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1. 发明公开

US20230257349A1 SUBSTITUTED (1,2,3,4-TETRAHYDROCYCLOPENTA[b]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS 审中-公开
公开(公告)号：US20230257349A1
公开(公告)日：2023-08-17
申请号：US17885683
申请日：2022-08-11
申请人： Arena Pharmaceuticals, Inc.
发明人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V. Moody , Xiuwen Zhu , Scott Stirn
IPC分类号： C07D209/94 , A61K31/404 , A61K31/497 , A61K31/4439 , A61K31/433 , A61K31/198 , A61K31/137 , C07D209/70 , C07D209/88 , C07D401/12 , C07D403/12 , C07D417/12 , C07C211/27 , C07C229/26 , C07C255/03 , C07C279/14 , C07D401/14
CPC分类号： C07D209/94 , A61K31/404 , A61K31/497 , A61K31/4439 , A61K31/433 , A61K31/198 , A61K31/137 , C07D209/70 , C07D209/88 , C07D401/12 , C07D403/12 , C07D417/12 , C07C211/27 , C07C229/26 , C07C255/03 , C07C279/14 , C07D401/14 , Y02A50/30
摘要： The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) 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 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.

2. 发明授权

US11555015B2 Compounds useful in the treatment of autoimmune and inflammatory disorders 有权
公开(公告)号：US11555015B2
公开(公告)日：2023-01-17
申请号：US17273681
申请日：2019-09-05
申请人： Arena Pharmaceuticals, Inc.
发明人： Abu J. M. Sadeque , Daniel J. Buzard
IPC分类号： C07D209/94 , C07H15/26
摘要： The present invention relates to certain compounds of Formula (Ia) 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 receptor-associated disorders, for example, a disease or disorder mediated by lymphocytes, an autoimmune disease or disorder, an inflammatory disease or disorder, an inflammatory skin disease or disorder, cancer, psoriasis, atopic dermatitis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, and acne, microbial infections or diseases and viral infections or diseases.

3. 发明申请

US20170217885A1 SUBSTITUTED 1,2,3,4-TETRAHYDROCYCLOPENTA[b]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS 审中-公开
公开(公告)号：US20170217885A1
公开(公告)日：2017-08-03
申请号：US15347130
申请日：2016-11-09
申请人： Arena Pharmaceuticals, Inc.
发明人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V. Moody , Xiuwen Zhu , Scott Stirn
IPC分类号： C07D209/94 , C07D417/12 , C07D403/12 , C07D401/12 , C07D401/14
CPC分类号： C07D209/94 , A61K31/137 , A61K31/198 , A61K31/404 , A61K31/433 , A61K31/4439 , A61K31/497 , C07C211/27 , C07C229/26 , C07C255/03 , C07C279/14 , C07D209/70 , C07D209/88 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , Y02A50/475
摘要： The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) 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 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.

4. 发明申请

US20170159088A1 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 审中-公开
公开(公告)号：US20170159088A1
公开(公告)日：2017-06-08
申请号：US15238014
申请日：2016-08-16
申请人： Arena Pharmaceuticals, Inc.
发明人： Antonio Garrido Montalban , Daniel J. Buzard , John A. DeMattei , Tawfik Gharbaoui , Stephen R. Johannsen , Ashwin M. Krishnan , Young Mi Kuhlman , You-An Ma , Michael John Martinelli , Suzanne Michiko Sato , Dipanjan Sengupta
IPC分类号： C12P17/10 , 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).

5. 发明申请

US20140038987A1 SUBSTITUTED 1,2,3,4-TETRAHYDROCYCLOPENTA[b]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS 有权
标题翻译：取代的1,2,3,4-四氢环戊二烯并[b]吲哚-3-基）乙酸衍生物用于治疗自身免疫和炎症性疾病
公开(公告)号：US20140038987A1
公开(公告)日：2014-02-06
申请号：US14048768
申请日：2013-10-08
申请人： Arena Pharmaceuticals, Inc.
发明人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V. Moody , Xiuwen Zhu , Scott Stirn
IPC分类号： C07D209/94 , C07D401/12 , C07C255/03 , C07C279/14 , C07C229/26 , C07C211/27 , C07D403/12 , C07D417/12
CPC分类号： C07D209/94 , A61K31/137 , A61K31/198 , A61K31/404 , A61K31/433 , A61K31/4439 , A61K31/497 , C07C211/27 , C07C229/26 , C07C255/03 , C07C279/14 , C07D209/70 , C07D209/88 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , Y02A50/475
摘要： The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) 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 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
摘要翻译：本发明涉及式（Ia）的某些取代的1,2,3,4-四氢环戊并[b]吲哚-3-基）乙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，例如作为激动剂的S1P1受体。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S1P1受体相关疾病例如牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应的方法，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，微生物感染或疾病以及病毒感染或疾病。

