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31. 发明授权

US07585882B2 Phosphodiesterase 4 inhibitors 失效
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：US07585882B2
公开(公告)日：2009-09-08
申请号：US11253812
申请日：2005-10-20
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： A61K31/4015 , A61K31/4025 , A61K31/433 , C07D207/12 , C07D285/08 , C07D403/12 , A61K31/341 , C07D407/10 , C07D407/14
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。

32. 发明申请

US20050272803A1 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：US20050272803A1
公开(公告)日：2005-12-08
申请号：US11186958
申请日：2005-07-22
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： C07D207/267 , A61K31/4015 , A61P9/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/16 , A61P37/08 , A61P43/00 , C07D207/26 , C07D207/27 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/4025 , C07D27/12 , C07D47/02
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。

33. 发明申请

US20110092475A1 2-SUBSTITUTED-ETHYNYLTHIAZOLE DERIVATIVES AND USES OF SAME 失效
标题翻译： 2-取代的乙酰基噻唑衍生物及其用途
公开(公告)号：US20110092475A1
公开(公告)日：2011-04-21
申请号：US12908588
申请日：2010-10-20
申请人： Allen Hopper , Anette Graven Sams , Gitte Kobberoee Mikkelsen , Mathivanan Packiarajan , Michel Grenon
发明人： Allen Hopper , Anette Graven Sams , Gitte Kobberoee Mikkelsen , Mathivanan Packiarajan , Michel Grenon
IPC分类号： A61K31/397 , C07D401/06 , A61K31/454 , C07D417/06 , A61K31/427 , C07D413/06 , A61K31/5377 , C07D277/56 , A61K31/426 , A61K31/496 , C07D403/06 , A61K31/55 , C07D471/04 , A61K31/437 , C07D491/10 , A61K31/438 , A61K31/538 , A61P25/00
CPC分类号： C07D277/24 , A61K31/4025 , A61K31/426 , A61K31/427 , A61K31/435 , A61K31/496 , A61K31/5377 , C07D277/56 , C07D417/06 , C07D417/14 , C07D471/04 , C07D487/08 , C07D491/10 , C07D491/107 , C07D495/04
摘要： The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.
摘要翻译：本发明提供式（I）的2-取代的乙炔基噻唑衍生物：其中R1，R2和X如本文所定义，或其药学上可接受的盐; 和药物组合物及其使用方法。

34. 发明授权

US07723348B2 Phosphodiesterase 4 inhibitors 失效
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：US07723348B2
公开(公告)日：2010-05-25
申请号：US12108833
申请日：2008-04-24
申请人： Allen Hopper , Robert F. Dunn , Erik Mikal Kuester , Richard D. Conticello
发明人： Allen Hopper , Robert F. Dunn , Erik Mikal Kuester , Richard D. Conticello
IPC分类号： A61K31/506 , A61K31/437 , A61K31/454 , A61K31/4155
CPC分类号： C07D405/12 , C07D231/12 , C07D231/56 , C07D403/04 , C07D403/14 , C07D405/04
摘要： Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.
摘要翻译：通过芳基和杂芳基吡唑化合物实现选择性PDE4抑制。与化合物如咯利普兰相比，化合物表现出改善的PDE4抑制，并且在抑制其他类型的PDE时显示出选择性。

35. 发明申请

US20070123570A1 Phosphodiesterase 4 inhibitors, including aminoindazole and aminobenzofuran analogs 失效
标题翻译：磷酸二酯酶4抑制剂，包括氨基吲唑和氨基苯并呋喃类似物
公开(公告)号：US20070123570A1
公开(公告)日：2007-05-31
申请号：US11642592
申请日：2006-12-21
申请人： Richard Schumacher , Allen Hopper , Ashok Tehim
发明人： Richard Schumacher , Allen Hopper , Ashok Tehim
IPC分类号： A61K31/4439 , A61K31/4433 , C07D405/02 , C07D403/02
CPC分类号： A61K31/343 , A61K31/416 , C07D231/56 , C07D401/12 , C07D405/12 , C07D405/14
摘要： PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs, The compounds of the present invention are of Formulas I and II: wherein R1, R2, R3, R4, R7 and R8 are as defined herein.
摘要翻译： PDE4抑制是通过新的化合物，例如氨基吲唑和氨基苯并呋喃类似物来实现的。本发明化合物具有式I和II：其中R 1，R 2，R 2， R 4，R 4，R 8和R 8如本文所定义。

