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61. 发明授权

US07268127B2 Azaindoles having serotonin receptor affinity 失效
标题翻译：阿魏醇具有5-羟色胺受体亲和力
公开(公告)号：US07268127B2
公开(公告)日：2007-09-11
申请号：US11165122
申请日：2005-06-24
申请人： Louise Edwards , Abdelmalik Slassi , Ashok Tehim , Tao Xin
发明人： Louise Edwards , Abdelmalik Slassi , Ashok Tehim , Tao Xin
IPC分类号： A01N43/00 , A01N43/58 , A61K31/55 , C07D241/36 , C07D471/00
CPC分类号： C07D471/04 , C07D519/00
摘要： Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: Wherein A, B, D, E, R1 to R3 and n are described herein. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.
摘要翻译：本文描述的是对5-HT 6受体具有亲和力的化合物，其具有通式I：其中A，B，D，E，R 1至R _{3＆gt;和n。还描述了这些化合物作为药物用于治疗其中涉及5-HT 6受体的抑制的适应症的用途，例如精神分裂症。}

62. 发明授权

US6133287A Piperidine-indole compounds having 5-HT.sub.6 affinity 失效
标题翻译：具有5-HT 6亲和力的哌啶 - 吲哚化合物
公开(公告)号：US6133287A
公开(公告)日：2000-10-17
申请号：US46669
申请日：1998-03-24
申请人： Abdelmalik Slassi , Louise Edwards , Anne O'Brien , Tao Xin , Ashok Tehim
发明人： Abdelmalik Slassi , Louise Edwards , Anne O'Brien , Tao Xin , Ashok Tehim
IPC分类号： A61K31/454 , C07D401/04 , A61K31/445
CPC分类号： C07D401/04 , A61K31/454
摘要： Described herein are compounds with affinity for the 5-HT.sub.6 receptor, which have the general formula: wherein:R.sup.1 is selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.2 is selected from the group consisting of H, C.sub.1-4 alkyl and benzyl;-- -- -- represents a single or double bond;R.sup.3 is selected from the group consisting of COR.sup.5 and SO.sub.2 R.sup.5 ;R.sup.4a is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;R.sup.4b is selected from the group consisting of H, hydroxy, halo, C.sub.3-7 cycloalkyloxy, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, benzyloxy, phenoxy, trifluoromethyl, trifluoromethoxy and vinyl;R.sup.4c is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;R.sub.4d is selected from the group consisting of H, OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; andR.sup.5 is selected from the group consisting of phenyl, pyridyl, thienyl, quinolinyl and naphthyl which are optionally substituted with 1-4 substituents selected from C.sub.1-4 alkoxy, C.sub.1-4 alkyl, halo, nitro, trifluoromethyl, trifluoromethoxy, 1,2-methylenedioxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl and C.sub.1-4 alkylS--. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT.sub.6 receptor is implicated, such as schizophrenia.
摘要翻译：本文描述的是对5-HT 6受体具有亲和性的化合物，其具有以下通式：其中：R 1选自H和C 1-4烷基; R 2选自H，C 1-4烷基和苄基; - - - 表示单键或双键; R3选自COR5和SO2R5; R 4a选自H，OH，卤素，C 1-4烷基和C 1-4烷氧基; R4b选自H，羟基，卤素，C 3-7环烷氧基，C 1-4烷氧基，C 1-4烷基，苄氧基，苯氧基，三氟甲基，三氟甲氧基和乙烯基; R4c选自H，OH，卤素，C 1-4烷基和C 1-4烷氧基; R4d选自H，OH，卤素，C 1-4烷基和C 1-4烷氧基; 并且R 5选自苯基，吡啶基，噻吩基，喹啉基和萘基，其任选被1-4个选自C 1-4烷氧基，C 1-4烷基，卤素，硝基，三氟甲基，三氟甲氧基，1,2-亚甲二氧基，C 1-4烷基羰基，C 1-4烷氧基羰基和C 1-4烷基。还描述了这些化合物作为药物用于治疗其中涉及5-HT 6受体的抑制的适应症如精神分裂症的用途。

