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    Pyrrolidine sulfonamides
    1.
    发明授权
    Pyrrolidine sulfonamides 失效
    吡咯烷磺酰胺

    公开(公告)号：US07019008B2

    公开(公告)日：2006-03-28

    申请号：US11119026

    申请日：2005-04-29

    Applicant: Dashyant Dhanak ,  Steven D. Knight ,  Jian Jin ,  Ralph A. Rivero ,  Anthony Sapienza

    Inventor： Dashyant Dhanak ,  Steven D. Knight ,  Jian Jin ,  Ralph A. Rivero ,  Anthony Sapienza

    IPC: A61K31/496 ,  C07D409/14

    CPC classification number: C07D409/12

    Abstract: A compound of Formula (I): wherein: R1 is C1-6 alkyl, benzyl, or (CH2)n—C(O)NH2; wherein the benzyl may be unsubstituted or substituted by one or two C1-6 alkyl, halogen, C1-6 alkoxy, or methylenedioxy groups; R2 is benzimidazolyl, quinolinyl, benzofuranyl, napthyl, indolyl, benzothiophenyl, phenyl, furanyl, thienyl, or pyridyl substituted or unsubstituted by one, two or three halogen, C1-3 alkyl, C1-3 alkoxy, or methylenedioxy groups; X1 and X2 are independently hydrogen, halogen, C1-3 alkyl, C1-3 alkoxy, nitro, CF3, or CN; n is 1, 2, or 3; m is 1, 2 or 3; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 式（I）的化合物：其中：R 1是C 1-6烷基，苄基或（CH 2 CH 2） -C（O）NH 2; 其中苄基可以是未取代的或被一个或两个C 1-6烷基，卤素，C 1-6烷氧基或亚甲二氧基取代; R 2是苯并咪唑基，喹啉基，苯并呋喃基，萘基，吲哚基，苯并噻吩基，苯基，呋喃基，噻吩基或被1,2或3个卤素取代或未取代的吡啶基， 亚烷基，C 1-3烷氧基或亚甲二氧基; X 1和X 2独立地是氢，卤素，C 1-3烷基，C 1-3烷氧基 ，硝基，CF 3或CN; n为1,2或3; m为1,2或3; 或其药学上可接受的盐。

    Substituted thiazoles and the use thereof as inhibitors of plasminogen activator inhibitor-1
    2.
    发明授权
    Substituted thiazoles and the use thereof as inhibitors of plasminogen activator inhibitor-1 有权
    取代的噻唑及其作为纤溶酶原激活物抑制剂-1的抑制剂的用途

    公开(公告)号：US06586453B2

    公开(公告)日：2003-07-01

    申请号：US09822351

    申请日：2001-04-02

    Applicant: Dale S. Dhanoa ,  Declan E. Ryan ,  Ingrid Deckman ,  Anthony Sapienza

    Inventor： Dale S. Dhanoa ,  Declan E. Ryan ,  Ingrid Deckman ,  Anthony Sapienza

    IPC: A61K31425

    CPC classification number: C07D417/04 ,  C07D277/38 ,  C07D277/42

    Abstract: The present invention relates to the use of aminothiazole derivatives of Formula I of as inhibitors of PAI-1, and to novel classes of aminothiazole derivatives, their synthesis and their use as inhibitors of PAI-1. It has been discovered that compounds of Formula I: or a solvate, hydrate or a pharmaceutically acceptable salt thereof, wherein Y, Ar1, Ar2, R1, R2, Z, m and n are described in the specification, inhibit plasminogen activator inhibitor-1 (PAI-1). These compounds can be used in the prophylaxis or for the treatment of thrombosis, angina pectoris, cerebral infarction, myocardial infarction, pulmonary infarction, intra-atrial thrombus in atrial fibrillation, deep venous thrombus, disseminated intravascular coagulation syndrome, diabetic complications, restenosis and stroke.

    Abstract translation: 本发明涉及式I的氨基噻唑衍生物作为PAI-1的抑制剂的用途，以及新类型的氨基噻唑衍生物，其合成及其作为PAI-1抑制剂的用途。 已经发现，说明书中描述了式I的化合物或其溶剂化物，水合物或其药学上可接受的盐，其中Y，Ar1，Ar2，R1，R2，Z，m和n在本说明书中描述了抑制纤溶酶原激活物抑制剂-1 PAI-1）。 这些化合物可用于预防或治疗血栓形成，心绞痛，脑梗塞，心肌梗死，肺梗死，心房颤动中的心房内血栓，深静脉血栓，弥散性血管内凝血综合征，糖尿病并发症，再狭窄和中风 。

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