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41. 发明申请

US20090131454A1 New compounds 067 失效
标题翻译：新化合物067
公开(公告)号：US20090131454A1
公开(公告)日：2009-05-21
申请号：US12285988
申请日：2008-10-17
申请人： Erwan Arzel , Louise Edwards , Methvin Isaac , Donald A. McLeod , Abdelmalik Slassi , Tao Xin
发明人： Erwan Arzel , Louise Edwards , Methvin Isaac , Donald A. McLeod , Abdelmalik Slassi , Tao Xin
IPC分类号： A61K31/497 , C07D401/14 , C07D403/14 , A61K31/506 , A61K31/4439
CPC分类号： C07D401/14 , C07D403/14
摘要： The present invention is directed to novel compounds, their use in therapy and pharmaceutical compositions comprising said novel compounds.
摘要翻译：本发明涉及新化合物，它们在治疗中的用途和包含所述新化合物的药物组合物。

42. 发明申请

US20050154027A1 Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists 失效
标题翻译：杂多环化合物及其作为代谢型谷氨酸受体拮抗剂的用途
公开(公告)号：US20050154027A1
公开(公告)日：2005-07-14
申请号：US10699563
申请日：2003-11-03
申请人： Bradford Wagenen , Thomas Stormann , Scott Moe , Susan Sheehan , Donald McLeod , Daryl Smith , Methvin Isaac , Abdelmalik Slassi
发明人： Bradford Wagenen , Thomas Stormann , Scott Moe , Susan Sheehan , Donald McLeod , Daryl Smith , Methvin Isaac , Abdelmalik Slassi
IPC分类号： C07D213/55 , C07D213/75 , C07D213/78 , C07D213/79 , C07D401/04 , C07D405/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D521/00 , A61K31/4439
CPC分类号： C07D213/75 , C07D213/55 , C07D213/78 , C07D213/79 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D405/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04
摘要： The present invention provides compounds and pharmaceutical compositions that act as antagonists at metabotropic glutamate receptors, and that are useful for treating neurological diseases and disorders. Methods of preparing the compounds also are disclosed.
摘要翻译：本发明提供了作为代谢型谷氨酸受体拮抗剂的化合物和药物组合物，其可用于治疗神经疾病和病症。还公开了制备化合物的方法。

43. 发明申请

US20070049578A1 Cinnamamide compounds as metabotropic glutamate receptor antagonists 审中-公开
标题翻译：肉桂酰胺化合物作为代谢型谷氨酸受体拮抗剂
公开(公告)号：US20070049578A1
公开(公告)日：2007-03-01
申请号：US11503182
申请日：2006-08-14
申请人： Louise Edwards , Methvin Isaac , Abdelmalik Slassi , Tao Xin , Peter Dove
发明人： Louise Edwards , Methvin Isaac , Abdelmalik Slassi , Tao Xin , Peter Dove
IPC分类号： A61K31/551 , A61K31/497 , A61K31/496 , C07D403/02
CPC分类号： C07D403/04 , C07D213/74 , C07D213/85 , C07D241/04 , C07D241/26 , C07D295/205 , C07D403/14 , C07D409/12 , C07F5/025
摘要： The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where R1, R2, R3, A, X, and n are defined in the description. The invention also includes pharmaceutical compositions and uses of, and processes of making the compounds, as well as methods of medical treatment of mGluR 5 mediated disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐或溶剂合物：其中R 1，R 2，R 3，A，X ，n在说明书中定义。本发明还包括药物组合物及其制备方法及其制备方法以及治疗mGluR5介导的病症的方法。

44. 发明申请

US20070037816A1 Bicyclic piperazines as metabotropic glutatmate receptor antagonists 审中-公开
标题翻译：双环哌嗪作为代谢型戊二酸受体拮抗剂
公开(公告)号：US20070037816A1
公开(公告)日：2007-02-15
申请号：US11498770
申请日：2006-08-04
申请人： Louise Edwards , Methvin Isaac , Abdelmalik Slassi , Guang-Ri Sun , Tao Xin , Alexander Minidis , Peter Dove
发明人： Louise Edwards , Methvin Isaac , Abdelmalik Slassi , Guang-Ri Sun , Tao Xin , Alexander Minidis , Peter Dove
IPC分类号： A61K31/498 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, A, Hy, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses of, and processes of making the compounds, as well as methods of medical treatment of mGluR5-mediated disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐或溶剂合物：其中Ar 1，A，Hy，R 1，m和n如说明书中所定义。本发明还包括药物组合物及其制备方法及其制备方法以及治疗mGluR5介导的病症的方法。

