公开(公告)号：WO0077010A3

公开(公告)日：2001-06-28

申请号：PCT/US0016373

申请日：2000-06-15

Applicant: DU PONT PHARM CO

Inventor： ROBICHAUD ALBERT J ,  LEE TAEKYU ,  DENG WEI ,  MITCHELL IAN S ,  HAYDAR SIMON ,  CHEN WENTING ,  MC CLUNG CHRISTOPHER D ,  CALVELLO EMILIE J B ,  ZAWROTNY DAVID M

IPC: C07D487/04 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61P1/00 ,  A61P3/04 ,  A61P15/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D221/18 ,  C07D223/32 ,  C07D407/08 ,  C07D409/08 ,  C07D471/04 ,  C07D471/06 ,  C07D471/14 ,  C07D471/16 ,  C07D487/16 ,  C07D491/06 ,  C07D495/06 ,  C07D498/16 ,  C07D513/04 ,  C07D513/16 ,  C07D519/00 ,  A61K31/4353

CPC classification number: C07D471/06 ,  C07D221/18 ,  C07D223/32 ,  C07D491/06 ,  C07D495/06

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R , R , R , R , R , R , R , X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract translation: 本发明涉及由结构式（I）表示的某些新化合物或其药学上可接受的盐形式，其中R 1，R 5，R 6a，R 6b，R 7，R 7， <8>，R 9，X，b，k，m和n，这里描述虚线。 本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。 本发明的化合物是血清素激动剂和拮抗剂，可用于控制或预防中枢神经系统疾病，包括肥胖症，焦虑症，抑郁症，精神病，精神分裂症，睡眠障碍，性障碍，偏头痛，与头痛相关的病症，社交恐怖症 ，以及胃肠道疾病如胃肠道运动功能障碍。

公开(公告)号：WO1996015112A1

公开(公告)日：1996-05-23

申请号：PCT/US1995014572

申请日：1995-11-07

Applicant: ACEA PHARMACEUTICALS, INC.

Inventor： ACEA PHARMACEUTICALS, INC. ,  STATE OF OREGON, acting by and through THE OREGON STATE BOARD OF HIGHER EDUCATION, acting for and on behalf of THE OREGON HEALTH SCIENCES UNIVERSITY AND THE UNIVERSITY OF OREGON, EUGENE, OREGON ,  KEANA, John, F., W. ,  GUZIKOWSKI, Anthony, P. ,  NOGALES, Daniel, F. ,  CAI, Sui, Xiong

IPC: C07D223/16

CPC classification number: C07D223/16 ,  C07D223/32 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: Disclosed are methods of preparing azepines by a multistep synthesis including a Diels-Alder reaction. Also disclosed are methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment an azepine which has high binding to the NMDA glycine site.

Abstract translation: 公开了通过包括Diels-Alder反应的多步合成来制备氮杂的方法。 还公开了治疗或预防与中风，缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗神经变性疾病包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征的治疗或预防方法，治疗或预防不良后果 兴奋性氨基酸的多动症以及治疗焦虑症，慢性疼痛，抽搐，诱导麻醉和治疗或预防阿片剂耐受性的公开通过向需要这种治疗的动物施用与NMDA甘氨酸位点具有高结合性的吖庚因 。

公开(公告)号：WO1989000561A1

公开(公告)日：1989-01-26

申请号：PCT/US1987001636

申请日：1987-07-15

Applicant: SCHERING CORPORATION

Inventor： SCHERING CORPORATION ,  BERGER, Joel, Gilbert ,  CHANG, Wei, Kong ,  GOLD, Elijah, Herman ,  CLADER, John, Welch

IPC: C07D223/32

CPC classification number: C07D223/32 ,  C07D495/04

Abstract: Certain fused trans-isomer benzazepines are useful in treating psychoses, depression, pain and hypertension. The compounds also may be useful as renal vasodilators. Pharmaceutical compositions, methods of preparation and novel intermediate compositions are disclosed.

