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公开(公告)号:US08507490B2
公开(公告)日:2013-08-13
申请号:US13122216
申请日:2009-11-05
申请人: Jolie Anne Bastian , Julia Marie Clay , Jeffrey Daniel Cohen , Philip Arthur Hipskind , Karen Lynn Lobb , Daniel Jon Sall , Michelle Lee Thompson , Takako Wilson (nee Takakuwa)
发明人: Jolie Anne Bastian , Julia Marie Clay , Jeffrey Daniel Cohen , Philip Arthur Hipskind , Karen Lynn Lobb , Daniel Jon Sall , Michelle Lee Thompson , Takako Wilson (nee Takakuwa)
IPC分类号: C07D401/14 , A61K31/501 , A61P35/00
CPC分类号: C07D401/04 , C07D401/14 , C07D417/14
摘要: The present invention provides novel tetrasubstituted pyridine hedgehog pathway antagonists of the following formula I (I) or a pharmaceutically acceptable salt thereof, wherein: X is C—R1 or N; R1 is hydrogen, fluoro or cyano; R2 is formula II (II), piperidinyl, or gem di-F-substituted cyclohexyl; R3 is methyl or trifluoromethyl; R4 is pyrrolidinyl, morpholinyl or pyridyl, amino or dimethylamino; R5 is trifluoromethyl or methylsulfonyl; R6 is hydrogen or methyl; and R7, R8, R9, R10 and R11 are independently hydrogen fluoro, cyano, chloro, methyl, trifluoromethyl, trifluoromethoxy or methylsulfonyl, provided that at least two of R7, R8, R9, R10 and R11 are hydrogen useful in the treatment of cancer.
摘要翻译: 本发明提供下式I(I)的新型四取代吡啶hedgehog途径拮抗剂或其药学上可接受的盐,其中:X为C-R 1或N; R1是氢,氟或氰基; R2是式II(II),哌啶基或gem二-F取代的环己基; R3是甲基或三氟甲基; R4是吡咯烷基,吗啉基或吡啶基,氨基或二甲基氨基; R5是三氟甲基或甲基磺酰基; R6是氢或甲基; 并且R 7,R 8,R 9,R 10和R 11中的至少两个是可用于治疗癌症的氢,并且R 7,R 8,R 9,R 10和R 11独立地为氢,氰基,氯,甲基,三氟甲基,三氟甲氧基或甲基磺酰基 。
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公开(公告)号:US20110263602A1
公开(公告)日:2011-10-27
申请号:US13122216
申请日:2009-11-05
申请人: Jolie Anne Bastian , Julia Marie Clay , Jeffrey Daniel Cohen , Philip Arthur Hipskind , Karen Lynn Lobb , Daniel Jon Sall , Michelle Lee Thompson , Takako Wilson (nee Takakuwa)
发明人: Jolie Anne Bastian , Julia Marie Clay , Jeffrey Daniel Cohen , Philip Arthur Hipskind , Karen Lynn Lobb , Daniel Jon Sall , Michelle Lee Thompson , Takako Wilson (nee Takakuwa)
IPC分类号: A61K31/5377 , A61P35/00 , C07D413/14 , C07D401/04 , C07D401/14 , A61K31/501
CPC分类号: C07D401/04 , C07D401/14 , C07D417/14
摘要: The present invention provides novel tetrasubstituted pyridine hedgehog pathway antagonists of the following formula I (I) or a pharmaceutically acceptable salt thereof, wherein: X is C—R1 or N; R1 is hydrogen, fluoro or cyano; R2 is formula II (II), piperidinyl, or gem di-F-substituted cyclohexyl; R3 is methyl or trifluoromethyl; R4 is pyrrolidinyl, morpholinyl or pyridyl, amino or dimethylamino; R5 is trifluoromethyl or methylsulfonyl; R6 is hydrogen or methyl; and R7, R8, R9, R10 and R11 are independently hydrogen fluoro, cyano, chloro, methyl, trifluoromethyl, trifluoromethoxy or methylsulfonyl, provided that at least two of R7, R8, R9, R10 and R11 are hydrogen useful in the treatment of cancer.
