发明名称 N-ACYL-2-SUBSTITUTED -4-(BENZIMIDAZOLYL- OR IMIDAZOPYRIDINYL-SUBSTITUTED RESIDUES)-PIPERIDINES AS TACHYKININ ANTAGONOSTS
摘要 N-heterocyclic compounds of formula (I), and their N-oxides, salts and isomers, are new. n = 0, 1 or 2; m = 1 or 2, provided that when m is 2, then n is 1; X = a bond, O, S or NR3; Q = O or NR3; R1 = Ar1, Ar1(1-6C alkyl) or di(Ar1)(1-6C alkyl), where the 1-6C alkyl groups are optionally substituted by OH, TO, oxo or a ketalised oxo substituent of formula OCH2CH2O or OCH2CH2CH2O; R2 = Ar2, Ar2(1-6C alkyl), Het or Het(1-6C alkyl); L = a group of formula (i) or (ii); p = 0, 1 or 2; Y, depending on whether the optional second bond is present or not, is (i) a bivalent radical of formula CH2, CH(OH), C(O), O, S, SO, SO2, NR3, CH2NR3 or CONR3, or (ii) a trivalent radical of formula CH; A=B is a bivalent radical of formula CH=CH, N=CH or CH=N; R3 = H or R; R4 = H, R, 3-7C cycloalkyl, Alk-R7 or Alk-Z-R8; Alk = 1-6C alkanediyl; Z = O, S or NR3; R7 = Ph (optionally substituted by 1-2 halo, R or RO); furanyl (optionally substituted by 1-2 R or hydroxy(1-6C alkyl)); thienyl (optionally substituted by 1-2 halo or R); oxazolyl, thiazolyl or pyridinyl (all optionally substituted by 1-2 R); R8 = R (optionally substituted by OH, COOH or COOR); R5 = H, halo, OH or RO; R6 = H, R or Ar1(1-6 alkyl); Ar1 = Ph (optionally substituted by 1-3 halo, T, T', CN, CONH2, TO or T'O); Ar2 = naphthalenyl, or Ph (optionally substituted by 1-3 OH, halo, CN, NO2, NH2, NHT, N(T)2, T, T', TO, T'O, COOH, COOT, CONH2, CONHT or CON(T)2); Het = pyrrolyl, pyrazolyl, imidazolyl, furanyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinolinyl, quinoxalinyl, indolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzofuranyl or benzothienyl (all optionally substituted on carbon by 1-2 halo, T or mono-, di- or tri(halo)methyl); T, T', R, = 1-4C alkyl, halo(1-4C alkyl), 1-6C alkyl respectively.
申请公布号 HU9903987(A2) 申请公布日期 2000.05.28
申请号 HU19990003987 申请日期 1996.12.20
申请人 Janssen Pharmaceutica N.V. 发明人 JANSSENS, FRANS EDUARD;LEENAERTS, JOSEPH ELISABETH;SOMMEN, FRANCOIS MARIA;SURLERRAUX, DOMINIQUE LOUIS NESTOR GHISLAINE
分类号 A61K31/00;A61K31/415;A61K31/435;A61K31/4418;A61K31/4427;A61K31/443;A61K31/4433;A61K31/4439;A61K31/444;A61K31/445;A61K31/4465;A61K31/4523;A61K31/454;A61K31/4545;A61K31/47;A61K31/4709;A61K31/495;A61K31/4965;A61K31/497;A61K31/498;A61K31/55;A61P1/00;A61P9/00;A61P11/00;A61P17/00;A61P25/00;A61P25/04;A61P29/00;A61P35/00;A61P37/00;A61P43/00;C07D401/06;C07D401/12;C07D401/14;C07D403/12;C07D405/14;C07D409/14;C07D413/14;C07D417/14;C07D471/04 主分类号 A61K31/00
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