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11.发明专利
公开(公告)号：CA2383298A1
公开(公告)日：2002-11-15
申请号：CA2383298
申请日：2002-05-10
Applicant: SERVIER LAB
Inventor： NOSJEAN OLIVIER , HUSSON-ROBERT BERNADETTE , DE NANTEUIL GUILLAUME , BENOIST ALAIN , LEVENS NIGEL , BOULANGER MICHELLE , PORTEVIN BERNARD
IPC: C07D295/10 , A61K31/40 , A61K31/426 , A61P3/04 , A61P3/08 , A61P3/10 , C07D207/16 , C07D277/04 , C07D277/06 , C07D295/185 , C07K5/02 , C07D417/02 , C07D207/04 , A61K31/427
Abstract: L'invention concerne de nouveaux composés répondant à la formule (I) (voir formule I) dans laquelle (voir formule II) représente un hétérocycle à 5 chaînons; Ak représente une chaîne alkylène ; X représente une liaison simple ou un groupement phényl~;ne ; R1 et R2, identiques ou différents, représentent chacun un atome d'hydrogène ou un groupement alkyle ; Y représente un groupement CHNO2 ou NR4 dans lequel R4 représente un atome d'hydrogène ou un groupement alkyle ; et R1 représente soit un groupement alkyle, nitro ou cyano, lorsque Y représente CHNO2, soit un groupement nitro ou cyano, lorsque Y représente NR4 ; sous réserve que , lorsque (voir formule III) représente un hétérocycl e azoté à 5 chaînons non substitués, Ak représente un groupement -(CH2)3-, X représente une liaison simple et Y représente NH, R3 ne peut représenter un groupement nitro. L'invention vise également des tautomères et isomères optiques des composés de formule (I), ainsi que leurs sels d'addition à un acide pharmaceutiquement acceptable. Les composés selon l'invention sont utiles en tant qu'inhibiteurs de dipeptidyl-peptidase IV, dans le traitement de l'intolérance au glucose et des maladies associées à l'hyperglycémie.
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公开(公告)号：CA2383298C
公开(公告)日：2008-01-29
申请号：CA2383298
申请日：2002-05-10
Applicant: SERVIER LAB
Inventor： NOSJEAN OLIVIER , DE NANTEUIL GUILLAUME , BOULANGER MICHELLE , PORTEVIN BERNARD , HUSSON-ROBERT BERNADETTE , LEVENS NIGEL , BENOIST ALAIN
IPC: C07D295/10 , C07D417/02 , A61K31/40 , A61K31/426 , A61K31/427 , A61P3/04 , A61P3/08 , A61P3/10 , C07D207/04 , C07D207/16 , C07D277/04 , C07D277/06 , C07D295/185 , C07K5/02
Abstract: L'invention concerne de nouveaux composés répondant à la formule (I) : (voir formule I) dans laquelle (voir formule II) représente un hétérocycle à 5 chaînons; Ak représente une chaîne alkylène ; X représente une liaison simple ou un groupement phénylène ; R1 e t R2, identiques ou différents, représentent chacun un atome d'hydrogène ou un groupement alkyle ; Y représente un groupement CHNO2 ou NR4 dans lequel R4 représente un atome d'hydrogène ou un groupement alkyle ; et R3 représente soit un groupement alkyle, nitro ou cyano, lorsque Y représente CHNO2, soit un groupement nitro ou cyano, lorsque Y représente NR4; sous réserve que , lorsque (voir formule II) représente un hétérocycle azoté à 5 chaînons non substitués, Ak représente un groupement -(CH2)3-, X représente une liaison simple et Y représente NH, R3 ne peut représenter un groupement nitro. L'invention vise également des tautomères et isomères optiques des composés de formule (I), ainsi que leurs sels d'addition à un acide pharmaceutiquement acceptable. Les composés selon l'invention sont utiles en tant qu'inhibiteurs de dipeptidyl-peptidase IV, dans le traitement de l'intolérance au glucose et des maladies associées à l'hyperglycémie.
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公开(公告)号：BR0202313A
公开(公告)日：2003-04-29
申请号：BR0202313
申请日：2002-06-18
Applicant: SERVIER LAB
Inventor： WIERZBICKI MICHEL , JEAN-MARIEFOURQUEZ , 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.
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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.
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公开(公告)号：SK285989B6
公开(公告)日：2008-01-07
申请号：SK8772002
申请日：2002-06-18
Applicant: SERVIER LAB
Inventor： WIERZBICKI MICHEL , FOURQUEZ JEAN-MARIE , LEVENS NIGEL , NOSJEAN OLIVIER , BOULANGER MICHELLE , HUSSON-ROBERT BERNADETTE
IPC: C07D295/00 , A61K31/00 , 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: Described are compounds of the formula (I), in which the substituents have meaning described in claims, method for their preparation and pharmaceutical compositions containing thereof in the treatment of glucose intolerance and of disorders associated with hyperglycaemia, such as type II diabetes or obesity.
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Patent Agency Ranking
公开(公告)号：SI1258476T1
公开(公告)日：2006-10-31
申请号：SI200230350
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: C07D207/00 , A61K31/00 , C07D295/10 , A61K31/40 , A61K31/426 , A61P3/00 , A61P3/04 , A61P3/08 , A61P3/10 , C07D207/16 , C07D277/00 , C07D277/04 , C07D277/06 , C07D295/00 , C07D295/185 , C07K5/02
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公开(公告)号：NO322155B1
公开(公告)日：2006-08-21
申请号：NO20022891
申请日：2002-06-17
Applicant: SERVIER LAB
Inventor： BOULANGER MICHELLE , WIERZBICKI MICHEL , LEVENS NIGEL , NOSJEAN OLIVIER , HUSSON-ROBERT BERNADETTE , FOURQUEZ JEAN-MARIE
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 , C07D237/14 , 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.
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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.
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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.
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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.
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