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22 条记录 (耗时 0.048 秒)

    Alpha-amino-acid compounds
    1.
    发明授权
    Alpha-amino-acid compounds 失效
    α-氨基酸化合物

    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。

    Alpha-amino acid sulphonyl compounds
    2.
    发明授权
    Alpha-amino acid sulphonyl compounds 失效
    α-氨基酸磺酰基化合物

    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。

    Piperidine compounds
    5.
    发明授权
    Piperidine compounds 失效
    哌啶化合物

    公开(公告)号：US5652246A

    公开(公告)日：1997-07-29

    申请号：US546263

    申请日：1995-10-20

    申请人： Guillaume de Nanteuil ,  Georges Remond ,  Bernard Portevin ,  Jacqueline Bonnet ,  Emmanuel Canet ,  Graham Birrell

    发明人： Guillaume de Nanteuil ,  Georges Remond ,  Bernard Portevin ,  Jacqueline Bonnet ,  Emmanuel Canet ,  Graham Birrell

    IPC分类号： A61K31/4427 ,  A61K31/445 ,  A61P1/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D401/06 ,  C07D471/04 ,  C07D471/02 ,  A61K31/415 ,  A61K31/44 ,  C07D235/22

    CPC分类号： C07D401/06 ,  C07D471/04

    摘要： The invention relates to the compounds of formula (I): ##STR1## in which: R.sub.1 represents alkyl, phenyl, naphthyl, pyridyl or thienyl group, each phenyl, naphthyl, pyridyl or thienyl optionally being substituted,R.sub.2 represents a hydrogen atom or a substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, cycloalkyl, piperidino or substituted or unsubstituted amino group,X represents CO or SO.sub.2,R.sub.3 represents hydrogen or alkyl,R.sub.4 represents alkyl, substituted or unsubstituted phenyl or trihalomethyl, or else R.sub.3 and R.sub.4 form, together with the carbon atoms which carry them, cyclo(C.sub.3 -C.sub.7)alkenyl,A represents phenyl, naphthyl or pyridyl ring, each phenyl, naphthyl or pyridyl ring optionally being substituted,their isomers, the corresponding quaternary ammonium salts of the piperidine and their addition salts with a pharmaceutically acceptable acid, an medicinal products containing the same are useful as antagonists of NK.sub.1 receptors.

    摘要翻译： 本发明涉及式（I）化合物：其中：R 1表示烷基，苯基，萘基，吡啶基或噻吩基，每个苯基，萘基，吡啶基或噻吩基任选被取代，R 2表示氢 原子或取代或未取代的烷基，取代或未取代的苯基，环烷基，哌啶子基或取代或未取代的氨基，X表示CO或SO 2，R 3表示氢或烷基，R 4表示烷基，取代或未取代的苯基或三卤甲基， R 4与携带它们的碳原子一起形成环（C 3 -C 7）链烯基，A代表苯基，萘基或吡啶环，每个苯基，萘基或吡啶基任选被取代，它们的异构体是相应的季铵盐 哌啶及其与药学上可接受的酸的加成盐，含有它们的药物可用作NK1受体的拮抗剂。

    Compounds derived from boronic acid
    8.
    发明授权
    Compounds derived from boronic acid 失效
    衍生自硼酸的化合物

    公开(公告)号：US5814622A

    公开(公告)日：1998-09-29

    申请号：US807569

    申请日：1997-02-27

    申请人： Guillaume de Nanteuil ,  Philippe Gloanec ,  Christine Lila ,  Bernard Portevin ,  Tony Verbeuren ,  Alain Rupin ,  Serge Simonet

    发明人： Guillaume de Nanteuil ,  Philippe Gloanec ,  Christine Lila ,  Bernard Portevin ,  Tony Verbeuren ,  Alain Rupin ,  Serge Simonet

    IPC分类号： A61K31/69 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P43/00 ,  C07F5/02 ,  C07F5/04

    CPC分类号： C07F5/025

    摘要： Compound of formula (I) ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, represent hydrogen or alkyl or alternatively R.sub.1 and R.sub.2 form, with the carbon atom which bears them, cycloalkyl, R.sub.3 represents hydrogen or alkyl, phenyl or benzyl, R.sub.4 represents: optionally substituted amino, optionally substituted amindino, optionally substituted guanidino, optionally substituted isothioureido, optionally substituted iminomethylamino, mercapto substituted with heterocyclic, or heterocyclic, R.sub.5 and R.sub.6 each represent hydrogen or alkyl, or ##STR2## forms a boronic ester of pinanediol, m represents an integer such that 0.ltoreq.m.ltoreq.6, n represents an integer such that 1.ltoreq.n.ltoreq.6, A represents any one of the following groups: * optionally substituted bicycloalkyl (C.sub.5 -C.sub.10)phenyl, * or a group of formula: ##STR3## A.sub.1 represents --CO--, --CS--, --SO.sub.2 --, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful as trypsin-like serine proteases.

    摘要翻译： 式（I）化合物其中：R 1和R 2相同或不同，代表氢或烷基，或者R1和R2与带有它们的碳原子形成环烷基，R3代表氢或 烷基，苯基或苄基，R4表示：任选取代的氨基，任选取代的氨基，任选取代的胍基，任选取代的异硫脲基，任选取代的亚氨基甲基氨基，被杂环或杂环取代的巯基，R 5和R 6各自表示氢或烷基， 形成蒎二醇的硼酸酯，m表示0≤n≤6的整数，n表示1≤n≤6的整数，A表示以下基团中的任一个：*任选地 取代的双环烷基（C 5 -C 10）苯基，或下式的基团：A 1表示-CO - ， - CS-，-SO 2 - ，其异构体及其与药学上可接受的酸或碱的加成盐，和 使用含有该药物的药用产品 作为胰蛋白酶样丝氨酸蛋白酶。