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    Piperidine compounds
    4.
    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。

    Preparation of phosphoramidon
    9.
    发明授权
    Preparation of phosphoramidon 失效
    磷酰胺的制备

    公开(公告)号：US5608045A

    公开(公告)日：1997-03-04

    申请号：US497812

    申请日：1995-07-03

    申请人： Guillaume de Nanteuil ,  Georges Remond ,  Tony Verbeuren

    发明人： Guillaume de Nanteuil ,  Georges Remond ,  Tony Verbeuren

    IPC分类号： A61K38/00 ,  A61K38/55 ,  A61P9/10 ,  A61P9/12 ,  C07F9/24 ,  C07F9/572 ,  C07K1/06 ,  C07K1/113 ,  C07K1/22 ,  C07K5/06 ,  C07K5/062 ,  C07G3/00 ,  C07F9/06 ,  C07F9/22

    CPC分类号： C07K5/06191 ,  C07F9/5728 ,  A61K38/00

    摘要： Compound of formula (I): ##STR1## in which: R.sub.1 represents a hydroxyl, alkoxy or amino (unsubstituted or substituted) group,R.sub.2 represents an unsubstituted or substituted alkyl group,X.sub.1 represents --NH--,X.sub.2 represents --O--,R.sub.3 represents a hydrogen atom or an alkyl or phenyl group,R.sub.4 represents an alkyl group which is always substituted with one or more hydroxyl, benzyloxy, benzyloxycarbonylamino, amino, mono- or dialkylamino, acetoxy or 2,2-dimethyl-1,3-dioxolan-4-yl groups, such groups being identical or different,R.sub.5 represents a 3-indolylmethyl, naphthylmethyl, alkyl, phenyl or benzyl group, its isomers as well as its addition salts with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful as endothelin convertase inhibitor.

    摘要翻译： 式（I）化合物：其中：R1表示羟基，烷氧基或氨基（未取代或取代的）基团，R2表示未取代或取代的烷基，X1表示-NH-，X2表示-O - ，R3表示氢原子或烷基或苯基，R4表示总是被一个或多个羟基，苄氧基，苄氧基羰基氨基，氨基，一或二烷基氨基，乙酰氧基或2,2-二甲基-1取代的烷基， 这些基团相同或不同，R 5表示3-吲哚基甲基，萘甲基，烷基，苯基或苄基，其异构体以及其与药学上可接受的酸或碱的加成盐，以及药用 含有它们的产物可用作内皮素转化酶抑制剂。

    New phosphonic acid compounds
    10.
    发明授权
    New phosphonic acid compounds 失效
    新型膦酸化合物

    公开(公告)号：US5591728A

    公开(公告)日：1997-01-07

    申请号：US497811

    申请日：1995-07-03

    申请人： Guillaume de Nanteuil ,  Georges Remond ,  Tony Verbeuren

    发明人： Guillaume de Nanteuil ,  Georges Remond ,  Tony Verbeuren

    IPC分类号： A61K38/00 ,  A61K38/55 ,  A61P9/10 ,  A61P9/12 ,  C07F9/24 ,  C07F9/572 ,  C07K1/06 ,  C07K1/113 ,  C07K1/22 ,  C07K5/06 ,  C07K5/062 ,  A61K31/675 ,  A61K31/66

    CPC分类号： C07K5/06191 ,  C07F9/5728 ,  A61K38/00

    摘要： Compound of formula (I): ##STR1## in which: R.sub.1 represents a hydroxyl, alkoxy or amino (unsubstituted or substituted) group,R.sub.2 represents an unsubstituted or substituted alkyl group,X.sub.1 represents --NH--,X.sub.2 represents --O--,R.sub.3 represents a hydrogen atom or an alkyl or phenyl group,R.sub.4 represents an alkyl group which is always substituted with one or more hydroxyl, benzyloxy, benzyloxycarbonylamino, amino, mono- or dialkylamino, acetoxy or 2,2-dimethyl-1,3-dioxolan-4-yl groups, such groups being identical or different,R.sub.5 represents a 3-indolylmethyl, naphthylmethyl, alkyl, phenyl or benzyl group, its isomers as well as its addition salts with a pharmaceutically acceptable acid or base,and medicinal products containing the same are useful as endothelin convertase inhibitor.

    摘要翻译： 式（I）化合物：其中：R1表示羟基，烷氧基或氨基（未取代或取代的）基团，R2表示未取代或取代的烷基，X1表示-NH-，X2表示-O - ，R3表示氢原子或烷基或苯基，R4表示总是被一个或多个羟基，苄氧基，苄氧基羰基氨基，氨基，一或二烷基氨基，乙酰氧基或2,2-二甲基-1取代的烷基， 这些基团相同或不同，R 5表示3-吲哚基甲基，萘甲基，烷基，苯基或苄基，其异构体以及其与药学上可接受的酸或碱的加成盐，以及药用 含有它们的产物可用作内皮素转化酶抑制剂。