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公开(公告)号:US08999998B2
公开(公告)日:2015-04-07
申请号:US13382145
申请日:2010-07-02
申请人: Paul Gibbons , Emily Hanan , Wendy Liu , Joseph P. Lyssikatos , Steven R. Magnuson , Rohan Mendonca , Richard Pastor , Thomas E. Rawson , Michael Siu , Mark Zak , Aihe Zhou , Bing-Yan Zhu
发明人: Paul Gibbons , Emily Hanan , Wendy Liu , Joseph P. Lyssikatos , Steven R. Magnuson , Rohan Mendonca , Richard Pastor , Thomas E. Rawson , Michael Siu , Mark Zak , Aihe Zhou , Bing-Yan Zhu
IPC分类号: C07D487/04 , A61K31/519
CPC分类号: C07D487/04
摘要: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.
摘要翻译: 其中R 1,R 2和R 3在本文中定义的式I化合物,对映异构体,非对映异构体,互变异构体或其药学上可接受的盐可用作一种或多种Janus激酶的抑制剂。 公开了包含式I化合物和药学上可接受的载体,佐剂或媒介物的药物组合物,以及对患者中Janus激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。
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公开(公告)号:US08609687B2
公开(公告)日:2013-12-17
申请号:US13471269
申请日:2012-05-14
申请人: Bing-Yan Zhu , Michael Siu , Steven R. Magnuson , Richard Pastor , He Haiying , Xiao Yisong , Zheng Jifu , Xu Xing , Zhao Junping , Christopher Hurley , Jun Liang , Wendy Liu , Joseph P. Lyssikatos
发明人: Bing-Yan Zhu , Michael Siu , Steven R. Magnuson , Richard Pastor , He Haiying , Xiao Yisong , Zheng Jifu , Xu Xing , Zhao Junping , Christopher Hurley , Jun Liang , Wendy Liu , Joseph P. Lyssikatos
IPC分类号: A61K31/437 , C07D471/02
CPC分类号: C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07D487/04
摘要: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.
摘要翻译: 其中R 1,R 2,R 3,R 4和R 5在本文中定义的式I化合物,对映异构体,非对映异构体,互变异构体或其药学上可接受的盐可用作JAK激酶抑制剂。 公开了包含式I化合物和药学上可接受的载体,佐剂或载体的药物组合物,以及治疗或减轻对患者中JAK激酶活性的抑制作用的疾病或病症的严重程度的方法。
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53.
公开(公告)号:US08399690B2
公开(公告)日:2013-03-19
申请号:US13018068
申请日:2011-01-31
申请人: Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人: Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号: C07D313/00 , C07D333/00
CPC分类号: C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译: 式I和II的苯并吡喃和苯并辛菌素化合物,包括立体异构体,几何异构体,互变异构体,溶剂合物,代谢物和药学上可接受的盐,可用于抑制脂质激酶,包括p110α和PI3K的其他同种型,并用于治疗疾病如癌症 由脂质激酶介导。 公开了使用式I和II的化合物在体外,原位和体内诊断,预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。
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公开(公告)号:US20120225855A1
公开(公告)日:2012-09-06
申请号:US13471269
申请日:2012-05-14
申请人: Bing-Yan Zhu , Michael Siu , Steven R. Magnuson , Richard Pastor , He Haiying , Xiao Yisong , Zheng Jifu , Xu Xing , Zhao Junping , Christopher Hurley , Jun Liang , Wendy Liu , Joseph P. Lyssikatos
发明人: Bing-Yan Zhu , Michael Siu , Steven R. Magnuson , Richard Pastor , He Haiying , Xiao Yisong , Zheng Jifu , Xu Xing , Zhao Junping , Christopher Hurley , Jun Liang , Wendy Liu , Joseph P. Lyssikatos
IPC分类号: C07D471/04 , A61K31/496 , A61K31/5377 , A61P9/00 , A61P3/10 , A61P37/00 , A61P25/00 , A61P1/16 , A61P37/08 , A61P25/28 , A61P19/08 , A61P31/00 , A61P35/04 , A61P35/02 , A61P9/10 , A61P25/16 , A61P17/00 , A61K31/437
CPC分类号: C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07D487/04
摘要: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.
