Patent ID: 6251911
Filing Date: 2001-06-26
Classification: A61P,C07D

Abstract:
A compound of formula I ##STR28##wherein m is an integer from 0 up to and including 3,v is 0 or 1,R is hydrogen or lower alkyl,R.sub.1 is halogen, cyano, amino, lower alkanoylamino, lower alkylamino, N,N-di-lower alkylamino, hydroxy, lower alkoxy, lower alkanoyloxy, carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkyl-carbamoyl, N,N-di-lower alkyl-carbamoyl, or lower alkyl that is unsubstituted or substituted by halogen, cyano, amino, lower alkanoylamino, lower alkylamino, N,N-di-lower alkylamino, hydroxy, lower alkoxy, lower alkanoyloxy, carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkyl-carbamoyl or by N,N-di-lower alkyl-carbamoyl, it being possible when several phenyl substituents R.sub.1 are present for those substituents to be identical or different from one another, anda) R.sub.2 is hydrogen and R.sub.3 is.alpha.) a radical of formula II ##STR29##wherein Y is oxygen or sulfur andR.sub.4 is.alpha..alpha.) an alkyl radical that is unsubstituted or substituted by amino, lower alkanoylamino, benzoylamino, benzyloxycarbonylamino, lower alkoxycarbonylamino, phenylamino or by benzylamino and that contains, including the substituents, from 4 to 20 carbon atoms,.alpha..beta.) phenylamino, benzylamino, naphthylamino or pyridylmethylamino, or alkylamino having from 4 to 11 carbon atoms, or.alpha..gamma.) phenyl, or monocyclic heterocyclyl bonded via a carbon atom and having 5 or 6 ring members and from 1 to 4 ring hetero atoms selected from nitrogen, oxygen and sulfur, any phenyl radicals present in the radical R.sub.4 being unsubstituted or substituted by one or more radicals selected from nitro, amino, lower alkanoylamino, lower alkylamino, di-lower alkylamino, halogen, cyano, trifluoromethyl, hydroxy, lower alkoxy, lower alkanoyloxy, carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkyl-carbamoyl, methylenedioxy and lower alkyl, it being possible when several phenyl substituents are present for those substituents to be identical or different from one another,.beta.) lower alkyl substituted by.beta..alpha.) unsubstituted or lower-alkyl-substituted monocyclic heterocyclyl bonded via a ring carbon atom and having 5 or 6 ring members and from 1 to 4 ring hetero atoms selected from nitrogen, oxygen and sulfur,.beta..beta.) phenyl substituted byi) phenyl,ii) unsubstituted or chloro-substituted phenoxy oriii) unsubstituted or lower-alkyl-substituted monocyclic heterocyclyl having 5 or 6 ring members and from 1 to 4 ring hetero atoms selected from nitrogen, oxygen and sulfur,.beta..gamma.) naphthyl,.beta..delta.) cycloalkyl having from 3 to 8 ring members that is unsubstituted or substituted by lower alkyl or by lower alkoxycarbonyl, or.beta..epsilon.) lower alkanoylamino, benzyloxycarbonylamino, lower alkoxycarbonylamino, benzoylamino, phenylamino, benzylamino, ureido, N.sup.3 phenyl-ureido, N.sup.3 -lower alkyl-ureido, N.sup.3,N.sup.3 -di-lower alkyl-ureido, amino-lower alkanoylamino, (lower alkoxycarbonylamino-lower alkanoyl)-amino, (benzyloxycarbonylamino-lower alkanoyl)-amino, prolyl-amino, (N-lower alkoxycarbonyl-propylamino, N.sup.3 -lower alkyl-thioureido, N.sup.3 -phenyl-thioureido, cyano, guanidino, amidino, toluenesulfonylamino, lower alkanesulfonylamino or unsubstituted or lower-alkyl-substituted monocyclic heterocyclylcarbonylamino having 5 or 6 ring members and from 1 to 4 ring hetero atoms selected from nitrogen, oxygen and sulfur, radicals mentioned in section OF) that contain a phenyl radical being unsubstituted or substituted in the phenyl radical by halogen, cyano, nitro, amino, lower alkanoylamino, lower alkylamino, N,N-di-lower alkylamino, hydroxy, lower alkoxy, lower alkanoyloxy, carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkyl-carbamoyl, N,N-di-lower alkyl-carbamoyl or by lower alkyl, or.gamma.) a radical of formula III ##STR30##wherein R.sub.5 is carboxy-lower alkanoylamino, benzyloxycarbonylamino, ureido, N.sup.3 -phenyl-ureido, N.sup.3 -(chloro-phenyl)-ureido, N.sup.3 -(lower alkoxy-phenyl)-ureido, N.sup.3 -lower alkyl-ureido, N.sup.3,N.sup.3 -di-lower alkyl-ureido, N.sup.3 -lower alkyl-thioureido, amino-lower alkanoyl-amino, (lower alkoxycarbonylamino-lower alkanoyl)-amino, (benzyloxycarbonylamino-lower alkanoyl)-amino, prolyl-amino, (N-lower alkoxycarbonyl-prolyl)-amino, hydroxy-lower alkanoyl-amino, di-lower alkylamino-methyleneamino, succinimido, phthalimido, guanidino or amidino,.delta.) unsubstituted or lower-alkyl-substituted monocyclic heterocyclyl bonded via a ring carbon atom and having 5 or 6 ring members and from 1 to 4 ring hetero atoms selected from nitrogen, oxygen and sulfur, or.epsilon.) lower alkanesulfonyl or unsubstituted or lower-alkyl-substituted benzenesulfonyl, orb) R.sub.2 and R.sub.3 together aredi-lower alkylamino-methyleneamino, or a substituted or unsubstituted alkylene or alkenylene radical having up to 15 carbon atoms, wherein from 1 to 3 carbon atoms may have been replaced by oxygen, sulfur or nitrogen,or a salt, solvate or tautomer thereof.