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    CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF PG12 RECEPTOR AGONISTS
    4.
    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
    5.
    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。

    Crystalline forms and processes for the preparation of cannabinoid receptor modulators
    8.
    发明授权
    Crystalline forms and processes for the preparation of cannabinoid receptor modulators 有权
    用于制备大麻素受体调节剂的结晶形式和方法

    公开(公告)号：US09458136B2

    公开(公告)日：2016-10-04

    申请号：US14001133

    申请日：2012-02-24

    申请人： Anthony C. Blackburn ,  Sangdon Han ,  Robert M. Jones ,  Antonio Garrido Montalban ,  Biman B. Pal ,  Jaimie Karyn Rueter

    发明人： Anthony C. Blackburn ,  Sangdon Han ,  Robert M. Jones ,  Antonio Garrido Montalban ,  Biman B. Pal ,  Jaimie Karyn Rueter

    IPC分类号： A61K31/4965 ,  C07D403/04 ,  A61K31/497

    CPC分类号： C07D403/04 ,  A61K31/497 ,  A61P29/00 ,  C07B2200/13

    摘要： The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor and are therefore useful in the treatment of CB2 receptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease.

    摘要翻译： 本发明涉及（1aS，5aS）-2-（4-氧 - 吡嗪-2-基）-1a，2,5,5a-四氢-1H-2,3-二氮杂 - 环丙烷[a] 顺式-4-羧酸（（S）-1-羟甲基-2,2-二甲基 - 丙基） - 酰胺（化合物1）及其药物组合物，其调节大麻素CB2受体的活性，因此可用于治疗 CB2受体介导的疾病，例如骨关节炎; 疼痛; 痛觉过敏 异常性疼痛 炎性痛觉过敏; 神经性痛觉过敏; 急性伤害感受 骨质疏松症 多发性硬化相关性痉挛状态; 自身免疫性疾病 过敏反应; CNS炎症例如; 动脉粥样硬化 不良免疫细胞活性和与选自以下的疾病相关的炎症：骨关节炎，过敏反应，贝切特氏病，移植排斥反应，血管炎，痛风，脊椎炎，病毒性疾病，细菌性疾病，狼疮，炎性肠病，自身免疫性肝炎和1型糖尿病 ; 年龄相关性黄斑变性; 咳嗽; 白血病; 淋巴瘤 CNS肿瘤; 前列腺癌; 阿尔茨海默氏病; 中风引起的损伤; 痴呆; 肌萎缩性侧索硬化; 和帕金森病。