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    C5A RECEPTOR ANTAGONISTS
    2.
    发明申请
    C5A RECEPTOR ANTAGONISTS 审中-公开
    C5A受体拮抗剂

    公开(公告)号：WO2006074964A1

    公开(公告)日：2006-07-20

    申请号：PCT/EP2006/000365

    申请日：2006-01-17

    Applicant: JERINI AG ,  HUMMEL, Gerd ,  LOCARDI, Elsa ,  POLAKOWSKI, Thomas ,  SCHARN, Dirk ,  SCHNATBAUM, Karsten

    Inventor： HUMMEL, Gerd ,  LOCARDI, Elsa ,  POLAKOWSKI, Thomas ,  SCHARN, Dirk ,  SCHNATBAUM, Karsten

    IPC: C07K7/06 ,  C07K7/64 ,  C07K14/47 ,  C07K14/705 ,  C07K7/56

    CPC classification number: C07K14/472 ,  C07K7/06 ,  C07K7/56 ,  C07K7/64

    Abstract: 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.

    Abstract translation: 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

    C5a-REZEPTOR-ANTAGONISTEN
    3.
    发明申请
    C5a-REZEPTOR-ANTAGONISTEN 审中-公开

    公开(公告)号：WO2005010030A3

    公开(公告)日：2005-02-03

    申请号：PCT/EP2004/008057

    申请日：2004-07-19

    Applicant: JERINI AG ,  HUMMEL, Gerd ,  LOCARDI, Elsa ,  POLAKOWSKI, Thomas ,  SCHARN, Dirk ,  SCHNATBAUM, Karsten

    Inventor： HUMMEL, Gerd ,  LOCARDI, Elsa ,  POLAKOWSKI, Thomas ,  SCHARN, Dirk ,  SCHNATBAUM, Karsten

    IPC: C07K7/06 ,  C07K14/47 ,  C07K14/705 ,  C07K7/50

    Abstract: C5a-Rezeptor-Antagonist, der Struktur (I), wobei X1 ein Radikal mit einer Masse von etwa 1-300 ist und wobei X1 gleich 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-, R5-B(OH)-, oder R5-CH=N-O-CH 2 -CO-, wobei R5 / R6 gleich H, F, Hydroxy, Alkyl, substituiertes Alkyl, Cycloalkyl, substituiertes Cycloalkyl, Heterocyclyl, substituiertes Heterocyclyl, Arylalkyl, substituiertes Arylalkyl, Aryl, substituiertes Aryl, Heteroaryl, substituiertes Heteroaryl, Acyl, substituiertes Acyl, Alkoxy, Alkoxyalkyl, substituiertes Alkoxyalkyl, Aryloxyalkyl oder substituiertes Aryloxyalkyl, X2 = Radikal (biologische Bindungseigenschaften einer Phenylalanin-Einheit mimikrierend), X3 / X4 = Spacer (Aminosäuren, Aminosäure-Analoga und Aminosäure-Derivate), X5 = Radikal (biologische Bindungseigenschaften einer Cyclohexylalanin- oder Homoleucin-Einheit mimikrierend), X6 = Radikal (biologische Bindungseigenschaften einer Tryptophan-Einheit mimikrierend), X7 = Radikal (biologische Bindungseigenschaften einer Norleucin- oder Phenylalanin-Einheit mimikrierend), eine chemische Bindung zwischen X3 und X7 ausgebildet ist.

    C5A RECEPTOR ANTAGONISTS
    8.
    发明申请
    C5A RECEPTOR ANTAGONISTS 审中-公开
    C5A受体拮抗剂

    公开(公告)号：WO2006128670A1

    公开(公告)日：2006-12-07

    申请号：PCT/EP2006/005141

    申请日：2006-05-30

    Applicant: JERINI AG ,  SCHNATBAUM, Karsten ,  SCHARN, Dirk ,  LOCARDI, Elsa ,  POLAKOWSKI, Thomas ,  RICHTER, Uwe ,  REINEKE, Ulrich ,  HUMMEL, Gerd

    Inventor： SCHNATBAUM, Karsten ,  SCHARN, Dirk ,  LOCARDI, Elsa ,  POLAKOWSKI, Thomas ,  RICHTER, Uwe ,  REINEKE, Ulrich ,  HUMMEL, Gerd

    IPC: C07C275/40 ,  A61K31/17

    CPC classification number: 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

    Abstract: 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.

    Abstract translation: 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。

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