公开(公告)号：WO2014116684A1

公开(公告)日：2014-07-31

申请号：PCT/US2014/012521

申请日：2014-01-22

Applicant: ROBERTS, Edward ,  MITTAPALLI, Gopi Kumar ,  VELLUCCI, Danielle ,  YANG, Jun ,  GUERRERO, Miguel ,  URBANO, Mariangela ,  ROSEN, Hugh

Inventor： ROBERTS, Edward ,  MITTAPALLI, Gopi Kumar ,  VELLUCCI, Danielle ,  YANG, Jun ,  GUERRERO, Miguel ,  URBANO, Mariangela ,  ROSEN, Hugh

IPC: A61K31/55 ,  A61K31/497

CPC classification number: C07D307/24 ,  C07D223/16 ,  C07D223/20 ,  C07D223/32 ,  C07D263/32 ,  C07D263/34 ,  C07D267/20 ,  C07D295/205 ,  C07D295/215 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

Abstract: The invention provides compounds that are modulators of neuropeptide Y (NPY) receptors, which can be selective inhibitors of NPY receptor Y2R. NPY receptor modulatory compounds are of the general formula Ar 2 -Y-Ar 1 -W-Ar 3 , wherein the variables are as defined herein. Compounds of the invention can be used for treatment of malconditions in patients wherein modulation of an NPY receptor is medically indicated, for example including drug or alcohol abuse, anxiety disorders, depression, stress-related disorders, neurological disorders, nerve degeneration, osteoporosis or bone loss, sleep/wake disorders, cardiovascular diseases, obesity, anorexia, inovulation, fertility disorders, angiogenesis, cell proliferation, learning and memory disorders, migraine and pain.

Abstract translation: 本发明提供了作为神经肽Y（NPY）受体调节剂的化合物，其可以是NPY受体Y2R的选择性抑制剂。 NPY受体调节化合物具有通式Ar2-Y-Ar1-W-Ar3，其中变量如本文所定义。 本发明的化合物可用于治疗在医学上指示NPY受体调节的患者中的病情，例如包括药物或酒精滥用，焦虑障碍，抑郁症，应激相关疾病，神经障碍，神经变性，骨质疏松症或骨骼 失眠，睡眠/觉醒障碍，心血管疾病，肥胖，厌食，排卵，生育障碍，血管生成，细胞增殖，学习和记忆障碍，偏头痛和疼痛。

公开(公告)号：WO2014100815A2

公开(公告)日：2014-06-26

申请号：PCT/US2013/077501

申请日：2013-12-23

Applicant: ABT HOLDING COMPANY

Inventor： ROBARGE, Mike ,  HARRINGTON, John ,  GERRISH, David ,  MECOM, John

IPC: C07D223/32 ,  C07D401/04 ,  C07D491/048 ,  C07D417/04

CPC classification number: C07D223/32 ,  C07D401/04 ,  C07D417/04 ,  C07D491/048 ,  C07D491/052

Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are benzazepine compounds. These compounds are serotonin receptor (5-HT 2c ) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT 2c ) is desired (e.g. addiction, anxiety, depression, obesity, and others).

Abstract translation: 本发明一般涉及一系列化合物，含有该化合物的药物组合物，以及该化合物和组合物作为治疗剂的用途。 更具体地，本发明的化合物是苯并氮杂化合物。 这些化合物是5-羟色胺受体（5-HT2c）配体，并且可用于治疗需要调节5-羟色胺受体（5-HT2c）的活性的疾病，病症和病症（例如成瘾，焦虑，抑郁，肥胖等） 。

公开(公告)号：WO2010077680A3

公开(公告)日：2010-10-14

申请号：PCT/US2009067197

申请日：2009-12-08

Applicant: VM DISCOVERY INC ,  WU JAY JIE-QUIANG ,  WANG LING

Inventor： WU JAY JIE-QUIANG ,  WANG LING

IPC: C07D487/04 ,  A61P29/00 ,  C07D403/14 ,  C07D417/12

CPC classification number: C07D498/06 ,  A61K31/496 ,  A61K31/497 ,  A61K45/06 ,  C07D215/20 ,  C07D221/06 ,  C07D223/32 ,  C07D241/44 ,  C07D261/20 ,  C07D265/36 ,  C07D279/16 ,  C07D295/13 ,  C07D307/77 ,  C07D403/14 ,  C07D407/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D493/06 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF recptor TrkA.

