公开(公告)号：US5561113A

公开(公告)日：1996-10-01

申请号：US427802

申请日：1995-04-26

申请人： Jean-Luc Fauchere ,  Nathalie Kucharczyk-Gentric ,  Joseph Paladino ,  Jacqueline Bonnet ,  Emmanuel Canet ,  Graham Birrell

发明人： Jean-Luc Fauchere ,  Nathalie Kucharczyk-Gentric ,  Joseph Paladino ,  Jacqueline Bonnet ,  Emmanuel Canet ,  Graham Birrell

IPC分类号： A61K38/17 ,  A61K38/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/04 ,  A61P29/00 ,  A61P37/08 ,  C07K1/06 ,  C07K1/113 ,  C07K5/02 ,  C07K5/023 ,  A61K38/05 ,  C07D257/04

CPC分类号： C07K5/0202 ,  A61K38/00

摘要： A compound of formula (I): ##STR1## in which: R represents naphthyl, 5,6,7,8-tetrahydronaphthyl, 1,2,3,4-tetrahydronaphthyl, thienyl, optionally substituted phenyl or (C.sub.3 -C.sub.7)cycloalkyl,n represents an integer such that 1.ltoreq.n.ltoreq.8, their enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as antagonists of substance P.

摘要翻译： 式（I）的化合物：其中：R表示萘基，5,6,7,8-四氢萘基，1,2,3,4-四氢萘基，噻吩基，任选取代的苯基或 （C3-C7）环烷基，n表示一个整数，使得它们的对映体，非对映异构体和差向异构体以及它们与药学上可接受的酸或碱的加成盐和含有它们的药用产物是有用的 作为物质P的拮抗剂。

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。