发明名称 Amidino compounds, their manufacture and use as medicament.
摘要 The invention relates to the compounds of the formula <CHEM> and pharmaceutically acceptable salts thereof, in which: R1 is amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical; R2 is hydrogen, halogen, trifluoromethyl, an aliphatic hydrocarbon radical, or is hydroxy which is etherified by an aliphatic alcohol, araliphatic alcohol, or aromatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; R3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, un organic carboxylic acid, a sulfonic acid, or a carbamic acid; X1 and X3, independently of one another, are oxygen (-O-) or sulphur (-S-); and X2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical; wherein the phenyl rings of formula I may be, independently of one another, further substituted by one or more substituents selected from halogen, trifluoromethyl, un aliphatic hydrocarbon radical, hydroxy, and hydroxy which is etherified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; wherein aryl in the above definitions may be, independently of one another, further substituted by one or more substituents selected from halogen, trifluoromethyl, un aliphatic hydrocarbon radical, hydroxy, and hydroxy which is etherified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; wherein a cycloaliphatic hydrocarbon radical may be substituted by an aliphatic radical. The compounds are useful as selective LTB-4 receptor antagonists in the treatment of conditions or syndromes in mammals which are responsive to LTB-4 receptor antagonism.
申请公布号 EP0518819(A2) 申请公布日期 1992.12.16
申请号 EP19920810423 申请日期 1992.06.02
申请人 CIBA-GEIGY AG 发明人 MORRISSEY, MICHAEL M.
分类号 A61K31/16;A61K31/085;A61K31/165;A61K31/166;A61K31/17;A61K31/18;A61P7/00;A61P9/08;A61P9/10;A61P11/00;A61P29/00;A61P37/08;A61P43/00;C07C257/10;C07C257/18;C07C257/20;C07C271/64;C07C275/56;C07C303/32;C07C309/04;C07C311/51;C07C319/18;C07C323/62;C07C323/63 主分类号 A61K31/16
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