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21. 发明授权

US6103743A Unsaturated amino acid derivatives 失效
标题翻译：不饱和氨基酸衍生物
公开(公告)号：US6103743A
公开(公告)日：2000-08-15
申请号：US369686
申请日：1999-08-06
申请人： Stanley Charles Bell , Kathleen Da Silva , Allen Hopper , Methvin Isaac , Eric A. Meade , Vassil Ilya Ognyanov , Abdelmalik Slassi
发明人： Stanley Charles Bell , Kathleen Da Silva , Allen Hopper , Methvin Isaac , Eric A. Meade , Vassil Ilya Ognyanov , Abdelmalik Slassi
IPC分类号： A61K31/198 , A61K31/381 , A61K31/4406 , C07C229/36 , A61K31/44 , A61K31/195 , A61K31/21 , A61K31/24 , A61K31/38
CPC分类号： A61K31/381 , A61K31/198 , A61K31/4406 , C07C229/36
摘要： Described herein are compounds having the general formula: ##STR1## Ar.sub.1 and Ar.sub.2 are independently selected aryl groups, optionally substituted with substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkanoyl, aralkyl, aralkyloxy, halo, NO.sub.2, Ph, CF.sub.3, CN, OH, methylenedioxy, ethylenedioxy, SO.sub.2 NRR', NRR', CO.sub.2 R (where R and R' are independently selected from the group consisting of H and alkyl) and a second aryl group, which may be substituted as above;wherein any cycloalkyl or aryl substituent is linked to Ar.sub.1 or Ar.sub.2 by a bridging element which may be a single bond, a vinylene group, an ethynylene group, a Z group, a --Z--(CH.sub.2).sub.n -- group, a --(CH.sub.2).sub.n --Z-- group, or a --Z--(CH.sub.2).sub.n --Z-- group, where Z represents an O atom, a S atom, an NH group or an N-alkyl group, and n is an integer from 1 to 4;wherein Ar.sub.1 and Ar.sub.2 may be attached to the central atom to which they are connected by a single bond, an alkylene, alkenylene or alkynylene group;R is H, alkyl or the counter ion for a basic addition salt;R.sub.1 and R.sub.2 are independently selected from the group consisting of H, alkyl and benzyl;R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently selected from the group consisting of H and alkyl;and a stereoisomer, salt, solvate and hydrate thereof.Also described is the use of these compounds as pharmaceuticals for the treatment of diseases in which inhibition of glycine transport via the GlyT-2 transporter is indicated.
摘要翻译：本文描述的是具有以下通式的化合物：Ar 1和Ar 2是独立选择的芳基，任选地被选自烷基，环烷基，烷氧基，烷酰基，芳烷基，芳烷氧基，卤素，NO 2，Ph，CF 3，CN， OH，亚甲二氧基，亚乙二氧基，SO 2 NRR'，NRR'，CO 2 R（其中R和R'独立地选自H和烷基）和可以如上取代的第二芳基; 其中任何环烷基或芳基取代基通过可以是单键的桥连元件连接到Ar 1或Ar 2上，亚乙烯基，亚乙炔基，Z基，-Z-（CH 2）n - 基， - （CH 2））nZ-基或-Z-（CH2）nZ-基，其中Z表示O原子，S原子，NH基或N-烷基，n是1至4的整数; 其中Ar1和Ar2可以通过单键连接到它们连接的中心原子上，亚烷基，亚烯基或亚炔基; R为H，烷基或碱式加成盐的抗衡离子; R1和R2独立地选自H，烷基和苄基; R3，R4，R5和R6独立地选自H和烷基; 和其立体异构体，盐，溶剂化物和水合物。还描述了这些化合物作为药物用于治疗通过GlyT-2转运蛋白抑制甘氨酸转运的疾病的用途。

22. 发明授权

US08153638B2 Metabotropic glutamate-receptor-potentiating isoindolones 有权
标题翻译：代谢型谷氨酸受体增强异吲哚酮
公开(公告)号：US08153638B2
公开(公告)日：2012-04-10
申请号：US12861336
申请日：2010-08-23
申请人： Bradford Van Wagenen , Radhakrishnan Ukkiramapandian , Joshua Clayton , Ian Egle , James R. Empfield , Methvin Isaac , Fupeng Ma , Abdelmalik Slassi , Gary Steelman , Rebecca Urbanek , Sally Walsh
发明人： Bradford Van Wagenen , Radhakrishnan Ukkiramapandian , Joshua Clayton , Ian Egle , James R. Empfield , Methvin Isaac , Fupeng Ma , Abdelmalik Slassi , Gary Steelman , Rebecca Urbanek , Sally Walsh
IPC分类号： A61K31/497 , A61K31/4439 , A61K31/4035 , A61K31/427 , C07D403/14 , C07D403/02 , C07D401/02 , C07D209/44 , C07D417/02
CPC分类号： C07D209/34 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D417/04
摘要： Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.
摘要翻译：式I化合物：其中R1，R2，R3，R4，R5，R6，R7，R8，R9和n如说明书中所定义，制备化合物的方法，制备中使用的新中间体，含有化合物和化合物在治疗中的用途。

