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1. 发明申请

WO0050398A3 PHENYL- AND PYRIDINYL DERIVATIVES AS NEUROKININ 1 ANTAGONISTS 审中-公开
标题翻译：苯并吡啶衍生物作为神经营养因子1拮抗剂
公开(公告)号：WO0050398A3
公开(公告)日：2001-04-05
申请号：PCT/EP0001224
申请日：2000-02-15
申请人： HOFFMANN LA ROCHE
发明人： BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC分类号： C07C211/44 , A61K31/167 , A61K31/44 , A61P25/00 , A61P29/00 , C07C211/54 , C07C233/29 , C07C233/33 , C07C233/44 , C07C317/14 , C07C317/40 , C07C323/41 , C07D213/75 , C07D213/79 , C07D213/81 , C07D295/12 , C07D295/135 , C07D401/04
CPC分类号： C07D213/75 , C07C233/29 , C07C233/33 , C07C233/44 , C07C317/40 , C07C323/41 , C07D295/135
摘要： The invention relates to compounds of general formula (I), wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R is hydrogen or halogen; or R and R may be together -CH=CH-CH=CH-; R is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R is independently from each other hydrogen, lower alkyl or form a cycloalkyl group; R is hydrogen, halogen, lower alkyl, lower alkoxy, -N(R )2, -N(R )S(O)2-lower alkyl, -N(R )C(O)R or a cyclic tertiary amine of the group (a); R is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R is hydrogen, hydroxy, lower alkyl, -N(R )CO-lower alkyl, hydroxy-lower alkyl, cyano, -CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R )-, -(CH2)mO-, -(CH2)mN(R )-, -N(R ) C(O)-, C(O)O- or -N(R )(CH2)m-; Y is -(CH2)n-, -O-, -S-, SO2-, -C(O)- or -N(R )-; Z is =N-, -CH= or -C(C1)=; n is 0 - 4; and, is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds of formula (I) have a high affinity to the NK-1 receptor.
摘要翻译：本发明涉及通式（I）的化合物，其中R是氢，低级烷基，低级烷氧基，卤素或三氟甲基; R 1是氢或卤素; 或R和R 1可以一起是-CH = CH-CH = CH-; R 2是氢，卤素，三氟甲基，低级烷氧基或氰基; R 3彼此独立地为氢，低级烷基或形成环烷基; R 4是氢，卤素，低级烷基，低级烷氧基，-N（R 5）2，-N（R 5）S（O）2-低级烷基，-N（R 5） C（O）R 5或（a）组的环状叔胺; R 5彼此独立地为氢，C 3-6 - 环烷基，苄基或低级烷基; R 6是氢，羟基，低级烷基，-N（R 5）CO-低级烷基，羟基 - 低级烷基，氰基，-CHO或5-或6-元杂环基，任选经由亚烷基键合，X是-C（O）N（R 5） - ， - （CH 2）m O - ， - （CH 2）m N（R 5） - ， - N（R 5）C（O），C（O）O-或-N（R 5）（CH 2）m - ; Y是 - （CH 2）n - ， - O - ， - S - ，SO 2 - ， - C（O） - 或-N（R 5） Z是= N-，-CH =或-C（C1）=; n为0-4; 是1或2; 及其药学上可接受的酸加成盐。已经表明式（I）化合物对NK-1受体具有高亲和力。

