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    • 3. 发明申请
      WO2006128670A1 C5A RECEPTOR ANTAGONISTS 审中-公开
    • C5A RECEPTOR ANTAGONISTS
    • C5A受体拮抗剂
    • WO2006128670A1
    • 2006-12-07
    • PCT/EP2006/005141
    • 2006-05-30
    • JERINI AG , SCHNATBAUM, Karsten , SCHARN, Dirk , LOCARDI, Elsa , POLAKOWSKI, Thomas , RICHTER, Uwe , REINEKE, Ulrich , HUMMEL, Gerd
    • SCHNATBAUM, Karsten , SCHARN, Dirk , LOCARDI, Elsa , POLAKOWSKI, Thomas , RICHTER, Uwe , REINEKE, Ulrich , HUMMEL, Gerd
    • C07C275/40 , A61K31/17
    • 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
    • The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure, Rl, R2, R3, R4, R5, R6, R7, R8, R9, Rl0, RI l, R12, R13, R14, R15, R16, Rl7, R18, Rl9, 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 (-CONH 2 ), substituted carbamoyl, carboxyl, carbamate, alkoxycarbonyl, substituted alkoxycarbonyl, acylamino, substituted acylamino, sulfamoyl (-SO 2 NH 2 ), substituted sulfamoyl, haloalkyl, haloalkyloxy, -C(O)H, trialkylsilyl and azido.
    • 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，R1O，R1，R12，R13，R14，R15 ，R 16，R 17，R 18，R 19，R 20，R 21和R 22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， 取代的酰基，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 < 取代的氨基甲酰基，羧基，氨基甲酸酯，烷氧基羰基，取代的烷氧基羰基，酰氨基，取代的酰基氨基，氨磺酰基（-SO 2 NH 2），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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 4. 发明申请
      WO2006074964A1 C5A RECEPTOR ANTAGONISTS 审中-公开
    • C5A RECEPTOR ANTAGONISTS
    • C5A受体拮抗剂
    • WO2006074964A1
    • 2006-07-20
    • PCT/EP2006/000365
    • 2006-01-17
    • JERINI AG , HUMMEL, Gerd , LOCARDI, Elsa , POLAKOWSKI, Thomas , SCHARN, Dirk , SCHNATBAUM, Karsten
    • HUMMEL, Gerd , LOCARDI, Elsa , POLAKOWSKI, Thomas , SCHARN, Dirk , SCHNATBAUM, Karsten
    • C07K7/06 , C07K7/64 , C07K14/47 , C07K14/705 , C07K7/56
    • C07K14/472 , C07K7/06 , C07K7/56 , C07K7/64
    • The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure: (I), whereby X1 is a radical having a mass of about 1-300, whereby X1 is preferably selected from the group comprising R5-, R5-CO-, R5-N(R6)-CO-, R5-O-CO-, R5-SO 2 -, R5-N(R6)-SO 2 -, R5-N(R6)-, R5-N(R6)-CS-, R5-N(R6)-C(NH)-, R5-CS-, R5-P(O)OH-5 R5-B(OH)-, and R5 -CH=N-O-CH 2 -CO-, whereby R5 and R6 are individually and independently selected from the group comprising H, F, hydroxy, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, arylalkyl, substituted arylalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, acyl, substituted acyl, alkoxy, alkoxyalkyl, substituted alkoxyalkyl, aryloxyalkyl and substituted aryloxyalkyl, X2 is a radical that mimics the biological binding characteristics of a phenylalanine unit, X3 and X4 are individually and independently a spacer, whereby the spacer is preferably selected from the group comprising amino acids, amino acid analogs and amino acid derivates, X5 is a radical that mimics the biological binding characteristics of a cyclohexylalanine or homoleucine unit, X6 is a radical that mimics the biological binding characteristics of a tryptophane unit, X7 is a radical that mimics the biological binding characteristics of a norleucine or phenylalanine unit, a chemical bond X3 and X7 is formed, and the connecting lines - in formula (I) indicate chemical bonds, whereby the chemical bond is individually and independently selected from the group comprising covalent bonds, ionic bonds and coordinative bonds, whereby preferably the bond is a chemical bond and more preferably the chemical bond is a bond selected from the group comprising amide bonds, disulfide bonds, ether bonds, thioether bonds, oxime bonds and aminotriazine bonds, whereby the compound is in particular useful for the manufacture of a medicament for the treatment of autoimmune diseases.
    • 本发明涉及具有以下结构的化合物，优选C5a受体拮抗剂：（I），其中X1是质量约1-300的基团，其中X1优选选自包含R5-， R5-CO-，R5-N（R6）-CO-，R5-O-CO-，R5-SO2 - ，R5-N（R6）-SO2
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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