公开(公告)号：US07772246B2

公开(公告)日：2010-08-10

申请号：US12182977

申请日：2008-07-30

Applicant: Jingrong Jean Cui ,  Judith Gail Deal ,  Danlin Gu ,  Chuangxing Guo ,  Mary Catherine Johnson ,  Robert Steven Kania ,  Susan Elizabeth Kephart ,  Maria Angelica Linton ,  Indrawan James McAlpine ,  Mason Alan Pairish ,  Cynthia Louise Palmer

Inventor： Jingrong Jean Cui ,  Judith Gail Deal ,  Danlin Gu ,  Chuangxing Guo ,  Mary Catherine Johnson ,  Robert Steven Kania ,  Susan Elizabeth Kephart ,  Maria Angelica Linton ,  Indrawan James McAlpine ,  Mason Alan Pairish ,  Cynthia Louise Palmer

IPC: A61K31/505

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D487/04

Abstract: The present invention is directed to compounds of Formula (I), and to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.

Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐，其合成及其作为Raf抑制剂的用途。

公开(公告)号：US07884117B2

公开(公告)日：2011-02-08

申请号：US12158241

申请日：2006-12-12

Applicant: Junhun Zhang ,  Anle Yang ,  Susan Elizabeth Kephart ,  Liming Dong ,  Chuangxing Guo ,  Yufeng Hong ,  Mary Catherine Johnson ,  Indrawan James McAlpine ,  Jayashree Tikhe ,  Haitao Li

Inventor： Junhun Zhang ,  Anle Yang ,  Susan Elizabeth Kephart ,  Liming Dong ,  Chuangxing Guo ,  Yufeng Hong ,  Mary Catherine Johnson ,  Indrawan James McAlpine ,  Jayashree Tikhe ,  Haitao Li

IPC: A61K31/422 ,  A61K31/4162 ,  C07D261/06 ,  C07D231/54

CPC classification number: C07D487/04

Abstract: Carbonylamino Pyrrolopyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.

Abstract translation: 提供式I的羰基氨基吡咯并吡唑化合物，包括这些化合物的组合物及其使用方法。 优选的式I化合物具有作为蛋白激酶抑制剂的活性，包括作为PAK4的抑制剂。

公开(公告)号：US20090221608A1

公开(公告)日：2009-09-03

申请号：US12182977

申请日：2008-07-30

Applicant: Jingrong Jean Cui ,  Judith Gail Deal ,  Danlin Gu ,  Chuangxing Guo ,  Mary Catherine Johnson ,  Robert Steven Kania ,  Susan Elizabeth Kephart ,  Maria Angelica Linton ,  Indrawan James McAlpine ,  Mason Alan Pairish ,  Cynthia Louise Palmer

Inventor： Jingrong Jean Cui ,  Judith Gail Deal ,  Danlin Gu ,  Chuangxing Guo ,  Mary Catherine Johnson ,  Robert Steven Kania ,  Susan Elizabeth Kephart ,  Maria Angelica Linton ,  Indrawan James McAlpine ,  Mason Alan Pairish ,  Cynthia Louise Palmer

IPC: A61K31/506 ,  C07D401/14 ,  A61K31/496 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D487/04

Abstract: The present invention is directed to compounds of Formula (I), and to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.

Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐，其合成及其作为Raf抑制剂的用途。

公开(公告)号：US07008953B2

公开(公告)日：2006-03-07

申请号：US10866059

申请日：2004-06-10

Applicant: Susan Elizabeth Kephart ,  Indrawan James McAlpine ,  Siegfried Heinz Reich

Inventor： Susan Elizabeth Kephart ,  Indrawan James McAlpine ,  Siegfried Heinz Reich

IPC: A61K31/4439 ,  C07D401/14

CPC classification number: C07D401/14

Abstract: 3,5 disubstituted indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating CDK dependent diseases to 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 as well as 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.

Abstract translation: 描述了调节和/或抑制细胞增殖的3,5二取代吲唑化合物，例如蛋白激酶的活性。 这些化合物和含有它们的药物组合物能够介导CDK依赖性疾病调节和/或抑制不期望的细胞增殖。 本发明还涉及含有这些化合物的药物组合物的治疗或预防用途，以及治疗癌症以及与不想要的血管发生和/或细胞增殖相关的其它疾病状态的方法，例如糖尿病性视网膜病变，新生血管性青光眼，类风湿性关节炎 和牛皮癣，通过施用有效量的这种化合物。