公开(公告)号：US20080090801A1

公开(公告)日：2008-04-17

申请号：US11854999

申请日：2007-09-13

申请人： Hengmiao Cheng ,  Dilip Bhumralkar ,  Klaus Dress ,  Jacqui Hoffman ,  Mary Johnson ,  Robert Kania ,  Phuong Le ,  Mitchell Nambu ,  Mason Pairish ,  Michael Plewe ,  Khanh Tran

发明人： Hengmiao Cheng ,  Dilip Bhumralkar ,  Klaus Dress ,  Jacqui Hoffman ,  Mary Johnson ,  Robert Kania ,  Phuong Le ,  Mitchell Nambu ,  Mason Pairish ,  Michael Plewe ,  Khanh Tran

IPC分类号： A61K31/519 ,  A61P35/00 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), and to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-Kα).

摘要翻译： 本发明涉及式（I）的新颖的4-甲基吡啶并嘧啶酮化合物及其盐，它们的合成及其作为磷酸肌醇3-激酶α（PI3-Kalpha）抑制剂的用途。

公开(公告)号：US20050197492A1

公开(公告)日：2005-09-08

申请号：US10824982

申请日：2004-04-15

申请人： Steven Bender ,  Robert Kania ,  Michele McTigue ,  Cynthia Palmer ,  Chris Pinko ,  John Wickersham

发明人： Steven Bender ,  Robert Kania ,  Michele McTigue ,  Cynthia Palmer ,  Chris Pinko ,  John Wickersham

IPC分类号： C07K14/71 ,  G06F19/16

CPC分类号： C07K14/71 ,  C07K2299/00 ,  G16B15/00

摘要： Polypeptides containing the kinase domain of a VEGFR are described. Also described are crystal structures of these polypeptides, including the crystal structures of VEGFR2KD:ligand complexes. The atomic coordinates derived from the crystal structures provide a three-dimensional description of the ligand-binding pocket of the kinase domain useful in drug discovery and design for the identification and design of modulators of kinase activity.

摘要翻译： 描述了含有VEGFR的激酶结构域的多肽。 还描述了这些多肽的晶体结构，包括VEGFR2KD：配体复合物的晶体结构。 衍生自晶体结构的原子坐标提供了可用于药物发现和设计用于激酶活性调节剂的设计的激酶结构域的配体结合口袋的三维描述。

公开(公告)号：US20050070508A1

公开(公告)日：2005-03-31

申请号：US10924528

申请日：2004-08-23

申请人： Jihong Lou ,  Robert Kania ,  Mingying He ,  Ru Zhou

发明人： Jihong Lou ,  Robert Kania ,  Mingying He ,  Ru Zhou

IPC分类号： A61P35/00 ,  C07D213/68 ,  C07D215/20 ,  C07D239/34 ,  C07D239/42 ,  C07D495/04 ,  A61K31/655 ,  A61K31/165 ,  A61K31/519

CPC分类号： C07D239/34 ,  C07D213/68 ,  C07D215/20 ,  C07D239/42 ,  C07D495/04

摘要： The invention relates to compounds represented by Formula (I): and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein each of R1a-d, R2a-b, R3, and X1 are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).

摘要翻译： 本发明涉及由式（I）表示的化合物及其前药，所述化合物或所述前药的药学上可接受的盐或溶剂合物，其中R 1a-d，R 2a-b，R 3， ，X 1如本文所定义。 本发明还涉及含有式（I）化合物的药物组合物以及通过施用式（I）的化合物来治疗哺乳动物的过度增殖性疾病的方法。

公开(公告)号：US20060160858A1

公开(公告)日：2006-07-20

申请号：US11305811

申请日：2005-12-16

申请人： Allen Borchardt ,  Robert Kania ,  Cynthia Palmer

发明人： Allen Borchardt ,  Robert Kania ,  Cynthia Palmer

IPC分类号： A61K31/444 ,  A61K31/4439 ,  A61K31/4162

CPC分类号： A61K31/416 ,  C07D231/56 ,  C07D401/06 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14

摘要： Indazole compounds that modulate and/or inhibit the ophthalmic diseases and the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating ophthalmic diseases and cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

公开(公告)号：US20060079548A1

公开(公告)日：2006-04-13

申请号：US11256477

申请日：2005-10-21

申请人： Michael Collins ,  Stephan Cripps ,  Judith Deal ,  Robert Kania ,  Jihong Lou ,  Mingying He ,  Cynthia Palmer ,  William Romines ,  Ru Zhou

发明人： Michael Collins ,  Stephan Cripps ,  Judith Deal ,  Robert Kania ,  Jihong Lou ,  Mingying He ,  Cynthia Palmer ,  William Romines ,  Ru Zhou

IPC分类号： A61K31/4743 ,  C07D498/02

CPC分类号： A61K31/4743 ,  C07D495/04

摘要： The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R11 and R14, R15, R16, and R17 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.

