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    • 6. 发明申请
    • CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF PGI2 RECEPTOR AGONISTS
    • 用于制备PGI2受体激动剂的晶体形式和方法
    • WO2011037613A1
    • 2011-03-31
    • PCT/US2010/002574
    • 2010-09-21
    • ARENA PHARMACEUTICALS, INC.BLACKBURN, Anthony C.SHAKYA, Sagar RajDEMATTEI, John A.CHUANG, Tsung-Hsun
    • BLACKBURN, Anthony C.SHAKYA, Sagar RajDEMATTEI, John A.CHUANG, Tsung-Hsun
    • C07C309/15C07C303/22A61K31/165A61P9/00C07C269/06C07C271/28
    • C07C303/22A61K31/325C07C269/06C07C309/15C07C2601/14C07C271/28
    • The present invention relates to salts of 2-(2-((4-(((4-chlorophenyl)(phenyl)-carbamoyloxy)methyl)cyclohexyl)methoxy)acetamido)ethanesulfonic acid (Compound 1) and crystalline forms, solvates and hydrates thereof. The present invention further relates to processes and intermediates useful in the preparation of Compound I and salts, solvates and hydrates thereof. Crystalline forms, salts, solvates and hydrates of the present invention and pharmaceutical compositions thereof are useful in the treatment of, for example, pulmonary arterial hypertension (PAH); platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; atherosclerosis; acne; type I diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).
    • 本发明涉及2-(2 - ((4 - ((((4-氯苯基)(苯基) - 氨基甲酰氧基)甲基)环己基)甲氧基)乙酰氨基)乙磺酸(化合物1)和结晶形式,溶剂合物和水合物 它们。 本发明还涉及可用于制备化合物I及其盐,溶剂合物和水合物的方法和中间体。 本发明的结晶形式,盐,溶剂合物和水合物及其药物组合物可用于治疗例如肺动脉高压(PAH); 血小板聚集; 冠状动脉疾病; 心肌梗死; 短暂性脑缺血发作; 心绞痛; 行程; 缺血再灌注损伤; 再狭窄; 房颤; 血块形成; 动脉粥样硬化; 哮喘或其症状; 糖尿病相关疾病; 青光眼或其他眼睛异常眼内疾病; 高血压; 炎; 银屑病; 牛皮癣关节炎 类风湿关节炎; 克罗恩病; 移植排斥反应 多发性硬化症 系统性红斑狼疮(SLE); 溃疡性结肠炎 动脉粥样硬化; 粉刺; I型糖尿病; 2型糖尿病; 败血症; 和慢性阻塞性肺疾病(COPD)。