公开(公告)号：US20080200491A1

公开(公告)日：2008-08-21

申请号：US11917731

申请日：2006-06-21

Applicant: Thuy-Anh Tran ,  Sangdon Han ,  P. Douglas Boatman

Inventor： Thuy-Anh Tran ,  Sangdon Han ,  P. Douglas Boatman

IPC: A61K31/438 ,  C07D471/10 ,  A61P9/10 ,  A61P25/02 ,  A61P25/16

CPC classification number: C07D471/10

Abstract: The present invention relates to certain 1,2-dihydro-spiro[3H-indole-3,4′-piperidine]compounds of Formula (Ia): and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein G, R1, R2, R3, R4, R5, and Ar are as disclosed herein (“Compound(s) of the Invention”), which are useful, for example, as cardio-protective and/or neuro-protective agents. The invention also provides pharmaceutical compositions comprising a Compound of the Invention and methods for treating, preventing and/or managing a vascular, cardiovascular or neurological disease or disorder, comprising administering to a patient in need thereof a Compound of the Invention.

Abstract translation: 本发明涉及式（Ia）的某些1,2-二氢螺[3H-吲哚-3,4'-哌啶]化合物及其药学上可接受的盐，溶剂化物和水合物，其中G，R1，R2，R3 ，R4，R5和Ar如本文所公开的（“本发明的化合物”），其可用作例如心保护和/或神经保护剂。 本发明还提供了包含本发明化合物和治疗，预防和/或控制血管，心血管或神经疾病或病症的方法的药物组合物，其包括向有需要的患者施用本发明的化合物。

公开(公告)号：US20050197350A1

公开(公告)日：2005-09-08

申请号：US10812075

申请日：2004-03-30

Applicant: Yoshinori Sekiguchi ,  Kosuke Kanuma ,  Katsunori Omodera ,  Tsuyoshi Busujima ,  Thuy-Anh Tran ,  Sangdon Han ,  Martin Casper ,  Bryan Kramer ,  Graeme Semple ,  Ning Zou

Inventor： Yoshinori Sekiguchi ,  Kosuke Kanuma ,  Katsunori Omodera ,  Tsuyoshi Busujima ,  Thuy-Anh Tran ,  Sangdon Han ,  Martin Casper ,  Bryan Kramer ,  Graeme Semple ,  Ning Zou

IPC: A61K31/47 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/517 ,  A61P1/14 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D215/42 ,  C07D239/48 ,  C07D239/94 ,  C07D239/95 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D239/48 ,  C07D215/42 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to novel compounds of the Formula (I): which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.

Abstract translation: 本发明涉及作为MCH受体拮抗剂的式（I）的新化合物。 这些组合物可用于药物组合物，其用途包括改善记忆功能，睡眠和觉醒，焦虑，抑郁，情绪障碍，癫痫发作，肥胖症，糖尿病，食欲和进食障碍，心血管疾病，高血压，血脂异常，心肌梗塞， 包括贪食症，厌食症，包括躁狂抑郁症，精神分裂症，del妄，痴呆，压力，认知障碍，注意力缺陷障碍，药物滥用障碍和包括帕金森氏病，癫痫和成瘾在内的运动障碍的暴饮暴食症。

公开(公告)号：US09458136B2

公开(公告)日：2016-10-04

申请号：US14001133

申请日：2012-02-24

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

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

IPC: A61K31/4965 ,  C07D403/04 ,  A61K31/497

CPC classification number: C07D403/04 ,  A61K31/497 ,  A61P29/00 ,  C07B2200/13

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.

Abstract translation: 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。

公开(公告)号：US20140018371A1

公开(公告)日：2014-01-16

申请号：US14007759

申请日：2012-03-30

Applicant: Robert M. Jones ,  Sangdon Han ,  Juerg Lehmann ,  Lars Thoresen

Inventor： Robert M. Jones ,  Sangdon Han ,  Juerg Lehmann ,  Lars Thoresen

IPC: A61K31/506 ,  C07D413/04 ,  A61K31/454 ,  C07D401/12 ,  A61K45/06 ,  A61K31/497 ,  C07D401/14 ,  C07D211/24 ,  C07D401/06 ,  A61K31/445 ,  A61K31/4545

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20130023494A1

公开(公告)日：2013-01-24

申请号：US13639652

申请日：2011-04-05

Applicant: Robert M. Jones ,  Sangdon Han ,  Daniel J. Buzard ,  Juerg Lehmann ,  Sanju Narayanan ,  Dawei Yue

Inventor： Robert M. Jones ,  Sangdon Han ,  Daniel J. Buzard ,  Juerg Lehmann ,  Sanju Narayanan ,  Dawei Yue

