公开(公告)号：US11771695B2

公开(公告)日：2023-10-03

申请号：US17478274

申请日：2021-09-17

Applicant: Arena Pharmaceuticals, Inc.

Inventor： 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: A61K31/497 ,  C07D231/54 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07F9/6558 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/675 ,  A61K45/06 ,  A61K31/13 ,  A61K31/485

CPC classification number: 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

Abstract: 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;

公开(公告)号：US20210060040A1

公开(公告)日：2021-03-04

申请号：US16849216

申请日：2020-04-15

Applicant: Arena Pharmaceuticals, Inc.

Inventor： 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: A61K31/675 ,  A61K31/416 ,  A61K45/06 ,  A61K31/4439 ,  A61K31/497

Abstract: 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;

公开(公告)号：US20180354907A1

公开(公告)日：2018-12-13

申请号：US15912700

申请日：2018-03-06

Applicant: Arena Pharmaceuticals, Inc.

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

IPC: C07D231/54 ,  C07D403/04 ,  C07D413/14 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07F9/6558 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12

CPC classification number: C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07F9/65583

Abstract: 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.

公开(公告)号：US20160271127A1

公开(公告)日：2016-09-22

申请号：US14956586

申请日：2015-12-02

Applicant: Arena Pharmaceuticals, Inc.

Inventor： 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: A61K31/497 ,  A61K31/675 ,  A61K31/4439 ,  A61K45/06 ,  A61K31/416

CPC classification number: 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

Abstract: 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;

公开(公告)号：US12109219B2

公开(公告)日：2024-10-08

申请号：US16849216

申请日：2020-04-15

Applicant: Arena Pharmaceuticals, Inc.

Inventor： 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: A61K31/675 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/497 ,  A61K45/06

CPC classification number: A61K31/675 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/497 ,  A61K45/06 ,  A61K31/416 ,  A61K2300/00

Abstract: 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;

公开(公告)号：US20230257349A1

公开(公告)日：2023-08-17

申请号：US17885683

申请日：2022-08-11

Applicant: Arena Pharmaceuticals, Inc.

Inventor： Robert M. Jones ,  Daniel J. Buzard ,  Sangdon Han ,  Sun Hee Kim ,  Juerg Lehmann ,  Brett Ullman ,  Jeanne V. Moody ,  Xiuwen Zhu ,  Scott Stirn

IPC: 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 classification number: 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

Abstract: 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.

公开(公告)号：US20190070149A1

公开(公告)日：2019-03-07

申请号：US15963635

申请日：2018-04-26

Applicant: Arena Pharmaceuticals, Inc.

Inventor： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jay Xu ,  Ning Zou

IPC: A61K31/415 ,  C07D231/12 ,  C07D417/12 ,  C07D413/12 ,  C07D231/16 ,  C07D405/12 ,  C07D403/12 ,  C07D401/12 ,  C07D409/12

Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

公开(公告)号：US10183930B2

公开(公告)日：2019-01-22

申请号：US15248300

申请日：2016-08-26

Applicant: Arena Pharmaceuticals, Inc.

Inventor： Anthony C. Blackburn ,  Sangdon Han ,  Robert M. Jones ,  Antonio Garrido Montalban ,  Biman B. Pal ,  Jaimie Karyn Rueter

IPC: C07D403/04 ,  A61K31/497 ,  A61P29/00

Abstract: 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.

公开(公告)号：US09328107B2

公开(公告)日：2016-05-03

申请号：US14166511

申请日：2014-01-28

Applicant: Arena Pharmaceuticals, Inc.

Inventor： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jay Xu ,  Ning Zou

IPC: C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: A61K31/415 ,  C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

Abstract translation: 本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。 化合物及其药物组合物涉及可用于治疗血小板凝集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法， 精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病， 相关疾病，进行性多灶性脑白质病等。

公开(公告)号：US20150265576A1

公开(公告)日：2015-09-24

申请号：US14634218

申请日：2015-02-27

Applicant: Arena Pharmaceuticals, Inc.

Inventor： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jay Xu ,  Ning Zou

IPC: A61K31/415

CPC classification number: A61K31/415 ,  C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.