公开(公告)号：US07087601B2

公开(公告)日：2006-08-08

申请号：US10497452

申请日：2002-11-26

申请人： Jeannie Arruda ,  Celine Bonnefous ,  Brian T. Campbell ,  Rowena V. Cube ,  Benito Munoz ,  Brian Stearns ,  Jean-Michel Vernier ,  Bowei Wang ,  Xiumin Zhao

发明人： Jeannie Arruda ,  Celine Bonnefous ,  Brian T. Campbell ,  Rowena V. Cube ,  Benito Munoz ,  Brian Stearns ,  Jean-Michel Vernier ,  Bowei Wang ,  Xiumin Zhao

IPC分类号： A61K31/5383 ,  A61K31/437 ,  C07D413/14 ,  C07D491/048

CPC分类号： C07D263/57 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D413/10

摘要： Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at the 3,4 positions, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

摘要翻译： 苯基化合物在1-位上被一个稠合的双环自由基组成，它由与六元碳环稠合的五元杂环，六元芳基或六元杂芳基形成，并进一步任选地被取代在3位上 ，4个位置是mGluR5调节剂，可用于治疗精神病和情绪障碍，例如精神分裂症，焦虑，抑郁和恐慌，以及治疗疼痛和其他疾病。

公开(公告)号：US20050065340A1

公开(公告)日：2005-03-24

申请号：US10497452

申请日：2002-11-26

申请人： Jeannie Arruda ,  Celine Bonnefous ,  Brian Campbell ,  Rowena Cube ,  Benito Munoz ,  Brian Stearns ,  Jean-Michel Vernier ,  Bowei Wang ,  Xiumin Zhao

发明人： Jeannie Arruda ,  Celine Bonnefous ,  Brian Campbell ,  Rowena Cube ,  Benito Munoz ,  Brian Stearns ,  Jean-Michel Vernier ,  Bowei Wang ,  Xiumin Zhao

IPC分类号： C07D263/56 ,  A61K31/422 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/34 ,  A61P25/36 ,  A61P29/00 ,  A61P43/00 ,  C07D263/57 ,  C07D413/10 ,  C07D498/04 ,  C07D521/00 ,  C07D471/02 ,  C07D413/02 ,  C07D417/02 ,  C07D43/02

CPC分类号： C07D263/57 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D413/10

摘要： Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at 2 the 3,4 positions, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

摘要翻译： 苯基化合物在1位上被一个稠合的双环形成，由与六元碳环稠合的五元杂环，六元芳基或六元杂芳基形成，并进一步任选地在2位上被取代 3,4位是用于治疗精神病和情绪障碍（例如精神分裂症，焦虑，抑郁和恐慌）以及治疗疼痛和其他疾病的mGluR5调节剂。

公开(公告)号：US20080293684A1

公开(公告)日：2008-11-27

申请号：US11658546

申请日：2005-07-26

申请人： Anthony B Pinkerton ,  Jean-Michel Vernier ,  Rowena V. Cube ,  John H. Hutchinson ,  Dehua Huang ,  Celine Bonnefous ,  Steven P. Govak ,  Theodore Kamenecka

发明人： Anthony B Pinkerton ,  Jean-Michel Vernier ,  Rowena V. Cube ,  John H. Hutchinson ,  Dehua Huang ,  Celine Bonnefous ,  Steven P. Govak ,  Theodore Kamenecka

IPC分类号： A61K31/397 ,  C07D311/02 ,  A61K31/353 ,  A61K31/12 ,  C07C49/213 ,  C07D211/72 ,  A61K31/44 ,  A61K31/505 ,  C07D239/02 ,  C07D217/22 ,  A61K31/472 ,  A61K31/497 ,  C07D401/02 ,  C07D213/24 ,  A61K31/4427 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4245 ,  A61P25/08 ,  A61P25/24 ,  A61P25/18 ,  C07D213/62 ,  A61K31/444 ,  A61K31/343 ,  C07D307/77 ,  C07D473/28 ,  A61K31/522 ,  A61K31/41 ,  C07D257/04 ,  C07D263/58 ,  A61K31/423 ,  A61K31/428 ,  C07D277/20 ,  C07D205/02 ,  C07D271/10 ,  C07D215/58 ,  A61K31/47 ,  C07D403/02 ,  C07D417/02 ,  A61K31/427

CPC分类号： C07D311/16 ,  C07C45/71 ,  C07C49/84 ,  C07C69/734 ,  C07C69/92 ,  C07C217/76 ,  C07C217/92 ,  C07C235/42 ,  C07C255/54 ,  C07C323/12 ,  C07D205/04 ,  C07D209/08 ,  C07D213/30 ,  C07D213/53 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/70 ,  C07D213/71 ,  C07D213/74 ,  C07D213/84 ,  C07D213/89 ,  C07D215/20 ,  C07D217/02 ,  C07D231/56 ,  C07D233/20 ,  C07D233/60 ,  C07D235/06 ,  C07D235/08 ,  C07D235/10 ,  C07D235/16 ,  C07D235/18 ,  C07D239/34 ,  C07D257/04 ,  C07D263/58 ,  C07D271/10 ,  C07D277/74 ,  C07D307/80 ,  C07D311/22 ,  C07D311/24 ,  C07D311/58 ,  C07D401/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/38

