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1. 发明申请

US20120295947A1 PROCESSES FOR THE PREPARATION OF (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMETHYL)BENZYLOXY)-1,2,3,4-TETRAHYDROCYCLOPENTA[B]INDOL-3-YL)ACETIC ACID AND SALTS THEREOF 有权
标题翻译：（R）-2-（7-（4-环丙基-3-（三氟甲基）苯甲酰基）-1,2,3,4-四氢环戊二烯并[B]吲哚-3-基）乙酸及其盐的制备方法
公开(公告)号：US20120295947A1
公开(公告)日：2012-11-22
申请号：US13575458
申请日：2011-01-27
申请人： Antonio Garrido Montalban , Daniel J. Buzard , John A. DeMattei , Tawfik Gharbaoui , Stephen R. Johannsen , Ashwin M. Krishnan , Young Mi Khulman , You-An Ma , Michael John Martinelli , Suzanne Michiko Sato , Dipanjan Sengupta
发明人： Antonio Garrido Montalban , Daniel J. Buzard , John A. DeMattei , Tawfik Gharbaoui , Stephen R. Johannsen , Ashwin M. Krishnan , Young Mi Khulman , You-An Ma , Michael John Martinelli , Suzanne Michiko Sato , Dipanjan Sengupta
IPC分类号： C12P17/10 , A61K31/403 , A61P25/00 , A61P37/06 , A61P9/12 , A61P17/10 , A61P29/00 , A61P17/06 , C07D209/70 , A61P3/10
CPC分类号： C12P17/10 , C07B2200/13 , C07C17/278 , C07D209/80 , C07D209/88 , C07D209/94 , C07D295/155
摘要： The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, 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-（7-（4-环戊基-3-（三氟甲基）苄氧基）-1,2,3,4-四氢环戊二烯并[b]吲哚-3 - 基）乙酸及其盐，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）。

2. 发明授权

US08853419B2 Processes for the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof 有权
标题翻译：（R）-2-（7-（4-环戊基-3-（三氟甲基）苄氧基）-1,2,3,4-四氢环戊二烯并[b]吲哚-3-基）乙酸及其盐的制备方法
公开(公告)号：US08853419B2
公开(公告)日：2014-10-07
申请号：US13575458
申请日：2011-01-27
申请人： Antonio Garrido Montalban , Daniel J. Buzard , John A. DeMattei , Tawfik Gharbaoui , Stephen R. Johannsen , Ashwin M. Krishnan , Young Mi Khulman , You-An Ma , Michael John Martinelli , Suzanne Michiko Sato , Dipanjan Sengupta
发明人： Antonio Garrido Montalban , Daniel J. Buzard , John A. DeMattei , Tawfik Gharbaoui , Stephen R. Johannsen , Ashwin M. Krishnan , Young Mi Khulman , You-An Ma , Michael John Martinelli , Suzanne Michiko Sato , Dipanjan Sengupta
IPC分类号： C07D209/80 , A61K31/403 , C07D209/94
CPC分类号： C12P17/10 , C07B2200/13 , C07C17/278 , C07D209/80 , C07D209/88 , C07D209/94 , C07D295/155
摘要： The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, 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-（7-（4-环戊基-3-（三氟甲基）苄氧基）-1,2,3,4-四氢环戊二烯并[b]吲哚-3 - 基）乙酸及其盐，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）。

3. 发明授权

US09458136B2 Crystalline forms and processes for the preparation of cannabinoid receptor modulators 有权
标题翻译：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。

4. 发明申请

US20100273797A1 ALPHA-KETOAMIDES AND DERIVATIVES THEREOF 审中-公开
标题翻译：阿尔法 - 卡特敏胺及其衍生物
公开(公告)号：US20100273797A1
公开(公告)日：2010-10-28
申请号：US12829701
申请日：2010-07-02
申请人： Erik Boman , Susana Conde Ceide , Russell Dahl , Nancy G. J. Delaet , Justin Ernst , Antonio Garrido Montalban , Jeffrey Kahl , Christopher Larson , Stephen Miller , Hiroshi Nakanishi , Edward Roberts , Eddine Saiah , Robert Sullivan , Zhijun Wang
发明人： Erik Boman , Susana Conde Ceide , Russell Dahl , Nancy G. J. Delaet , Justin Ernst , Antonio Garrido Montalban , Jeffrey Kahl , Christopher Larson , Stephen Miller , Hiroshi Nakanishi , Edward Roberts , Eddine Saiah , Robert Sullivan , Zhijun Wang
IPC分类号： A61K31/5377 , A61K31/5375 , A61K31/437 , A61P9/00 , A61P19/02 , A61P1/00 , A61P29/00 , A61P37/06 , A61P25/00 , A61P25/28 , A61P3/04 , A61P17/00
CPC分类号： A61K31/416 , C07D207/40 , C07D231/12 , C07D231/40 , C07D239/47 , C07D249/12 , C07D253/075 , C07D295/088 , C07D403/12 , C07D471/04 , C07D487/04 , Y02A50/401 , Y02A50/409 , Y02A50/411
摘要： The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions medicated by cytokines such as arthritis.
摘要翻译：本发明提供可用作细胞因子抑制剂的低分子量化合物及其组合物。特别地，本发明的化合物可用作抗炎剂。还提供了用于制备这些药剂的方法及其在预防或治疗由诸如关节炎的细胞因子药物治疗的病症中的用途。

