发明名称 Substituted arylalkylamines as neurokinin antagonists
摘要 A compound represented by the structural formula I or a pharmaceutically acceptable salt thereof, wherein; A1 is OR6, N(R6)(R7), S(O)eR13 or (C(R6)(R7))1-6N(R6)(R7) and A2 is H, or A1 and A2 together are O, C(R6)(R7) or NOR6, Q is R5-phenyl, T is R4-aryl, b is 0, 1 or 2, b1 is 1 or 2, X is O, NR6, N(R6)C(O), OC(O)NR6 or N(R6)C(O)O, R4 and R5 are independently 1-3 substituents independently selected from the group consisting of H, halogeno, OR6, OC(O)R6, OC(O)N(R6)(R7), N(R6)(R7), C1-6 alkyl, CF3, C2F5, COR6, CO2R6, CON(R6)(R7), S(O)eR13, CN, OCF3, NR6CO2R16, NR6COR7, NR8CON(R6)(R7), R15-phenyl, R15-benzyl, NO2, N(R6)S(O)2R13 or S(O)2N(R6)(R7) or adjacent R4 substituents or adjacent R5 substituents can form a OCH2O group and R4 can also be R15-heteroaryl, R6, R7, R8, R8a, and R13 are independently selected from the group consisting of H, C1-6 alkyl, C2-C6 hydroxyalkyl, C1-C6 alkoxy-C1-C6 alkyl, R15-phenyl, and R15-benzyl or R6 and R7, together with the nitrogen to which they are attached, form a ring of 5 to 6 members, wherein 0, 1 or 2 ring members are selected from the group consisting of O, S and N(R19), R9 and R9a are independently selected from the group consisting of R6 and OR6, provided that when R9 is OH, X is N(R6)C(O), R10 is independently selected from the group consisting of H and C1-6 alkyl, R15 is 1 to 3 substituents independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, halogeno, CF3, C2F5, COR10, CO2R10, C(O)N(R10)2, S(O)eR10, CN, N(R10)COR10, N(R10)CON(R10)2 and NO2, R16 is C1-6 alkyl, R15-phenyl or R15-benzyl, R19 is H, C1-C6 alkyl, C(O)N(R10)2, CO2R10, (C(R8)(R9))fCO2R10 or (C(R8)(R9))uC(O)N(R10)2, f is 1-6, u is 0-6, Z is formula II or formula III, g is 1, j is 1 or 0, h is 2, k is 2 or 3, J is two hydrogen atoms or O, L is H, C1-C6 alkyl, C1-C6 alkenyl, CH2 cycloalkyl, R15-benzyl, R15-heteroaryl, C(O)R6, (CH2)mOR6, (CH2)mN(R6)(R7), (CH2)mC(O)OR6 or (CH2)mC(O)N(R6)(R7), L1 is H, R28 is H, OH, phenyl or H2NC(O) and R29 is H or R4-phenyl. The abovementioned compounds are useful in the treatment of asthma, cough, bronchospasm, central nervous system diseases, inflammatory diseases and gastrointestinal disorders.
申请公布号 NZ334966(A) 申请公布日期 2000.10.27
申请号 NZ19960334966 申请日期 1996.10.28
申请人 SCHERING CORPORATION 发明人 REICHARD, GREGORY A;ASLANIAN, ROBERT G
分类号 A61K31/445;A61K31/451;A61P1/00;A61P11/06;A61P25/00;A61P29/00;A61P43/00;C07D211/52;(IPC1-7):C07D211/52 主分类号 A61K31/445
代理机构 代理人
主权项
地址