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71. 发明授权

US5824676A 5-HT2 receptor ligands 失效
标题翻译： 5-HT2受体配体
公开(公告)号：US5824676A
公开(公告)日：1998-10-20
申请号：US763255
申请日：1996-12-10
申请人： Ashok Tehim , Jian-min Fu , Sumanas Rakhit
发明人： Ashok Tehim , Jian-min Fu , Sumanas Rakhit
IPC分类号： C07D243/38 , C07D267/20 , A61K31/55 , C07D403/04 , C07D413/04 , C07D417/04
CPC分类号： C07D243/38 , C07D267/20
摘要： Described herein are 5-HT2 receptor-selective compounds of Formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings; X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO; X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--; R.sub.1 is C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; and R.sub.2, R.sub.3 and R.sub.4 are independently selected from H and R.sub.1 ; and acid addition salts, solvates and hydrates thereof. Their use as ligands for serotonin 5-HT2 receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the 5-HT2 receptor is implicated, such as hypertension, thrombosis, migraine, vasospasm, ischemia, depression, anxiety, schizophrenia, sleep disorders and appetite disorders is also described.
摘要翻译：本文描述的是式I的5-HT 2受体选择性化合物：其中：A和B独立地选择，任选取代的饱和或不饱和的5-或6-元，均 - 或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，所以; X2-选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; R1是任选被选自OH，卤素，C 1-4烷基和C 1-4烷氧基的取代基取代的C 1-6烷基; 并且R 2，R 3和R 4独立地选自H和R 1; 及其酸加成盐，溶剂化物和水合物。它们用作5-羟色胺5-HT2受体鉴定和药物筛选程序的配体，以及用作治疗其中涉及5-HT2受体的适应症的药物，例如高血压，血栓形成，偏头痛，血管痉挛，局部缺血，抑郁，焦虑，还描述了精神分裂症，睡眠障碍和食欲障碍。

72. 发明授权

US5602120A Benzyl-substituted compounds having dopamine receptor affinity 失效
标题翻译：具有多巴胺受体亲和力的苄基取代的化合物
公开(公告)号：US5602120A
公开(公告)日：1997-02-11
申请号：US354766
申请日：1994-12-12
申请人： Jian-Min Fu , Ashok Tehim , Robert A. Kirby
发明人： Jian-Min Fu , Ashok Tehim , Robert A. Kirby
IPC分类号： C07D267/20 , A61K31/55 , C07D413/04 , C07D417/04
CPC分类号： C07D267/20
摘要： Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from CH and N;Z is cyanoR.sub.1 represents C.sub.1-4 alkyl;m is 0, 1, 2 or 3;n is 0, 1 or 2;q is 1 or 2; andD is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是具有以下通式的D4受体选择性化合物：其中：A和B独立选择，任选取代的饱和或不饱和的5-或6-元，杂环或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，所以; X2 - - - 选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; Y选自CH和N; Z是氰基，R 1表示C 1-4烷基; m为0,1,2或3; n为0,1或2; q为1或2; 且D为5,6或7元饱和或不饱和的均聚或杂环; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗其中涉及D4受体的适应症的药物，例如精神分裂症。

