公开(公告)号：DK1258476T3

公开(公告)日：2006-10-30

申请号：DK02291192

申请日：2002-05-14

Applicant: SERVIER LAB

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

IPC: C07D207/16 ,  C07D295/10 ,  A61K31/40 ,  A61K31/426 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  C07D277/04 ,  C07D277/06 ,  C07D295/18 ,  C07D295/185 ,  C07K5/02

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：DE60208763T2

公开(公告)日：2006-09-28

申请号：DE60208763

申请日：2002-03-27

Applicant: SERVIER LAB

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

IPC: C07D295/18 ,  A61K31/395 ,  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 ,  C07K5/06 ,  C07K5/062 ,  C07K5/078 ,  C07K5/087 ,  C07K5/097

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：DE60212759D1

公开(公告)日：2006-08-10

申请号：DE60212759

申请日：2002-05-14

Applicant: SERVIER LAB

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

IPC: C07D207/16 ,  C07D295/10 ,  A61K31/40 ,  A61K31/426 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  C07D277/04 ,  C07D277/06 ,  C07D295/18 ,  C07D295/185 ,  C07K5/02

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：SI1245568T1

公开(公告)日：2006-04-30

申请号：SI200230261

申请日：2002-03-27

Applicant: SERVIER LAB

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

IPC: C07D295/00 ,  C07D295/18 ,  A61K31/00 ,  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 ,  C07D207/00 ,  C07D207/16 ,  C07D231/00 ,  C07D231/04 ,  C07D233/00 ,  C07D233/06 ,  C07D233/48 ,  C07D277/00 ,  C07D277/04 ,  C07D277/06 ,  C07D277/10 ,  C07D295/22 ,  C07D403/12 ,  C07K5/00 ,  C07K5/062 ,  C07K5/078 ,  C07K5/087 ,  C07K5/097

公开(公告)号：AT316080T

公开(公告)日：2006-02-15

申请号：AT02290755

申请日：2002-03-27

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 ,  A61K31/395 ,  C07K5/06

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：AU781822B2

公开(公告)日：2005-06-16

申请号：AU4882202

申请日：2002-06-18

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 ,  C07D209/08

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：DK1270562T3

公开(公告)日：2005-01-24

申请号：DK02291501

申请日：2002-06-17

Applicant: SERVIER LAB

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

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

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：DE60201296D1

公开(公告)日：2004-10-28

申请号：DE60201296

申请日：2002-06-17

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

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：PL354565A1

公开(公告)日：2002-12-30

申请号：PL35456502

申请日：2002-06-17

Applicant: SERVIER LAB

Inventor： WIERZBICKI MICHEL ,  FOURQUES JEAN-MARIE ,  LEVENS NIGEL ,  HUSSON-ROBERT BERNARDETTE ,  NOSJEAN OLIVIER ,  BOULANGER MICHELLE

IPC: A61K31/16 ,  A61K31/397 ,  A61K31/40 ,  C07D295/18 ,  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 ,  C07C237/32

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：NO20022891L

公开(公告)日：2002-12-19

申请号：NO20022891

申请日：2002-06-17

Applicant: SERVIER LAB

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

IPC: A61K31/16 ,  C07D295/18 ,  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 ,  C07D207/02

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.