Compositions and methods for inhibiting TGF-Beta
    3.
    发明申请
    Compositions and methods for inhibiting TGF-Beta 失效
    用于抑制TGF-β的组合物和方法

    公开(公告)号:US20070142408A1

    公开(公告)日:2007-06-21

    申请号:US11653679

    申请日:2007-01-16

    CPC分类号: C07D471/04

    摘要: This invention provides compounds that are useful for treating patients having a TGF-β-mediated disease, particularly an ALK5-mediated disease. The compounds are represented by formula I: wherein: a-b is CH2CH2, CH2CH2CH2, CH═CH, CH═N, or N═CH; Z is N or C—F; and G is C1-6 aliphatic or a phenyl, naphthyl, or 5-6 membered heteroaryl ring.

    摘要翻译: 本发明提供可用于治疗患有TGF-β介导的疾病,特别是ALK5介导的疾病的患者的化合物。 化合物由式I表示:其中:ab是CH 2 CH 2 CH 2,CH 2 CH 2 CH 2 CH 2,CH-CH,CH-N或N-CH; Z是N或C-F; 和G为C 1-6脂族基或苯基,萘基或5-6元杂芳基环。

    COMPOSITIONS AND METHODS FOR INHIBITING TGF-BETA
    4.
    发明申请
    COMPOSITIONS AND METHODS FOR INHIBITING TGF-BETA 失效
    用于抑制TGF-β的组合物和方法

    公开(公告)号:US20080108656A1

    公开(公告)日:2008-05-08

    申请号:US11941284

    申请日:2007-11-16

    IPC分类号: A61K31/47 C07D215/38 A61P9/00

    CPC分类号: C07D401/12 C07D405/14

    摘要: The present invention provides compounds of the formula: and pharmaceutically acceptable isomers, salts, hydrates, solvates, and prodrug derivatives thereof, wherein R1, R6, R7, R8, Pg, and n are those defined herein. The present invention also provides pharmaceutical compositions comprising the same and methods for using the same. In particular, compounds of Formula I are useful in modulating TGF-β activity.

    摘要翻译: 本发明提供下式的化合物及其药学上可接受的异构体,盐,水合物,溶剂合物和前药衍生物,其中R 1,R 6,R 6, 7,R 8,P g和n是本文定义的那些。 本发明还提供了包含该组合物的药物组合物及其使用方法。 特别地,式I化合物可用于调节TGF-β活性。

    Nitrogenous heterocyclic compounds
    6.
    发明申请
    Nitrogenous heterocyclic compounds 审中-公开
    含氮杂环化合物

    公开(公告)号:US20060063770A1

    公开(公告)日:2006-03-23

    申请号:US11200456

    申请日:2005-08-08

    IPC分类号: A61K31/517

    摘要: The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

    摘要翻译: 本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。 本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。 在一个特定方面,本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐,以及预防或治疗细胞增殖性疾病如动脉硬化,血管 重建,癌症和肾小球硬化症。

    SUBSTITUTED-(QUINAZOLINYL)PHENYL THIOPHENYL-SULFONYLUREAS, METHODS FOR MAKING AND INTERMEDIATES THEREOF
    9.
    发明申请
    SUBSTITUTED-(QUINAZOLINYL)PHENYL THIOPHENYL-SULFONYLUREAS, METHODS FOR MAKING AND INTERMEDIATES THEREOF 审中-公开
    取代 - (喹喔啉基)苯基噻吩磺酰亚胺,其制备方法及其中间体

    公开(公告)号:US20070208045A1

    公开(公告)日:2007-09-06

    申请号:US11556518

    申请日:2006-11-03

    IPC分类号: A61K31/517 C07D409/02

    CPC分类号: C07D409/12

    摘要: The present invention provides sulfonylurea compounds of formula (VIII) and pharmaceutically acceptable derivatives thereof and a process for making thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention also provides a method for inhibition platelet ADP receptor and preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a compound of formula (VIII) or a pharmaceutically acceptable salt or forms thereof.

    摘要翻译: 本发明提供式(VIII)的磺酰脲化合物及其药学上可接受的衍生物及其制备方法。 各种形式的化合物是有效的血小板ADP受体抑制剂,可用于各种药物组合物中,并且特别有效预防和/或治疗心血管疾病,特别是与血栓形成有关的疾病。 本发明还提供了可用于该方法的中间体化合物,以及通过该方法生产的最终产物及其盐或前药。 本发明还提供了抑制血小板ADP受体并预防或治疗哺乳动物血栓形成和血栓形成相关病症的方法,包括施用治疗有效量的式(Ⅷ)化合物或其药学上可接受的盐或其形式的步骤。