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    • 1. 发明申请
    • Thiophene amino acid derivatives, process for preparing them and pharmaceutical compositions containing them
    • 噻吩氨基酸衍生物,其制备方法和含有它们的药物组合物
    • US20050014816A1
    • 2005-01-20
    • US10884059
    • 2004-07-02
    • Delphine CompereAnne-Claude DublanchetKarine CourteStephane BlaisPierre DucrotPhilippe CluzeauAlexis Denis
    • Delphine CompereAnne-Claude DublanchetKarine CourteStephane BlaisPierre DucrotPhilippe CluzeauAlexis Denis
    • A61K31/381A61K31/4436A61P11/00C07D333/34C07D333/38C07D409/10C07
    • C07D333/38C07D409/10
    • The invention provides compounds of Formula (I), stereoisomers thereof, or pharmaceutically acceptable salts of said compounds or stereoisomers, wherein R1, R2, m, p, q, R7 and R8 are as defined below, as well as compositions comprising the same, processes for making the same, and methods of using the same to treat a variety of diseases, including, those requiring interaction with metalloproteases, and more specifically with macrophage metalloelastase (MMP-12), and for the prevention and treatment of respiratory pathologies such as chronic obstructive bronchopneumopathy (COPD), emphysema, chronic bronchitis, chronic pulmonary inflammation, asthma, cystic fibrosis, acute respiratory distress syndrome (ARDS), respiratory allergies including allergic rhinitis, and also diseases associated with the production of TNFα including severe fibrotic pulmonary disease, pulmonary sarcoidosis and silicosis. The compounds of the present invention also show inhibitory activity on metalloprotease-13 (MMP-13), making them useful for the treatment of pathologies involving this enzyme, such as cancer, osteoporosis, osteoarthritis, arthritis, rheumatoid arthritis, atherosclerosis, multiple sclerosis and cardiac insufficiency.
    • 本发明提供式(I)化合物,其立体异构体或所述化合物或立体异构体的药学上可接受的盐,其中R 1,R 2,m,p,q,R 7和R 8如下所定义,以及包含其的组合物, 制备相同的方法,以及使用它们治疗各种疾病的方法,包括需要与金属蛋白酶相互作用的那些疾病,更具体地涉及巨噬细胞金属弹性蛋白酶(MMP-12),以及用于预防和治疗呼吸道病症如 慢性阻塞性支气管肺病(COPD),肺气肿,慢性支气管炎,慢性肺部炎症,哮喘,囊性纤维化,急性呼吸窘迫综合征(ARDS),包括过敏性鼻炎在内的呼吸系统过敏,以及包括严重纤维性肺病在内的TNFα产生相关疾病, 肺结节病和矽肺。 本发明的化合物还显示对金属蛋白酶-13(MMP-13)的抑制活性,使其可用于治疗涉及该酶的病理学,例如癌症,骨质疏松症,骨关节炎,关节炎,类风湿性关节炎,动脉粥样硬化,多发性硬化和 心功能不全