Patent ID: 6365584
Filing Date: 2002-04-02
Classification: A61P,C07D

Abstract:
A compound of the formula (I) wherein:R1 is: (a) C1-C6-alkyl, C2-C6-alkenyl or C2-C6-alkynyl, each of which is unsubstituted or mono-, di- or trisubstituted by one or more substituents selected from the group consisting of hydroxy, C1-C4-alkoxy, CF3, phenoxy, COOH, halogen, â€”CO(C1-C4-alkoxy), â€”CONH2, â€”COâ€”NH(C1-C4-alkyl), â€”COâ€”N(C1-C4-alkyl)2, â€”NH2, â€”NH(C1-C4-alkyl), â€”N(C1-C4-alkyl)2 and C1-C4-alkoxy-phenoxy, (b) C3-C8-cycloalkyl optionally linked via a C1-C4-alkylene bridge, which is unsubstituted or mono-, di- or trisubstituted by one or more substituents selected from the group consisting of hydroxy, C1-C4-alkoxy, carboxy, halogen, C1-C4-alkoxycarbonyl and CF3, (c) phenyl-C1-C4-alkyl, which is unsubstituted or mono-, di- or trisubstituted by one or more substituents selected from the group consisting of hydroxy, C1-C4-alkoxy, carboxy, halogen, C1-C4-alkoxycarbonyl and CF3, or (d) a 5- or 6-membered, saturated or unsaturated heterocyclic group linked directly or via a C1-C4-alkylene bridge, which contains one or two hetero atoms selected from the group consisting of oxygen, nitrogen or sulphur and which is unsubstituted or substituted by C1-C4-alkyl or benzyl; R2 is â€”C(&boxH;NH)NH2 or â€”CH2â€”NH2; R3 is phenyl, benzyl, naphthyl, furanyl, benzofuranyl, quinolyl, isoquinolyl, thienyl or benzothienyl; and, R4 is: (a) C1-C6-alkyl group, which is mono- or disubstituted by one or two substituents selected from the group consisting of â€”NH2, â€”NH(C1-C4-alkyl), â€”N(C1-C4-alkyl)2, â€”C(&boxH;NH)NH2 and â€”NHâ€”C(&boxH;NH)NH2, (b) a 5-, 6- or 7-membered, saturated or unsaturated heterocyclic group linked directly or via a C1-C4-alkylene bridge or via a C1-C4-alkylene-CO bridge which contains one, two or three hetero atoms selected from the group consisting of oxygen, nitrogen and sulphur and which is unsubstituted or substituted by C1-C4-alkyl, C1-C4-hydroxyalkyl, benzyl or pyridyl, (c) C3-C8-cycloalkyl, which is unsubstituted or mono- or disubstituted by one or two substituents selected from the group consisting of â€”NH2, â€”NH(C1-C4-alkyl), â€”N(C1-C4-alkyl)2, â€”C(&boxH;NH)NH2 and â€”NHâ€”C(&boxH;NH)NH2, (d) phenyl, benzyl or phenylethyl, each of which is unsubstituted or mono- or disubstituted at the phenyl ring by one or two substituents selected from the group consisting of â€”NH2, â€”NH(C1-C4-alkyl), â€”N(C1-C4-alkyl)2, â€”C1-C4-alkyl-NH2, â€”C(&boxH;NH)NH2 and â€”NHâ€”C(&boxH;NH)NH2; or a tautomer or pharmaceutically acceptable salt thereof.