Patent ID: 6482827
Filing Date: 2002-11-19
Classification: C07B,C07C,C07D

Abstract:
A compound that is an amine derivative of formula (I): wherein:W is â€”CONHOH; wherein:R1 and R2, which are the same or different, are each independently hydrogen; a group G, that is methyl, C2-C10 alkyl, C2-C10 alkenyl, C3-C7 cycloalkyl, cycloalkyl-C1-C10-alkyl, aryl, aryl-C1-C10-alkyl, aryl-C2-C10-alkenyl, said methyl, alkyl, alkenyl, cycloalkyl, and aryl groups being unsubstituted or substituted by one to three substituents; SO2â€”G, wherein G is as defined above; SOâ€”G, wherein G is as defined above; SO2â€”NH2; SO2â€”NHG; or SO2â€”NGGâ€², wherein G is as defined above and Gâ€², which is the same or different, is as defined above for G; wherein:R3 is C1-C15 alkyl, either unsubstituted or substituted by a C3-C7 cycloalkyl group, the alkyl and/or the cycloalkyl group being either unsubstituted, or substituted by one to three substituents selected from methyl, ethyl, C3-C4 linear or branched alkyl, fluoro, chloro, C1-C4 alkoxy, nitro, amino, dimethylamino, carboxy and carboxymethyl; or R3 is a group â€”Râ€”Xâ€”R1, wherein: R is a chemical bond, â€”CH2â€”, â€”(CH2)mâ€” wherein m is an integer from 2 to 5, â€”CH&boxH;CHâ€”, â€”CH2CH&boxH;CHâ€”, phenylene (i.e., â€”C6H4â€”), â€”CH2CH&boxH;CHâ€”C6H4â€”, â€”CH2CH2CH&boxH;CHâ€”, â€”CH2â€”CCâ€”, â€”CH2CH2â€”CCâ€”, â€”CH2CH2CH&boxH;CHâ€”C6H4â€”, â€”CH2â€”CCâ€”C6H4â€”, or â€”CH2CH2â€”CCâ€”C6H4â€”; X is a direct bond, an oxygen atom, a sulfur atom, or a sulfinyl â€”S(O)â€”, sulfonyl â€”S(O)2 or carbamoyl group â€”CONHâ€” or â€”NHCOâ€”; and R1 is C1-C6 alkyl, C2-C6 alkenyl, phenyl, phenyl-(C1-C6)-alkyl, phenyl-(C2-C6)-alkenyl, either unsubstituted or substituted by a group selected from F, Cl, Br, C1-C4 alkyl, C1-C4 alkoxy, alkylthio, arylthio, alkylsulfonyl, and arylsulfonyl; wherein:Q, is a secondary or tertiary carboxyamide, and is: a group â€”CONHG or â€”CONGGâ€², wherein G and Gâ€² are as defined above; a group â€”CONHâ€”CHGGâ€², wherein G and Gâ€² are as defined above; a group â€”CONGâ€³â€”CHGGâ€², wherein Gâ€³, being the same or different, is defined as G above; a group â€”CONHâ€”CH2â€”CHGGâ€², a group â€”CONGâ€³â€”CH2â€”CHGGâ€², wherein G, Gâ€² and Gâ€³ are as defined above; or a group â€”CO-azaheterocyclyl, wherein said carboxy group is bound to a ring nitrogen in said azaheterocyclyl group, that is either unsubstituted or substituted at any carbon or additional nitrogen atom, with the proviso that when Q is â€”CONHG and G is methyl, alkyl-methyl, cyclo-alkyl-methyl, aryl-methyl or heterocyclyl-methyl, then such methyl or substituted methyl cannot be further substituted by a group â€”(CH2)tâ€”CO2H, wherein t is 0, or esters and amides thereof;or a pharmaceutically acceptable salt, physiologically hydrolyzable derivative, solvate or hydrate thereof.