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1. 发明申请

WO2004007499A1 3-FURANYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS 审中-公开
标题翻译：托吡醇作为激酶抑制剂的3-FURANYL模拟物
公开(公告)号：WO2004007499A1
公开(公告)日：2004-01-22
申请号：PCT/EP2003/050293
申请日：2003-07-08
申请人： JANSSEN PHARMACEUTICA N.V. , LACRAMPE, Jean, Fernand, Armand , CONNORS, Richard, William , HO, Chih, Yung , RICHARDSON, Alan , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes , BAKKER, Annette, Cornelia
发明人： LACRAMPE, Jean, Fernand, Armand , CONNORS, Richard, William , HO, Chih, Yung , RICHARDSON, Alan , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes , BAKKER, Annette, Cornelia
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention concerns the compounds of formula (I) the N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents an integer being 0 or 1; n represents an integer being 0, 1 or 2; R 1 represents C 1-4 alkyl, C 1-4 alkyl substituted with pyridinyl, phenyl, piperidinyl or piperidinyl substituted with C 1-4- alkyloxycarbonyl; R 2 represents hydrogen or C 1-4 alkyl; R 3 represents hydrogen or C 1-4 alkyl; or R 2 and R 3 taken together with the carbon atom to which they are attached form cyclopentyl or piperidinyl wherein said cyclopentyl or piperidinyl each independently may optionally be substituted with one, or where possible, two or three substituents each independently selected from C 1-4 alkyloxycarbonyl, phenylcarbonyl or -C(=NH)-NH 2 ; R 4 represents halo or C 1-4 alkyloxy; R 5 represents Het 2 , C 1-4 alkyl substituted with one or where possible more substituents being selected from hydroxy, halo, Het 3 or NR 6 R 7 , or C 1-4 alkyloxy substituted with one or where possible more substituents being selected from Het 4 or -C(=O)-Het 4 ; R 6 and R 7 are each independently selected from hydrogen, C 1-4 alkyl, Het 5 or C 1-4 alkyl substituted with one or where possible more substituents being selected from hydroxy or Het 5 ; Het 2 represents piperazinyl; Het 3 represents a heterocycle selected from morpholinyl, pyrrolidinyl, piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C 1-4 alkyl preferably methyl, aminosulfonyl, mono- or di(C 1-4 alkyl)aminosulfonyl, hydroxyC 1 -4 alkyloxyC 1-4 alkyl, C 1-4 alkyloxyC 1-4 alkyl or C 1-4 alkyloxy; Het 4 represents a heterocycle selected from morpholinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three C 1-4 alkyl substituents, preferably methyl; Het 5 represents a heterocycle selected from pyridinyl, pyrrolidinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, C 1-4 alkyloxycarbonyl or mono- or di(C 1-4 alkyl)aminosulfonyl.
摘要翻译：本发明涉及式（I）化合物的N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中m表示0或1的整数; n表示0或1或2的整数; R 1表示C 1-4烷基，被吡啶基取代的C 1-4烷基，苯基，哌啶基或被C 1-4 - 烷氧基羰基取代的哌啶基; R 2表示氢或C 1-4烷基; R 3表示氢或C 1-4烷基; 或R 2和R 3与它们所连接的碳原子一起形成环戊基或哌啶基，其中所述环戊基或哌啶基各自独立地可以任选被一个或可能的两个或三个取代基各自独立地选择 C 1-4烷氧基羰基，苯基羰基或-C（= NH）-NH 2; R 4表示卤素或C 1-4烷氧基; R 5表示Het 2，被一个或多个可能的更多选自羟基，卤素，Het 3或NR 6 R 7的取代基取代的C 1-4烷基，或被一个或多个在可能的情况下更多的取代基选自Het 4或-C（= O）-Het 4; R 6和R 7各自独立地选自氢，C 1-4烷基，Het 5或被一个或多个可能的更多取代基选自羟基或Het 5取代的C 1-4烷基; Het 2表示哌嗪基; Het 3表示选自吗啉基，吡咯烷基，哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可以任选地被一个取代，或者如果可能的话，两个或三个取代基各自独立地选自C 1-4烷基，优选甲基，氨基磺酰基，单 - 或二（C 1-4烷基）氨基磺酰基，羟基C 1-4烷氧基C 1-4烷基，C 1-4烷氧基C 1-4烷基或C 1-4烷氧基; Het 4表示选自吗啉基或哌嗪基的杂环，其中所述单环杂环各自独立地可以任选地被一个取代，或在可能的情况下被两个或三个C 1-4烷基取代基，优选甲基取代; Het 5表示选自吡啶基，吡咯烷基或哌啶基的杂环，其中所述单环杂环各自独立地可以任选地被一个或两个或三个取代基独立地选自氨基磺酰基，C 1-4烷氧基羰基或单或二（C1 1-4烷基）氨基磺酰基。

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