摘要： The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

摘要翻译： 本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的化合物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及其中涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

公开(公告)号：US20080312286A1

公开(公告)日：2008-12-18

申请号：US11658490

申请日：2005-07-26

申请人： Anthony B. Pinkerton ,  Jean-Michel Vernier ,  Rowena Cube ,  John Hutchinson ,  Celine Bonnefous ,  Theodore Kamenecka

发明人： Anthony B. Pinkerton ,  Jean-Michel Vernier ,  Rowena Cube ,  John Hutchinson ,  Celine Bonnefous ,  Theodore Kamenecka

IPC分类号： C07D257/04 ,  A61K31/41 ,  C07C307/02 ,  A61K31/18 ,  C07C233/02 ,  A61K31/454 ,  C07D401/02 ,  A61K31/192 ,  C07C65/00 ,  C07D213/80 ,  A61K31/44 ,  A61K31/343 ,  C07D307/78 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/08

CPC分类号： C07C233/91 ,  C07C59/90 ,  C07C65/40 ,  C07C311/51 ,  C07C2601/08 ,  C07C2602/08 ,  C07D257/04 ,  C07D307/79 ,  C07D401/04

摘要： The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

摘要翻译： 本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的化合物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及其中涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

公开(公告)号：US07408067B2

公开(公告)日：2008-08-05

申请号：US10500517

申请日：2002-07-29

申请人： Peter Charles Astles ,  Stephen Richard Baker ,  Celine Bonnefous ,  Jean Michel Vernier ,  Martine Keenan ,  Adam Jan Sanderson

发明人： Peter Charles Astles ,  Stephen Richard Baker ,  Celine Bonnefous ,  Jean Michel Vernier ,  Martine Keenan ,  Adam Jan Sanderson

IPC分类号： C07D211/22 ,  C07D401/00

CPC分类号： C07D401/06 ,  C07D207/12 ,  C07D211/54 ,  C07D223/06 ,  C07D401/12 ,  C07D405/06 ,  C07D413/12 ,  C07D417/06

摘要： Compounds comprising an aza-cyclic portion and an aromatic portion linked via a sulphur atom are disclosed. The compounds disclosed are selective modulators of beta 4 subtype nicotinic acetylcholine receptors and are useful for the treatment of dysfunctions of the central and autonomic nervous systems.

摘要翻译： 公开了包含氮杂环状部分和通过硫原子连接的芳香族部分的化合物。 所公开的化合物是β4亚型烟碱乙酰胆碱受体的选择性调节剂，并且可用于治疗中枢神经系统和自主神经系统的功能障碍。

公开(公告)号：US20070149547A1

公开(公告)日：2007-06-28

申请号：US10589407

申请日：2005-02-09

申请人： Celine Bonnefous ,  Theodore Kamenecka ,  Jean-Michel Vernier

发明人： Celine Bonnefous ,  Theodore Kamenecka ,  Jean-Michel Vernier

IPC分类号： A61K31/497 ,  A61K31/444 ,  C07D403/02 ,  C07D401/02

CPC分类号： C07D401/12 ,  C07D213/81 ,  C07D241/26 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07F7/0812

摘要： The present invention is directed to novel amides such as those of Formula (I): (I) which are mGluR5 modulators useful in the treatment or prevention of diseases and conditions in which mGluR5 is involved, including but not limited to psychiatric and mood disorders such as schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders, such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal, obesity and other diseases. The invention is also directed to pharmaceutical compositions comprising these compounds. This invention further provides a method of treatment of these disorders and conditions by the administration of an effective amount of these novel amides and/or compositions containing these compounds.

摘要翻译： 本发明涉及新型酰胺，例如式（I）：（I）的那些酰胺，其为可用于治疗或预防涉及mGluR5的疾病和病症的mGluR5调节剂，包括但不限于精神和心境障碍 作为精神分裂症，焦虑症，抑郁症，双相性精神障碍和恐慌，以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律和睡眠障碍，如转移工作诱导的睡眠障碍和时差，药物 成瘾，药物滥用，戒毒，肥胖等疾病。 本发明还涉及包含这些化合物的药物组合物。 本发明还提供了一种通过施用有效量的这些新型酰胺和/或含有这些化合物的组合物来治疗这些病症和病症的方法。

公开(公告)号：US07700591B2

公开(公告)日：2010-04-20

申请号：US11129512

申请日：2005-05-13

申请人： Stephen D. Goble ,  Sander G. Mills ,  Lihu Yang ,  Alexander Pasternak ,  Celine Bonnefous ,  Theodore M Kamenecka ,  Jean-Michel Vernier ,  John H. Hutchinson ,  Essa Hu ,  Steven Govek

发明人： Stephen D. Goble ,  Sander G. Mills ,  Lihu Yang ,  Alexander Pasternak ,  Celine Bonnefous ,  Theodore M Kamenecka ,  Jean-Michel Vernier ,  John H. Hutchinson ,  Essa Hu ,  Steven Govek

IPC分类号： A61K31/535 ,  C07D265/12 ,  C07D498/00

CPC分类号： C07D413/08 ,  C07D413/14 ,  C07D417/14

摘要： Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.