73. 发明授权

US09303027B2 Kappa opioid receptor agonists 有权
标题翻译：卡帕阿片受体激动剂
公开(公告)号：US09303027B2
公开(公告)日：2016-04-05
申请号：US13811020
申请日：2011-07-19
申请人： Pradip Kumar Sasmal , Vamsee Krishna Chintakunta , Vijay Potluri , Ish Kumar Khanna , Ashok Tehim , Mahaboobi Jaleel , Thomas Hogberg , Oystein Rist , Lisbeth Elster , Thomas Michael Frimurer , Lars-Ole Gerlach
发明人： Pradip Kumar Sasmal , Vamsee Krishna Chintakunta , Vijay Potluri , Ish Kumar Khanna , Ashok Tehim , Mahaboobi Jaleel , Thomas Hogberg , Oystein Rist , Lisbeth Elster , Thomas Michael Frimurer , Lars-Ole Gerlach
IPC分类号： C07D419/12 , C07D207/09 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D207/12 , C07D209/34 , C07D213/76 , C07D215/12 , C07D215/227 , C07D231/56 , C07D249/18 , C07D261/20 , C07D263/56 , C07D263/58 , C07D275/06 , C07D277/30 , C07D279/02 , C07D295/13
CPC分类号： C07D419/12 , C07D207/09 , C07D207/12 , C07D209/34 , C07D213/76 , C07D215/12 , C07D215/227 , C07D231/56 , C07D249/18 , C07D261/20 , C07D263/56 , C07D263/58 , C07D275/06 , C07D277/30 , C07D279/02 , C07D295/13 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
摘要翻译：本发明涉及一系列具有通式（I）的取代的化合物，包括其立体异构体和/或其药学上可接受的盐。（I）其中A，m，R 1，R 2，R 3，R 4如本文所定义。本发明还涉及制备这些化合物包括中间体的方法。本发明的化合物在κ（αKα）阿片受体（KOR）位点是有效的。因此，本发明的化合物可用作药物，特别是用于治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性疼痛以及相关疾病，特别是周边功能在CNS。

74. 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。

75. 发明授权

US07700631B2 Phosphodiesterase 4 inhibitors 失效
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：US07700631B2
公开(公告)日：2010-04-20
申请号：US11378615
申请日：2006-03-20
申请人： Richard A. Schumacher , Elizabeth Doorly Graham , Allen T. Hopper , Ashok Tehim
发明人： Richard A. Schumacher , Elizabeth Doorly Graham , Allen T. Hopper , Ashok Tehim
IPC分类号： C07D213/02 , C07D419/02 , A61K31/44
CPC分类号： C07D213/89 , C07D401/06 , C07D401/12 , C07D405/12
摘要： PDE4 inhibition is achieved by novel nitroxide compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formulas I-III: wherein A, B, D, R1, R2, R3, R7, R8, R9, R10 and R6 are as defined herein.
摘要翻译：通过新的硝基氧化合物，例如N-取代的苯胺和二苯胺类似物来实现PDE4抑制。本发明的化合物是式I-III：其中A，B，D，R 1，R 2，R 3，R 7，R 8，R 9，R 10和R 6如本文所定义。

76. 发明申请

US20100010020A1 PHOSPHODIESTERASE 4 INHIBITORS 审中-公开
公开(公告)号：US20100010020A1
公开(公告)日：2010-01-14
申请号：US12564636
申请日：2009-09-22
申请人： Ruiping LIU , Hans-Jurgen Ernst Hess , Allen Hopper , Ashok Tehim , Yujing Rong
发明人： Ruiping LIU , Hans-Jurgen Ernst Hess , Allen Hopper , Ashok Tehim , Yujing Rong
IPC分类号： A61K31/52 , A61P25/28
CPC分类号： C07D473/40
摘要： PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.

77. 发明申请

US20100004236A1 PHOSPHODIESTERASE 4 INHIBITORS 审中-公开
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：US20100004236A1
公开(公告)日：2010-01-07
申请号：US12393634
申请日：2009-02-26
申请人： Ashok Tehim , Allen T. Hopper , Ruiping Liu , Hans-Juregen Ernst Hess , Yajing Rong
发明人： Ashok Tehim , Allen T. Hopper , Ruiping Liu , Hans-Juregen Ernst Hess , Yajing Rong
IPC分类号： A61K31/52 , C07D473/34 , A61P25/28 , A61P25/18 , A61P25/36 , A61P25/24 , A61P11/00 , A61P37/08 , A61P29/00 , A61P25/16 , A61P9/00 , A61P31/18 , C07D413/14 , A61K31/5377 , A61K31/496
CPC分类号： C07D473/34 , C07D473/14
摘要： PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.
摘要翻译：通过式I的新化合物实现PDE4抑制：其中R1和R2如本文所定义。

