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71. 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。

72. 发明申请

US20090118270A1 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：US20090118270A1
公开(公告)日：2009-05-07
申请号：US12329214
申请日：2008-12-05
申请人： Francisco Xavier Talamas , Joan Marie Caroon , Robert Dunn , Allen Hopper , Erik Kuester , Richard Schumacher , Ashok Tehim
发明人： Francisco Xavier Talamas , Joan Marie Caroon , Robert Dunn , Allen Hopper , Erik Kuester , Richard Schumacher , Ashok Tehim
IPC分类号： A61K31/5377 , C07D417/12 , A61K31/4439 , A61K31/506 , A61P25/18 , A61P25/24 , C07D401/12 , C07D413/02
CPC分类号： C07D211/58 , C07D401/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： PDE4 inhibition is achieved by novel compounds, e.g., N-substituted diarylamine analogs. The compounds of the present invention are of Formulas I-III: wherein A, B, D, E, G, J, K, R1, R2, R3, R4, R11, R12, R13, R14, R21, R22, R23 and R24 are as defined herein.
摘要翻译： PDE4抑制通过新化合物，例如N-取代的二芳基胺类似物来实现。本发明化合物是式I-III：其中A，B，D，E，G，J，K，R1，R2，R3，R4，R11，R12，R13，R14，R21，R22，R23和 R 24如本文所定义。

73. 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。

74. 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.

75. 发明申请

US20070078139A1 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：US20070078139A1
公开(公告)日：2007-04-05
申请号：US11602283
申请日：2006-11-21
申请人： Richard Schumacher , William Brubaker , Michael De Vivo , Hans-Jurgen Hess , Allen Hopper , Ashok Tehim , Ruiping Liu , Axel Unterbeck
发明人： Richard Schumacher , William Brubaker , Michael De Vivo , Hans-Jurgen Hess , Allen Hopper , Ashok Tehim , Ruiping Liu , Axel Unterbeck
IPC分类号： A61K31/505 , A61K31/4965 , A61K31/44 , A61K31/426 , A61K31/47 , A61K31/381 , A61K31/34 , A61K31/137
CPC分类号： C07D213/74 , A61K31/137 , A61K31/16 , A61K31/34 , A61K31/381 , A61K31/426 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/4965 , A61K31/505 , C07C217/92 , C07C229/60 , C07D211/26 , C07D213/38 , C07D213/61 , C07D213/80 , C07D215/12 , C07D217/22 , C07D241/12 , C07D277/28 , C07D307/20 , C07D307/52 , C07D317/58 , C07D333/20 , C07D401/12 , C07D405/12 , C07D405/14 , C07F7/1804
摘要： PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3and R4 are as defined herein.
摘要翻译：通过新化合物，例如N-取代的苯胺和二苯胺类似物来实现PDE4的抑制。本发明的化合物是式I的化合物：其中R 1，R 2，R 3和R 4， >如本文所定义。

76. 发明申请

US20060135535A1 Phosphodiesterase 4 inhibitors 失效
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：US20060135535A1
公开(公告)日：2006-06-22
申请号：US11253812
申请日：2005-10-20
申请人： Allen Hopper , Robert Dunn , Erik Kuester , Richard Conticello , Ruiping Liu , Ashok Tehim
发明人： Allen Hopper , Robert Dunn , Erik Kuester , Richard Conticello , Ruiping Liu , Ashok Tehim
IPC分类号： A61K31/497 , A61K31/433 , A61K31/4245
CPC分类号： C07D207/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D407/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
摘要翻译：选择性PDE4的抑制是通过新的化合物，例如4-（取代的 - 苯基）-2-吡咯烷酮化合物实现的。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。本公开还涉及制备这种化合物的方法，含有这些化合物的组合物及其使用方法。

77. 发明申请

US20050026913A1 Phosphodiesterase 4 inhibitors 失效
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：US20050026913A1
公开(公告)日：2005-02-03
申请号：US10825610
申请日：2004-04-16
申请人： Ashok Tehim , Allen Hopper , Ruiping Liu , Erik Kuester , Robert Dunn , Thomas Renau
发明人： Ashok Tehim , Allen Hopper , Ruiping Liu , Erik Kuester , Robert Dunn , Thomas Renau
IPC分类号： A61P25/16 , A61P25/18 , A61P25/28 , C07D207/26 , C07D405/12 , C07D417/14 , C07D417/02 , C07D413/02 , C07
CPC分类号： C07D207/26 , C07D405/12 , C07D417/14
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。

78. 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。

79. 发明授权

US06667336B2 GlyT-1 inhibitors 失效
标题翻译： GlyT-1抑制剂
公开(公告)号：US06667336B2
公开(公告)日：2003-12-23
申请号：US10077579
申请日：2002-02-15
申请人： Zhaoqing Wang , William Delaney , Ashok Tehim , Shawn Maddaford , Ian Egle , Richard Schumacher , Allen T. Hopper
发明人： Zhaoqing Wang , William Delaney , Ashok Tehim , Shawn Maddaford , Ian Egle , Richard Schumacher , Allen T. Hopper
IPC分类号： A61K3138
CPC分类号： C07D409/10 , C07D333/20
摘要： The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了治疗神经和神经精神障碍的药物，其包含下式化合物或其药学上可接受的盐。

80. 发明申请

US20090306156A1 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：US20090306156A1
公开(公告)日：2009-12-10
申请号：US12535432
申请日：2009-08-04
申请人： Allen HOPPER , Robert Francis Dunn , Erik Mikal Kuester , Richard Dennis Conticello , Ruiping Liu , Ashok Tehim
发明人： Allen HOPPER , Robert Francis Dunn , Erik Mikal Kuester , Richard Dennis Conticello , Ruiping Liu , Ashok Tehim
IPC分类号： A61K31/429 , A61K31/426 , A61K31/4025 , A61K31/4015 , C07D415/00 , C07D405/12 , C07D207/00
CPC分类号： C07D207/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D407/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
摘要翻译：选择性PDE4的抑制是通过新的化合物，例如4-（取代的 - 苯基）-2-吡咯烷酮化合物实现的。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。本公开还涉及制备这种化合物的方法，含有这些化合物的组合物及其使用方法。

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