公开(公告)号：AT331705T

公开(公告)日：2006-07-15

申请号：AT02291192

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

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：SI1270562T1

公开(公告)日：2004-12-31

申请号：SI200230031

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 ,  A61K31/397 ,  A61K31/40 ,  A61K31/403 ,  A61K31/426 ,  A61K31/4453 ,  A61K31/5375 ,  A61P3/00 ,  A61P3/04 ,  C07D295/18 ,  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：PT1270562E

公开(公告)日：2004-11-30

申请号：PT02291501

申请日：2002-06-17

Applicant: SERVIER LAB

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

IPC: A61K31/16 ,  A61K31/397 ,  A61K31/40 ,  A61K31/403 ,  A61K31/426 ,  A61K31/4453 ,  A61K31/5375 ,  A61P3/00 ,  A61P3/04 ,  C07D295/18 ,  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：AR034516A1

公开(公告)日：2004-02-25

申请号：ARP020102275

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 ,  A61K31/675 ,  A61K31/155 ,  A61K31/401 ,  A61K31/44

Abstract: Compuestos de la fórmula (1) donde A representa un anillo de carbono saturado opcionalmente sustitutido que tiene entre 4 y 8 miembros de anillo, R1 y R4 que pueden ser idénticos o diferentes, representan, cada uno un átomo de hidrógeno o un grupo acilo, R2 y R3 que pueden ser idénticos o diferentes, representan, cada uno, un átomo de hidrógeno o un grupo alquilo, R5 y R6, que pueden ser idénticos o diferentes, representan, cada uno un átomo de hidrógeno o un grupo alquilo, o R5 y R6 juntos, con el átomo de nitrógeno que los lleva, forman un heterociclo con contenido de nitrógeno opcionalmente sustituido, estereoisómeros de los mismos, y también, sales de adición de los mismos con un ácido farmacéuticamente aceptable. Medicamentos antidiabéticos.

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：HK1050357A1

公开(公告)日：2003-06-20

申请号：HK03101863

申请日：2003-03-14

Applicant: SERVIER LAB

Inventor： NANTEUIL GUILLAUME DE ,  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 ,  C07D ,  A61P ,  A61K

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：HK1050186A1

公开(公告)日：2003-06-13

申请号：HK03102394

申请日：2003-04-03

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 ,  C07C ,  C07D ,  A61K ,  A61P

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：HU0201646A2

公开(公告)日：2003-02-28

申请号：HU0201646

申请日：2002-05-14

Applicant: SERVIER LAB

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

IPC: A61K31/40 ,  C07D295/10 ,  A61K31/426 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  C07D207/16 ,  C07D277/04 ,  C07D277/06 ,  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：ZA200204865B

公开(公告)日：2003-02-20

申请号：ZA200204865

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: A61K31/16 ,  A61K31/397 ,  A61K31/40 ,  A61K31/403 ,  C07D295/18 ,  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 ,  C07C ,  C07D ,  A61K ,  A61P

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：ZA200202525B

公开(公告)日：2002-10-24

申请号：ZA200202525

申请日：2002-03-28

Applicant: SERVIER LAB

Inventor： NANTEUIL GUILLAUME DE ,  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 ,  C07D ,  A61K ,  A61P

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.