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    Crystalline forms and processes for the preparation of cannabinoid receptor modulators
    1.
    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。

    MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO
    2.
    发明申请
    MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
    GPR119受体的调节剂和与之相关的疾病的治疗

    公开(公告)号：US20140051629A1

    公开(公告)日：2014-02-20

    申请号：US13825601

    申请日：2011-09-21

    申请人： Robert M. Jones ,  Juerg Lehmann ,  Weichao Chen ,  Jeffrey Edwards ,  Glen Marquez ,  Michael E. Morgan ,  Abu J.M. Sadeque ,  Sun Hee Kim

    发明人： Robert M. Jones ,  Juerg Lehmann ,  Weichao Chen ,  Jeffrey Edwards ,  Glen Marquez ,  Michael E. Morgan ,  Abu J.M. Sadeque ,  Sun Hee Kim

    IPC分类号： C07D413/14 ,  A61K45/06 ,  A61K31/506

    CPC分类号： C07D413/14 ,  A61K31/506 ,  A61K45/06

    摘要： The present invention relates to the GPR119 receptor agonists: 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N,N-dimethylbenzamide; -fluoro-4-(5-fluoro-6-(4-(3-(2-fluoro-propan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N-methylbenzamide; and 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)benzamide, and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single pharmaceutical agent or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

    摘要翻译： 本发明涉及GPR119受体激动剂：3-氟-4-（5-氟-6-（4-（3-（2-氟丙-2-基）-1,2,4-恶二唑-5-基 ）哌啶-1-基）嘧啶-4-基氨基）-N，N-二甲基苯甲酰胺; - 氟-4-（5-氟-6-（4-（3-（2-氟 - 丙-2-基）-1,2,4-恶二唑-5-基）哌啶-1-基） 吡啶-4-基氨基）-N-甲基苯甲酰胺; 和3-氟-4-（5-氟-6-（4-（3-（2-氟丙-2-基）-1,2,4-恶二唑-5-基）哌啶-1-基） 4-氨基）苯甲酰胺及其药学上可接受的盐，溶剂合物和水合物，其可用作单一药剂或与一种或多种另外的药剂如DPP-IV抑制剂，双胍类，α 葡萄糖苷酶抑制剂，胰岛素类似物，磺酰脲类，SGLT2抑制剂，氯噻嗪，噻唑烷二酮或抗糖尿病肽类似物，用于治疗例如选自以下的病症：GPR119-受体相关病症; 通过增加肠降血糖素的分泌而改善的状况; 通过增加血液肠降血糖水平来改善病情; 以低骨量为特征的病症; 神经障碍 代谢相关疾病; 2型糖尿病; 肥胖; 和相关的并发症。

    Generic crimped rotor for an electric brushless direct current motor
    7.
    发明授权
    Generic crimped rotor for an electric brushless direct current motor 有权
    用于电动无刷直流电动机的通用卷曲转子

    公开(公告)号：US07994675B2

    公开(公告)日：2011-08-09

    申请号：US12569890

    申请日：2009-09-29

    申请人： Robert M. Jones ,  Joseph M. Lisiecki

    发明人： Robert M. Jones ,  Joseph M. Lisiecki

    IPC分类号： H02K1/30

    CPC分类号： H02K1/278 ,  H02K3/38 ,  H02K5/04 ,  H02K5/18 ,  H02K5/225 ,  H02K11/33 ,  H02K16/00 ,  H02K21/16 ,  H02K29/08 ,  H02K2213/12

    摘要： A rotor having a substantially cylindrical configuration for use in a brushless direct current electric motor having a high torque to size ratio. The rotor has an outer peripheral surface. The rotor also has a central rotor shaft and a first and second retaining ends mounted on the central rotor shaft and spaced from one another. The rotor also has a plurality of magnets configured to provide a magnetic flux with a stator disposed around the central rotor shaft. The magnets are radially disposed on the shaft and the rotor also has a sheath. The sheath is crimped around the radially disposed permanent magnets, and holds the magnets around the shaft. The sheath is lightweight and minimizes a gap between the permanent magnets and the stator to provide for an electromagnetic flux between the magnets and the stator windings, and for rotation of the central rotor shaft.

    摘要翻译： 具有大体圆柱形构造的转子，用于具有高扭矩与大尺寸比的无刷直流电动机。 转子具有外周面。 转子还具有中心转子轴和安装在中心转子轴上并彼此间隔开的第一和第二保持端。 转子还具有多个磁体，其被配置为提供磁通量，该定子设置在中心转子轴周围。 磁体径向设置在轴上，转子也具有护套。 鞘被卷绕在径向设置的永磁体周围，并将磁体保持在轴周围。 护套是轻质的，并且使永磁体和定子之间的间隙最小化，以提供磁体和定子绕组之间的电磁通量，并且用于中心转子轴的旋转。