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    Crystalline forms and processes for the preparation of cannabinoid receptor modulators
    3.
    发明授权
    Crystalline forms and processes for the preparation of cannabinoid receptor modulators 有权

    公开(公告)号：US10183930B2

    公开(公告)日：2019-01-22

    申请号：US15248300

    申请日：2016-08-26

    申请人： Arena Pharmaceuticals, Inc.

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

    IPC分类号： C07D403/04 ,  A61K31/497 ,  A61P29/00

    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.

    Pharmaceutical compositions comprising GPR119 agonists which act as peptide YY (PYY) secretagogues
    4.
    发明授权
    Pharmaceutical compositions comprising GPR119 agonists which act as peptide YY (PYY) secretagogues 有权
    包含作为肽YY（PYY）促分泌素的GPR119激动剂的药物组合物

    公开(公告)号：US08883714B2

    公开(公告)日：2014-11-11

    申请号：US13757171

    申请日：2013-02-01

    申请人： Arena Pharmaceuticals, Inc.

    发明人： Zhi-Liang Chu ,  James N. Leonard ,  Robert M. Jones

    IPC分类号： A01N61/00 ,  A61K31/00 ,  G01N33/50 ,  G01N33/68

    CPC分类号： G01N33/68 ,  G01N33/5044 ,  G01N2333/726 ,  G01N2800/042 ,  G01N2800/044 ,  G01N2800/065 ,  G01N2800/108 ,  G01N2800/323

    摘要： The present invention relates to methods of using GPR119 receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY, such as conditions modulated by stimulation of NPY Y2 receptor (Y2R). Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition modulated by PYY, such as a condition modulated by stimulation of Y2R. Conditions modulated by PYY such as may be a condition modulated by stimulation of Y2R include bone-related conditions, metabolic disorders, angiogenesis-related conditions, ischemia-related conditions, convulsive disorders, malabsorptive disorders, cancers, and inflammatory disorders.

    摘要翻译： 本发明涉及使用GPR119受体鉴定肽YY（PYY）促分泌素和可用于治疗由PYY调节的病症的化合物的方法，例如通过刺激NPY Y2受体（Y2R）调节的病症。 GPR119受体的激动剂可用作治疗或预防由PYY调节的病症的治疗剂，例如通过刺激Y2R调节的病症。 由PYY调节的病症例如可能是通过Y2R刺激调节的病症包括骨相关病症，代谢紊乱，血管生成相关病症，缺血相关病症，惊厥症，吸收不良障碍，癌症和炎症性疾病。

    CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF CANNABINOID RECEPTOR MODULATORS
    5.
    发明申请
    CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF CANNABINOID RECEPTOR MODULATORS 有权

    公开(公告)号：US20210380560A1

    公开(公告)日：2021-12-09

    申请号：US17202946

    申请日：2021-03-16

    申请人： Arena Pharmaceuticals, Inc.

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

    IPC分类号： C07D403/04 ,  A61K31/497 ,  A61P29/00

    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.

    SUBSTITUTED TRICYCLIC ACID DERIVATIVES AS S1P1 RECEPTOR AGONISTS USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
    9.
    发明申请
    SUBSTITUTED TRICYCLIC ACID DERIVATIVES AS S1P1 RECEPTOR AGONISTS USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS 审中-公开
    作为S1P1受体激动剂治疗自身免疫性疾病和炎症性疾病有用的替代三聚酸衍生物

    公开(公告)号：US20150336966A1

    公开(公告)日：2015-11-26

    申请号：US14817954

    申请日：2015-08-04

    申请人： Arena Pharmaceuticals, Inc.

    发明人： Robert M. Jones ,  Daniel J. Buzard ,  Andrew M. Kawasaki ,  Sun Hee Kim ,  Lars Thoresen ,  Juerg Lehmann ,  Xiuwen Zhu

    IPC分类号： C07D487/04 ,  C07D471/04

    CPC分类号： C07D487/04 ,  C07D471/04

    摘要： The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.

    摘要翻译： 本发明涉及某些取代的式（I）的三环酸衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为S1P1受体的激动剂。 本发明还提供了含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗S1P1相关病症的方法，例如牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应，多发性 硬化症，系统性红斑狼疮，溃疡性结肠炎，I型糖尿病，痤疮，心肌缺血再灌注损伤，高血压肾病，肾小球硬化，胃炎，多发性肌炎，甲状腺炎，白癜风，肝炎，胆汁性肝硬化，微生物感染和相关疾病，病毒感染和相关疾病 ，由淋巴细胞介导的疾病和病症，自身免疫疾病，炎性疾病和癌症。