Patent ID: 6512000
Filing Date: 2003-01-28
Classification: A61K,C07D

Abstract:
A method for treating an inflammatory or allergic disease, which method comprises administering to a host in need of such treatment a therapeutically effective amount of a compound of the formula (I)â€‰wherein:R1 denotes C1-C10-alkyl, which may optionally be mono-, di- or tri-substituted by one or more of the groups C1-C4-alkoxy, phenoxy, hydroxyphenoxy, C1-C4-alkoxy-phenoxy, C3-C6-cycloalkyl, â€”NH2, â€”NH(C1-C4-alkyl), â€”N(C1-C4-alkyl)2, â€”NHâ€”COâ€”(C1-C4-alkyl), â€”COâ€”NH2, â€”COâ€”NHâ€”(C1-C4-alkyl) or â€”NHâ€”CO-benzyl, or phenyl-C1-C4-alkyl, wherein the phenyl ring may optionally be mono-, di- or tri- substituted by one or more of the groups C1-C4-alkyl, CF3, fluorine, chlorine, bromine, COOH or COOâ€”C1-C4-alkyl, or a 5 or 6 membered, saturated or unsaturated heterocyclic group linked via a single bond or via a C1-C4-alkylene bridge, which heterocyclic group contains one, two or three heteroatoms selected from the group consisting of oxygen, nitrogen and sulphur and which may optionally be mono-, di- or tri-substituted by one or more of the groups C1-C4-alkyl, optionally by C1-C4-alkyl substituted phenyl or optionally by C1-C4-alkyl substituted benzyl or to which a benzene ring may optionally be fused via two adjacent carbon atoms; R2 denotes â€”C(&boxH;NH)NH2 or â€”CH2â€”NH2; R3 and R4 which may be identical or different, denote hydrogen, C1-C6-alkyl, which may be mono- or disubstituted by one or more of the groups COOH, COOâ€”C1-C4-alkyl, C3-C6-cycloalkyl, â€”NH2, â€”NH(C1-C4-alkyl), â€”N(C1-C4-alkyl)2, â€”NHphenyl, â€”N(phenyl)2, â€”NHbenzyl, â€”N(benzyl)2, â€”NHâ€”COâ€”(C1-C4-alkyl), â€”C(&boxH;NH)NH2 or â€”NHâ€”C(&boxH;NH)NH2, or phenyl-C1-C4-alkyl, wherein the C1-C4-alkylene bridge may optionally be substituted by phenyl, COOH or COOâ€”C1-C4-alkyl and wherein the phenyl ring may optionally be mono-, di- or tri-substituted, directly or via a C1-C4-alkylene bridge, by one or more of the groups C1-C4-alkyl, C1-C4-alkoxy, CF3, fluorine, chlorine, bromine, COOH, COOâ€”C1-C4-alkyl, â€”NH2, â€”NH(C1-C4-alkyl), â€”N(C1-C4-alkyl)2, â€”NHphenyl, â€”N(phenyl)2, â€”NHbenzyl, â€”N(benzyl)2, â€”NHâ€”COâ€”(C1C4-alkyl), â€”C(&boxH;NH)NH2 or â€”NHâ€”C(&boxH;NH)NH2, or a 5-, 6- or 7-membered, saturated or unsaturated heterocyclic group linked directly or via a C1-C4-alkylene bridge, which heterocyclic group contains one, two, three or four heteroatoms selected from the group consisting of oxygen, nitrogen and sulphur and which may optionally be mono-, di- or tri-substituted by one or more of the groups C1-C4-alkyl, phenyl or benzyl or to which a benzene ring may optionally be fused via two adjacent carbon atoms, or C3-C8-cycloalkyl, naphthyl or phenyl, which may optionally be mono-, di- or tri-substituted by one or more of the groups C1-C4-alkyl, C1-C4-alkoxy, phenyloxy, benzyloxy, CF3, fluorine, chlorine, bromine, COOH or COOâ€”C1-C4-alkyl, or R3 and R4 together with the nitrogen atom form a 5-, 6- or 7-membered, saturated or unsaturated heterocyclic group, which heterocyclic group optionally contains one or two further heteroatoms selected from the group consisting of oxygen, nitrogen and sulphur and which may optionally be substituted by one or more of the groups C1-C4-alkyl, C5-C6-cycloalkyl, benzyl, which may optionally be substituted by C1-C4-alkyl, pyridyl or phenyl, optionally substituted by C1-C4-alkyl, C1-C4-alkoxy or hydroxy, or a tautomer or pharmaceutically acceptable salt thereof.