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    Cannabinoid receptor modulators
    12.
    发明授权
    Cannabinoid receptor modulators 有权
    大麻素受体调节剂

    公开(公告)号：US08778950B2

    公开(公告)日：2014-07-15

    申请号：US13392074

    申请日：2010-08-27

    申请人： Robert M. Jones ,  Sangdon Han ,  Lars Thoresen ,  Jae-Kyu Jung ,  Sonja Strah-Pleynet ,  Xiuwen Zhu ,  Yifeng Xiong ,  Dawei Yue

    发明人： Robert M. Jones ,  Sangdon Han ,  Lars Thoresen ,  Jae-Kyu Jung ,  Sonja Strah-Pleynet ,  Xiuwen Zhu ,  Yifeng Xiong ,  Dawei Yue

    IPC分类号： A61K31/4965 ,  A01N43/56 ,  A61K31/415 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D231/54 ,  C07D487/00

    CPC分类号： C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07F9/65583

    摘要： The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; 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： 本发明涉及某些式Ia化合物及其药物组合物，其调节大麻素CB2受体的活性。 本发明还涉及某些式Ia化合物及其药物组合物，其调节CB1受体和CB2受体的活性。 本发明的化合物及其药物组合物涉及可用于治疗以下疼痛的方法：疼痛，例如骨和关节疼痛，肌肉疼痛，牙痛，偏头痛和其他头痛疼痛，炎性疼痛，神经性疼痛，疼痛发生于 与骨关节炎相关的治疗和疼痛的不利影响; 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; 动脉粥样硬化 不良免疫细胞活性和炎症; 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。

    Processes for the preparation of S1P1 receptor modulators and crystalline forms thereof
    14.
    发明授权
    Processes for the preparation of S1P1 receptor modulators and crystalline forms thereof 有权
    制备S1P1受体调节剂及其结晶形式的方法

    公开(公告)号：US09085581B2

    公开(公告)日：2015-07-21

    申请号：US13581846

    申请日：2011-03-02

    申请人： Robert M. Jones ,  Daniel J. Buzard ,  Tawfik Gharbaoui ,  Benjamin R. Johnson ,  Michelle Kasem ,  Thomas O. Schrader ,  Scott Stirn

    发明人： Robert M. Jones ,  Daniel J. Buzard ,  Tawfik Gharbaoui ,  Benjamin R. Johnson ,  Michelle Kasem ,  Thomas O. Schrader ,  Scott Stirn

    IPC分类号： C07D487/16 ,  A61K31/403 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro -7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

    摘要翻译： 本发明涉及可用于制备（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H- - 吡咯并[1,2-a]吲哚-1-基）乙酸，其盐和结晶形式。 化合物（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H-吡咯并[1,2-a]吲哚-1-基） 乙酸被鉴定为可用于治疗S1P1受体相关疾病的S1P1受体调节剂，例如由淋巴细胞介导的疾病和病症，移植排斥反应，自身免疫性疾病和病症，炎性疾病和病症（例如急性和 慢性炎性病症），癌症和特征在于血管完整性的潜在缺陷或与血管发生相关的病症，例如可能是病理性的（例如，可能发生在炎症，肿瘤发展和动脉粥样硬化中）。

    PROCESSES FOR THE PREPARATION OF S1P1 RECEPTOR MODULATORS AND CRYSTALLINE FORMS THEREOF
    15.
    发明申请
    PROCESSES FOR THE PREPARATION OF S1P1 RECEPTOR MODULATORS AND CRYSTALLINE FORMS THEREOF 有权
    制备S1P1受体调节剂的方法及其结晶形式

    公开(公告)号：US20120329848A1

    公开(公告)日：2012-12-27

    申请号：US13581846

    申请日：2011-03-02

    申请人： Robert M. Jones ,  Daniel J. Buzard ,  Tawfik Gharbaoui ,  Benjamin R. Johnson ,  Michelle Kasem ,  Thomas O. Schrader ,  Scott Stirn