45. 发明授权

US06716837B1 Heterocyclic compounds for the treatment of migraine 失效
标题翻译：用于治疗偏头痛的杂环化合物
公开(公告)号：US06716837B1
公开(公告)日：2004-04-06
申请号：US09709579
申请日：2000-11-13
申请人： Louise Edwards , Methvin Isaac , Shawn Maddaford , Abdelmalik Slassi , Tao Xin
发明人： Louise Edwards , Methvin Isaac , Shawn Maddaford , Abdelmalik Slassi , Tao Xin
IPC分类号： C07D40112
CPC分类号： C07F7/0814 , C07D209/08 , C07D231/56 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either —NH— or —N═; is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c and d is at least 2 and the sum of e and f is at least 2; and salts and solvates thereof.
摘要翻译：本文描述了可用于治疗偏头痛的化合物，其具有以下通式：其中：W是CH基团或N原子; Z是N或C-R4; B和D独立地选自CH和N，条件是B和D中的至少一个是CH，进一步的条件是仅当W和Z都不是N时，B和D中的一个可以表示N; A是式II，III或IV的基团，使得A组含有至少1个N原子; NR 7是-NH-或-N =; 是单键或双键; 当是单键; 或者，当是双键时，一个C原子; Y是NH，N-烷基，N-苄基或CH2基团; U和V各自表示N原子或CH基团，条件是两者不能为N; a和b独立地为0或1; c是0至3的整数; d为1〜3的整数; e为1〜2的整数; f为0〜3的整数; g为3〜6的整数，h为2〜3的整数，使得c和d的和为至少2，e和f的和为至少2; 及其盐和溶剂合物。

46. 发明授权

US07960422B2 Pharmaceutically active compounds containing tetrazolyl and triazolyl rings 失效
标题翻译：含有四唑基和三唑基环的药物活性化合物
公开(公告)号：US07960422B2
公开(公告)日：2011-06-14
申请号：US12285988
申请日：2008-10-17
申请人： Erwan Arzel , Louise Edwards , Methvin Isaac , Donald A. McLeod , Abdelmalik Slassi , Tao Xin
发明人： Erwan Arzel , Louise Edwards , Methvin Isaac , Donald A. McLeod , Abdelmalik Slassi , Tao Xin
IPC分类号： A61K31/41
CPC分类号： C07D401/14 , C07D403/14
摘要： Compounds of formula (I) wherein R1 is as well as pharmaceutically acceptable salts, hydrates and/or enantiomers thereof are useful as compounds that exhibit activity at metabotropic glutamate receptors.
摘要翻译：其中R 1及其药学上可接受的盐，水合物和/或对映异构体的式（I）化合物可用作在代谢型谷氨酸受体上显示活性的化合物。

47. 发明申请

US20080312240A1 Bicyclic Piperazines as Metabotropic Glutatmate Receptor Antagonists 审中-公开
标题翻译：双环哌嗪作为代谢型谷氨酸受体拮抗剂
公开(公告)号：US20080312240A1
公开(公告)日：2008-12-18
申请号：US11997541
申请日：2006-08-04
申请人： Louise Edwards , Methvin Isaac , Abdelmalik Slassi , Guang-Ri Sun , Tao Xin , Alexander Minidis , Peter Dove
发明人： Louise Edwards , Methvin Isaac , Abdelmalik Slassi , Guang-Ri Sun , Tao Xin , Alexander Minidis , Peter Dove
IPC分类号： A61K31/4985 , C07D401/14 , C07D403/14 , A61P25/00 , A61P1/00 , C07D413/14 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, A, Hy, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses of, and processes of making the compounds, as well as methods of medical treatment of mGluR5-mediated disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐或溶剂化物：其中Ar1，A，Hy，R1，m和n如说明书中所定义。本发明还包括药物组合物及其制备方法及其制备方法以及治疗mGluR5介导的病症的方法。