63. 发明授权

US08148394B2 Azaindoles having serotonin receptor affinity 失效
标题翻译：阿魏醇具有5-羟色胺受体亲和力
公开(公告)号：US08148394B2
公开(公告)日：2012-04-03
申请号：US11835325
申请日：2007-08-07
申请人： Louise Edwards , Abdelmalik Slassi , Ashok Tehim , Tao Xin
发明人： Louise Edwards , Abdelmalik Slassi , Ashok Tehim , Tao Xin
IPC分类号： A01N43/42 , A61K31/44 , C07D221/02
CPC分类号： C07D471/04 , C07D519/00
摘要： Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: wherein A, B, D, E, R1 to R3 and n are described herein. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.
摘要翻译：本文描述的是对5-HT 6受体具有亲和力的化合物，其具有通式I：其中A，B，D，E，R 1至R 3和n如本文所述。还描述了这些化合物作为药物用于治疗其中涉及5-HT 6受体的抑制的适应症如精神分裂症的用途。

64. 发明授权

US06686374B1 Azaindoles having serotonin receptor affinity 失效
标题翻译：阿魏醇具有5-羟色胺受体亲和力
公开(公告)号：US06686374B1
公开(公告)日：2004-02-03
申请号：US09636592
申请日：2000-08-10
申请人： Louise Edwards , Abdelmalik Slassi , Ashok Tehim , Tao Xin
发明人： Louise Edwards , Abdelmalik Slassi , Ashok Tehim , Tao Xin
IPC分类号： C07D40104
CPC分类号： C07D471/04 , C07D519/00
摘要： Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: wherein: R represents a group of Formula II or Formula III; one of A, B D or E is a N atom, the remainder being CH groups; R1 is selected from the group consisting of SO2Ar, C(O)Ar, CH2Ar and Ar; R2, R3 and R4 are independently selected from the group consisting of H and alkyl; represents a single or double bond, with the proviso that there is only one double bond in the ring at a time; n is an integer of from 1-3; Z is selected from the group consisting of C, CH and N, provided that when is a double bond, Z is C and when is a single bond, Z is selected from CH and N; Ar is an optionally substituted aryl group; with the proviso that when R is a group of Formula II, R1 is SO2Ar. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.
摘要翻译：本文描述的是对具有通式I的5-HT 6受体具有亲和性的化合物：其中：R代表式II或式III的基团; A，BD或E之一是N原子，其余是CH基 ; R 1选自SO 2 Ar，C（O）Ar，CH 2 Ar和Ar; R 2，R 3和R 4独立地选自H和烷基;表示单键或双键，条件是一次在环中只有一个双键; n是1-3的整数; Z选自C，CH和N，条件是当双键，Z是C并且是单一时键，Z选自CH和N; Ar是任选取代的芳基;条件是当R是式II的基团时，R 1是SO 2 Ar。还描述了这些化合物作为药物治疗适应症的用途，其中抑制的5-HT6受体是牵连的，如精神分裂症。

65. 发明授权

US06329390B1 5-Bicycloindole compounds 失效
标题翻译： 5-双环吲哚化合物
公开(公告)号：US06329390B1
公开(公告)日：2001-12-11
申请号：US09116946
申请日：1998-07-17
申请人： Abdelmalik Slassi , Jalaj Arora , Ashok Tehim
发明人： Abdelmalik Slassi , Jalaj Arora , Ashok Tehim
IPC分类号： A61K4342
CPC分类号： C07D471/04
摘要： Disclosed herein are compounds selective for a 5-HT1D receptor, the compounds having the general formula (I): Also disclosed is the use of these compounds as pharmaceuticals to treat indications where stimulation of a 5-HT1D receptor is indicated such as migrane.
摘要翻译：本文公开了对5-HT1D受体选择性的化合物，具有通式（I）的化合物：还公开了这些化合物作为药物用于治疗其中指示5-HT1D受体的刺激如migrane的适应症的用途。

66. 发明授权

US07868008B2 Substituted isoindolones and their use as metabotropic glutamate receptor potentiators 失效
标题翻译：取代的异吲哚酮及其作为代谢型谷氨酸受体增强剂的用途
公开(公告)号：US07868008B2
公开(公告)日：2011-01-11
申请号：US12063018
申请日：2006-02-15
申请人： Bradford Van Wagenen , Radhakrishnan Ukkiramapandian , Joshua Clayton , Ian Egle , James 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 Empfield , Methvin Isaac , Fupeng Ma , Abdelmalik Slassi , Gary Steelman , Rebecca Urbanek , Sally Walsh
IPC分类号： C07D209/46 , C07D401/06 , C07D401/14 , A61K31/4035 , A61K31/454
CPC分类号： C07D209/46 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/04 , C07D413/14
摘要： The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 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R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9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。

67. 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。

68. 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。

69. 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。

70. 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。

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