    发明人： Robert M. Jones ,  Daniel J. Buzard ,  Tawfik Gharbaoui ,  Benjamin R. Johnson ,  Michelle Kasem ,  Thomas O. Schrader ,  Scott Stirn

    IPC分类号： C07D487/04 ,  C07C41/01 ,  A61P37/00 ,  A61P9/10 ,  A61P3/10 ,  A61P17/10 ,  A61P1/16 ,  A61P17/06 ,  A61K31/407 ,  A61P1/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions eases characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

    摘要翻译： 本发明涉及可用于制备（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H- - 吡咯并[1,2-a]吲哚-1-基）乙酸，其盐和结晶形式。 化合物（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H-吡咯并[1,2-a]吲哚-1-基） 乙酸被鉴定为可用于治疗S1P1受体相关疾病的S1P1受体调节剂，例如由淋巴细胞介导的疾病和病症，移植排斥反应，自身免疫性疾病和病症，炎性疾病和病症（例如急性和 慢性炎性病症），癌症和病症特征在于血管完整性的潜在缺陷或与血管发生相关的疾病，例如可能是病理性的（例如，可能发生在炎症，肿瘤发展和动脉粥样硬化中）。

    MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO
    17.
    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。

    Modulators of metabolism and the treatment of disorders related thereto
    19.
    发明申请
    Modulators of metabolism and the treatment of disorders related thereto 审中-公开
    代谢调节剂和与之有关的疾病的治疗

    公开(公告)号：US20100004272A1

    公开(公告)日：2010-01-07

    申请号：US12307545

    申请日：2007-07-05

    申请人： Robert M. Jones ,  Juerg Lehmann

    发明人： Robert M. Jones ,  Juerg Lehmann

    IPC分类号： A61K31/506 ,  C07D401/14 ,  A61P3/10 ,  A61P3/06 ,  A61P3/08 ,  A61P3/04

    CPC分类号： C07D401/14

    摘要： The present invention relates to 4-[6-(6-methanesulfonyl-2-methyl-pyridin-3-ylamino)-5-methyl-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, pharmaceutically acceptable salts, solvates and hydrates thereof that are modulators of glucose metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.

    摘要翻译： 本发明涉及4- [6-（6-甲磺酰基-2-甲基 - 吡啶-3-基氨基）-5-甲基 - 嘧啶-4-基氧基] - 哌啶-1-甲酸异丙酯，其药学上可接受的盐， 其是葡萄糖代谢调节剂的溶剂合物和水合物。 因此，本发明的化合物可用于治疗代谢相关疾病及其并发症，例如糖尿病和肥胖症。

    MODULATORS OF METABOLISM AND THE TREATMENT OF DISORDERS RELATED THERETO
    20.
    发明申请
    MODULATORS OF METABOLISM AND THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
    代谢调节剂和相关疾病的治疗

    公开(公告)号：US20090286816A1

    公开(公告)日：2009-11-19

    申请号：US12307549

    申请日：2007-07-05

    申请人： Robert M. Jones ,  Juerg Lehmann ,  Amy Siu-Ting Wong

    发明人： Robert M. Jones ,  Juerg Lehmann ,  Amy Siu-Ting Wong

    IPC分类号： A61K31/506 ,  C07D401/14 ,  A61P3/00

    CPC分类号： C07D401/14

    摘要： The present invention relates to 4-[5-Methoxy-6-(2-methyl-6-[1,2,4]triazol-1-yl-pyridin-3-ylamino)-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, pharmaceutically acceptable salts, solvates and hydrates thereof that are modulators of glucose metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity. (Formula I)

    摘要翻译： 本发明涉及4- [5-甲氧基-6-（2-甲基-6- [1,2,4]三唑-1-基 - 吡啶-3-基氨基） - 嘧啶-4-基氧基] 1-羧酸异丙酯，其药学上可接受的盐，溶剂化物和水合物，其是葡萄糖代谢的调节剂。 因此，本发明的化合物可用于治疗代谢相关疾病及其并发症，例如糖尿病和肥胖症。 （式I）