发明名称 New azolyl-substituted indole derivatives and analogs, useful as antifungal and antiparasitic drugs effective e.g. against Candida albicans, Aspergillus fumigatus and Leishmania
摘要 Azolyl- or azolylalkyl-substituted indole, indoline or indazole derivatives (including pyrido analogs) (I) are new. Indole, indoline or indazole derivatives of formula (I) and their enantiomers, diastereomers and acid addition salts are new. A = -C(R2)=C(R3)-, -CHR2-CHR3- or -N=C(R3)- (with the N bonded to NR1); R1-R7 = -(CRR')m-(CR''R''')n-(CHX)p-Het, H, lower alkyl, halo, lower trifluoroalkyl, CN, alkoxy, alkoxycarbonyl, carboxamido, optionally substituted (os) phenyl, phenylalkyl or halophenylalkyl, provided that at least one -(CRR')m-(CR''R''')n-(CHX)p-Het chain is present; R, R' = H, lower alkyl, alkenyl, cycloalkyl, os phenyl, halophenylalkyl or benzotriazolyl, or CRR' = 5- or 6-membered saturated ring, os by lower alkyl, F or Cl; R'', R''' = lower alkyl, os phenyl, halophenylalkyl, OH, alkoxy or acyloxy; Het = 1H-imidazol-1-yl, 2-methyl-1H-imidazol-1-yl, 1H-1,2,4-triazol-1-yl, 4H-1,2,4-triazol-4-yl or tetrazol-5-yl; X = H, lower alkyl or os phenyl; m, n, p = 0-5; ring W = phenyl or pyridine ring (i.e. one of CR4, CR5, CR6 and CR7 is optionally replaced by N); provided that: (i) if A = N=CR3, then R1 is other than benzyl or os ethyl when R3 = H; and (ii) if A = C(R2)=C(R3), then R2 is other than os benzyl when R2 = R3 = H.
申请公布号 FR2814073(A1) 申请公布日期 2002.03.22
申请号 FR20000012050 申请日期 2000.09.21
申请人 YANG JI CHEMICAL COMPANY, LTD 发明人 LE BORGNE MARC;NA YOUNG MIN;PAGNIEZ FABRICE;LE BAUT GUILLAUME;LE PAPE PATRICE;ABDALA HIAM
分类号 A61K31/404;A61K31/41;A61K31/4155;A61K31/4178;A61K31/4196;A61K31/4355;A61P31/00;A61P31/10;A61P33/00;C07D403/04;C07D403/06;C07D471/04;C07D521/00;(IPC1-7):A61K31/419;A61K31/417;A61K31/437;C07D403/14 主分类号 A61K31/404
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