摘要翻译： 通过使用苯并恶嗪的环氮通过酰胺部分连接到苯并恶嗪基的环戊基化合物，并进一步被杂环部分取代，由式I表示的化合物：其用于调节CCR-2趋化因子受体以预防或治疗炎症 和免疫调节性疾病和疾病，过敏性疾病，特应性病症，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及自身免疫性病态如类风湿性关节炎和动脉粥样硬化; 和包含这些化合物的药物组合物以及这些化合物和组合物的用途。

公开(公告)号：US20070027321A1

公开(公告)日：2007-02-01

申请号：US10570068

申请日：2004-08-27

申请人： Theodore Kamenecka ,  Jean-Michel Vernier ,  Celine Bonnefous ,  Steven Govek ,  John Hutchinson

发明人： Theodore Kamenecka ,  Jean-Michel Vernier ,  Celine Bonnefous ,  Steven Govek ,  John Hutchinson

IPC分类号： A61K31/4743 ,  C07D471/02 ,  C07D401/02 ,  C07D417/14

CPC分类号： C07D213/74 ,  C04B35/632 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04

摘要： The present invention is directed to novel bipyridyl amine and ether compounds such as those of Formula (I): (I) (where R?1#191, R?2#191, R?3#191, X and Y are as defined herein) which are mGluR5 modulators useful in the treatment or prevention of diseases and conditions in which mGluR5 is involved, including but not limited to psychiatric and mood disorders such as schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders, such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal, obesity and other diseases. The invention is also directed to pharmaceutical compositions comprising these compounds. This invention further provides a method of treatment of these disorders and conditions by the administration of an effective amount of these novel bipyridyl amine and/or ether compounds and/or compositions containing these compounds.

摘要翻译： 本发明涉及新型联吡啶胺和醚化合物，例如式（I）的那些：（I）（其中R 1＃191，R 2＃191，R 3＃191，X和Y如上所定义） 这是mGluR5调节剂，其可用于治疗或预防涉及mGluR5的疾病和病症，包括但不限于精神和心境障碍如精神分裂症，焦虑，抑郁，双相情感障碍和恐慌，以及在 治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律和睡眠障碍，如转移工作诱导的睡眠障碍和时差，药物成瘾，药物滥用，药物戒断，肥胖症等疾病。 本发明还涉及包含这些化合物的药物组合物。 本发明还提供了通过施用有效量的这些新型联吡啶胺和/或醚化合物和/或含有这些化合物的组合物来治疗这些病症和病症的方法。

公开(公告)号：US20060069088A1

公开(公告)日：2006-03-30

申请号：US11129512

申请日：2005-05-13

申请人： Stephen Goble ,  Sander Mills ,  Lihu Yang ,  Alexander Pasternak ,  Celine Bonnefous ,  Theodore Kamenecka ,  Jean-Michel Vernier ,  John Hutchinson ,  Essa Hu ,  Steven Govek

发明人： Stephen Goble ,  Sander Mills ,  Lihu Yang ,  Alexander Pasternak ,  Celine Bonnefous ,  Theodore Kamenecka ,  Jean-Michel Vernier ,  John Hutchinson ,  Essa Hu ,  Steven Govek

IPC分类号： A61K31/542 ,  A61K31/538 ,  A61K31/519 ,  C07D498/02 ,  C07D487/02 ,  C07D491/02

CPC分类号： C07D413/08 ,  C07D413/14 ,  C07D417/14

摘要： Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.

摘要翻译： 通过使用苯并恶嗪的环氮通过酰胺部分连接到苯并恶嗪基的环戊基化合物，并进一步被杂环部分取代，由式I表示的化合物：

公开(公告)号：US20130012561A1

公开(公告)日：2013-01-10

申请号：US13613467

申请日：2012-09-13

申请人： Nicholas D. SMITH ,  Mehmet Kahraman ,  Steven P. Govek ,  Johnny Y. Nagasawa ,  Andiliy G. Lai ,  Jackaline D. Julien ,  Celine Bonnefous

发明人： Nicholas D. SMITH ,  Mehmet Kahraman ,  Steven P. Govek ,  Johnny Y. Nagasawa ,  Andiliy G. Lai ,  Jackaline D. Julien ,  Celine Bonnefous

IPC分类号： A61K31/416 ,  A61P35/00

CPC分类号： C07D231/56 ,  A61K31/416 ,  A61K31/7056 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  A61K31/7105 ,  C07C215/10 ,  C07D209/08 ,  C07D215/227 ,  C07D217/24 ,  C07D249/18 ,  C07D265/18 ,  C07D277/68 ,  C07D279/16 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D495/04

摘要： Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.