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12. 发明授权

US08461204B2 Cysteinyl compounds, compositions and methods of use 有权
标题翻译：半胱氨酰化合物，组合物和使用方法
公开(公告)号：US08461204B2
公开(公告)日：2013-06-11
申请号：US13566839
申请日：2012-08-03
申请人： Jeffry B. Stock , Maxwell Stock , Keshava Rapole , Seung-Yub Lee , Michael Voronkov , Eduardo Perez , Joel Gordon , Shuyi Chen
发明人： Jeffry B. Stock , Maxwell Stock , Keshava Rapole , Seung-Yub Lee , Michael Voronkov , Eduardo Perez , Joel Gordon , Shuyi Chen
IPC分类号： A61K31/198 , C07C323/24 , A61K31/197 , C07C323/59
CPC分类号： A61K31/197 , C07C323/59
摘要： Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, the compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g., Parkinson's disease).
摘要翻译：除此之外，本发明提供能够有效抑制嗜中性粒细胞，巨噬细胞和血小板中G蛋白或GPCR介导的炎症反应的新型化合物。特别地，本发明的化合物作为水肿抑制剂，红斑抑制剂和MPO抑制剂（髓过氧化物酶），含有相同化合物的药物组合物及其用于治疗可能受益于水肿，红斑和MPO的疾病的用途抑制，如炎症（急性或慢性），哮喘，自身免疫性疾病和慢性阻塞性肺疾病（COPD）（例如肺气肿，慢性支气管炎和小气道疾病等），免疫系统的炎症反应，皮肤疾病例如，对于患有酒渣鼻，特应性皮炎，脂溢性皮炎，牛皮癣的患者，肠易激综合征（例如，Chron氏病和溃疡性结肠炎等）以及中枢神经系统疾病（例如帕金森病）的患者减少急性皮肤刺激。

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