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1. 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。

2. 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.

3. 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;

4. 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;

5. 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;

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

US08637555B2 Tetrazole derivatives and methods of treatment of metabolic-related disorders thereof 失效
标题翻译：四唑衍生物及其代谢相关病症的治疗方法
公开(公告)号：US08637555B2
公开(公告)日：2014-01-28
申请号：US10535345
申请日：2004-10-29
申请人： Graeme Semple , Thomas Schrader , Philip J. Skinner , Steven L. Colletti , Tawfik Gharbaoui , Jason E. Imbriglio , Jae-Kyu Jung , Rui Liang , Subharekha Raghavan , Darby Schmidt , James R. Tata
发明人： Graeme Semple , Thomas Schrader , Philip J. Skinner , Steven L. Colletti , Tawfik Gharbaoui , Jason E. Imbriglio , Jae-Kyu Jung , Rui Liang , Subharekha Raghavan , Darby Schmidt , James R. Tata
IPC分类号： A61K31/407 , C07D231/54
CPC分类号： C07D491/04 , C07D403/04 , C07D495/04
摘要： The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 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 metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
摘要翻译：本发明涉及式（I）的某些四唑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RUP25受体的激动剂。本发明还提供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代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病，综合征-X等。此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等。

9. 发明授权

US07241792B2 Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof 有权
标题翻译：融合的吡唑衍生物及其代谢相关病症的治疗方法
公开(公告)号：US07241792B2
公开(公告)日：2007-07-10
申请号：US11315753
申请日：2005-12-22
申请人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
发明人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
IPC分类号： A61K31/407 , C07D231/54
CPC分类号： C07D403/04 , C07D209/80 , C07D209/88 , C07D231/54 , C07D265/36 , C07D471/04 , C07D471/14
摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 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 metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
摘要翻译：本发明涉及式（Ia）的某些稠合吡唑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RUP25受体的激动剂。本发明还提供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代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病的方法，综合征-X等。此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂，DP受体拮抗剂等。

10. 发明申请

US20090258892A1 FUSED PYRAZOLE DERIVATIVES AND METHODS OF TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF 审中-公开
标题翻译：熔化的吡唑衍生物及其代谢相关疾病的治疗方法
公开(公告)号：US20090258892A1
公开(公告)日：2009-10-15
申请号：US12433704
申请日：2009-04-30
申请人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
发明人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
IPC分类号： A61K31/437 , C07D231/54 , C07D403/04 , A61K31/416 , A61K31/41 , A61K31/40
CPC分类号： C07D403/04 , C07D209/80 , C07D209/88 , C07D231/54 , C07D265/36 , C07D471/04 , C07D471/14
摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 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 metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
摘要翻译：本发明涉及式（Ia）的某些稠合吡唑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RUP25受体的激动剂。本发明还提供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代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病的方法，综合征-X等。此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂，DP受体拮抗剂等。

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