Novel 1,3-dihydro-2H-indol-2one derivatives, process for preparing them and pharmaceutical compositions containing them
    3.
    发明申请
    Novel 1,3-dihydro-2H-indol-2one derivatives, process for preparing them and pharmaceutical compositions containing them 有权
    新的1,3-二氢-2H-吲哚-2-酮衍生物,其制备方法和含有它们的药物组合物

    公开(公告)号:US20040209938A1

    公开(公告)日:2004-10-21

    申请号:US10835209

    申请日:2004-04-29

    IPC分类号: A61K031/404 C07D43/04

    摘要: The invention relates to compounds of formula: 1 as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.

    摘要翻译: 本发明涉及下式的化合物及其与矿物或有机酸及其溶剂合物和/或水合物的可能盐,其对V1b受体或对于精氨酸的V1b和V1a受体具有亲和性和选择性 - 加压素 本发明还涉及制备它们的方法,可用于制备它们的中间式式(II)化合物,含有它们的药物组合物及其用于制备药用产品的用途。

    Methods of use of thrombin receptor antagonists
    5.
    发明申请
    Methods of use of thrombin receptor antagonists 审中-公开
    凝血酶受体拮抗剂的使用方法

    公开(公告)号:US20040192753A1

    公开(公告)日:2004-09-30

    申请号:US10705282

    申请日:2003-11-10

    IPC分类号: A61K031/404 A61K031/365

    摘要: A method of treating a therapeutic condition comprising administering to a mammal in need of such treatment an effective amount of at least one compound of the formulas: 1 or a pharmaceutically acceptable isomer, salt, solvate or co-crystal form thereof, wherein the substituents are as defined in the specification, wherein said therapeutic condition is a cardiovascular or circulatory disease or condition, an inflammatory disease or condition, a respiratory tract or disease or condition, cancer, acute renal failure, astrogliosis, a fibrotic disorder of the liver, kidney, lung or intestinal tract, Alzheimer's disease, diabetes, diabetic neuropathy, rheumatoid arthritis, neurodegenerative disease, neurotoxic disease, systemic lupus erythematosus, multiple sclerosis, osteoporosis, glaucoma, macular degeneration, psoriasis, radiation fibrosis, endothelial dysfunction, a wound or a spinal cord injury, or a symptom or result thereof. Combination therapy with other therapeutically effective agents is also disclosed.

    摘要翻译: 治疗治疗条件的方法包括向需要这种治疗的哺乳动物施用有效量的至少一种下式的化合物或其药学上可接受的异构体,盐,溶剂合物或共晶体形式,其中取代基为 在该说明书中定义,其中所述治疗条件是心血管或循环系统疾病或病症,炎性疾病或病症,呼吸道或疾病或病症,癌症,急性肾衰竭,星形胶质细胞增生,肝,肾,肺的纤维化病症 或肠道,阿尔茨海默病,糖尿病,糖尿病性神经病,类风湿性关节炎,神经变性疾病,神经毒性疾病,系统性红斑狼疮,多发性硬化,骨质疏松症,青光眼,黄斑变性,银屑病,放射纤维化,内皮功能障碍,伤口或脊髓损伤 ,或其症状或结果。 还公开了与其它治疗有效药物的联合治疗。

    Mannich base prodrugs of 3-(Pyrrol-2-yl-methylidene)-2-indolinone derivatives
    9.
    发明申请
    Mannich base prodrugs of 3-(Pyrrol-2-yl-methylidene)-2-indolinone derivatives 失效
    曼尼希碱3-(吡咯-2-基 - 亚甲基)-2-二氢吲哚酮衍生物的前药

    公开(公告)号:US20040127544A1

    公开(公告)日:2004-07-01

    申请号:US10743909

    申请日:2003-12-24

    IPC分类号: A61K031/404 C07D43/14

    摘要: The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (nullPKsnull). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

    摘要翻译: 本发明涉及调节蛋白激酶(“PK”)活性的某些3-(吡咯-2-基亚甲基)-2-二氢吲哚酮衍生物的曼尼希碱前体药物。 还公开了包含这些化合物的药物组合物,使用包含这些化合物的药物组合物治疗与异常PK活性有关的疾病的方法及其制备方法。