula (I): wherein: R 1 and R 2 , which may be identical or different, each represents hydrogen, acyl or alkyl, Ar represents aryl or heteroaryl, A represents a group selected from: R 4 represents hydrogen or alkyl, R 5 represents hydrogen, alkyl, aryl or heteroaryl, R 3 represents aryl, heteroaryl, dicyclopropylmethyl or benzhydryl, or A-R 3 represents an optionally substituted naphthyl group, with the exclusion of 2,5-dihydroxy-3-(4-methoxyphenyl)-6-(2-phenylethenyl)-1,4-benzoquinone, 2,5-dihydroxy-3-(4-methoxyphenyl)-6-(2-naphthyl)-1,4-benzoquinone and 2,5-dihydroxy-3-(2-naphthyl)-6-phenyl-1,4-benzoquinone. Medicinal products containing the same which are useful in the treatment of diseases associated with a deregulation of glycaemia.

公开(公告)号：FR2822826B1

公开(公告)日：2003-05-09

申请号：FR0104142

申请日：2001-03-28

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  BENOIST ALAIN ,  LEVENS NIGEL ,  NOSJEAN OLIVIER ,  HUSSON ROBERT BERNADETTE

IPC: C07D295/18 ,  A61K31/40 ,  A61K31/4178 ,  A61K31/426 ,  A61K31/5377 ,  A61K38/00 ,  A61P1/00 ,  A61P1/02 ,  A61P3/04 ,  A61P3/10 ,  A61P31/18 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07B57/00 ,  C07D207/16 ,  C07D231/04 ,  C07D233/06 ,  C07D233/48 ,  C07D277/04 ,  C07D277/06 ,  C07D277/10 ,  C07D295/22 ,  C07D403/12 ,  C07K5/062 ,  C07K5/078 ,  C07K5/087 ,  C07K5/097 ,  C07D207/08

Abstract: Sulfonated amino acid derivatives (I), their optical isomers and acid addition salts, are new. Sulfonated amino acid derivatives (I), their optical isomers and acid addition salts, are new. ring A = a 5 membered nitrogen heterocycle that may be substituted by cyano; R1 = H, 1-6C alkyl or acyl, prolyl, alanyl, histidylprolyl, or phenylalanylprolyl; Ak = 1-6C alkylene or heteroalkylene; X = a bond or phenylene optionally substituted by one or more groups selected from halogens, 1-6C alkyl, alkoxy or polyhaloalkyl, or OH; R2 = 1-6C alkyl (optionally substituted by one or more groups selected from aryl, 1-6C alkylsulfonyl, 3-7C cycloalkylsulfonyl, 3-7C cycloalkyl, and halogen), 3-10C cycloalkyl, or a group -NR2aR2b; R2a and R2b = H, 1-6C alkyl, or together with the N atom they form a nitrogen heterocycle; Y = -NR3, -NH-CH=N-, -C(=NH)-NH-, or -NR4-C(=NR5)-NR6-; R3 = H, 1-6C alkyl, 3-7C cycloalkyl, or aryl; R4, R5, R6 = H, 1-6C alkyl; or R4 and R6 together, or R5 and R6 together = imidazolidine or dihydrobenzimidazole in which the term nitrogen heterocycle encompasses a monocyclic saturated ring of 5 - 7 members having 1 - 3 heteroatoms at least one of which is N and others may be N, O or S, and the term 1-6c alkylene encompasses a group that may be straight or branched and one methylene group may be replaced by an atom or O or S.

公开(公告)号：FR2824825A1

公开(公告)日：2002-11-22

申请号：FR0106375

申请日：2001-05-15

Applicant: SERVIER LAB

Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  BENOIST ALAIN ,  LEVENS NIGEL ,  NOSJEAN OLIVIER ,  HUSSON ROBERT BERNADETTE ,  BOULANGER MICHELLE

IPC: C07D295/10 ,  A61K31/40 ,  A61K31/426 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  C07D207/16 ,  C07D277/04 ,  C07D277/06 ,  C07D295/185 ,  C07K5/02 ,  C07D207/42

Abstract: Alpha amino acid derivatives (I), their optical isomers and addition salts, are new. Alpha amino acid derivatives of formula (I), their optical isomers and addition salts, are new: A = five-membered heterocycle, optionally substituted by a cyano group; Ak = 1-6C alkylene; X = single bond or phenylene; R1, R2, R4 = H or 1-6C alkyl; Y = NR4 or CH-NO2; R3 = NO2 or CN; and provided that: (i) when Y is CH-NO2, then R3 may further be 1-6C alkyl; and (ii) when A is unsubstituted, then Ak is propylene, X is a bond, Y is NH and R3 is NO2, are excluded.