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公开(公告)号：US20100063066A1
公开(公告)日：2010-03-11
申请号：US12438967
申请日：2007-08-31
申请人： Alexandre J. Buckmelter , Joseph P. Lyssikatos , Greg Miknia , Li Ren , Steven Mark Wenglowsky , Bryson Rast
发明人： Alexandre J. Buckmelter , Joseph P. Lyssikatos , Greg Miknia , Li Ren , Steven Mark Wenglowsky , Bryson Rast
IPC分类号： A61K31/497 , C07D401/14 , C07D471/04 , A61K31/4439 , A61P35/00
CPC分类号： C07D491/04
摘要： Compounds of Formulas (I), (IIA) and (IIIA) are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formulas (I), (IIA) and (IIIA) and stereoisomers and pharmaceutically acceptable salts thereof, 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），（IIA）和（IIIA）的化合物可用于抑制Raf激酶和用于治疗由此介导的病症。 使用式（I），（IIA）和（IIIA）化合物及其立体异构体及其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞中的这种病症或相关病理学的方法 条件被公开。
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公开(公告)号：US20090203585A1
公开(公告)日：2009-08-13
申请号：US12299258
申请日：2007-03-13
CPC分类号： C07K7/56 , A61K38/00 , Y02A50/401
摘要： The present invention relates to phenylurea derivatives of capreomycin I, IIB, IIA, or IB, and metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present invention are useful as antibacterial agents for treating bacterial infections and for treating disorders caused by bacterial infections. The present invention also relates to pharmaceutical compositions containing such compounds and to methods of treating bacterial infections by administering such compounds. The present invention also relates to methods of preparing such compounds.
摘要翻译： 本发明涉及卷曲霉素I，IIB，IIA或IB的苯基脲衍生物及其代谢产物及其药学上可接受的盐和溶剂化物。 本发明的化合物可用作治疗细菌感染和治疗由细菌感染引起的疾病的抗菌剂。 本发明还涉及含有这些化合物的药物组合物和通过施用这些化合物治疗细菌感染的方法。 本发明还涉及制备这些化合物的方法。
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公开(公告)号：US07294616B2
公开(公告)日：2007-11-13
申请号：US11261717
申请日：2005-10-31
IPC分类号： A61K38/12
CPC分类号： C07K7/56 , A61K38/00 , Y02A50/401 , Y02A50/473
摘要： The present subject matter relates to phenylurea capreomycin derivatives, and to metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present subject matter are useful as antibacterial agents for treating bacterial infections and for treating disorders caused by bacterial infections. The present subject matter also relates to pharmaceutical compositions containing such compounds and to methods of treating bacterial infections by administering such compounds. The present subject matter also relates to methods of preparing such compounds.
摘要翻译： 本主题涉及苯脲卷曲霉素衍生物及其代谢物及其药学上可接受的盐和溶剂化物。 本发明的化合物可用作用于治疗细菌感染和治疗由细菌感染引起的疾病的抗菌剂。 本发明还涉及含有这些化合物的药物组合物和通过施用这些化合物治疗细菌感染的方法。 本发明还涉及制备这些化合物的方法。
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公开(公告)号：US20110144085A1
公开(公告)日：2011-06-16
申请号：US13059902
申请日：2009-08-18
申请人： Shelley Allen , Laura L. Celeste , T. Gregg Davis , Robert Kirk DeLisle , Julie Marie Greschuk , Stefan D. Gross , Erik James Hicken , Leila J. Jackson , Nicholas C. Kallan , Joseph P. Lyssikatos , Fredrik P. Marmsater , Mark C. Munson , Jed Pheneger , Bryson Rast , John E. Robinson , Stephen T. Schlachter , George T. Topalov , A. Dale Wright , Qian Zhao
发明人： Shelley Allen , Laura L. Celeste , T. Gregg Davis , Robert Kirk DeLisle , Julie Marie Greschuk , Stefan D. Gross , Erik James Hicken , Leila J. Jackson , Nicholas C. Kallan , Joseph P. Lyssikatos , Fredrik P. Marmsater , Mark C. Munson , Jed Pheneger , Bryson Rast , John E. Robinson , Stephen T. Schlachter , George T. Topalov , A. Dale Wright , Qian Zhao
IPC分类号： A61K31/55 , C07D471/04 , A61K31/437 , A61K31/513 , A61K31/5377 , A61P35/00 , A61P25/00 , A61P29/00
CPC分类号： C07D471/04
摘要： Compounds of Formula (I), in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of immune cell-associated diseases and disorders, such as inflammatory and autoimmune diseases.
