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    Phenol derivatives and their use as rotamase inhibitors
    6.
    发明申请
    Phenol derivatives and their use as rotamase inhibitors 审中-公开
    苯酚衍生物及其作为旋转异构酶抑制剂的用途

    公开(公告)号：US20070054904A1

    公开(公告)日：2007-03-08

    申请号：US10528139

    申请日：2003-09-18

    申请人： Jochen Knolle ,  Mike Schutkowski ,  Gerd Hummel ,  Thomas Tradler ,  Laurence Jobron ,  Claudia Christner ,  Dirk Scharn ,  Roland Stragies ,  Christoph Gibson ,  Frank Osterkamp

    发明人： Jochen Knolle ,  Mike Schutkowski ,  Gerd Hummel ,  Thomas Tradler ,  Laurence Jobron ,  Claudia Christner ,  Dirk Scharn ,  Roland Stragies ,  Christoph Gibson ,  Frank Osterkamp

    IPC分类号： A61K31/277 ,  A61K31/17

    CPC分类号： A61K31/155 ,  A61K31/135 ,  A61K31/165 ,  A61K31/17 ,  A61K31/18 ,  Y02A50/401 ,  Y02A50/406 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/465 ,  Y02A50/471 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/481 ,  Y02A50/483

    摘要： The present invention is related to a compound of the formula (I), (II), (III), (IV), (V): wherein Z1, Z2, Z3 and Z4 are each and independently selected from the group comprising C(O)—, —C(S)—, —C(O)—NR10—, —C(S)—NR11—, —C(N—CN)—NR12—, —S(O)—, —S(O2)—, —S(O)—NR13—, and —S(O2)—NR14—, —O—, —S— or are each and individually absent; X is a spacer and is independently selected from the group comprising -M1-L1-K-L2-M2-, wherein Y. is selected from the group comprising alkyl, substituted alkyl, straight alkyl, substituted straight alkyl, branched alkyl, substituted branched alkyl, straight alkenyl, substituted straight alkenyl, branched alkenyl, substituted branched alkenyl, straight alkynyl, substituted straight alkynyl, branched alkynyl, substituted branched alkynyl, cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, heterocyclyl, substituted heterocyclyl, mono-unsaturated heterocyclyl, poly-unsaturated heterocyclyl, mono-substituted poly-unsaturated heterocyclyl, poly-substituted poly-unsaturated heterocyclyl, mono-substituted mono-unsaturated heterocyclyl, poly-substituted mono-unsaturated heterocyclyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl, wherein Y is different from a peptide or is absent.

    摘要翻译： 本发明涉及式（I），（II），（III），（IV），（V）的化合物：其中Z 1，Z 2， Z，Z 3和Z 4各自独立地选自C（O） - ， - C（S） - ， - C（O）-NR C（S）-NR 11 - ， - C（N-CN）-NR 12 - ， - S（O ） - ， - （O 2 - ） - ， - S（O）-NR 13 - 和-S（O）2 - NR 14 - ， - O - ， - S-或各自不存在; X是间隔基，并且独立地选自-M1-L1-K-L2-M2-，其中Y选自烷基，取代的烷基，直链烷基，取代的直链烷基，支链烷基，取代的支链 烷基，直链烯基，取代的直链烯基，支链烯基，取代的支链烯基，直链炔基，取代的直链炔基，支链炔基，取代的支链炔基，环烷基，取代的环烷基，环烯基，取代的环烯基，杂环基，取代的杂环基，单不饱和杂环基， 多取代的多不饱和杂环基，多取代的多不饱和杂环基，单取代的单不饱和杂环基，多取代的单不饱和杂环基，芳基，取代的芳基，杂芳基和取代的杂芳基，其中Y是 不同于肽或不存在。

    C5a receptor antagonists
    9.
    发明授权
    C5a receptor antagonists 失效
    C5a受体拮抗剂

    公开(公告)号：US08071810B2

    公开(公告)日：2011-12-06

    申请号：US11915892

    申请日：2006-05-30

    申请人： Karsten Schnatbaum ,  Dirk Scharn ,  Elsa Locardi ,  Thomas Polakowski ,  Uwe Richter ,  Ulrich Reineke ,  Gerd Hummel

    发明人： Karsten Schnatbaum ,  Dirk Scharn ,  Elsa Locardi ,  Thomas Polakowski ,  Uwe Richter ,  Ulrich Reineke ,  Gerd Hummel

    IPC分类号： C07C275/00 ,  C07C273/00

    CPC分类号： C07C275/40 ,  C07C235/40 ,  C07C275/26 ,  C07C275/30 ,  C07C2602/08 ,  C07C2602/10 ,  C07D207/327 ,  C07D213/40 ,  C07D213/61 ,  C07D215/40 ,  C07D235/06 ,  C07D237/08 ,  C07D239/42 ,  C07D241/42 ,  C07D311/20 ,  C07D335/02

    摘要： The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21 and R22 are individually and independently selected from the group comprising H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, substituted heteroarylalkyl, alkoxyl, substituted alkoxyl, aryloxy, substituted aryloxy, arylalkyloxy, substituted arylalkyloxy, acyloxy, substituted acyloxy, halogen, hydroxyl, nitro, cyano, acyl, substituted acyl, mercapto, alkylthio, substituted alkylthio, amino, substituted amino, alkylamino, substituted alkylamino, bisalkyl amino, substituted bisalkyl amino, cyclic amino, substituted cyclic amino, carbamoyl (—CONH2), substituted carbamoyl, carboxyl, carbamate, alkoxycarbonyl, substituted alkoxycarbonyl, acylamino, substituted acylamino, sulfamoyl (—SO2NH2), substituted sulfamoyl, haloalkyl, haloalkyloxy, —C(O)H, trialkylsilyl and azido.

    摘要翻译： 本发明涉及具有以下结构的化合物，优选C5a受体拮抗剂：R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，R14，R15， R16，R17，R18，R19，R20，R21和R22各自独立地选自H，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基，环烷基，取代的环烷基，杂环基，取代的杂环基，芳基 ，取代的芳基，杂芳基，取代的杂芳基，芳基烷基，取代的芳基烷基，杂芳基烷基，取代的杂芳基烷基，烷氧基，取代的烷氧基，芳氧基，取代的芳氧基，芳基烷氧基，取代的芳基烷氧基，酰氧基，取代的酰氧基，卤素，羟基，硝基，氰基， 酰基，巯基，烷硫基，取代的烷硫基，氨基，取代的氨基，烷基氨基，取代的烷基氨基，双烷基氨基，取代的双烷基氨基，环状氨基，取代的环状氨基，氨基甲酰基（-CONH 2） 氨基甲酰基，羧基，氨基甲酸酯，烷氧基羰基，取代的烷氧基羰基，酰氨基，取代的酰氨基，氨磺酰基（-SO2NH2），取代的氨磺酰基，卤代烷基，卤代烷氧基，-C（O）H，三烷基甲硅烷基和叠氮基。