Patent ID: 6180636
Filing Date: 2001-01-30
Classification: A61P,C07D

Abstract:
A compound of formula I ##STR24##in which n is 0 to 3,q is 0 or 1,R is halogen, lower alkyl, hydroxymethyl, aminomethyl, hydroxyl, lower alkanoyloxy, lower alkoxy, carboxyl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl, cyano, amino, lower alkanoylamino, lower alkylamino, N,N-di-lower alkylamino or trifluoromethyl, it being possible, if two or more radicals R are present in the molecule, for these to be identical to or different from one another,one of the radicals R.sub.1 and R.sub.2 is hydrogen or lower alkyl,and the other of the radicals R.sub.1 and R.sub.2 isa) a radical of the formula II ##STR25##in which u is 1 to 3 andone or more radicals R.sub.4 is selected from the group consisting of amidino, guanidino, ureido, N.sup.3 -lower alkylureido, N.sup.3,N.sup.3 -di-lower alkylureido, N.sup.3 -phenylureido, N.sup.3,N.sup.3 -diphenylureido, thiocarbamoyl, thioureido, N.sup.3 -lower alkylthioureido, N.sup.3,N.sup.3 -di-lower alkylthioureido, lower alkoxycarbonylamino, benzyloxycarbonylamino, morpholine-4-carbonyl, piperazine-1-carbonyl, 4-lower alkylpiperazine-1-carbonyl, lower alkylsulfonylamino, benzenesulfonylamino, toluenesulfonylamino, thiophene-2-carbonylamino, furan-2-carbonylamino, benzylamino, hydroxymethyl, aminomethyl or a radical of the formula --N.dbd.C(R.sub.5)--R.sub.6, in which R.sub.5 is hydrogen or lower alkyl and R.sub.6 is di-lower alkylamino, piperidino, 4-lower alkylpiperazino or morpholino, and the other radical(s) R.sub.4 is (are) halogen, lower alkyl, hydroxyl, lower alkanoyloxy, lower alkoxy, carboxyl, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl, cyano, amino, lower alkanoylamino, lower alkylamino, N,N-di-lower alkylamino or trifluoromethyl, it being possible, if two or more radicals R.sub.4 are present in the molecule, for these to be identical to or different from one another, or isb) a radical of the formula III ##STR26##in which R.sub.7 is lower alkoxy or benzyloxy and R.sub.8 is hydroxyl or benzyloxy, or isc) amino-lower alkyl, in which the amino group is substituted by one or two hydroxy-lower alkyl, amino-lower alkyl, carboxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, benzyloxycarbonyl-lower alkyl or benzyl radicals, which in the phenyl moiety are unsubstituted or substituted by halogen, lower alkyl, hydroxymethyl, aminomethyl, hydroxyl, lower alkanoyloxy, lower alkoxy, carboxyl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl, cyano, amino, lower alkanoylamino, lower alkylamino, N,N-di-lower alkylamino or trifluoromethyl, or isd) piperidine-1-carbonyl, piperazine-1-carbonyl, 4-lower alkylpiperazine-1-carbonyl, morpholine-4-carbonyl, thiocarbamoyl, a heterocyclic radical bonded via a ring carbon atom and having five ring members and 1-4 ring heteroatoms, selected from oxygen, nitrogen and sulfur, or ise) 4-lower alkylpiperazinomethyl or a lower alkyl radical which is substituted by a heterocyclic radical other than piperazinyl and having five or six ring members and 1-4 ring heteroatoms, selected from oxygen, nitrogen and sulfur, or isf) a radical of the formula --CH.dbd.N--OR.sub.9 in which R.sub.9 is hydrogen or lower alkyl, org) if q is 1, additionally to the definitions given above in the sections a) to f) can also be phenyl which is substituted by halogen, lower alkyl, trifluoromethyl or lower alkoxy, andR.sub.3 is hydrogen, lower alkyl, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl,or a salts thereof.