5. 发明申请

US20140135345A1 CRYSTALLINE FORMS AND PROCESSES FOR THE PREPARATION OF CANNABINOID RECEPTOR MODULATORS 有权
标题翻译：用于制备CANNABINOID受体调节剂的晶体形式和方法
公开(公告)号：US20140135345A1
公开(公告)日：2014-05-15
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： C07D403/04
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受体介导的病症，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。

6. 发明申请

US20100093734A1 CYTOKINE INHIBITORS 有权
标题翻译：细胞因子抑制剂
公开(公告)号：US20100093734A1
公开(公告)日：2010-04-15
申请号：US12637712
申请日：2009-12-14
申请人： Erik Boman , Susana Conde Ceide , Russell Dahl , Nancy G.J. Delaet , Justin Ernst , Antonio Garrido Montalban , Jeffrey Kahl , Christopher Larson , Stephen Miller , Hiroshi Nakanishi , Edward Roberts , Eddine Saiah , Robert Sullivan , Zhijun Wang
发明人： Erik Boman , Susana Conde Ceide , Russell Dahl , Nancy G.J. Delaet , Justin Ernst , Antonio Garrido Montalban , Jeffrey Kahl , Christopher Larson , Stephen Miller , Hiroshi Nakanishi , Edward Roberts , Eddine Saiah , Robert Sullivan , Zhijun Wang
IPC分类号： A61K31/5375 , C07D295/14
CPC分类号： A61K31/416 , C07D207/40 , C07D231/12 , C07D231/40 , C07D239/47 , C07D249/12 , C07D253/075 , C07D295/088 , C07D403/12 , C07D471/04 , C07D487/04 , Y02A50/401 , Y02A50/409 , Y02A50/411
摘要： The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions mediated by cytokines such as arthritis.
摘要翻译：本发明提供可用作细胞因子抑制剂的低分子量化合物及其组合物。特别地，本发明的化合物可用作抗炎剂。还提供了制备这些试剂的方法及其在预防或治疗由细胞因子如关节炎介导的病症中的用途。

7. 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;

8. 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;

9. 发明授权

US07919617B2 Cytokine inhibitors 有权
标题翻译：细胞因子抑制剂
公开(公告)号：US07919617B2
公开(公告)日：2011-04-05
申请号：US12637712
申请日：2009-12-14
申请人： Erik Boman , Susana Conde Ceide , Russell Dahl , Nancy G. J. Delaet , Justin Ernst , Antonio Garrido Montalban , Jeffrey Kahl , Christopher Larson , Stephen Miller , Hiroshi Nakanishi , Edward Roberts , Eddine Saiah , Robert Sullivan , Zhinjun Wang
发明人： Erik Boman , Susana Conde Ceide , Russell Dahl , Nancy G. J. Delaet , Justin Ernst , Antonio Garrido Montalban , Jeffrey Kahl , Christopher Larson , Stephen Miller , Hiroshi Nakanishi , Edward Roberts , Eddine Saiah , Robert Sullivan , Zhinjun Wang
IPC分类号： C07D265/30 , A61K31/5377
CPC分类号： A61K31/416 , C07D207/40 , C07D231/12 , C07D231/40 , C07D239/47 , C07D249/12 , C07D253/075 , C07D295/088 , C07D403/12 , C07D471/04 , C07D487/04 , Y02A50/401 , Y02A50/409 , Y02A50/411
摘要： The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions mediated by cytokines such as arthritis.
摘要翻译：本发明提供可用作细胞因子抑制剂的低分子量化合物及其组合物。特别地，本发明的化合物可用作抗炎剂。还提供了制备这些试剂的方法及其在预防或治疗由细胞因子如关节炎介导的病症中的用途。

10. 发明授权

US07897599B2 Cytokine inhibitors 有权
公开(公告)号：US07897599B2
公开(公告)日：2011-03-01
申请号：US12637714
申请日：2009-12-14
申请人： Erik Boman , Susana Conde Ceide , Russell Dahl , Nancy G. J. Delaet , Justin Ernst , Antonio Garrido Montalban , Jeffrey Kahl , Christopher Larson , Stephen Miller , Hiroshi Nakanishi , Edward Roberts , Eddine Saiah , Robert Sullivan , Zhinjun Wang
发明人： Erik Boman , Susana Conde Ceide , Russell Dahl , Nancy G. J. Delaet , Justin Ernst , Antonio Garrido Montalban , Jeffrey Kahl , Christopher Larson , Stephen Miller , Hiroshi Nakanishi , Edward Roberts , Eddine Saiah , Robert Sullivan , Zhinjun Wang
IPC分类号： A61K31/535 , C07D265/30
CPC分类号： A61K31/416 , C07D207/40 , C07D231/12 , C07D231/40 , C07D239/47 , C07D249/12 , C07D253/075 , C07D295/088 , C07D403/12 , C07D471/04 , C07D487/04 , Y02A50/401 , Y02A50/409 , Y02A50/411
摘要： The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions mediated by cytokines such as arthritis.

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