IPC: A61K31/445 ,  C07D413/04 ,  A61K31/454 ,  C07D401/04 ,  A61K31/506 ,  C07D401/14 ,  C07D401/12 ,  A61K31/497 ,  A61K31/501 ,  C07D417/14 ,  A61K31/541 ,  A61K31/4523 ,  A61P19/00 ,  A61P25/00 ,  A61P3/00 ,  A61P3/10 ,  A61P3/04 ,  A61K31/4985 ,  A61K31/69 ,  A61K31/4745 ,  A61K31/522 ,  A61K31/53 ,  A61K31/519 ,  C07D211/46

CPC classification number: C07D211/46 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14

Abstract: 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 additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, 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.

Abstract translation: 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另外的药剂如DPP-IV抑制剂组合使用， 双胍类，SGLT2抑制剂或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。

公开(公告)号：US20110130409A1

公开(公告)日：2011-06-02

申请号：US13055333

申请日：2009-07-22

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

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

IPC: A61K31/497 ,  C07D209/94 ,  C07D403/12 ,  C07D401/12 ,  C07D417/12 ,  A61K31/403 ,  A61K31/4439 ,  A61K31/433 ,  A61P37/06 ,  A61P29/00 ,  A61P35/00 ,  A61P17/06 ,  A61P25/28 ,  A61P3/10 ,  A61P1/00 ,  A61P17/10 ,  A61P31/00 ,  A61P31/12

CPC classification number: 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

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.

Abstract translation: 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。

公开(公告)号：US09597340B2

公开(公告)日：2017-03-21

申请号：US14001132

申请日：2012-02-24

Applicant: 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

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

CPC classification number: A61K31/675 ,  A61K31/416 ,  A61K31/4439 ,  A61K31/497 ,  A61K45/06 ,  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：US20150126477A1

公开(公告)日：2015-05-07

申请号：US14001132

申请日：2012-02-24

Applicant: 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

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 ,  A61K31/4439 ,  A61K31/497 ,  A61K45/06 ,  A61K31/416

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

Abstract translation: 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;

公开(公告)号：US20140235622A1

公开(公告)日：2014-08-21

申请号：US14166511

申请日：2014-01-28

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

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

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

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.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.

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。 本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT2A 5-羟色胺受体相关疾病的方法。

公开(公告)号：US20140066369A1

公开(公告)日：2014-03-06

申请号：US14112384

申请日：2012-04-18

Applicant: Robert M. Jones ,  Daniel J. Buzard ,  Sangdon Han ,  Sun Hee Kim ,  Juerg Lehmann ,  Dawei Yue ,  Xiuwen Zhu

Inventor： Robert M. Jones ,  Daniel J. Buzard ,  Sangdon Han ,  Sun Hee Kim ,  Juerg Lehmann ,  Dawei Yue ,  Xiuwen Zhu

IPC: C07D295/205 ,  A61K45/06 ,  C07D239/42 ,  A61K31/506 ,  A61K31/496 ,  A61K31/499 ,  C07D249/08 ,  C07D403/12 ,  C07D257/04 ,  C07D487/08 ,  A61K31/4995 ,  C07D241/38 ,  A61K31/495 ,  C07D271/07

CPC classification number: C07D295/205 ,  A61K31/495 ,  A61K31/496 ,  A61K31/499 ,  A61K31/4995 ,  A61K31/506 ,  A61K45/06 ,  C07D207/325 ,  C07D213/68 ,  C07D213/71 ,  C07D213/85 ,  C07D231/12 ,  C07D233/60 ,  C07D239/34 ,  C07D239/42 ,  C07D241/04 ,  C07D241/08 ,  C07D241/38 ,  C07D249/06 ,  C07D249/08 ,  C07D249/10 ,  C07D257/04 ,  C07D271/06 ,  C07D271/07 ,  C07D295/21 ,  C07D295/26 ,  C07D305/08 ,  C07D401/12 ,  C07D403/12 ,  C07D471/08 ,  C07D487/08

Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, 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 condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

Abstract translation: 本发明涉及式I化合物及其药学上可接受的盐，溶剂合物和水合物，其可用作单一药剂或与一种或多种另外的药剂组合使用，例如DPP-IV抑制剂，双胍类， α-葡糖苷酶抑制剂，胰岛素类似物，磺酰脲类，SGLT2抑制剂，氯噻嗪，噻唑烷二酮或抗糖尿病肽类似物，在治疗中例如选自：GPR119-受体相关病症 ; 通过增加血液肠降血糖水平来改善病情; 以低骨量为特征的病症; 神经障碍 代谢相关疾病; 2型糖尿病; 肥胖; 和相关的并发症。