23. 发明申请

US20100280082A1 Metabotropic Glutamate Receptor Oxadiazole Ligands and Their Use as Potentiators 审中-公开
标题翻译：代谢型谷氨酸受体恶二唑配体及其用作电位器
公开(公告)号：US20100280082A1
公开(公告)日：2010-11-04
申请号：US12663362
申请日：2008-06-05
申请人： Joshua Clayton , Ian Egle , James Empfield , James Folmer , Methvin Isaac , Fupeng Ma , Abdelmalik Slassi
发明人： Joshua Clayton , Ian Egle , James Empfield , James Folmer , Methvin Isaac , Fupeng Ma , Abdelmalik Slassi
IPC分类号： A61K31/4245 , C07D413/14 , A61K31/496 , C07D487/08 , A61P25/00 , A61P29/00 , A61P25/16 , A61P25/14 , A61P25/30 , A61P25/28
CPC分类号： C07D413/14 , C07D413/04 , C07D487/08
摘要： Compounds of Formula (I) wherein R1, R2, R3 R4 and Q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.
摘要翻译：式（I）的化合物，其中R 1，R 2，R 3，R 4和Q如说明书中所述，药学上可接受的盐，制备方法，药物组合物及其使用方法。

24. 发明申请

US20100144710A1 Piperazine and Piperidine MGLUR5 Potentiators 审中-公开
标题翻译：哌嗪和哌啶MGLUR5电位器
公开(公告)号：US20100144710A1
公开(公告)日：2010-06-10
申请号：US12530351
申请日：2008-02-28
申请人： Jalaj Arora , Methvin Isaac , Abdelmalik Slassi , Louise Edwards , Satheesh Nair , Fupeng Ma
发明人： Jalaj Arora , Methvin Isaac , Abdelmalik Slassi , Louise Edwards , Satheesh Nair , Fupeng Ma
IPC分类号： A61K31/496 , C07D401/04 , C07D403/04 , A61K31/551 , A61P25/18 , A61P25/00
CPC分类号： C07D213/61 , C07D213/84 , C07D213/85 , C07D241/24 , C07D295/192 , C07D401/12 , C07D405/12 , C07D417/12
摘要： Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof, wherein A, B, D, Ar1, Ar2, R2, R3, R4, a, m and n are defined in the specification, methods for the use thereof, processes for making and pharmaceutical compositions containing the same.
摘要翻译：式I化合物或其药学上可接受的盐或溶剂化物，其中A，B，D，Ar1，Ar2，R2，R3，R4，a，m和n在本说明书中定义，其使用方法，制备方法和含有该组合物的药物组合物。

25. 发明授权

US07691892B2 Tetrazole compounds and their use as metabotropic glutamate receptor antagonists 失效
标题翻译：四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：US07691892B2
公开(公告)日：2010-04-06
申请号：US11060463
申请日：2005-02-18
申请人： Martin Johansson , Alexander Minidis , Karin Staaf , David Wensbo , Donald McLeod , Louise Edwards , Methvin Isaac , Anne O'Brien , Abdelmalik Slassi , Tao Xin , Tomislav Stefanac
发明人： Martin Johansson , Alexander Minidis , Karin Staaf , David Wensbo , Donald McLeod , Louise Edwards , Methvin Isaac , Anne O'Brien , Abdelmalik Slassi , Tao Xin , Tomislav Stefanac
IPC分类号： A61K31/41 , C07D257/04
CPC分类号： C07D257/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D471/04 , C07D487/04
摘要： The present invention relates to new compounds of formula I, wherein P, Q, X1, X2, X3, X4, R1, R2, m and p, are as defined as in formula I, or, salts, solvates or solvated salts 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 4，R 1，R 2，m和p如式I中所定义，或其盐，溶剂合物或溶剂化盐，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和所述化合物在治疗中的用途。

26. 发明授权

US07678796B2 MGluR5 modulators I 失效
标题翻译： MGluR5调制器
公开(公告)号：US07678796B2
公开(公告)日：2010-03-16
申请号：US11790417
申请日：2007-04-25
申请人： Andreas Wallberg , Karolina Nilsson , Björn Holm , Mats Nagard , Kenneth Granberg , Abdelmalik Slassi , Louise Edwards , Methvin Isaac , Tao Xin , Tomislav Stefanac
发明人： Andreas Wallberg , Karolina Nilsson , Björn Holm , Mats Nagard , Kenneth Granberg , Abdelmalik Slassi , Louise Edwards , Methvin Isaac , Tao Xin , Tomislav Stefanac
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/513 , A61K31/497 , A61K31/496 , A61K31/501 , C07D413/02 , C07D417/14 , A61P1/00
CPC分类号： C07D413/14 , C07D401/14 , C07D403/14
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。

