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1. 发明申请

US20140206649A1 CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译： CANNABINOID受体调节剂
公开(公告)号：US20140206649A1
公开(公告)日：2014-07-24
申请号：US14001131
申请日：2012-02-24
申请人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Anthony Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
发明人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Anthony Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
IPC分类号： A61K31/675 , A61K31/416 , A61K31/4439 , A61K45/06 , A61K31/497
CPC分类号： A61K31/497 , A61K31/13 , A61K31/416 , A61K31/4439 , A61K31/485 , A61K31/675 , A61K45/06 , C07D231/54 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07F9/65583
摘要： Provided are certain methods useful in the treatment of pain comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;
摘要翻译：提供有用于治疗疼痛的某些方法，包括施用式Ia化合物及其调节大麻素CB 2受体活性的药物组合物;

2. 发明授权

US09597340B2 Cannabinoid receptor modulators 有权
公开(公告)号：US09597340B2
公开(公告)日：2017-03-21
申请号：US14001132
申请日：2012-02-24
申请人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
发明人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
IPC分类号： A61K31/4439 , A61K31/675 , A61K31/416 , A61K45/06 , A61K31/497
CPC分类号： A61K31/675 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K45/06 , A61K2300/00
摘要： Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;

3. 发明申请

US20150126477A1 CANNABINOID RECEPTOR MODULATORS 有权
标题翻译： CANNABINOID受体调节剂
公开(公告)号：US20150126477A1
公开(公告)日：2015-05-07
申请号：US14001132
申请日：2012-02-24
申请人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
发明人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
IPC分类号： A61K31/675 , A61K31/4439 , A61K31/497 , A61K45/06 , A61K31/416
CPC分类号： A61K31/675 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K45/06 , A61K2300/00
摘要： Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;
摘要翻译：提供某些方法可用于治疗癌症，包括施用式Ia化合物及其药物组合物，其调节大麻素CB2受体的活性;

4. 发明授权

US08778950B2 Cannabinoid receptor modulators 有权
标题翻译：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。

5. 发明授权

US09944606B2 Cannabinoid receptor modulators 有权
公开(公告)号：US09944606B2
公开(公告)日：2018-04-17
申请号：US13616918
申请日：2012-09-14
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： C07F9/6558 , C07D401/12 , C07D403/12 , C07D413/14 , C07D231/54 , C07D403/04 , C07D413/12 , C07D401/04 , C07D401/14 , C07D405/14
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.

6. 发明申请

US20130165412A1 CANNABINOID RECEPTOR MODULATORS 有权
标题翻译： CANNABINOID受体调节剂
公开(公告)号：US20130165412A1
公开(公告)日：2013-06-27
申请号：US13616918
申请日：2012-09-14
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： C07F9/6558 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D231/54 , C07D403/04
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。

7. 发明申请

US20120214766A1 CANNABINOID RECEPTOR MODULATORS 有权
标题翻译： CANNABINOID受体调节剂
公开(公告)号：US20120214766A1
公开(公告)日：2012-08-23
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： A61K31/416 , A61P19/02 , C07D231/54 , C07D413/06 , A61K31/5377 , C07D401/12 , A61K31/4439 , C07D401/04 , C07D403/04 , A61K31/497 , C07D413/12 , C07D413/14 , A61K31/501 , C07D409/04 , C07D403/12 , C07D401/14 , C07D405/12 , C07D405/14 , A61K31/454 , C07F9/6558 , A61K31/675 , A61P29/00
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。

8. 发明授权

US08415484B2 Substituted tricyclic acid derivatives as S1P1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders 有权
标题翻译：取代的三环酸衍生物作为可用于治疗自身免疫性和炎症性疾病的S1P1受体激动剂
公开(公告)号：US08415484B2
公开(公告)日：2013-04-09
申请号：US13060477
申请日：2009-08-26
申请人： Robert M. Jones , Daniel J. Buzard , Andrew M. Kawasaki , Sun Hee Kim , Lars Thoresen , Juerg Lehmann , Xiuwen Zhu
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： C07D403/02 , C07D487/00 , C07D471/14 , C07D487/12 , C07D401/00 , C07D403/14 , A61K31/44 , A61K31/415 , A61K31/40
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。

9. 发明申请

US20110160243A1 SUBSTITUTED TRICYCLIC ACID DERIVATIVES AS S1P1 RECEPTOR AGONISTS USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS 有权
标题翻译：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：US20110160243A1
公开(公告)日：2011-06-30
申请号：US13060477
申请日：2009-08-26
申请人： Robert M. Jones , Daniel J. Buzard , Andrew M. Kawasaki , Sun Hee Kim , Lars Thoresen , Juerg Lehmann , Xiuwen Zhu
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： A61K31/437 , C07D487/04 , C07D471/04 , A61K31/407 , A61K31/4188 , A61K31/4439 , A61K31/4155 , A61P29/00 , A61P17/06 , A61P37/06 , A61P25/28 , A61P3/10 , A61P13/12 , A61P9/10 , A61P17/10 , A61P1/00 , A61P31/00 , A61P31/12
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。

10. 发明申请

US20140018371A1 Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto 审中-公开
标题翻译： GPR119受体的调节剂和与之相关的疾病的治疗
公开(公告)号：US20140018371A1
公开(公告)日：2014-01-16
申请号：US14007759
申请日：2012-03-30
申请人： Robert M. Jones , Sangdon Han , Juerg Lehmann , Lars Thoresen
发明人： Robert M. Jones , Sangdon Han , Juerg Lehmann , Lars Thoresen
IPC分类号： A61K31/506 , C07D413/04 , A61K31/454 , C07D401/12 , A61K45/06 , A61K31/497 , C07D401/14 , C07D211/24 , C07D401/06 , A61K31/445 , A61K31/4545
CPC分类号： A61K31/506 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K45/06 , C07D211/22 , C07D211/24 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/04 , C07D413/06
摘要： The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
摘要翻译：本发明涉及式（Ia）化合物及其药学上可接受的盐，溶剂合物和水合物，其可用作单一试剂或与一种或多种药剂组合使用，例如DPP-IV抑制剂，双胍或α-葡糖苷酶抑制剂，用于治疗例如选自以下的病症：GPR119-受体相关病症; 通过增加血液肠降血糖水平来改善病情; 代谢相关疾病; 2型糖尿病; 肥胖; 和相关的并发症。

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