78. 发明申请

US20090176799A1 PHOSPHODIESTERASE 4 INHIBITORS 审中-公开
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：US20090176799A1
公开(公告)日：2009-07-09
申请号：US12325433
申请日：2008-12-01
申请人： Liu Ruiping , Mike De Vivo , Hans-Jurgen Ernst Hess , Allen Hopper , Erik Kreuster , Ashok Tehim
发明人： Liu Ruiping , Mike De Vivo , Hans-Jurgen Ernst Hess , Allen Hopper , Erik Kreuster , Ashok Tehim
IPC分类号： A61K31/496 , C07D207/26 , A61K31/4015 , C07D403/02
CPC分类号： C07D207/26 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds like rolipram and show selectivity with regard to inhibition of other classes of PDEs. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein.
摘要翻译：选择性PDE4抑制由4-（取代的 - 苯基）-2-吡咯烷酮化合物实现。与化合物如咯利普兰相比，化合物表现出改善的PDE4抑制，并且显示关于抑制其它类别的PDE的选择性。本发明的化合物具有式I：其中R 1，R 2和R 3如本文所定义。

79. 发明申请

US20080287484A1 Neurotrophin antagonist compositions 审中-公开
标题翻译：神经营养因子拮抗剂组合物
公开(公告)号：US20080287484A1
公开(公告)日：2008-11-20
申请号：US11905406
申请日：2007-09-28
申请人： Ashok Tehim , Xiannong Chen
发明人： Ashok Tehim , Xiannong Chen
IPC分类号： A61K31/473
CPC分类号： C07D221/14 , A61K31/473 , A61K31/4738 , C07D401/04 , C07D401/06 , C07D405/06
摘要： A pharmaceutical composition comprising a compound of Formula I wherein R1 is selected from, inter alia, alkyl, aryl-loweralkyl, heterocycle-loweralkyl, loweralkyl-carbonate; optionally substituted amino; benzimidaz-2-yl; optionally substituted phenyl; loweralkyl-(R5)(R6) wherein one of R5 and R6 is selected from H and the other is selected from carboxy, carboxy-loweralkyl and loweralkoxycarbonyl; NHCH2CH2OX wherein X represents an in vivo hydrolyzable ester; and R2 and R3 are independently selected from H, NO2, halo, di(loweralkyl)amino, cyano, C(O)OH, phenyl-S—, loweralkyl, and Z(O)OR7 wherein Z is selected from C and S and R7 is selected from H, loweralkylamino and arylamino; or pharmaceutically acceptable salts or certain in vivo hydrolyzable esters or amides thereof, in an amount effective to inhibit neurotrophin-mediated activity, and a suitable carrier, is described.The compositions are useful to inhibit undesirable neurotrophin-mediated activity such as the neurite outgrowth that occurs in some neurodegenerative disease states.
摘要翻译：一种药物组合物，其包含式I化合物，其中R 1选自烷基，芳基 - 低级烷基，杂环 - 低级烷基，低级烷基 - 碳酸酯; 任选取代的氨基; 苯并咪唑-2-基; 任选取代的苯基; 低级烷基 - （R 5）（R 6）其中R 5和R 6中的一个选自H 另一个选自羧基，羧基 - 低级烷基和低级烷氧基羰基; NHCH 2 CH 2 OX其中X表示体内可水解的酯; R 2和R 3独立地选自H，NO 2，卤素，二（低级烷基）氨基，氰基，C（O） OH，苯基-S-，低级烷基和Z（O）OR 7其中Z选自C和S，R 7选自H，低级烷基氨基和芳基氨基; 或其药学上可接受的盐或某些体内可水解的酯或酰胺，以有效抑制神经营养因子介导的活性的量和合适的载体。该组合物可用于抑制不期望的神经营养因子介导的活性，例如在一些神经变性疾病状态中发生的神经突生长。

80. 发明授权

US07342021B2 Phosphodiesterase 4 inhibitors 失效
公开(公告)号：US07342021B2
公开(公告)日：2008-03-11
申请号：US10067996
申请日：2002-02-08
申请人： Ruiping Liu , Hans-Jurgen Ernst Hess , Allen Hopper , Ashok Tehim , Yajing Rong
发明人： Ruiping Liu , Hans-Jurgen Ernst Hess , Allen Hopper , Ashok Tehim , Yajing Rong
IPC分类号： C07D473/34 , A61K31/52 , A61P37/08 , A61P25/28 , A61P29/00
CPC分类号： C07D473/40
摘要： PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.

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