6. 发明申请

US20160016904A1 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：US20160016904A1
公开(公告)日：2016-01-21
申请号：US14870752
申请日：2015-09-30
申请人： Arena Pharmaceuticals, Inc.
发明人： Antonio Garrido Montalban , Daniel J. Buzard , John A. DeMattei , Tawfik Gharbaoui , Stephen R. Johannsen , Ashwin M. Krishnan , Young Mi Kuhlman , You-An Ma , Michael John Martinelli , Suzanne Michiko Sato , Dipanjan Sengupta
IPC分类号： C07D209/94 , C12P17/10
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-(trifluromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (I) 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）。

7. 发明申请

US20150336966A1 SUBSTITUTED TRICYCLIC ACID DERIVATIVES AS S1P1 RECEPTOR AGONISTS USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS 审中-公开
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：US20150336966A1
公开(公告)日：2015-11-26
申请号：US14817954
申请日：2015-08-04
申请人： Arena Pharmaceuticals, Inc.
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： C07D487/04 , C07D471/04
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。

8. 发明申请

US20150335618A1 SUBSTITUTED 1,2,3,4-TETRAHYDROCYCLOPENTA[b]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS 有权
标题翻译：取代的1,2,3,4-四氢环戊二烯并[b]吲哚-3-基）乙酸衍生物用于治疗自身免疫和炎症性疾病
公开(公告)号：US20150335618A1
公开(公告)日：2015-11-26
申请号：US14817455
申请日：2015-08-04
申请人： Arena Pharmaceuticals, Inc.
发明人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V. Moody , Xiuwen Zhu , Scott Stirn
IPC分类号： A61K31/404 , A61K31/137 , A61K31/433 , A61K31/198 , A61K31/497 , A61K31/4439
CPC分类号： C07D209/94 , A61K31/137 , A61K31/198 , A61K31/404 , A61K31/433 , A61K31/4439 , A61K31/497 , C07C211/27 , C07C229/26 , C07C255/03 , C07C279/14 , C07D209/70 , C07D209/88 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , Y02A50/475
摘要： The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) 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 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
摘要翻译：本发明涉及式（Ia）的某些取代的1,2,3,4-四氢环戊并[b]吲哚-3-基）乙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，例如作为激动剂的S1P1受体。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S1P1受体相关疾病例如牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应的方法，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，微生物感染或疾病以及病毒感染或疾病。

9. 发明授权

US09175320B2 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：US09175320B2
公开(公告)日：2015-11-03
申请号：US14464251
申请日：2014-08-20
申请人： ARENA PHARMACEUTICALS, INC.
发明人： Antonio Garrido Montalban , Daniel J. Buzard , John A. DeMattei , Tawfik Gharbaoui , Stephen R. Johannsen , Ashwin M. Krishnan , Young Mi Kuhlman , You-An Ma , Michael John Martinelli , Suzanne Michiko Sato , Dipanjan Sengupta
IPC分类号： C07D209/80 , C07D209/94 , C12P17/10 , C07C17/278 , C07D209/88 , C07D295/155
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）。

10. 发明申请

US20220259627A1 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
公开(公告)号：US20220259627A1
公开(公告)日：2022-08-18
申请号：US17474777
申请日：2021-09-14
申请人： Arena Pharmaceuticals, Inc.
发明人： Antonio Garrido Montalban , Daniel J. Buzard , John A. DeMattei , Tawfik Gharbaoui , Stephen R. Johannsen , Ashwin M. Krishnan , Young Mi Kuhlman , You-An Ma , Michael John Martinelli , Suzanne Michiko Sato , Dipanjan Sengupta
IPC分类号： C12P17/10 , C07D209/80 , C07D209/94 , C07C17/278 , C07D209/88 , C07D295/155
摘要： The present invention relates to processes and intermediates useful in the preparation of 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).

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