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公开(公告)号:US20090060912A1
公开(公告)日:2009-03-05
申请号:US12188984
申请日:2008-08-08
申请人: John N. Nuss , Sabina Pecchi , Paul A. Renhowe
发明人: John N. Nuss , Sabina Pecchi , Paul A. Renhowe
IPC分类号: A61K31/5377 , C07D413/14 , A61K31/551 , A61P35/00 , A61K39/395 , C07D243/08
CPC分类号: C07D239/42 , C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要: Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and combinations with other agents. A method of treating a patient comprises administering a pharmaceutical formulation according to the invention to a patient in need thereof.
摘要翻译: 提供具有式I的化合物,其中变量具有本文所述的值。 药物制剂包括其化合物或其药学上可接受的盐和药学上可接受的载体以及与其它药剂的组合。 治疗患者的方法包括向有需要的患者施用根据本发明的药物制剂。
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公开(公告)号:US07423148B2
公开(公告)日:2008-09-09
申请号:US10719896
申请日:2003-11-21
申请人: John N. Nuss , Sabina Pecchi , Paul A. Renhowe
发明人: John N. Nuss , Sabina Pecchi , Paul A. Renhowe
IPC分类号: C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , A61K31/506 , A61K31/496 , A61K31/5377 , A61P35/00
CPC分类号: C07D239/42 , C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要: Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and combinations with other agents. A method of treating a patient comprises administering a pharmaceutical formulation according to the invention to a patient in need thereof.
摘要翻译: 提供具有式I的化合物,其中变量具有本文所述的值。 药物制剂包括其化合物或其药学上可接受的盐和药学上可接受的载体以及与其它药剂的组合。 治疗患者的方法包括向有需要的患者施用根据本发明的药物制剂。
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公开(公告)号:US20100003246A1
公开(公告)日:2010-01-07
申请号:US12383035
申请日:2009-03-19
申请人: Zilin Hunag , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
发明人: Zilin Hunag , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
IPC分类号: A61K31/444 , C07D401/14 , C07D403/14 , C07D471/04 , A61K31/506 , A61K31/437 , A61P35/00 , A61K31/4545 , A61K31/7068 , A61K31/505 , A61K33/24 , A61K39/395
CPC分类号: C07D498/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
摘要翻译: 提供了新的取代的杂环化合物,含有它们的组合物,以及使用它们来抑制Raf激酶活性的方法。 新化合物和组合物可以单独使用或与至少一种另外的药物组合使用,用于治疗Raf激酶介导的病症,例如癌症。
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54.
公开(公告)号:US5958792A
公开(公告)日:1999-09-28
申请号:US485006
申请日:1995-06-07
申请人: Manoi C. Desai , John M. Nuss , Kerry L. Spear , Rajinder Singh , Paul A. Renhowe , Edward G. Brown , Lutz Richter , Barbara O. Scott
发明人: Manoi C. Desai , John M. Nuss , Kerry L. Spear , Rajinder Singh , Paul A. Renhowe , Edward G. Brown , Lutz Richter , Barbara O. Scott
IPC分类号: C07D239/42 , C07B61/00 , C07C235/84 , C07D207/16 , C07D211/76 , C07D211/86 , C07D213/85 , C07D223/16 , C07D307/46 , C07D309/32 , C07D491/052 , C07D493/04 , C07K1/04 , C40B40/04 , C40B50/00 , G01N33/543 , A61K38/06 , G01N33/53 , G01N33/545
CPC分类号: C40B50/14 , C07C231/12 , C07K1/047 , C40B40/04 , C07B2200/11
摘要: The invention relates to libraries of cyclic organic compounds and method of producing and assaying such libraries. According to the invention, each cyclic organic compound is constructed from a starting material in the form of a solid surface derivatized with a starting resin. Compounds are reacted with the resin to add or to form a cyclic group. The reactions are preferable carried out using a split resin procedure so that different compounds can be reacted with a plurality of subamounts so as to increase the size of the library. For example, compounds are reacted with a solid support bound starting resin to obtain a compound which includes an aldehyde functional group wherein the aldehyde compound or compounds reacted with it have substituents which are varied such that a mixture of products is obtained. The invention further relates to methods of producing combinatorial libraries of cyclic organic compounds from substrate bound compounds by cleaving the compounds from the support after synthesizing is completed and to assaying libraries of such compounds.