27. 发明申请

US20100016403A1 USE OF D-SERINE DERIVATIVES FOR THE TREATMENT OF ANXIETY DISORDERS 失效
标题翻译：使用D-丝氨酸衍生物治疗恶心病
公开(公告)号：US20100016403A1
公开(公告)日：2010-01-21
申请号：US12519041
申请日：2007-12-14
申请人： Guy Higgins , Abdelmalik Slassi , Methvin Isaac
发明人： Guy Higgins , Abdelmalik Slassi , Methvin Isaac
IPC分类号： A61K31/24 , C07C229/34 , C07C237/20 , C07D333/22 , A61K31/197 , A61K31/165 , A61K31/381 , A61P25/22
CPC分类号： C07D333/22 , A61K31/165 , A61K31/381 , C07C233/11 , C07C233/15 , C07C233/51 , C07C271/22 , C07C311/46
摘要： Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias. wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R8; R1 is chosen from: alkyl or haloalkyl; R2 is chosen from: H, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7; R3, R4 and R5 are independently chosen from: H or alkyl; R6 and R7 are independently chosen from: H or alkyl; and R8 is chosen from: OH, CN, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7.
摘要翻译：式I化合物可用于治疗焦虑症，例如广泛性焦虑症（GAD），恐慌发作，创伤后应激障碍（PTSD），强迫症（OCD）和社交恐怖症。其中：A选自：芳基或杂芳基，A任选被至多5个独立选择的基团取代; R8; R1选自：烷基或卤代烷基; R 2选自：H，C（O）R 6，C（O）OR 6，SO 2 R 6或C（O）NR 6 R 7; R3，R4和R5独立地选自：H或烷基; R6和R7独立地选自：H或烷基; 并且R 8选自：OH，CN，卤素，烷基，烷氧基，卤代烷基，卤代烷氧基，C（O）R 6，C（O）OR 6，SO 2 R 6或C（O）NR 6 R 7。

28. 发明申请

US20090192169A1 Bicyclic Benzimidazole Compounds and Their Use as Metabotropic Glutamate Receptor Potentiators 审中-公开
标题翻译：双环苯并咪唑化合物及其用作代谢型谷氨酸受体电位器
公开(公告)号：US20090192169A1
公开(公告)日：2009-07-30
申请号：US12225310
申请日：2007-03-29
申请人： Ian Egle , Methvin Isaac , Rebecca Urbanek , Frances M. McLaren , Sally B. Walsh , Gary B. Steelman , Dean G. Brown , David Nugiel , Deborah W. Chen , Abdelmalik Slassi , Fupeng Ma
发明人： Ian Egle , Methvin Isaac , Rebecca Urbanek , Frances M. McLaren , Sally B. Walsh , Gary B. Steelman , Dean G. Brown , David Nugiel , Deborah W. Chen , Abdelmalik Slassi , Fupeng Ma
IPC分类号： A61K31/454 , C07D401/06 , C07D403/06 , A61P35/00 , A61K31/496 , A61K31/4184
CPC分类号： C07D401/06 , C07D235/06 , C07D235/14 , C07D401/14 , C07D403/06 , C07D403/12
摘要： Compounds of Formula I: wherein A, B, D, L, R1, R2, R3, R4, m, 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：式I的化合物：其中A，B，D，L，R 1，R 2，R 3，R 4，m和n如说明书中对式I所定义。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。

29. 发明申请

US20090111824A1 AMIDE LINKED HETEROAROMATIC DERIVATIVES AS MODULATORS OF MGLUR5 审中-公开
标题翻译：作为MGLUR5的调节剂的酰胺偶联异构体衍生物
公开(公告)号：US20090111824A1
公开(公告)日：2009-04-30
申请号：US12258169
申请日：2008-10-24
申请人： Emma Bratt , Kenneth Granberg , Methvin Isaac , Mats Nagard , Abdelmalik Slassi
发明人： Emma Bratt , Kenneth Granberg , Methvin Isaac , Mats Nagard , Abdelmalik Slassi
IPC分类号： A61K31/501 , C07D403/14 , C07D413/14 , C07D403/04 , A61K31/4439
CPC分类号： C07D403/14 , C07D403/04 , 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。

30. 发明授权

US07476684B2 Compounds for the treatment of neurological, psychiatric or pain disorders 失效
标题翻译：用于治疗神经，精神或疼痛障碍的化合物
公开(公告)号：US07476684B2
公开(公告)日：2009-01-13
申请号：US11523717
申请日：2006-09-20
申请人： Alexander Minidis , David Wensbo , Methvin Isaac , Abdelmalik Slassi , Jalaj Arora , Tao Xin , Louise Edwards , Caroline Eriksson , Veronica Profir , Per-Olov Bergstrom
发明人： Alexander Minidis , David Wensbo , Methvin Isaac , Abdelmalik Slassi , Jalaj Arora , Tao Xin , Louise Edwards , Caroline Eriksson , Veronica Profir , Per-Olov Bergstrom
IPC分类号： A61K31/4439 , C07D413/14
CPC分类号： C07D413/14
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。

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