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51. 发明申请

US20060019997A1 Triazole compounds and their use as metabotropic glutamate receptor antagonists 审中-公开
标题翻译：三唑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：US20060019997A1
公开(公告)日：2006-01-26
申请号：US11060366
申请日：2005-02-18
申请人： Louise Edwards , Methvin Isaac , Martin Johansson , Johan Malmberg , Alexander Minidis , Karin Staaf , Abdelmalik Slassi , David Wensbo , Tomislav Stefanac , Tao Xin
发明人： Louise Edwards , Methvin Isaac , Martin Johansson , Johan Malmberg , Alexander Minidis , Karin Staaf , Abdelmalik Slassi , David Wensbo , Tomislav Stefanac , Tao Xin
IPC分类号： A61K31/4439 , A61K31/4196 , A61K31/4245 , C07D413/14 , C07D403/14
CPC分类号： C07D401/12 , C07D231/12 , C07D231/14 , C07D249/06 , C07D249/08 , C07D249/10 , C07D249/12 , C07D401/04 , C07D401/14 , C07D403/12 , C07D413/14
摘要： The present invention relates to new compounds of formula I, wherein P, Q, X1, X2, X3, X4 X7, X8, R1, R2, R3, m, n, and p are as defined as in formula I, or salts, or hydrates thereof, processes for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
摘要翻译：本发明涉及新的式I化合物，其中P，Q，X 1，X 2，X 3，X 3， 4个X 7，X 8，R 1，R 2，R 3， m，n和p如式I所定义，或其盐或水合物，其制备方法及其制备中使用的新中间体，含有所述化合物的药物组合物以及所述化合物的用途化合物治疗。

52. 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。

53. 发明申请

US20080312246A1 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：US20080312246A1
公开(公告)日：2008-12-18
申请号：US11997444
申请日：2006-08-04
申请人： Louise Edwards , Abdelmalik Slassi , Methvin Isaac , Donald Mcleod , Tao Xin
发明人： Louise Edwards , Abdelmalik Slassi , Methvin Isaac , Donald Mcleod , Tao Xin
IPC分类号： A61K31/496 , A61P25/00 , A61P1/00 , C07D413/14 , A61K31/497
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化合物或其药学上可接受的盐或溶剂合物：其中Ar1，Ar2，Hy，L，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。

54. 发明申请

US20070255061A1 5-Fluoro-, Chloro-and Cyano-Pyridin-2-Yl-Tetrazoles as Ligands of the Metabotropic Glutamate Receptor-5 审中-公开
标题翻译： 5-氟 - ，氯 - 和氰基 - 吡啶-2-基 - 四唑作为代谢型谷氨酸受体-5的配体
公开(公告)号：US20070255061A1
公开(公告)日：2007-11-01
申请号：US10582051
申请日：2004-12-13
申请人： David Wensbo , Louise Edwards , Methvin Isaac , Donald McLeod , Abdelmalik Slassi , Tao Xin , Thomas Stormann
发明人： David Wensbo , Louise Edwards , Methvin Isaac , Donald McLeod , Abdelmalik Slassi , Tao Xin , Thomas Stormann
IPC分类号： A61K31/4439 , A61K31/41 , A61P1/00 , A61P25/00 , A61P25/18 , C07D257/04 , C07D401/04 , C12N5/06 , C12N5/08
CPC分类号： C07D213/84 , C07D401/04
摘要： The present invention relates to new compounds of formula I, wherein Z, Q, X1, X2, R1 and R2, are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
摘要翻译：本发明涉及新的式I化合物，其中Z，Q，X 1，X 2，R 1和R 2如式I中所定义，或其盐，溶剂合物或溶剂化盐，其制备方法，含有所述化合物和所述化合物在治疗中的用途。

55. 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。

56. 发明授权

US07576077B2 Fused heterocyclic compounds and their use as metabotropic glutamate receptor antagonists 失效
标题翻译：稠合杂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：US07576077B2
公开(公告)日：2009-08-18
申请号：US11060560
申请日：2005-02-18
申请人： David Wensbo , Martin Johansson , Alexander Minidis , Karin Staaf , Annika Kers , Louise Edwards , Methvin Isaac , Tom Stefanac , Abdelmalik Slassi , Don McLeod , Tao Xin
发明人： David Wensbo , Martin Johansson , Alexander Minidis , Karin Staaf , Annika Kers , Louise Edwards , Methvin Isaac , Tom Stefanac , Abdelmalik Slassi , Don McLeod , Tao Xin
IPC分类号： A61P25/00 , C07D487/02 , A61K31/55
CPC分类号： C07D211/22 , C07D223/08 , C07D241/18 , C07D273/02 , C07D403/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： The present invention is directed to compounds of formula I: wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, R1, R2, R3, R4, and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
摘要翻译：本发明涉及式I化合物：其中X1，X2，X3，X4，X5，X6，X7，X8，X9，X10，R1，R2，R3，R4和n如描述。本发明还涉及制备化合物的方法和用于制备中的新中间体，含有该化合物的药物组合物，以及该化合物在治疗中的用途。

57. 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。

58. 发明申请

US20070259923A1 MGluR5 modulators IV 审中-公开
标题翻译： MGluR5调节剂
公开(公告)号：US20070259923A1
公开(公告)日：2007-11-08
申请号：US11790428
申请日：2007-04-25
申请人： Methvin Isaac , Abdelmalik Slassi , Louise Edwards , Tao Xin , Andreas Wallberg , Tomislav Stefanac
发明人： Methvin Isaac , Abdelmalik Slassi , Louise Edwards , Tao Xin , Andreas Wallberg , Tomislav Stefanac
IPC分类号： A61K31/4439 , C07D413/14
CPC分类号： C07D207/16 , C07D207/08 , C07D207/09 , C07D213/78 , C07D213/79 , C07D413/04 , C07D413/14
摘要： The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
摘要翻译：本发明涉及新化合物，其制备方法，其在治疗中的应用和包含新化合物的药物组合物。

59. 发明申请

US20070259895A1 MGluR5 modulators VI 审中-公开
标题翻译： MGluR5调制剂VI
公开(公告)号：US20070259895A1
公开(公告)日：2007-11-08
申请号：US11790424
申请日：2007-04-25
申请人： Methvin Isaac , Abdelmalik Slassi , Louise Edwards , Tao Xin , Tomislav Stefanac , Peter Dove , Mats Nagard
发明人： Methvin Isaac , Abdelmalik Slassi , Louise Edwards , Tao Xin , Tomislav Stefanac , Peter Dove , Mats Nagard
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
摘要翻译：本发明涉及新化合物，其制备方法，其在治疗中的应用和包含新化合物的药物组合物。

60. 发明申请

US20070259860A1 MGluR5 modulators V 审中-公开
标题翻译： MGluR5调制器
公开(公告)号：US20070259860A1
公开(公告)日：2007-11-08
申请号：US11790429
申请日：2007-04-25
申请人： Andreas Wallberg , Karolina Nilsson , Kenneth Granberg , Saswati Ghosal , Abdelmalik Slassi , Louise Edwards , Methvin Isaac , Tao Xin , Tomislav Stefanac , Peter Dove
发明人： Andreas Wallberg , Karolina Nilsson , Kenneth Granberg , Saswati Ghosal , Abdelmalik Slassi , Louise Edwards , Methvin Isaac , Tao Xin , Tomislav Stefanac , Peter Dove
IPC分类号： A61K31/5513 , A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
摘要翻译：本发明涉及新化合物，其制备方法，其在治疗中的应用和包含新化合物的药物组合物。

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