公开(公告)号：US20050182088A1

公开(公告)日：2005-08-18

申请号：US10500516

申请日：2002-07-29

Applicant: Peter Astles ,  Stephen Baker ,  Rowena Cube ,  Jose Martinez-Perez ,  Ana Mateo Herranz ,  Jean Vernier ,  Colin Dell ,  Sonia Gutierrez ,  Lourdes Prieto ,  Martine Keenan ,  Adam Sanderson ,  Colin Smith

Inventor： Peter Astles ,  Stephen Baker ,  Rowena Cube ,  Jose Martinez-Perez ,  Ana Mateo Herranz ,  Jean Vernier ,  Colin Dell ,  Sonia Gutierrez ,  Lourdes Prieto ,  Martine Keenan ,  Adam Sanderson ,  Colin Smith

IPC: A61K31/46 ,  A61K31/55 ,  C07D451/04 ,  C07D451/14 ,  C07D471/02 ,  A61K31/4745 ,  C07D453/04

CPC classification number: A61K31/46 ,  A61K31/55 ,  C07D451/04 ,  C07D451/14

Abstract: The present invention relates to compounds that modulate neurotransmission by promoting the release of neurotransmitters such as acetylcholine, dopamine and norepinephrine. More particularly, the present invention relates to thio-bridged aryl compounds that are capable of modulating acetylcholine receptors and pharmaceutical compositions comprising such compounds. The compounds disclosed are useful for the treatment of dysfunctions of the central and autonomic nervous systems.

Abstract translation: 本发明涉及通过促进神经递质如乙酰胆碱，多巴胺和去甲肾上腺素的释放来调节神经传递的化合物。 更具体地，本发明涉及能够调节乙酰胆碱受体的硫代桥连芳基化合物和包含这些化合物的药物组合物。 所公开的化合物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：US20080312286A1

公开(公告)日：2008-12-18

申请号：US11658490

申请日：2005-07-26

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

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

IPC: 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 classification number: C07C233/91 ,  C07C59/90 ,  C07C65/40 ,  C07C311/51 ,  C07C2601/08 ,  C07C2602/08 ,  C07D257/04 ,  C07D307/79 ,  C07D401/04

Abstract: 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.

Abstract translation: 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：US20050288346A1

公开(公告)日：2005-12-29

申请号：US10524704

申请日：2003-08-22

Applicant: Rowena Cube ,  Anthony Pinkerton ,  Jean-Michel Vernier ,  Xiumin Zhao

Inventor： Rowena Cube ,  Anthony Pinkerton ,  Jean-Michel Vernier ,  Xiumin Zhao

IPC: A61K31/41 ,  A61P25/00 ,  C07D257/02 ,  C07D257/04

CPC classification number: C07D257/04

Abstract: 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.

Abstract translation: 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：US20080167322A1

公开(公告)日：2008-07-10

申请号：US11884325

申请日：2006-02-14

Applicant: Anthony B. Pinkerton ,  Rowena Cube ,  John Hutchinson ,  Dehua Huang ,  Jean-Michel Vernier ,  Dong-Ming Shen

Inventor： Anthony B. Pinkerton ,  Rowena Cube ,  John Hutchinson ,  Dehua Huang ,  Jean-Michel Vernier ,  Dong-Ming Shen

IPC: A61K31/497 ,  C07D231/10 ,  A61K31/4155 ,  A61P19/02 ,  C07D401/02 ,  A61K31/4439

CPC classification number: C07D231/38 ,  C07D231/12 ,  C07D231/22 ,  C07D401/12 ,  C07D403/12

Abstract: Substituted pyrazole compounds 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.

Abstract translation: 取代的吡唑化合物，由式I表示：用于调节CCR-2趋化因子受体以预防或治疗炎性和免疫调节性疾病和疾病，过敏性疾病，特应性疾病，包括过敏性鼻炎，皮炎，结膜炎和哮喘的化合物，以及 作为自身免疫性病变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：US20080096935A1

公开(公告)日：2008-04-24

申请号：US11666072

申请日：2005-10-21

Applicant: Anthony Pinkerton ,  Jean-Michel Vernier ,  Rowena Cube ,  John Hutchinson

Inventor： Anthony Pinkerton ,  Jean-Michel Vernier ,  Rowena Cube ,  John Hutchinson

IPC: A61K31/4412 ,  A61K31/4196 ,  A61K31/4152

CPC classification number: C07D213/30 ,  C07D207/32 ,  C07D213/65 ,  C07D213/70 ,  C07D231/12 ,  C07D235/18 ,  C07D249/08

Abstract: 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.

Abstract translation: 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：US20070054912A1

公开(公告)日：2007-03-08

申请号：US11595149

申请日：2006-11-09

Applicant: Peter Astles ,  Stephen Baker ,  Rowena Cube ,  Jose Martinez-Perez ,  Ana Mateo Herranz ,  Jean Vernier ,  Colin Dell ,  Sonia Gutierrez ,  Lourdes Prieto ,  Martine Keenan ,  Adam Sanderson ,  Colin Smith

Inventor： Peter Astles ,  Stephen Baker ,  Rowena Cube ,  Jose Martinez-Perez ,  Ana Mateo Herranz ,  Jean Vernier ,  Colin Dell ,  Sonia Gutierrez ,  Lourdes Prieto ,  Martine Keenan ,  Adam Sanderson ,  Colin Smith

IPC: A61K31/53 ,  C07D471/02 ,  A61K31/519 ,  A61K31/498 ,  A61K31/4745

CPC classification number: A61K31/46 ,  A61K31/55 ,  C07D451/04 ,  C07D451/14

Abstract: Compounds comprising an aza-bicyclic portion and an aromatic portion linked via an optionally oxidized sulphur atom are disclosed. The compounds disclosed are useful for the treatment of dysfunctions of the central and autonomic nervous systems.

Abstract translation: 公开了包含氮杂双环部分和通过任选氧化的硫原子连接的芳族部分的化合物。 所公开的化合物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：US20050065340A1

公开(公告)日：2005-03-24

申请号：US10497452

申请日：2002-11-26

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

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

IPC: 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 classification number: C07D263/57 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D413/10

Abstract: 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.

Abstract translation: 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。