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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
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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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。
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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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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。
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公开(公告)号:US6166072A
公开(公告)日:2000-12-26
申请号:US342492
申请日:1999-06-29
申请人: Stanley Charles Bell , Michael De Vivo , Allen Hopper , Methvin Isaac , Anne O'Brien , Vassil Ilya Ognyanov , Richard Schumacher
发明人: Stanley Charles Bell , Michael De Vivo , Allen Hopper , Methvin Isaac , Anne O'Brien , Vassil Ilya Ognyanov , Richard Schumacher
IPC分类号: C07C323/60 , A61K31/21
CPC分类号: C07C323/60
摘要: Described herein are compounds having the general formula: ##STR1## wherein: Ar.sup.1 and Ar.sup.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.sup.1 or Ar.sup.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.sup.1 and Ar.sup.2 may be attached to the central atom to which they are connected by a single bond, an alkylene, alkenylene or alkynylene group;wherein Ar.sup.1 and Ar.sup.2 may be attached to the central atom to which they are connected by a single bond, an alkylene, alkenylene or alkynylene group;R.sup.3 is selected from the group consisting of H and aryl, which may be substituted as for Ar.sup.1 ;R.sup.4 and R.sup.5 are independently selected from the group consisting of H, alkyl, alkanoyl, benzoyl and benzyl.
摘要翻译: 本文描述的是具有以下通式的化合物:其中: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)和可如上所述被取代的第二芳基; 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; 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 3选自H和芳基,其可以被取代为Ar 1; R 4和R 5独立地选自H,烷基,烷酰基,苯甲酰基和苄基。
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