摘要翻译: 本发明提供下式I(I)的新型四取代吡啶hedgehog途径拮抗剂或其药学上可接受的盐,其中:X为C-R 1或N; R1是氢,氟或氰基; R2是式II(II),哌啶基或gem二-F取代的环己基; R3是甲基或三氟甲基; R4是吡咯烷基,吗啉基或吡啶基,氨基或二甲基氨基; R5是三氟甲基或甲基磺酰基; R6是氢或甲基; 并且R 7,R 8,R 9,R 10和R 11中的至少两个是可用于治疗癌症的氢,并且R 7,R 8,R 9,R 10和R 11独立地为氢,氰基,氯,甲基,三氟甲基,三氟甲氧基或甲基磺酰基 。
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公开(公告)号:US08445493B2
公开(公告)日:2013-05-21
申请号:US13122225
申请日:2009-11-09
申请人: Jolie Anne Bastian , Julia Marie Clay , Takako Wilson (nee Takakuwa) , Michelle Lee Thompson , Daniel Jon Sall , Philip Arthur Hipskind
发明人: Jolie Anne Bastian , Julia Marie Clay , Takako Wilson (nee Takakuwa) , Michelle Lee Thompson , Daniel Jon Sall , Philip Arthur Hipskind
IPC分类号: C07D401/04 , A61K31/501 , A61P35/00
CPC分类号: C07D403/04
摘要: The present invention provides novel tetrasubstituted pyridazine hedgehog pathway antagonists useful in the treatment of cancer.
摘要翻译: 本发明提供可用于治疗癌症的新型四取代哒嗪猬草素途径拮抗剂。
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4.TETRASUBSTITUTED PYRIDAZINES HEDGEHOG PATHWAY ANTAGONISTS 失效
标题翻译: 四甲基磷酰胆碱(HEDGEHOG PATHWAY ANTAGONISTS)公开(公告)号:US20110178093A1
公开(公告)日:2011-07-21
申请号:US13122225
申请日:2009-11-09
申请人: Jolie Anne Bastian , Julia Marie Clay , Takako Wilson (nee Takakuwa) , Michelle Lee Thompson , Daniel Jon Sall , Philip Arthur Hipskind
发明人: Jolie Anne Bastian , Julia Marie Clay , Takako Wilson (nee Takakuwa) , Michelle Lee Thompson , Daniel Jon Sall , Philip Arthur Hipskind
IPC分类号: A61K31/501 , C07D403/04 , A61P35/00
CPC分类号: C07D403/04
摘要: The present invention provides novel tetrasubstituted pyridazine hedgehog pathway antagonists useful in the treatment of cancer.
摘要翻译: 本发明提供可用于治疗癌症的新型四取代哒嗪猬草素途径拮抗剂。
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公开(公告)号:US08404687B2
公开(公告)日:2013-03-26
申请号:US13122212
申请日:2009-10-22
IPC分类号: A01N43/58 , A01N43/60 , A61K31/495 , C07D237/30
CPC分类号: C07D403/04
摘要: The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.
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公开(公告)号:US20110190304A1
公开(公告)日:2011-08-04
申请号:US13122212
申请日:2009-10-22
IPC分类号: A61K31/502 , C07D237/34 , A61P35/00
CPC分类号: C07D403/04
摘要: The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.
摘要翻译: 本发明提供了可用于治疗癌症的新的1,4-二取代的二嗪嗪hedgehog途径拮抗剂。
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公开(公告)号:US07981892B2
公开(公告)日:2011-07-19
申请号:US12935655
申请日:2009-04-01
IPC分类号: A01N43/58 , A61K31/50 , C07D237/30
CPC分类号: C07D401/04
摘要: The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.
摘要翻译: 本发明提供了可用于治疗癌症的新的1,4-二取代的二嗪嗪hedgehog途径拮抗剂。
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公开(公告)号:US20100324048A1
公开(公告)日:2010-12-23
申请号:US12815439
申请日:2010-06-15
IPC分类号: A61K31/50 , C07D401/14 , A61P35/04
CPC分类号: C07D401/14
摘要: The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.
摘要翻译: 本发明提供了可用于治疗癌症的新的1,4-二取代的二嗪嗪hedgehog途径拮抗剂。
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公开(公告)号:US20120316174A1
公开(公告)日:2012-12-13
申请号:US13590481
申请日:2012-08-21
IPC分类号: A61K31/502 , A61P25/02 , A61P35/00
CPC分类号: C07D401/14
摘要: The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.
摘要翻译: 本发明提供了可用于治疗癌症的新的1,4-二取代的二嗪嗪hedgehog途径拮抗剂。
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公开(公告)号:US09000023B2
公开(公告)日:2015-04-07
申请号:US13590481
申请日:2012-08-21
IPC分类号: A61K31/415 , C07D231/12 , C07D401/14
CPC分类号: C07D401/14
摘要: The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.
摘要翻译: 本发明提供了可用于治疗癌症的新的1,4-二取代的二嗪嗪hedgehog途径拮抗剂。
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