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    2,4-dioxo-3-quinazolinylaryl sulfonylureas
    2.
    发明授权
    2,4-dioxo-3-quinazolinylaryl sulfonylureas 失效
    2,4-二氧代-3-喹唑啉基芳基磺酰脲

    公开(公告)号：US07109332B2

    公开(公告)日：2006-09-19

    申请号：US10956004

    申请日：2004-09-29

    申请人： Robert M. Scarborough ,  Wolin Huang ,  Anjali Pandey ,  Shawn M. Bauer ,  Xiaoming Zhang ,  Zhaozhong J. Jia

    发明人： Robert M. Scarborough ,  Wolin Huang ,  Anjali Pandey ,  Shawn M. Bauer ,  Xiaoming Zhang ,  Zhaozhong J. Jia

    IPC分类号： C07D409/12 ,  C07D409/14 ,  A61K31/517 ,  A61P7/02

    CPC分类号： C07D409/12 ,  C07D409/14

    摘要： 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds having the formula: wherein R is a member selected from the group consisting of H and C1-6 alkyl; R1 is a member selected from the group consisting of H, C1-6 alkyl, C1-6 haloalkyl, C3-5 cycloalkyl and C3-5 cycloalkyl-alkyl; R2 is a member selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy, cyano and —C(O)R2a, wherein R2a is a member selected from the group consisting of C1-6 alkoxy and (C1-6 alkyl)0-2 amino; L is a 1 to 3 carbon linking group selected from the group consisting of —CH2—, —CH(CH3)—, —CH2CH2—, —CH2CH(CH3)— and —CH2CH2CH2—; L1 is a linking group selected from the group consisting of a bond and —CH2—; L2 is a linking group selected from the group consisting of a bond, —NH— and —CH2—; and Ar1 is an aromatic ring selected from the group consisting of benzene, pyridine and pyrimidine; are provided. The compounds are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.

    摘要翻译： 2,4-二氧代-3-喹唑啉基芳基磺酰脲类化合物，其具有下式：其中R是选自H和C 1-6烷基的成员; R 1是选自H，C 1-6烷基，C 1-6卤代烷基，C 1 -C 6烷基，C 1 -C 6烷基， 3-5个环烷基和C 3-5环烷基 - 烷基; R 2是选自H，卤素，C 1-6 - 烷基，C 2-6 - 烯基，C 1 -C 6烷基， C 1-6烷基，C 1-6烷氧基，氰基和-C（O）R 2a， 其中R 2a是选自C 1-6烷氧基和（C 1-6烷基）烷基的成员， 0-2氨基; L是选自-CH 2 - ， - CH（CH 3 CH 3） - ， - CH 2 - ， - CH 2 CH 2（CH 3 CH 3） - 和-CH 2 CH 2 CH 2 - ; L 1是选自键和-CH 2 - 的连接基团。 L 2是从由-NH-和-CH 2 - 的键组成的组中的连接基团。 和Ar 1是选自苯，吡啶和嘧啶的芳环; 被提供。 该化合物可用于抑制ADP-血小板聚集，特别是在治疗血栓形成和血栓相关病症或病症中。

    Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof
    6.
    再颁专利
    Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof 失效
    含氮杂环化合物及其制备含氮杂环化合物的方法及其中间体

    公开(公告)号：USRE43098E1

    公开(公告)日：2012-01-10

    申请号：US11866275

    申请日：2007-10-02

    申请人： James Kanter ,  Anjali Pandey ,  James Robinson ,  Robert M. Scarborough ,  Carroll Scarborough, legal representative

    发明人： James Kanter ,  Anjali Pandey ,  James Robinson ,  Robert M. Scarborough

    IPC分类号： A61K31/495 ,  C07D487/00 ,  C07D487/04 ,  C07D239/94

    摘要： The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. 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 further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.

    摘要翻译： 本发明提供了含氮杂环化合物及其药学上可接受的盐及其制备方法。 这些化合物对抑制这种激酶活性的激酶的磷酸化具有抑制活性。 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。 本发明进一步提供了通过抑制激酶的磷酸化来抑制哺乳动物激酶和治疗疾病状态的方法，包括向有需要的患者施用有效量的本发明化合物。

    Compositions and methods for inhibiting TGF-β
    7.
    发明授权
    Compositions and methods for inhibiting TGF-β 失效
    用于抑制TGF-β的组合物和方法

    公开(公告)号：US07943640B2

    公开(公告)日：2011-05-17

    申请号：US11941284

    申请日：2007-11-16

    申请人： Anjali Pandey ,  Robert M. Scarborough ,  Meenakshi S. Venkatraman

    发明人： Anjali Pandey ,  Robert M. Scarborough ,  Meenakshi S. Venkatraman

    IPC分类号： A61K31/04

    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R1，R6，R7，R8，Pg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- 活动。

    Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof
    9.
    发明授权
    Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof 失效
    含氮杂环化合物及其制备含氮杂环化合物的方法及其中间体

    公开(公告)号：US07709640B2

    公开(公告)日：2010-05-04

    申请号：US11313289

    申请日：2005-12-19

    申请人： James Kanter ,  Anjali Pandey ,  James Robinson ,  Robert M. Scarborough

    发明人： James Kanter ,  Anjali Pandey ,  James Robinson ,  Robert M. Scarborough

    IPC分类号： C07D295/182

    CPC分类号： C07D239/94

    摘要： The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. 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 further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.

    摘要翻译： 本发明提供含氮杂环化合物及其药学上可接受的盐及其制备方法。 这些化合物对抑制这种激酶活性的激酶的磷酸化具有抑制活性。 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。 本发明进一步提供了通过抑制激酶的磷酸化来抑制哺乳动物激酶和治疗疾病状态的方法，包括向有需要的患者施用有效量的本发明化合物。