36. 发明授权

US07205320B2 Phosphodiesterase 4 inhibitors 失效
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：US07205320B2
公开(公告)日：2007-04-17
申请号：US10754600
申请日：2004-01-12
申请人： Richard A. Schumacher , William F. Brubaker , Michael De Vivo , Hans-Jürgen Ernst Hess , Allen Hopper , Ashok Tehim , Ruiping Liu , Axel Unterbeck
发明人： Richard A. Schumacher , William F. Brubaker , Michael De Vivo , Hans-Jürgen Ernst Hess , Allen Hopper , Ashok Tehim , Ruiping Liu , Axel Unterbeck
IPC分类号： A61K31/4406 , A61K31/4439 , C07D213/38 , C07D401/12
CPC分类号： C07D213/73 , C07C217/84 , C07C217/88 , C07C217/92 , C07C2601/02 , C07C2601/08 , C07C2601/16 , C07C2602/08 , C07D213/38 , C07D215/12 , C07D333/16 , C07D333/32 , C07D401/12 , C07D405/12 , 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, R3 and R4 are as defined herein.
摘要翻译：通过新化合物，例如N-取代基实现PDE4抑制

37. 发明申请

US20060211865A1 Phosphodiesterase 4 inhibitors 失效
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：US20060211865A1
公开(公告)日：2006-09-21
申请号：US11378615
申请日：2006-03-20
申请人： Richard Schumacher , Elizabeth Graham , Allen Hopper , Ashok Tehim
发明人： Richard Schumacher , Elizabeth Graham , Allen Hopper , Ashok Tehim
IPC分类号： A61K31/4439 , C07D405/02 , C07D403/02 , C07D213/26
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的化合物：其中A，B，D，R 1，R 2，R 3， R 7，R 8，R 9，R 10和R 6均为如本文所定义。

38. 发明授权

US06699890B2 Phosphodiesterase 4 inhibitors 失效
标题翻译：磷酸二酯酶4抑制剂
公开(公告)号：US06699890B2
公开(公告)日：2004-03-02
申请号：US10051309
申请日：2002-01-22
申请人： Richard A. Schumacher , William F. Brubaker , Michael De Vivo , Hans-Jürgen Ernst Hess , Allen Hopper , Ashok Tehim , Ruiping Liu , Axel Unterbeck
发明人： Richard A. Schumacher , William F. Brubaker , Michael De Vivo , Hans-Jürgen Ernst Hess , Allen Hopper , Ashok Tehim , Ruiping Liu , Axel Unterbeck
IPC分类号： C07D21340
CPC分类号： C07D213/73 , A61K31/426 , A61K31/445 , A61K31/47 , A61K31/4965 , A61K31/505 , C07C217/84 , C07C217/88 , C07C217/92 , C07C229/60 , C07C2601/02 , C07C2601/08 , C07C2601/16 , C07C2602/08 , C07D211/26 , C07D213/38 , C07D213/61 , C07D213/74 , C07D213/80 , C07D215/12 , C07D217/22 , C07D241/12 , C07D277/28 , C07D307/20 , C07D307/52 , C07D317/58 , C07D333/16 , C07D333/20 , C07D333/32 , 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 , R3 and 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。本发明的化合物具有式I：其中R 1，R 2，R 3和R 4如本文所定义。

39. 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。

40. 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.

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