-
公开(公告)号:US20050288346A1
公开(公告)日:2005-12-29
申请号:US10524704
申请日:2003-08-22
IPC分类号: A61K31/41 , A61P25/00 , C07D257/02 , C07D257/04
CPC分类号: C07D257/04
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: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:US20110230526A1
公开(公告)日:2011-09-22
申请号:US13016304
申请日:2011-01-28
申请人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号: A61K31/4439 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/28
CPC分类号: C07D417/06 , C07D417/14 , C07D471/04
摘要: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译: 由于它们在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质,鉴定了具有药物性质特征的独特系列化合物。 具体地说,通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择,其中环被选定的取代基取代,得到 具有优异药物性质的化合物。 本发明包括这些杂环化合物的药学上可接受的盐形式,特别是氯化物盐和三氟乙酸盐。
-
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。
-
5.
公开(公告)号:US20120289696A1
公开(公告)日:2012-11-15
申请号:US13558537
申请日:2012-07-26
申请人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号: C07D417/06 , C07D417/14 , C07D471/04
CPC分类号: C07D417/06 , C07D417/14 , C07D471/04
摘要: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译: 由于在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质,鉴定了具有药物性质特征的独特系列化合物。 具体地说,通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择,其中环被选定的取代基取代,得到 具有优异药物性质的化合物。 本发明包括这些杂环化合物的药学上可接受的盐形式,特别是氯化物盐和三氟乙酸盐。
-
公开(公告)号:US07879882B2
公开(公告)日:2011-02-01
申请号:US11664902
申请日:2005-10-06
申请人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号: A61P25/00 , A61K31/44 , C07D417/14
CPC分类号: C07D417/06 , C07D417/14 , C07D471/04
摘要: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译: 由于它们在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质,鉴定了具有药物性质特征的独特系列化合物。 具体地说,通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择,其中环被选定的取代基取代,得到 具有优异药物性质的化合物。 本发明包括这些杂环化合物的药学上可接受的盐形式,特别是氯化物盐和三氟乙酸盐。
-
公开(公告)号:US08609852B2
公开(公告)日:2013-12-17
申请号:US13558537
申请日:2012-07-26
申请人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号: A61P25/00 , A61K31/55 , A61K31/54 , A61K31/505 , A61K31/44 , A61K31/47 , A61K31/445 , C07D401/00 , C07D403/00 , C07D417/00 , C07D239/02 , C07D211/00
CPC分类号: C07D417/06 , C07D417/14 , C07D471/04
摘要: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译: 由于在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质,鉴定了具有药物性质特征的独特系列化合物。 具体地说,通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择,其中环被选定的取代基取代,得到 具有优异药物性质的化合物。 本发明包括这些杂环化合物的药学上可接受的盐形式,特别是氯化物盐和三氟乙酸盐。
-
公开(公告)号:US08242143B2
公开(公告)日:2012-08-14
申请号:US13016304
申请日:2011-01-28
申请人: Nicholas D. Cosford , Thomas J. Seiders , Joseph Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人: Nicholas D. Cosford , Thomas J. Seiders , Joseph Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号: A61P25/00 , A61K31/44 , C07D417/00
CPC分类号: C07D417/06 , C07D417/14 , C07D471/04
摘要: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译: 由于在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质,鉴定了具有药物性质特征的独特系列化合物。 具体地说,通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择,其中环被选定的取代基取代,得到 具有优异药物性质的化合物。 本发明包括这些杂环化合物的药学上可接受的盐形式,特别是氯化物盐和三氟乙酸盐。
-
公开(公告)号:US20090203903A1
公开(公告)日:2009-08-13
申请号:US11664902
申请日:2005-10-06
申请人: Nicholas D. Cosford , Thomas J. Seiders , Joseph Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人: Nicholas D. Cosford , Thomas J. Seiders , Joseph Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号: C07D417/14 , C07D417/06
CPC分类号: C07D417/06 , C07D417/14 , C07D471/04
摘要: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译: 由于在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质,鉴定了具有药物性质特征的独特系列化合物。 具体地说,通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择,其中环被选定的取代基取代,得到 具有优异药物性质的化合物。 本发明包括这些杂环化合物的药学上可接受的盐形式,特别是氯化物盐和三氟乙酸盐。
-
-
-
-
-
-
-
-