摘要翻译: 本发明涉及循环有机化合物的文库以及生产和测定这些文库的方法。 根据本发明,每种环状有机化合物由起始树脂衍生化的固体表面形式的原料构成。 化合物与树脂反应以加成或形成环状基团。 反应优选使用裂解树脂方法进行,使得不同的化合物可以与多个次级基团反应,从而增加文库的大小。 例如,使化合物与固体支持体结合的起始树脂反应,得到包含醛官能团的化合物,其中醛化合物或与其反应的化合物具有变化的取代基,从而得到产物的混合物。 本发明还涉及通过在合成完成后从载体上切割化合物和测定这些化合物的文库,从底物结合的化合物生产环状有机化合物的组合文库的方法。
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公开(公告)号:US20130210818A1
公开(公告)日:2013-08-15
申请号:US13396339
申请日:2012-02-14
申请人: Zilin Huang , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
发明人: Zilin Huang , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
IPC分类号: A61K31/444 , A61K31/506 , C07D403/14 , C07D405/14 , A61K31/4439 , C07D417/14 , C07D471/04 , C07D413/14 , A61K31/496 , C07D487/04 , A61K31/4985 , C07D498/04 , A61K31/5383 , A61K31/4709 , A61K31/5377 , A61P35/00 , C07D401/14
CPC分类号: A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/5383 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04 , A61K2300/00
摘要: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
摘要翻译: 提供了新的取代的杂环化合物,含有它们的组合物,以及使用它们来抑制Raf激酶活性的方法。 新化合物和组合物可以单独使用或与至少一种另外的药物组合使用,用于治疗Raf激酶介导的病症,例如癌症。
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公开(公告)号:US06759417B2
公开(公告)日:2004-07-06
申请号:US10452786
申请日:2003-06-02
申请人: Paul A. Renhowe , Cynthia M. Shafer
发明人: Paul A. Renhowe , Cynthia M. Shafer
IPC分类号: A61K3138
CPC分类号: C07D471/04 , C07D495/04
摘要: Organic compounds having the structural formulas I, II, and III are provided where the variables have the values described herein and R1 and R2 in structure I join together to form a 5 to 7 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group in structures I and II. Pharmaceutical formulations include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.
摘要翻译: 提供具有结构式I,II和III的有机化合物,其中变量具有本文所述的值,并且结构I中的R 1和R 2连接在一起形成5至7元取代或未取代的环,包括在 至少一个O,N或S原子,Z是结构I和II中的O,S,NH或NR基团。药物制剂包括有机化合物或其药学上可接受的盐和药学上可接受的载体。 治疗患者的方法包括向有需要的患者施用本发明的药物制剂。
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公开(公告)号:US08865732B2
公开(公告)日:2014-10-21
申请号:US13396339
申请日:2012-02-14
申请人: Zilin Huang , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
发明人: Zilin Huang , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
IPC分类号: A61K31/505 , C07D241/02
CPC分类号: A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/5383 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04 , A61K2300/00
摘要: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
摘要翻译: 提供了新的取代的杂环化合物,含有它们的组合物,以及使用它们来抑制Raf激酶活性的方法。 新化合物和组合物可以单独使用或与至少一种另外的药物组合使用,用于治疗Raf激酶介导的病症,例如癌症。
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公开(公告)号:US08129394B2
公开(公告)日:2012-03-06
申请号:US12383035
申请日:2009-03-19
申请人: Zilin Hunag , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
发明人: Zilin Hunag , Jeff Jin , Timothy Machajewski , William R. Antonios-McCrea , Maureen McKenna , Daniel Poon , Paul A. Renhowe , Martin Sendzik , Cynthia Shafer , Aaron Smith , Yongjin Xu , Qiong Zhang , Zheng Chen
IPC分类号: A61K31/4965 , A61K31/505 , A01N43/54 , C07D403/00 , C07D401/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号: C07D498/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要: Novel imidazole compounds of the general formula are disclosed, wherein R1 and R2 comprise heteroaryl groups. These compounds and compositions containing them are useful in methods to treat Raf kinase-mediated disorders such as cancer.
摘要翻译: 公开了通式的新型咪唑化合物,其中R 1和R 2包含杂芳基。 这些含有它们的化合物和组合物可用于治疗Raf激酶介导的疾病如癌症的方法。
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公开(公告)号:US07642278B2
公开(公告)日:2010-01-05
申请号:US11261995
申请日:2005-10-27
IPC分类号: A01N43/52 , C07D235/00
CPC分类号: C07D403/04
摘要: Organic compounds having the structure I are provided where the variables have the values described herein. A method of inhibiting c-ABL in a patient includes administering an effective amount of a compound of structure I, a tautomer of the compound, a pharmaceutically acceptable salt of the compound, or a pharmaceutically acceptable salt of the tautomer to the patient.
摘要翻译: 提供具有结构I的有机化合物,其中变量具有本文所述的值。 抑制患者中c-ABL的方法包括向患者施用有效量的结构I化合物,化合物的互变异构体,化合物的药学上可接受的盐或互变异构体的药学上可接受的盐。
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