48. 发明申请

US20070037820A1 Substituted piperazines as metabotropic glutamate receptor antagonists 审中-公开
标题翻译：取代的哌嗪作为代谢型谷氨酸受体拮抗剂
公开(公告)号：US20070037820A1
公开(公告)日：2007-02-15
申请号：US11498835
申请日：2006-08-04
申请人： Louise Edwards , Abdelmalik Slassi , Methvin Isaac , Donald McLeod
发明人： Louise Edwards , Abdelmalik Slassi , Methvin Isaac , Donald McLeod
IPC分类号： A61K31/497 , A61K31/496 , C07D413/14 , C07D413/02
CPC分类号： C07D413/12 , C07D261/08 , C07D401/12 , C07D403/12
摘要： The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, Ar2, Hy, L, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses thereof, processes for making the compounds, as well as methods for the medical treatment of mGluR5-mediated disorders.
摘要翻译：本发明涉及式I化合物或其药用盐或溶剂化物：其中Ar 1，Ar 2，Hy，L，R 1，，m和n如说明书中所定义。本发明还包括药物组合物及其用途，制备该化合物的方法，以及用于治疗mGluR5介导的病症的方法。

49. 发明授权

US07935703B2 Piperazines and piperidines as Mglur5 potentiators 失效
标题翻译：哌嗪和哌啶类作为Mglur5增效剂
公开(公告)号：US07935703B2
公开(公告)日：2011-05-03
申请号：US12160959
申请日：2007-01-05
申请人： Abdelmalik Slassi , Methvin Isaac , Jalaj Arora , Dean Brown
发明人： Abdelmalik Slassi , Methvin Isaac , Jalaj Arora , Dean Brown
IPC分类号： A61K31/497 , A61K31/4965 , A61K31/445 , A01N43/40 , C07D211/60 , C07D403/00 , C07D241/04 , C07D295/00 , C07D401/00
CPC分类号： C07D295/108 , C07D211/70 , C07D213/30 , C07D213/61 , C07D213/74 , C07D213/85 , C07D233/64 , C07D239/26 , C07D241/12 , C07D277/24 , C07D295/155 , C07D333/16 , C07D401/12 , C07D409/12
摘要： Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: wherein Ar1, Ar2, A, X, Y, m, n and R1, R2, R3, R4 and R5 are as described in the specification, processes for their preparation, pharmaceutical formulations comprising them and their use in therapy, particularly in the therapy of neurological and psychiatric disorders associated with glutamate dysfunction.
摘要翻译：式I化合物或其药学上可接受的盐或溶剂合物：其中Ar1，Ar2，A，X，Y，m，n和R1，R2，R3，R4和R5如说明书中所述，其制备方法，包括它们及其在治疗中的用途，特别是用于治疗与谷氨酸功能障碍相关的神经和精神障碍。

50. 发明申请

US20090023711A1 Piperazines and Piperidines as Mglur5 Potentiators 失效
标题翻译：哌嗪类和哌啶类作为Mglur5电位器
公开(公告)号：US20090023711A1
公开(公告)日：2009-01-22
申请号：US12160959
申请日：2007-01-05
申请人： Abdelmalik Slassi , Methvin Isaac , Jalaj Arora , Dean Brown
发明人： Abdelmalik Slassi , Methvin Isaac , Jalaj Arora , Dean Brown
IPC分类号： A61K31/551 , C07D241/04 , A61K31/495 , A61K31/496 , C07D243/08 , C07D401/14 , C07D211/06 , A61K31/451
CPC分类号： C07D295/108 , C07D211/70 , C07D213/30 , C07D213/61 , C07D213/74 , C07D213/85 , C07D233/64 , C07D239/26 , C07D241/12 , C07D277/24 , C07D295/155 , C07D333/16 , C07D401/12 , C07D409/12
摘要： Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: wherein Ar1, Ar2, A, X, Y, m, n and R1, R2, R3, R4 and R5 are as described in the specification, processes for their preparation, pharmaceutical formulations comprising them and their use in therapy, particularly in the therapy of neurological and psychiatric disorders associated with glutamate dysfunction.
摘要翻译：式I化合物或其药学上可接受的盐或溶剂合物：其中Ar1，Ar2，A，X，Y，m，n和R1，R2，R3，R4和R5如说明书中所述，其制备方法，包括它们及其在治疗中的用途，特别是用于治疗与谷氨酸功能障碍相关的神经和精神障碍。

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