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    CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF PG12 RECEPTOR AGONISTS
    6.
    发明申请
    CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF PG12 RECEPTOR AGONISTS 审中-公开
    用于制备PG12受体激动剂的晶体形式和方法

    公开(公告)号：US20120225937A1

    公开(公告)日：2012-09-06

    申请号：US13497616

    申请日：2010-09-21

    申请人： Anthony C. Blackburn ,  Sagar Raj Shakya ,  John A. DeMattei ,  Tsung-Hsun Chuang

    发明人： Anthony C. Blackburn ,  Sagar Raj Shakya ,  John A. DeMattei ,  Tsung-Hsun Chuang

    IPC分类号： A61K31/27 ,  A61P9/12 ,  A61P7/02 ,  A61P9/10 ,  A61P9/00 ,  A61P27/06 ,  A61P25/02 ,  A61P13/12 ,  A61P27/02 ,  A61P29/00 ,  A61P17/06 ,  A61P19/02 ,  A61P37/06 ,  A61P25/00 ,  A61P37/00 ,  A61P1/04 ,  A61P17/10 ,  A61P3/10 ,  A61P11/00 ,  A61P11/06 ,  A61P1/00 ,  C07C309/15

    CPC分类号： C07C303/22 ,  A61K31/325 ,  C07C269/06 ,  C07C309/15 ,  C07C2601/14 ,  C07C271/28

    摘要： 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).

    摘要翻译： 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 其中。 本发明还涉及可用于制备化合物I及其盐，溶剂化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; 动脉粥样硬化血栓形成 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）。

    CRYSTALLINE FORMS OF (R)-1-{2-[4`- (3-METHOXY-PROPANE-1- SULFONYL)-BIPHENYL-4-YL]-ETHYL}-2-METHYL-PYRROLIDINE, AND COMPOSITIONS, AND METHODS RELATED THERETO
    7.
    发明申请
    CRYSTALLINE FORMS OF (R)-1-{2-[4`- (3-METHOXY-PROPANE-1- SULFONYL)-BIPHENYL-4-YL]-ETHYL}-2-METHYL-PYRROLIDINE, AND COMPOSITIONS, AND METHODS RELATED THERETO 审中-公开
    （R）-1- {2- [4'-（3-甲氧基 - 丙烷-1-磺酰基） - 联苯-4-基] - 乙基} -2-甲基 - 吡咯烷的晶体形式及其组合物及方法 THERETO

    公开(公告)号：US20100292288A1

    公开(公告)日：2010-11-18

    申请号：US12663415

    申请日：2008-06-06

    申请人： Anthony C. Blackburn ,  John A. DeMattei ,  Ryan M. Hart ,  Young Mi Khulman ,  Michael Mesleh ,  Jeffrey Smith

    发明人： Anthony C. Blackburn ,  John A. DeMattei ,  Ryan M. Hart ,  Young Mi Khulman ,  Michael Mesleh ,  Jeffrey Smith

    IPC分类号： A61K31/40 ,  C07D207/04 ,  A61P25/28 ,  A61P25/08 ,  A61P25/00 ,  A61P25/24 ,  A61P3/04 ,  A61P25/20 ,  A61P25/18 ,  A61P11/00 ,  A61P29/00

    CPC分类号： C07D207/06

    摘要： The present invention is directed to novel salts of (R)-1-{2-[4′-(3-methoxy-propane-1-sulfonyl)-biphenyl-4-yl]-ethyl}-2-methyl-pyrrolidine, and crystalline forms, and compositions thereof that modulate the activity of the histamine H3-receptor and are useful in the treatment of histamine H3-receptor associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, pain, dementia, Alzheimer's disease and the like.

    摘要翻译： 本发明涉及（R）-1- {2- [4' - （3-甲氧基 - 丙磺酰基） - 联苯-4-基] - 乙基} -2-甲基 - 吡咯烷的新型盐， 调节组胺H3受体活性的结晶形式及其组合物，可用于治疗组胺H3受体相关疾病，例如认知障碍，癫痫，脑创伤，抑郁症，肥胖症，睡眠障碍和 觉醒，如发作性睡病，转移综合征，嗜睡作为药物的副作用，维持警惕以帮助完成任务等，猝死，睡眠过多，嗜睡综合征，时差，睡眠呼吸暂停等，注意力缺陷 过敏性疾病（ADHD），精神分裂症，过敏反应，上呼吸道过敏反应，过敏性鼻炎，鼻充血，疼痛，痴呆，阿尔茨海默氏病等。