公开(公告)号：US06593312B2

公开(公告)日：2003-07-15

申请号：US10173993

申请日：2002-06-18

申请人： Michel Wierzbicki ,  Jean-Marie Fourquez ,  Nigel Levens ,  Bernadette Husson-Robert ,  Olivier Nosjean ,  Michelle Boulanger

发明人： Michel Wierzbicki ,  Jean-Marie Fourquez ,  Nigel Levens ,  Bernadette Husson-Robert ,  Olivier Nosjean ,  Michelle Boulanger

IPC分类号： A61K31425

CPC分类号： C07C237/14 ,  C07C2601/08 ,  C07C2601/14 ,  C07D205/04 ,  C07D207/20 ,  C07D209/52 ,  C07D277/04 ,  C07D295/185

摘要： 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.

摘要翻译： 式（I）的化合物：其中：表示任选取代的具有4至8个环成员的饱和碳环，可以相同或不同的R 1和R 4各自表示氢或酰基，R 2和R 3可以相同 或不同的，各自表示氢或烷基，R 5和R 6可以相同或不同，各自表示氢或烷基，或者R 5和R 6一起与带有氮原子一起形成任选取代的含氮杂环，其立体异构体 ，以及其与药学上可接受的酸的加成盐。含有该药物的药物可用于治疗葡萄糖不耐症或与高血糖相关的病症。

公开(公告)号：US06706742B2

公开(公告)日：2004-03-16

申请号：US10146272

申请日：2002-05-15

申请人： Guillaume De Nanteuil ,  Bernard Portevin ,  Alain Benoist ,  Nigel Levens ,  Olivier Nosjean ,  Bernadette Husson-Robert ,  Michelle Boulanger

发明人： Guillaume De Nanteuil ,  Bernard Portevin ,  Alain Benoist ,  Nigel Levens ,  Olivier Nosjean ,  Bernadette Husson-Robert ,  Michelle Boulanger

IPC分类号： C07D27704

CPC分类号： C07D295/185 ,  C07D207/16 ,  C07D277/04 ,  C07D277/06 ,  Y02P20/55

摘要： Compound selected from those of formula (I): wherein: represents an optionally substituted 5-membered nitrogen-containing heterocycle, Ak represents an alkylene chain, X represents a single bond or phenylene, R1 and R2, which may be identical or different, each represent hydrogen or alkyl, R3 represents alkyl, nitro or cyano, Y represents NR4 or CHNO2, R4 represents hydrogen or alkyl, its tautomers when they exist, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid, with the exclusion of compounds wherein, simultaneously, represents an unsubstituted 5-membered nitrogen-containing heterocycle, Ak represents —(CH2)3—, X represents a single bond, Y represents NH and R3 represents nitro. Medicinal products containing the same which are useful as dipeptidyl peptidase IV inhibitors.

摘要翻译： 选自式（I）的化合物的化合物：其中：表示任选取代的5元含氮杂环，Ak表示亚烷基链，X表示单键或亚苯基，R 1和R 2可以相同或不同，各自相同或不同 代表氢或烷基，R3代表烷基，硝基或氰基，Y代表NR4或CHNO2，R4代表氢或烷基，其互变异构体存在时，其光学异构体及其与药学上可接受的酸的加成盐，排除化合物 其中，同时代表未取代的5元含氮杂环，Ak表示 - （CH2）3-，X表示单键，Y表示NH，R3表示硝基。含有该二价基团的肽酶IV 抑制剂。

公开(公告)号：US06716843B2

公开(公告)日：2004-04-06

申请号：US10109407

申请日：2002-03-28

申请人： Guillaume De Nanteuil ,  Bernard Portevin ,  Alain Benoist ,  Nigel Levens ,  Olivier Nosjean ,  Bernadette Husson-Robert

发明人： Guillaume De Nanteuil ,  Bernard Portevin ,  Alain Benoist ,  Nigel Levens ,  Olivier Nosjean ,  Bernadette Husson-Robert

IPC分类号： A61K3140

CPC分类号： C07D277/04 ,  C07D207/16 ,  C07D231/04 ,  C07D233/06 ,  C07D277/06 ,  C07D277/10 ,  Y02P20/55

摘要： Compound of formula (I): wherein:  represents an optionally substituted, 5-membered, nitrogen-containing heterocycle, R1 represents hydrogen, alkyl, acyl, prolyl, alanyl, histidylprolyl or phenylalanylprolyl, Ak represents an alkylene or heteroalkylene chain, X represents a single bond or optionally substituted phenylene, R2 represents optionally substituted alkyl, (C3-C10)cycloalkyl, or —NR2aR2b wherein R2a and R2b, which may be the same or different, each represent hydrogen or alkyl or, together with the nitrogen atom carrying them, form a nitrogen-containing heterocycle, Y represents R3 represents hydrogen or a group selected from alkyl, (C3-C7) cycloalkyl and aryl, R4, R5 and R6, which may be the same or different, each represent hydrogen or alkyl, or R4 and R6, or R5 and R6, together with the atoms carrying them, form an imidazolidine or dihydrobenzimidazole ring, its optical isomers and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful as inhibitors of dipeptidyl-peptidase IV.

摘要翻译： 式（I）化合物：其中：表示任选取代的5元含氮杂环，R 1表示氢，烷基，酰基，脯氨酰基，丙氨酰，组氨酰脯氨酰基或苯丙氨酰脯氨酰基，Ak表示亚烷基或杂亚烷基链，X表示 单键或任选取代的亚苯基，R 2表示任选取代的烷基，（C 3 -C 10）环烷基或-NR 2 a R 2b，其中可以相同或不同的R 2a和R 2b各自代表氢或烷基，或与携带它们的氮原子一起 ，形成含氮杂环，Y表示R 3表示氢或选自烷基，（C 3 -C 7）环烷基和芳基的基团，R 4，R 5和R 6可以相同或不同，各自表示氢或烷基，或R 4 和R6或R5和R6与携带它们的原子一起形成咪唑烷或二氢苯并咪唑环，其光学异构体及其与药学上可接受的酸的加成盐。含有相同的喔 ch可用作二肽基肽酶IV的抑制剂。