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公开(公告)号:US20100087434A1
公开(公告)日:2010-04-08
申请号:US12618025
申请日:2009-11-13
申请人: Andrew P. Degnan , Kevin W. Gillman , Derek J. Denhart , Jonathan L. Ditta , Ramkumar Rajamani , Ying Han , George O. Tora
发明人: Andrew P. Degnan , Kevin W. Gillman , Derek J. Denhart , Jonathan L. Ditta , Ramkumar Rajamani , Ying Han , George O. Tora
IPC分类号: A61K31/5377 , C07D401/12 , C07D413/14 , A61K31/506 , A61K31/445
CPC分类号: C07D401/12 , C07D211/22 , C07D405/12 , C07D409/12 , C07D417/12
摘要: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.
摘要翻译: 本发明包括式I化合物,包括其药学上可接受的盐,其药物组合物及其在治疗与速激肽或5-羟色胺或两者的过量或不平衡相关的疾病中的用途。
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公开(公告)号:US08383821B2
公开(公告)日:2013-02-26
申请号:US12618025
申请日:2009-11-13
申请人: Andrew P. Degnan , Kevin W. Gillman , Derek J. Denhart , Jonathan L. Ditta , Ramkumar Rajamani , Ying Han , George O. Tora
发明人: Andrew P. Degnan , Kevin W. Gillman , Derek J. Denhart , Jonathan L. Ditta , Ramkumar Rajamani , Ying Han , George O. Tora
IPC分类号: A61K31/4523 , C07D403/14
CPC分类号: C07D401/12 , C07D211/22 , C07D405/12 , C07D409/12 , C07D417/12
摘要: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.
摘要翻译: 本发明包括式I化合物,包括其药学上可接受的盐,其药物组合物及其在治疗与速激肽或5-羟色胺或两者的过量或不平衡相关的疾病中的用途。
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公开(公告)号:US20070249607A1
公开(公告)日:2007-10-25
申请号:US11734809
申请日:2007-04-13
申请人: Andrew Degnan , Kevin Gillman , Derek Denhart , Jonathan Ditta , Ramkumar Rajamani , Ying Han , George Tora
发明人: Andrew Degnan , Kevin Gillman , Derek Denhart , Jonathan Ditta , Ramkumar Rajamani , Ying Han , George Tora
IPC分类号: A61K31/5377 , A61K31/53 , A61K31/497 , A61K31/496 , A61K31/513 , A61K31/501 , A61K31/4545 , A61K31/454 , C07D413/02 , C07D403/02 , C07D401/02
CPC分类号: C07D401/12 , C07D211/22 , C07D405/12 , C07D409/12 , C07D417/12
摘要: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.
摘要翻译: 本发明包括式I化合物,包括其药学上可接受的盐,其药物组合物及其在治疗与速激肽或5-羟色胺或两者的过量或不平衡相关的疾病中的用途。
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公开(公告)号:US08604024B2
公开(公告)日:2013-12-10
申请号:US13477143
申请日:2012-05-22
申请人: Lorin A. Thompson, III , Jianliang Shi , Yong-Jin Wu , Lawrence R. Marcin , Ramkumar Rajamani , Mendi A. Higgins
发明人: Lorin A. Thompson, III , Jianliang Shi , Yong-Jin Wu , Lawrence R. Marcin , Ramkumar Rajamani , Mendi A. Higgins
IPC分类号: C07D279/08 , C07D513/04 , C07D417/10
CPC分类号: C07D279/08 , C07D417/04 , C07D417/10 , C07D417/12 , C07D513/04
摘要: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein X is selected from the group of CH2, O, and NR2; m=0 or 1; R1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is a bond, —NHCO—, —NH—, or L and Z together can be absent; Z is a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, acetyl, and methanesulfonyl; and R3, R4 and R5 are independently selected from hydrogen or C1-4alkyl.