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公开(公告)号:US20090131407A1
公开(公告)日:2009-05-21
申请号:US12096586
申请日:2006-12-14
IPC分类号: A61K31/55 , C12N9/99 , A61K31/4188 , A61K31/4196 , C07D487/14 , C07D495/14 , A61P35/00
CPC分类号: C07D497/16
摘要: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I): I wherein X, Y, Z, R1, R2, R3, Ra, Rb, and n are as described herein.
摘要翻译: 本发明提供新的激酶抑制剂,其可用作例如治疗恶性肿瘤的治疗剂,其中化合物具有通式(I):其中X,Y,Z,R 1,R 2,R 3,R a,R b和n为 如本文所述。
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公开(公告)号:US06638980B1
公开(公告)日:2003-10-28
申请号:US09576633
申请日:2000-05-24
IPC分类号: A61K31165
CPC分类号: C07D213/40 , C07C311/16 , C07C311/46 , C07D217/22 , C07D295/192 , C07D295/26 , C07D307/52 , C07D401/12
摘要: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
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公开(公告)号:US06245743B1
公开(公告)日:2001-06-12
申请号:US09077001
申请日:1998-05-15
IPC分类号: A61K3800
CPC分类号: C07K5/0202 , A61K38/00 , C07K5/06086 , C07K5/06095 , C07K5/0817
摘要: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
摘要翻译: 公开了与哺乳动物因子Xa具有活性的新型化合物,其盐和与其相关的组合物。 该化合物在体外或体内可用于预防或治疗凝血障碍。
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公开(公告)号:US06211183B1
公开(公告)日:2001-04-03
申请号:US09058564
申请日:1998-04-13
IPC分类号: A61K3169
CPC分类号: C07D295/205 , C07D211/26 , C07D241/08 , C07D243/08 , C07D295/15 , C07D401/06 , C07D401/12 , C07D417/12 , C07D417/14
摘要: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
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公开(公告)号:US6046169A
公开(公告)日:2000-04-04
申请号:US486386
申请日:1995-06-07
CPC分类号: C07K5/06191 , A61K38/00
摘要: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
摘要翻译: 公开了与哺乳动物因子Xa具有活性的新型化合物,其盐和与其相关的组合物。 该化合物在体外或体内可用于预防或治疗凝血障碍。
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公开(公告)号:US08889673B2
公开(公告)日:2014-11-18
申请号:US13529946
申请日:2012-06-21
申请人: Bing-Yan Zhu , Michael Siu , Steven R. Magnuson , Richard Pastor , He Haiying , Xiao Yisong , Zheng Jifu , Xu Xing , Zhao Junping , Wendy Liu
发明人: Bing-Yan Zhu , Michael Siu , Steven R. Magnuson , Richard Pastor , He Haiying , Xiao Yisong , Zheng Jifu , Xu Xing , Zhao Junping , Wendy Liu
IPC分类号: A61K31/5377 , A61K31/454 , A61K31/497 , A61K31/4196 , A61K31/4439 , A61K31/496 , C07D211/00 , C07D413/02 , C07D403/02 , C07D249/08 , C07D401/02 , C07D471/04
CPC分类号: C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/06
摘要: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.
摘要翻译: 其中R 1,R 2,R 3,R 4和R 5在本文中定义的式I化合物,对映异构体,非对映异构体,互变异构体或其药学上可接受的盐可用作JAK激酶抑制剂。 公开了包含式I化合物和药学上可接受的载体,佐剂或载体的药物组合物,以及治疗或减轻对患者中JAK激酶活性的抑制作用的疾病或病症的严重程度的方法。
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