摘要翻译： 本发明涉及由式I表示的化合物及其前体药物或代谢物，或所述化合物，所述前药和所述代谢产物的药学上可接受的盐或溶剂合物，其中Z，Y，R 11和R R 15，R 16，R 16和R 17如本文所定义。 本发明还涉及含有式I化合物的药物组合物和通过施用式I化合物来治疗哺乳动物中过度增殖性疾病的方法。

公开(公告)号：US20060014821A1

公开(公告)日：2006-01-19

申请号：US10918612

申请日：2004-08-13

申请人： Mingying He ,  Robert Kania ,  Jihong Lou ,  Simon Planken

发明人： Mingying He ,  Robert Kania ,  Jihong Lou ,  Simon Planken

IPC分类号： A61K31/4015 ,  C07D207/26

CPC分类号： C07D207/26

摘要： The invention relates to methods of inhibiting SARS-related coronavirus viral replication activity comprising contacting a SARS-related coronavirus protease with a therapeutically effective amount of a SARS 3C like protease inhibitor, and compositions comprising the same.

摘要翻译： 本发明涉及抑制SARS相关冠状病毒病毒复制活性的方法，包括使SARS相关冠状病毒蛋白酶与治疗有效量的SARS 3C样蛋白酶抑制剂接触，以及包含该SARS相关冠状病毒病毒复制活性的组合物。

公开(公告)号：US20050124662A1

公开(公告)日：2005-06-09

申请号：US10992146

申请日：2004-11-18

申请人： Robert Kania ,  Steven Bender ,  Allen Borchardt ,  Stephan Cripps ,  Cynthia Louise Palmer ,  Anna Maria Tempczyk-Russell ,  Michael Varney ,  Michael Raymond Collins

发明人： Robert Kania ,  Steven Bender ,  Allen Borchardt ,  Stephan Cripps ,  Cynthia Louise Palmer ,  Anna Maria Tempczyk-Russell ,  Michael Varney ,  Michael Raymond Collins

IPC分类号： C07D209/18 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  A61K31/4439 ,  A61K31/416

CPC分类号： C07D401/12 ,  C07D209/18 ,  C07D401/14 ,  C07D403/12

摘要： Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

公开(公告)号：US20050137395A1

公开(公告)日：2005-06-23

申请号：US11015508

申请日：2004-12-16

申请人： Yufeng Hong ,  Robert Kania

发明人： Yufeng Hong ,  Robert Kania

IPC分类号： A61K31/4709 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C11D17/00

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04

摘要： The invention relates to compounds represented by Formula (I): and to pharmaceutically acceptable salts or solvates of said compounds, wherein each of A, R3-8, X3, X5, m, and n are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).

摘要翻译： 本发明涉及由式（I）表示的化合物：和所述化合物的药学上可接受的盐或溶剂合物，其中A，R 3，X 3，X 3， 本文定义了X 5，m和n。 本发明还涉及含有式（I）化合物的药物组合物以及通过施用式（I）的化合物来治疗哺乳动物的过度增殖性疾病的方法。

公开(公告)号：US20050090509A1

公开(公告)日：2005-04-28

申请号：US10928674

申请日：2004-08-26

申请人： Jihong Lou ,  Robert Kania ,  Mingying He

发明人： Jihong Lou ,  Robert Kania ,  Mingying He

IPC分类号： A61P35/00 ,  C07D495/04 ,  C07D498/02 ,  A61K31/4743 ,  A61K31/519

CPC分类号： C07D495/04

摘要： The invention relates to compounds represented by Formula (I): and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein each of X1-X5 and R1-R5 are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).

摘要翻译： 本发明涉及由式（I）表示的化合物及其前药，所述化合物或所述前药的药学上可接受的盐或溶剂化物，其中X 1〜X 5 >和R 1〜R 5 5定义在本文中。 本发明还涉及含有式（I）化合物的药物组合物以及通过施用式（I）的化合物来治疗哺乳动物的过度增殖性疾病的方法。

公开(公告)号：US20060094763A1

公开(公告)日：2006-05-04

申请号：US11264493

申请日：2005-10-31

申请人： Qiang Ye ,  Ryan Hart ,  Robert Kania ,  Michael Ouellette ,  Zhen Wu ,  Scott Zook

发明人： Qiang Ye ,  Ryan Hart ,  Robert Kania ,  Michael Ouellette ,  Zhen Wu ,  Scott Zook

IPC分类号： A61K31/4439 ,  C07D403/02

CPC分类号： C07D401/06

摘要： The present invention relates to novel polymorphic forms of 6-[2-(methylcarbamoyl)phenylsulfanyl]-3-E-[2-(pyridin-2-yl)ethenyl]indazole, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a hyperproliferative disorder or a mammalian disease condition mediated by protein kinase activity.

摘要翻译： 本发明涉及6- [2-（甲基氨基甲酰基）苯基硫烷基] -3-E- [2-（吡啶-2-基）乙烯基]吲唑的新型多晶型物及其制备方法。 这种多晶型物可以是药物组合物的组分，并且可以用于治疗由蛋白激酶活性介导的过度增殖性疾病或哺乳动物疾病状况。