2. 发明申请

WO0073278A2 5-PHENYL-PYRIMIDINE DERIVATIVES 审中-公开
标题翻译： 5-苯基 - 吡啶衍生物
公开(公告)号：WO0073278A2
公开(公告)日：2000-12-07
申请号：PCT/EP0004702
申请日：2000-05-24
申请人： HOFFMANN LA ROCHE
发明人： BOES MICHAEL , GALLEY GUIDO , GODEL THIERRY , HOFFMANN TORSTEN , HUNKELER WALTER , SCHNIDER PATRICK , STADLER HEINZ
IPC分类号： A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61P1/04 , A61P1/08 , A61P9/00 , A61P11/02 , A61P11/06 , A61P17/02 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P37/08 , A61P43/00 , C07D213/00 , C07D239/00 , C07D239/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/46 , C07D239/48 , C07D295/00 , C07D401/04
CPC分类号： C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48
摘要： The invention relates to compounds of general formula (I) wherein R is hydrogen or halogen; R is hydrogen, halogen, lower alkyl or lower alkoxy; R is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R /R are independently from each other hydrogen or lower alkyl; R is lower alkyl, lower alkoxy, amino, hydroxy, hydroxy-lower alkyl, -(CH2)n-piperazinyl, optionally substituted by lower alkyl, -(CH2)n-morpholinyl, -(CH2)n+1-imidazolyl, -O-(CH2)n+1-morpholinyl, -O-(CH2)n+1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, -NH-(CH2)n+1N(R )2, -(CH2)n-NH-(CH2)n+1N(R )2, -(CH2)n+1N(R )2, or -O-(CH2)n+1N(R )2, wherein R is hydrogen or lower alkyl; R is hydrogen; R and R or R and R may be together with the two carbon ring atoms -CH=CH-CH=CH-, with the proviso that n for R is 1; n is independently 0 - 2; and X is -C(O)N(R )- or -N(R )C(O)-; and pharmaceutically acceptable acid addition salts thereof. Compounds of formula (I) have a high affinity to the NK-1 receptor. They are therefore useful for the treatment or diseases which relate to this receptor.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1是氢或卤素; R 2是氢，卤素，低级烷基或低级烷氧基; R 3是卤素，三氟甲基，低级烷氧基或低级烷基; R 4 / R 4彼此独立地为氢或低级烷基; - （CH 2）n - 吗啉基， - （CH 2）n + 1-烷基， - （CH 2）n - 咪唑基，-O-（CH 2）n + 1-吗啉基，-O-（CH 2）n + 1-哌啶基，低级烷基 - 硫烷基，低级烷基 - 磺酰基，苄基氨基，-NH-（CH 2）n + 4“>）2， - （CH 2）n -NH-（CH 2）n + 1N（R 4”）2， - （CH 2）n + 1N（R 4“）2或-O- CH 2）n + 1N（R 4“）2，其中R 4是氢或低级烷基; R 6是氢; R 2和R 6或R 1和R” 6>可以与两个碳环原子-CH = CH-CH = CH-一起，条件是R 1的n为1; n独立地为0-2;且X为-C（O）N （R 4） - 或-N（R 4）C（O） - 及其药学上可接受的酸加成盐。式（I）化合物对NK-1受体具有高亲和力因此可用于与该受体相关的治疗或疾病。

3. 发明申请

WO9924022A2 ISOQUINOLINE DERIVATIVES FOR USE AGAINST CNS DISORDERS 审中-公开
标题翻译：用于中枢神经系统疾病的异喹啉衍生物
公开(公告)号：WO9924022A2
公开(公告)日：1999-05-20
申请号：PCT/EP9806920
申请日：1998-11-02
申请人： HOFFMANN LA ROCHE
发明人： GODEL THIERRY , HUNKELER WALTER
IPC分类号： A61K31/472 , A61K31/4725 , A61K31/4741 , A61K31/00
CPC分类号： A61K31/472 , A61K31/4725 , A61K31/4741
摘要： The invention relates to the use of isoquinoline derivatives of general formula (I) wherein R , R and R are hydrogen, halogen, lower alkyl, lower alkoxy or R and R taken together form a methylenedioxy group, Z is (a), (b), (c) or (d); R is CF3, halogen, lower alkoxy, lower alkyl or lower alkyl-halogen; p is 1-3; n is 0-5 and of their pharmaceutically acceptable salts in the treatment of disorders which are associated with 5HT7 receptors.
摘要翻译：本发明涉及通式（I）的异喹啉衍生物，其中R 1，R 2和R 3为氢，卤素，低级烷基，低级烷氧基或R 2和R 3为氢，一起形成亚甲二氧基，Z是（a），（b），（c）或（d）; R为CF 3，卤素，低级烷氧基，低级烷基或低级烷基 - 卤素; p为1-3; n为0-5及其药学上可接受的盐，用于治疗与5HT7受体相关的病症。

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