Abstract translation: 本发明涉及新型合成取代的杂环化合物和含有能够抑制或拮抗受体酪氨酸激酶家族（Tropomysosin Related Kinases，Trk），特别是神经生长因子（NGF）受体TrkA的家族的合成取代杂环化合物和药物组合物。 本发明还涉及这些化合物在治疗和/或预防疼痛，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成或与异常髓鞘或脱髓鞘有关的疾病，病症或损伤或与异常活动有关的疾病或病症 的NGF吸收器TrkA。

公开(公告)号：WO02034760A2

公开(公告)日：2002-05-02

申请号：PCT/US2001/051175

申请日：2001-10-23

IPC: C07D209/44 ,  C07D209/62 ,  C07D215/08 ,  C07D217/06 ,  C07D223/16 ,  C07D223/32 ,  C07D401/12 ,  C07D413/04 ,  C07D491/10 ,  C07H

CPC classification number: C07D401/12 ,  C07D209/44 ,  C07D209/62 ,  C07D215/08 ,  C07D217/06 ,  C07D223/16 ,  C07D223/32 ,  C07D413/04 ,  C07D491/10

Abstract: The invention relates to substituted urea compounds which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis, or idiopathic pulmonary fibrosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, treating and/or preventing rejection of transplanted organs, and inflammatory bowel disease, all in mammals, by the use of substituted urea compounds which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators maybe useful in the treatment of HIV infection.

Abstract translation: 本发明涉及作为CCR5受体的调节剂，激动剂或拮抗剂的取代的脲化合物。 此外，本发明涉及治疗和预防CCR5介导的疾病状态，包括但不限于哮喘和特应性疾病（例如特应性皮炎和过敏），类风湿性关节炎，结节病或特发性肺纤维化等纤维化 疾病，动脉粥样硬化，牛皮癣，自身免疫性疾病如多发性硬化，治疗和/或预防移植器官的排斥，以及哺乳动物的炎症性肠病，都是通过使用作为CCR5受体拮抗剂的取代脲化合物。 此外，由于CD8 + T细胞与COPD有牵连，因此CCR5可能在其募集中发挥作用，因此CCR5拮抗剂可为COPD治疗提供潜在的治疗方法。 此外，由于CCR5是HIV进入细胞的共同受体，选择性受体调节剂也可用于治疗HIV感染。

公开(公告)号：WO01070677A1

公开(公告)日：2001-09-27

申请号：PCT/GB2001/001154

申请日：2001-03-15

IPC: A61K31/18 ,  A61K31/277 ,  A61K31/343 ,  A61K31/357 ,  A61K31/381 ,  A61K31/40 ,  A61K31/407 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/425 ,  A61K31/438 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/4535 ,  A61K31/47 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/55 ,  A61P25/28 ,  A61P43/00 ,  C07C211/42 ,  C07C251/44 ,  C07C311/07 ,  C07C311/09 ,  C07C311/11 ,  C07C311/14 ,  C07C311/20 ,  C07C311/24 ,  C07C311/29 ,  C07C323/67 ,  C07D207/06 ,  C07D207/36 ,  C07D211/14 ,  C07D211/18 ,  C07D213/30 ,  C07D213/38 ,  C07D213/71 ,  C07D213/81 ,  C07D215/12 ,  C07D223/32 ,  C07D233/84 ,  C07D249/08 ,  C07D271/10 ,  C07D271/107 ,  C07D275/02 ,  C07D277/20 ,  C07D277/36 ,  C07D277/42 ,  C07D277/54 ,  C07D285/14 ,  C07D285/16 ,  C07D295/088 ,  C07D295/092 ,  C07D295/135 ,  C07D295/18 ,  C07D295/26 ,  C07D307/64 ,  C07D307/81 ,  C07D319/18 ,  C07D333/20 ,  C07D333/34 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D487/08 ,  C07D491/08 ,  C07D491/10 ,  C07D491/107 ,  C07D513/10 ,  C07D521/00 ,  C07D213/70 ,  C07D215/20 ,  C07D295/22