摘要翻译： 其中A，B，R1，R1a，R2，R3，R4，R5，R6和R7具有本说明书中给出的含义的式（I）化合物是可用于治疗免疫细胞相关的受体酪氨酸抑制剂 疾病和病症，例如炎性和自身免疫性疾病。
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公开(公告)号：US08575145B2
公开(公告)日：2013-11-05
申请号：US13059902
申请日：2009-08-18
申请人： Shelley Allen , Laura L. Celeste , T. Gregg Davis , Robert Kirk DeLisle , Julie Marie Greschuk , Stefan D. Gross , Erik James Hicken , Leila J. Jackson , Nicholas C. Kallan , Joseph P. Lyssikatos , Fredrik P. Marmsater , Mark C. Munson , Jed Pheneger , Bryson Rast , John E. Robinson , Stephen T. Schlachter , George T. Topalov , A. Dale Wright , Qian Zhao
发明人： Shelley Allen , Laura L. Celeste , T. Gregg Davis , Robert Kirk DeLisle , Julie Marie Greschuk , Stefan D. Gross , Erik James Hicken , Leila J. Jackson , Nicholas C. Kallan , Joseph P. Lyssikatos , Fredrik P. Marmsater , Mark C. Munson , Jed Pheneger , Bryson Rast , John E. Robinson , Stephen T. Schlachter , George T. Topalov , A. Dale Wright , Qian Zhao
IPC分类号： A61K31/55 , A61K31/437 , A61K31/513 , A61K31/5377 , C07D471/04 , A61P35/00 , A61P25/00 , A61P29/00
CPC分类号： C07D471/04
摘要： Compounds of Formula (I), in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of immune cell-associated diseases and disorders, such as inflammatory and autoimmune diseases.
摘要翻译： 其中A，B，R1，R1a，R2，R3，R4，R5，R6和R7具有本说明书中给出的含义的式（I）化合物是可用于治疗免疫细胞相关的受体酪氨酸抑制剂 疾病和病症，例如炎性和自身免疫性疾病。
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6.发明授权公开(公告)号：US08623889B2
公开(公告)日：2014-01-07
申请号：US13325751
申请日：2011-12-14
IPC分类号： A01N43/42 , A61K31/44 , A61K31/47 , C07D221/02 , C07D471/02 , C07D217/00
CPC分类号： C07D471/04 , A61K31/47 , A61K31/4725 , C07D217/22 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/04
摘要： The invention provides novel compounds having the general formula: wherein X1 is N or N+O−, and one of X2, X3 and X4 is N or N+—O− and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.
摘要翻译： 本发明提供具有以下通式的新化合物：其中X 1是N或N + O-，X 2，X 3和X 4中的一个是N或N + -O-，X 2，X 3和X 4的其余部分是C。R2，R3 ，R4，R5，R6。 A，B和Y如本文所述。 此外，式I的组合物化合物和使用方法在本文中进一步描述。
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公开(公告)号：US20130109656A1
公开(公告)日：2013-05-02
申请号：US13586355
申请日：2012-08-15
申请人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robinson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtli
发明人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robinson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtli
IPC分类号： C07F9/6539 , C07D419/04 , C07D513/04 , C07D417/04
CPC分类号： C07D513/04 , C07D285/12 , C07D417/04 , C07D417/14 , C07D419/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D497/04 , C07F9/65395
摘要： This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
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公开(公告)号：US08003805B2
公开(公告)日：2011-08-23
申请号：US12824477
申请日：2010-06-28
IPC分类号： A61K31/422 , A61K31/4245 , A61K31/4184 , C07D403/04 , C07D413/04
CPC分类号： C07D235/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/06 , C07D417/12
摘要： Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.
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公开(公告)号：US07893065B2
公开(公告)日：2011-02-22
申请号：US12186202
申请日：2008-08-05
申请人： Allison L. Marlow , Eli M. Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
发明人： Allison L. Marlow , Eli M. Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
IPC分类号： C07D237/20 , A61K31/50 , A61P29/00 , A61P35/00
CPC分类号： C07D213/80 , A61K31/437 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/5025 , A61K31/5377 , A61K45/06 , C07D209/46 , C07D213/82 , C07D215/48 , C07D231/56 , C07D237/24 , C07D237/28 , C07D237/32 , C07D239/74 , C07D401/04 , C07D401/06 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , A61K2300/00
摘要： Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, and W are as defined in the specification. Such compounds are MEK inhibitors and are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative and inflammatory diseases in mammals and pharmaceutical compositions containing such compounds.
摘要翻译： 公开了式I化合物及其药学上可接受的盐和前药，其中R1，R2，R7，R8，R9和W如说明书中所定义。 这些化合物是MEK抑制剂，并且可用于治疗过度增殖性疾病，例如癌症和炎症，以及哺乳动物中的炎性病症。 还公开了使用这些化合物治疗哺乳动物中过度增生和炎性疾病的方法和含有这些化合物的药物组合物。
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10.发明申请COMPOSITIONS COMPRISING N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS AND METHODS OF USE THEREOF 有权包含作为MEK抑制剂的N 3烷氧基苯并咪唑衍生物的组合物及其使用方法公开(公告)号：US20100260714A1
公开(公告)日：2010-10-14
申请号：US12824547
申请日：2010-06-28
IPC分类号： A61K38/21 , A61K38/43 , A61K33/24 , A61K31/704 , A61K31/5375 , A61K31/513 , A61K31/4745 , A61K31/454 , A61K31/42 , A61K31/4184 , A61P35/00
CPC分类号： C07D235/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/06 , C07D417/12
摘要： Disclosed are pharmaceutical compositions comprising 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof. Also disclosed are methods of using such compositions for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals.
摘要翻译： 公开了包含6-（4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基 - 乙氧基） - 酰胺或其药学上可接受的盐的药物组合物。 还公开了使用这种组合物抑制哺乳动物异常细胞生长或治疗过度增殖性疾病的方法。
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