摘要翻译: 包括其药学上可接受的盐的式(I)化合物在本文中阐述:其中X选自CH 2,O和NR 2; m = 0或1; 每个实例的R 1选自卤素,羟基,氨基,C 1-4烷基氨基,C 1-4二烷基氨基,卤代C 1-4烷基,CN,C 1 -C 6烷基或环烷基,C 1 -C 6烷氧基和C 2 -C 4炔基; L是键,-NHCO-,-NH-或L和Z可以不存在; Z是可以被0-3个选自卤素,卤代C 1-4烷氧基,4-甲氧基苯基,羟基,氨基,C 1 -C 10 - 芳基的取代基取代的C 6 -C 10 - 芳基或5-10元杂环基, C 1-4烷基氨基,卤代C 1-4烷基,CN,C 1 -C 6烷基或环烷基,C 1 -C 6烷氧基和C 2 -C 4炔基; R 2选自氢,苄基,C 1 -C 6烷基或环烷基,C 1 -C 6烷氧基,乙酰基和甲磺酰基; 并且R 3,R 4和R 5独立地选自氢或C 1-4烷基。
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公开(公告)号:US20100120770A1
公开(公告)日:2010-05-13
申请号:US12595065
申请日:2008-04-09
申请人: Anne Marinier , Marco Dodier , Stephan Roy , Kurt Zimmermann , Xiaopeng Sang , Mark D. Wittman , David R. Langley , Ramkumar Rajamani
发明人: Anne Marinier , Marco Dodier , Stephan Roy , Kurt Zimmermann , Xiaopeng Sang , Mark D. Wittman , David R. Langley , Ramkumar Rajamani
IPC分类号: A61K31/4545 , A61K31/444 , A61K31/5377 , A61P35/00
CPC分类号: C07D417/14
摘要: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof.The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's disease.
摘要翻译: 本发明提供式I化合物及其药学上可接受的盐。 式I噻唑基化合物抑制酪氨酸激酶活性,从而使它们用作抗癌剂和治疗阿尔茨海默氏病。
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公开(公告)号:US20130131051A1
公开(公告)日:2013-05-23
申请号:US13477143
申请日:2012-05-22
申请人: LORIN A. THOMPSON, III , Jianliang Shi , Yong-Jin Wu , Lawrence R. Marcin , Ramkumar Rajamani , Mendi A. Higgins
发明人: LORIN A. THOMPSON, III , Jianliang Shi , Yong-Jin Wu , Lawrence R. Marcin , Ramkumar Rajamani , Mendi A. Higgins
IPC分类号: C07D279/08 , C07D513/04 , C07D417/10
CPC分类号: C07D279/08 , C07D417/04 , C07D417/10 , C07D417/12 , C07D513/04
摘要: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein X is selected from the group of CH2, O, and NR2; m=0 or 1; R1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is a bond, —NHCO—, —NH—, or L and Z together can be absent; Z is a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, acetyl, and methanesulfonyl; and R3, R4 and R5 are independently selected from hydrogen or C1-4alkyl.
摘要翻译: 包括其药学上可接受的盐的式(I)化合物在本文中阐述:其中X选自CH 2,O和NR 2; m = 0或1; 每个实例的R 1选自卤素,羟基,氨基,C 1-4烷基氨基,C 1-4二烷基氨基,卤代C 1-4烷基,CN,C 1 -C 6烷基或环烷基,C 1 -C 6烷氧基和C 2 -C 4炔基; L是键,-NHCO-,-NH-或L和Z可以不存在; Z是可以被0-3个选自卤素,卤代C 1-4烷氧基,4-甲氧基苯基,羟基,氨基,C 1 -C 10 - 芳基的取代基取代的C 6 -C 10 - 芳基或5-10元杂环基, C 1-4烷基氨基,卤代C 1-4烷基,CN,C 1 -C 6烷基或环烷基,C 1 -C 6烷氧基和C 2 -C 4炔基; R 2选自氢,苄基,C 1 -C 6烷基或环烷基,C 1 -C 6烷氧基,乙酰基和甲磺酰基; 并且R 3,R 4和R 5独立地选自氢或C 1-4烷基。
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公开(公告)号:US20130115190A1
公开(公告)日:2013-05-09
申请号:US13459403
申请日:2012-04-30
申请人: Sheldon Hiebert , Ramkumar Rajamani , Li-Qiang Sun , Eric Mull , Eric P. Gillis , Michael S. Bowsher , Qian Zhao , Nicholas A. Meanwell , Kishore V. Renduchintala , Kandhasamy Sarkunam , Pulicharla Nagalakshmi , P. V. K. Suresh Babu , Paul Michael Scola