CPC classification number: C07D213/30 ,  A61K31/18 ,  A61K31/40 ,  C07C311/07 ,  C07C311/09 ,  C07C311/11 ,  C07C311/14 ,  C07C311/20 ,  C07C311/24 ,  C07C323/67 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/44 ,  C07C2602/46 ,  C07C2603/72 ,  C07C2603/78 ,  C07D207/36 ,  C07D211/14 ,  C07D211/18 ,  C07D213/71 ,  C07D213/81 ,  C07D215/12 ,  C07D223/32 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D271/107 ,  C07D277/36 ,  C07D285/14 ,  C07D285/16 ,  C07D295/088 ,  C07D295/135 ,  C07D295/26 ,  C07D307/64 ,  C07D307/81 ,  C07D319/18 ,  C07D333/34 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D487/08 ,  C07D491/08 ,  C07D491/10 ,  C07D513/10

Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures of formula (I) (where the variables are as defined in the claims). The compounds are inhibitors of gamma -secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.

Abstract translation: 公开了一类化合物，其包含式（I）的磺酰胺基取代的桥连双环烷基结构（其中变量如权利要求中所定义）。 这些化合物是γ-分泌酶的抑制剂，因此可用于治疗和/或预防阿尔茨海默氏病。

公开(公告)号：WO00077002A1

公开(公告)日：2000-12-21

申请号：PCT/US2000/016498

申请日：2000-06-15

IPC: C07D487/04 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61P1/00 ,  A61P3/04 ,  A61P15/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D221/18 ,  C07D223/32 ,  C07D407/08 ,  C07D409/08 ,  C07D471/04 ,  C07D471/06 ,  C07D471/14 ,  C07D471/16 ,  C07D487/16 ,  C07D491/06 ,  C07D495/06 ,  C07D498/16 ,  C07D513/04 ,  C07D513/16 ,  C07D519/00 ,  A61K31/5517

CPC classification number: C07D471/06 ,  C07D221/18 ,  C07D223/32 ,  C07D491/06 ,  C07D495/06

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R , R , R , R , R , R , R , X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract translation: 本发明涉及由结构式（I）表示的某些新化合物或其药学上可接受的盐形式，其中R 1，R 5，R 6a，R 6b，R 7，R 7， <8>，R 9，X，b，k，m和n，这里描述虚线。 本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。 本发明的化合物是血清素激动剂和拮抗剂，可用于控制或预防中枢神经系统疾病，包括肥胖症，焦虑症，抑郁症，精神病，精神分裂症，睡眠障碍，性障碍，偏头痛，与头痛相关的病症，社交恐怖症 ，以及胃肠道疾病如胃肠道运动功能障碍。

公开(公告)号：WO00077001A1

公开(公告)日：2000-12-21

申请号：PCT/US2000/016375

申请日：2000-06-15

IPC: C07D487/04 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61P1/00 ,  A61P3/04 ,  A61P15/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D221/18 ,  C07D223/32 ,  C07D407/08 ,  C07D409/08 ,  C07D471/04 ,  C07D471/06 ,  C07D471/14 ,  C07D471/16 ,  C07D487/16 ,  C07D491/06 ,  C07D495/06 ,  C07D498/16 ,  C07D513/04 ,  C07D513/16 ,  C07D519/00 ,  A61K31/407

CPC classification number: C07D471/06 ,  C07D221/18 ,  C07D223/32 ,  C07D491/06 ,  C07D495/06

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I): or pharmaceutically acceptable salt forms thereof, wherein R , R , R , R , R , R , R , X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract translation: 本发明涉及由结构式（I）表示的某些新化合物：或其药学上可接受的盐形式，其中R 1，R 5，R 6a，R 6b，R 7， R 8，R 9，X，b，k，m和n，这里描述虚线。 本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。 本发明的化合物是血清素激动剂和拮抗剂，可用于控制或预防中枢神经系统疾病，包括肥胖症，焦虑症，抑郁症，精神病，精神分裂症，睡眠障碍，性障碍，偏头痛，与头痛相关的病症，社交恐怖症 ，以及胃肠道疾病如胃肠道运动功能障碍。