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159 条记录 (耗时 0.033 秒)

    Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
    54.
    发明申请
    Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) 失效
    取代的3-羰基-1H-吲哚-1-基乙酸衍生物作为纤溶酶原激活物抑制剂-1（PAI-1）的抑制剂

    公开(公告)号：US20040122070A1

    公开(公告)日：2004-06-24

    申请号：US10731723

    申请日：2003-12-09

    申请人： Wyeth

    发明人： Lee D. Jennings

    IPC分类号： A61K031/422 ,  A61K031/405 ,  C07D413/02 ,  C07D45/02 ,  C07D49/02

    CPC分类号： C07D409/06 ,  C07D209/10 ,  C07D209/12

    摘要： Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives of formula I are provided: 1 wherein: R1, R2, R3, R4 and R5 are as defined herein which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.

    摘要翻译： 提供式I的取代的3-羰基-1H-吲哚-1-基乙酸衍生物：其中：R1，R2，R3，R4和R5如本文所定义，其可用作纤溶酶原激活物抑制剂-1（PAI- 1）用于治疗由纤维蛋白溶解性疾病如深静脉血栓形成和冠心病引起的病症以及肺纤维化。

    Novel imidazolidinedione derivatives and use thereof as drugs
    55.
    发明申请
    Novel imidazolidinedione derivatives and use thereof as drugs 失效
    新型咪唑烷二酮衍生物及其作为药物的用途

    公开(公告)号：US20040110811A1

    公开(公告)日：2004-06-10

    申请号：US10473889

    申请日：2003-10-02

    发明人： Yusuke Sakai ,  Jun Inoue

    IPC分类号： C07D263/46 ,  C07D233/72 ,  A61K031/422 ,  A61K031/421 ,  A61K031/4164

    CPC分类号： C07D235/02 ,  C07D233/80 ,  C07D263/44 ,  C07D413/06

    摘要： The present invention is to provide an imidazolidinedione derivative and oxazolidinedione derivative represented by the following general Formula (I) having the chymase and/or tryptase inhibition activity 1 nullwherein R1 and R2 are the same or different, and denote a lower alkyl group or a phenyl group, or R1 and R2 are taken together to form a ring, R3 denotes an optionally substituted naphthyl group or heterocyclic group, A denotes oxygen or NR4 (R4 is hydrogen or optionally substituted lower alkyl group), or NB2R5 (R5 is aryl group, and B2 is carbonyl group or sulfonyl group), and B1 denotes a carbonyl group or a sulfonyl groupnull, or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明提供由具有糜酶和/或类胰蛋白酶抑制活性的其他通式（I）表示的咪唑烷二酮衍生物和恶唑烷二酮衍生物[其中R 1和R 2相同或不同，表示 低级烷基或苯基，或R 1和R 2一起形成环，R 3表示任选取代的萘基或杂环基，A表示氧或NR 4（R 或者NB 2 R 5（R 5为芳基，B 2为羰基或磺酰基），B 1表示氢或任选取代的低级烷基 羰基或磺酰基]，或其药学上可接受的盐。

    Phenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
    57.
    发明申请
    Phenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia 失效
    苯氧基 - 乙酸可用于治疗胰岛素抵抗和高血糖症

    公开(公告)号：US20040102480A1

    公开(公告)日：2004-05-27

    申请号：US10300997

    申请日：2002-11-21

    申请人： Wyeth

    发明人： Michael S. Malamas ,  Jay E. Wrobel ,  Arlene J. Dietrich ,  Zenan Li ,  Iwan Gunawan

    IPC分类号： A61K031/4439 ,  A61K031/427 ,  A61K031/422 ,  A61K031/4178 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02

    CPC分类号： C07D333/60 ,  C07D307/80 ,  C07D333/56

    摘要： This invention provides compounds of Formula I having the structure 1 wherein: A is O, S, or N; B is null(CH2)mnull, nullCH(OH)null, or carbonyl; R1 is hydrogen, halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, or trifluoromethyl; R2 is alkyl of 1-18 carbon atoms, aryl of 6-10 carbon atoms, arylalkyl of 7-15 carbon atoms, Het-alkyl wherein the alkyl moiety is 1-6 carbon atoms; Het is 2 R2a is alkylene of 1-3 carbon atoms; G is oxygen, sulfur, or nitrogen; R3, R4 are each, independently, hydrogen, halogen, alkyl of 1-3 carbon atoms, aryl of 6-10 carbon atoms or a heterocyclic ring of 5 to 7 ring atom containing 1 to 3 heteroatoms selected from oxygen, nitrogen, sulfur; R5 is hydrogen, alkyl of 1-6 carbon atoms, nullCH(R7)R8, nullC(CH2)nCO2R9, nullC(CH3)2CO2R9, nullCH(R7)(CH2)nCO2R9, or CH(R7)C6H4CO2R9; R6 is hydrogen, halogen, alkyl of 1-6 carbon atoms, or nullOR5; mnull1-6; nnull1-6; R7 is hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms, or arylalkyl of 7-15 carbon atoms; R8 is nullCO2R10, nullCONHR10, tetrazole, or nullPO3; R9 and R10 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms, or arylalkyl of 7-15 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

    摘要翻译： 本发明提供具有以下结构的式I化合物：其中：A是O，S或N; B是 - （CH 2）m - ， - CH（OH） - 或羰基; R 1是氢，卤素，1-6个碳原子的烷基，1-6个碳原子的烷氧基或三氟甲基; R 2是1-18个碳原子的烷基，6-10个碳原子的芳基，7-15个碳原子的芳基烷基，其中烷基部分是1-6个碳原子的Het-烷基; Het是R 2a是1-3个碳原子的亚烷基; G是氧，硫或氮; R 3，R 4各自独立地为氢，卤素，1-3个碳原子的烷基，6-10个碳原子的芳基或含有1至3个选自以下的杂原子的5至7个环原子的杂环： 氧，氮，硫; R 5是氢，1-6个碳原子的烷基，-CH（R 7）R 8，-C（CH 2）n CO 2 R 9，-C（CH 3）2 CO 2 R 9，-CH （R 7）（CH 2）n CO 2 R 9或CH（R 7）C 6 H 4 CO 2 R 9; R 6是氢，卤素，1-6个碳原子的烷基或-OR 5; m = 1-6; n = 1-6; R 7是氢，1-6个碳原子的烷基，6-10个碳原子的芳基或7-15个碳原子的芳基烷基; R 8是-CO 2 R 10，-CONHR 10，四唑或-PO 3; R 9和R 10各自独立地为氢，1-6个碳原子的烷基，6-10个碳原子的芳基或7-15个碳原子的芳基烷基; 或其药学上可接受的盐，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。