发明人: Sheldon Hiebert , Ramkumar Rajamani , Li-Qiang Sun , Eric Mull , Eric P. Gillis , Michael S. Bowsher , Qian Zhao , Nicholas A. Meanwell , Kishore V. Renduchintala , Kandhasamy Sarkunam , Pulicharla Nagalakshmi , P. V. K. Suresh Babu , Paul Michael Scola
CPC分类号: C07K5/0823 , A61K31/13 , A61K31/4745 , A61K31/7056 , A61K38/00 , A61K38/06 , A61K38/2013 , A61K38/204 , A61K38/2053 , A61K38/21 , A61K38/212 , A61K45/06 , C07D487/04 , C07K5/0804 , C07K5/0827 , A61K2300/00
摘要: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
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公开(公告)号:US08044087B2
公开(公告)日:2011-10-25
申请号:US12566286
申请日:2009-09-24
IPC分类号: A61K31/407 , C07D209/00 , C07D495/02
CPC分类号: C07D513/18 , C07K5/0804 , C07K5/081
摘要: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
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公开(公告)号:US08957203B2
公开(公告)日:2015-02-17
申请号:US13459403
申请日:2012-04-30
申请人: Sheldon Hiebert , Ramkumar Rajamani , Li-Qiang Sun , Eric Mull , Eric P. Gillis , Michael S. Bowsher , Qian Zhao , Nicholas A. Meanwell , Kishore V. Renduchintala , Kandhasamy Sarkunam , Pulicharla Nagalakshmi , P. V. K. Suresh Babu , Paul Michael Scola
发明人: Sheldon Hiebert , Ramkumar Rajamani , Li-Qiang Sun , Eric Mull , Eric P. Gillis , Michael S. Bowsher , Qian Zhao , Nicholas A. Meanwell , Kishore V. Renduchintala , Kandhasamy Sarkunam , Pulicharla Nagalakshmi , P. V. K. Suresh Babu , Paul Michael Scola
IPC分类号: C07D225/00 , C07D295/00 , C07D245/00 , C07D225/04 , C07D487/00 , C07D487/04 , C07K5/083 , C07K5/08 , A61K38/20 , A61K38/21 , A61K45/06 , A61K31/13 , A61K31/4745 , A61K31/7056 , A61K38/00
CPC分类号: C07K5/0823 , A61K31/13 , A61K31/4745 , A61K31/7056 , A61K38/00 , A61K38/06 , A61K38/2013 , A61K38/204 , A61K38/2053 , A61K38/21 , A61K38/212 , A61K45/06 , C07D487/04 , C07K5/0804 , C07K5/0827 , A61K2300/00
摘要: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
摘要翻译: 公开了具有通式(I)的丙型肝炎病毒抑制剂。 还公开了包含化合物的组合物和使用该化合物抑制HCV的方法。
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公开(公告)号:US08343999B2
公开(公告)日:2013-01-01
申请号:US12595065
申请日:2008-04-09
申请人: Anne Marinier , Marco Dodier , Stephan Roy , Kurt Zimmermann , Xiaopeng Sang , Mark D. Wittman , David R. Langley , Ramkumar Rajamani
发明人: Anne Marinier , Marco Dodier , Stephan Roy , Kurt Zimmermann , Xiaopeng Sang , Mark D. Wittman , David R. Langley , Ramkumar Rajamani
IPC分类号: A61K31/4427 , C07D417/14
CPC分类号: C07D417/14
摘要: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's disease.
摘要翻译: 本发明提供式I化合物及其药学上可接受的盐。 式I噻唑基化合物抑制酪氨酸激酶活性,从而使它们用作抗癌剂和治疗阿尔茨海默氏病。
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