专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US09273013B2 Quinazoline derivatives 有权
标题翻译：喹唑啉衍生物
公开(公告)号：US09273013B2
公开(公告)日：2016-03-01
申请号：US13744878
申请日：2013-01-18
申请人： Janssen Pharmaceutica N.V.
发明人： Eddy Jean Edgard Freyne , Timothy Pietro Suren Perera , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Gaston Stanislas Marcella Diels , Werner Constant Johan Embrechts , Peter Ten Holte , Frederik Jan Rita Rombouts , Carsten Schultz-Fademrecht
IPC分类号： C07D239/02 , C07D239/94 , C07D239/88 , C07D239/93 , C07C229/16 , C07C229/40
CPC分类号： C07D498/06 , C07C229/16 , C07C229/40 , C07D239/88 , C07D239/93 , C07D239/94
摘要： The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl, —O—N═CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-4alkyl optionally substituted with phenyl or hydroxy; R20 and R21 are hydrogen or C1-4alkyl optionally substituted with C1-4alkyloxy; Het20, Het21 and Het22 are a heterocycle selected from the group consisting pyrrolidinyl, 2-pyrrolidinonyl or piperidinyl optionally substituted with hydroxy.
摘要翻译：本发明涉及下式的化合物其中Z代表NH; Y代表任选被氨基，一或二（C 1-4烷基）氨基或C 1-4烷氧基羰基氨基 - ， - C 3-7烯基-CO-的氨基取代的-C 3-9烷基 - ， - C 2-9烯基 - ， - 氨基，一或二（C 1-4烷基）氨基 - 或C 1-4烷氧基羰基氨基 - ，C 1-5烷基-NR 13 -C 1-5烷基 - ， - C 1-5烷基-NR 14 -CO-C 1-5烷基 - C 1-6烷基-CO-NH - ， - C 1-5烷基-CO NR 15 -C 1-5烷基 - ， - C 1-3烷基-NH-CO-Het 20 - ， - C 1-2烷基-CO-Het 21 -CO-， - C 1-2烷基 -NH-CO-CR16R17-NH-，-C1-2烷基-CO-NH-CR18R19-CO-，-C1-2烷基-CO-NR20-C1-3烷基-CO-或-NR22-CO-C1-3烷基 - NH-; X1表示直接键，O或-O-C 1-2烷基 - ; X 2表示直接键，-CO-C 1-2烷基 - ，NR 12，-NR 12 -C 1-2烷基，-O-N = CH-或-C 1-2烷基 - ; R1和R2是氢或卤素; R3是氢; R4代表氢或C1-4烷氧基; R 12和R 13是氢或C 1-4烷基; R14和R15是氢; R 16和R 17各自独立地表示氢或C 1-4烷基; R 18和R 19是氢或任选被苯基或羟基取代的C 1-4烷基; R 20和R 21是氢或任选被C 1-4烷氧基取代的C 1-4烷基; Het20，Het21和Het22是选自吡咯烷基，2-吡咯烷基或任选被羟基取代的哌啶基的杂环。

2. 发明授权

US09040511B2 3-cyano-quinoline derivatives with antiproliferative activity 有权
标题翻译：具有抗增殖活性的3-氰基 - 喹啉衍生物
公开(公告)号：US09040511B2
公开(公告)日：2015-05-26
申请号：US13796377
申请日：2013-03-12
申请人： Janssen Pharmaceutica N.V.
发明人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Buijnsters , Kristof Van Emelen , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
IPC分类号： C07D413/02 , A61K31/47 , C07D215/54 , C07D498/06 , A61K31/4748
CPC分类号： C07D215/54 , A61K31/4748 , C07D498/06
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.
摘要翻译：本发明涉及下式的化合物：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Z代表NH; Y表示-C3-9烷基，-C1-5烷基-NR12-C1-5烷基，-C 1-6烷基-NH-CO-或-CO-NH-C 1-6烷基; X1表示-O-; X 2表示直接键，-NR 11 -C 1-2烷基 - ， - NR 11 -CH 2 - ， - C 1-2烷基 - ， - O-C 1-2烷基，-O-或-O-CH 2 - 。 R1表示氢或卤素; R 2表示氢，氰基，卤素，羟基羰基 - ，C 1-4烷氧基羰基 - ，Het 16 - 羰基 - 或Ar 5; R 3表示氢，羟基，C 1-4烷氧基 - ，Ar 4 -C 1-4烷氧基或R 3表示被一个或多个可能的两个或多个选自C 1-4烷氧基 - 或Het 2 - 的取代基取代的C 1-4烷氧基; R10表示氢; R11表示氢，C1-4烷基或C1-4烷基 - 氧 - 羰基 - ; R12表示Het14-C1-4烷基，特别是吗啉基-C 1-4烷基; Het2表示选自任选被C 1-4烷基，优选甲基取代的吗啉基或哌啶基的杂环; Het14代表吗啉基; Het16表示选自吗啉基或吡咯烷基的杂环; Ar4表示苯基; Ar 5表示任选被氰基取代的苯基。

3. 发明申请

US20130197022A1 3-CYANO-QUINOLINE DERIVATIVES WITH ANTIPROLIFERATIVE ACTIVITY 审中-公开
标题翻译：具有抗增殖活性的3-氰基喹啉衍生物
公开(公告)号：US20130197022A1
公开(公告)日：2013-08-01
申请号：US13796377
申请日：2013-03-12
申请人： Janssen Pharmaceutica N.V.
发明人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Buijnsters , Kristof Van Emelen , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
IPC分类号： A61K31/4748 , C07D215/54
CPC分类号： C07D215/54 , A61K31/4748 , C07D498/06
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.
摘要翻译：本发明涉及下式的化合物：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Z代表NH; Y表示-C3-9烷基，-C1-5烷基-NR12-C1-5烷基，-C 1-6烷基-NH-CO-或-CO-NH-C 1-6烷基; X1表示-O-; X 2表示直接键，-NR 11 -C 1-2烷基 - ， - NR 11 -CH 2 - ， - C 1-2烷基 - ， - O-C 1-2烷基，-O-或-O-CH 2 - 。 R1表示氢或卤素; R 2表示氢，氰基，卤素，羟基羰基 - ，C 1-4烷氧基羰基 - ，Het 16 - 羰基 - 或Ar 5; R 3表示氢，羟基，C 1-4烷氧基 - ，Ar 4 -C 1-4烷氧基或R 3表示被一个或多个可能的两个或多个选自C 1-4烷氧基 - 或Het 2 - 的取代基取代的C 1-4烷氧基; R10表示氢; R11表示氢，C1-4烷基或C1-4烷基 - 氧 - 羰基 - ; R12表示Het14-C1-4烷基，特别是吗啉基-C 1-4烷基; Het2表示选自任选被C 1-4烷基，优选甲基取代的吗啉基或哌啶基的杂环; Het14代表吗啉基; Het16表示选自吗啉基或吡咯烷基的杂环; Ar4表示苯基; Ar 5表示任选被氰基取代的苯基。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式