Patent ID: 6642248
Filing Date: 2003-11-04
Classification: A61P,C07D

Abstract:
A compound selected from those of formula (I): wherein:X and Y, which may be the same or different, represent, independently of one another, a group selected from: hydrogen and halogen, mercapto, cyano, nitro, linear or branched (C1-C6)alkyl, linear or branched (C1-C6)-trihaloalkyl and linear or branched trihalo-(C1-C6)alkyl-carbonylamino, groups of formulae â€”ORa, â€”NRaRb, â€”NRaâ€”C(O)-T1, â€”Oâ€”C(O)â€”T1, â€”O-T2â€”NRaRb, â€”O-T2-ORa, â€”NRa-T2-NRaRb, â€”NRa-T2-ORa and â€”NRa-T2-CO2Ra wherein: Ra represents a group selected from hydrogen and linear or branched (C1-C6) alkyl, aryl and aryl-(C1-C6)alkyl wherein the alkyl moiety is linear or branched, Rb represents a group selected from hydrogen and linear or branched (C1-C6) alkyl, aryl and aryl-(C1-C6)alkyl wherein the alkyl moiety is linear or branched, or â€ƒRa+Rb, together with the nitrogen atom carrying them, form a monocyclic 5- or 6-membered heterocycle optionally containing in the cyclic system a second hetero atom selected from oxygen and nitrogen, T1 represents a group selected from linear or branched (C1-C6) alkyl, linear or branched (C2-C6) alkenyl, aryl, aryl-(C1-C6)alkyl (wherein the alkyl moiety is linear or branched), and linear or branched (C1-C6) alkylene substituted by a group selected from â€”ORa and â€”NRaRb wherein Ra and Rb are as defined hereinbefore, T2 represents linear or branched (C1-C6) alkylene, it being understood that the substituents X and Y may be present on either of the two adjacent benzene rings, R1 represents hydrogen or linear or branched (C1-C6) alkyl, R2 represents a group selected from hydrogen and linear or branched (C1-C6) alkyl, â€”ORa, â€”NRaRb, â€”NRaâ€”C(O)-T1, â€”Oâ€”C(O)-T1, â€”O-T2-NRaRb, â€”O-T2-ORa, â€”NRa-T2-NRaRb, â€”NRa-T2-ORa and â€”NRa-T2-CO2Ra, wherein Ra, Rb, T1 and T2 are as defined hereinbefore, R3, R4, which may be the same or different, represent, independently of one another, hydrogen or linear or branched (C1-C6) alkyl, W represents a group of formula â€”CH(R5)â€”CH(R6)â€”, â€”CH&boxH;C(R7)â€”, â€”C(R7)&boxH;CHâ€” or â€”C(O)â€”CH(R8)â€” wherein: R5 and R6 represent, independently of the other, a group selected from â€”W1â€”C(W2)â€” â€”W4â€”C(W2)-Tâ€²1, â€”W1â€”S(O)nâ€”W3-T1 and â€”W1â€”S(O)n-T1 wherein: W1 represents oxygen or sulphur or nitrogen substituted by hydrogen or by linear or branched (C1-C6) alkyl, aryl or aryl-(C1-C6)alkyl wherein the alkyl moiety is linear or branched, W2 represents oxygen or sulphur, W3 represents oxygen or sulphur or nitrogen substituted by hydrogen or by linear or branched C1-C6) alkyl, aryl or aryl-(C1-C6)alkyl wherein the alkyl moiety is linear or branched, a bond when T1 represents linear or branched (C2-C6) alkenyl, W4 represents sulphur or nitrogen substituted by hydrogen or by linear or branched (C1-C6)alkyl, aryl or aryl-(C1-C6)alkyl wherein the alkyl moiety is linear or branched, T1 is as defined hereinbefore, Tâ€²1 represents a group selected from linear or branched (C2-C6) alkenyl, aryl, aryl-(C1-C6)alkyl (wherein the alkyl moiety is linear or branched), linear or branched (C1-C6) alkylene substituted by a group selected from â€”ORa and â€”NRaRb wherein Ra and Rb are as defined hereinbefore, n represents an integer selected from 1 and 2, â€ƒalternatively, one of R5 and R6 represents, independently of the other, a group as defined hereinbefore and the other represents a group selected from hydrogen, hydroxy, linear or branched (C1-C6) alkoxy, linear or branched (C1-C6)alkyl-carbonyloxy, arylcarbonyloxy, aryl-(C1-C6)alkyl-carbonyloxy (wherein the alkyl moiety is linear or branched), and amino optionally substituted by one or two, identical or different, linear or branched (C1-C6)alkyl, R7 represents a group selected from hydroxy, linear or branched (C1-C6) alkoxy, â€”C(W2)-T1, â€”W1â€”C(W2)â€”W3-T1, â€”W1â€”C(W2)-T1, â€”W1â€”S(O)nâ€”W3-T1 and â€”W1â€”S(O)n-T1 wherein W1, W2, W3, T1 and n are as defined hereinbefore, or R7 may represent hydrogen when R2 represents â€”Oâ€”T2-ORa and/or when X represents hydrogen and Y, located in the 13-position of the naphthyl system of the pentacyclic skeleton, represents amino optionally substituted by one or two identical or different groups selected independently of one another from linear or branched (C1-C6)alkyl, linear or branched (C1-C6)acyl and linear or branched trihalo-(C1-C6)alkyl-carbonyl, R8 represents linear or branched (C1-C6) alkoxy or linear or branched (C1-C6)alkyl-carbonyloxy, or may have the additional meaning of hydroxy when R2 represents â€”O-T2-ORa as defined hereinbefore, its enantiomers, diastereoisomers, N-oxides, and addition salts thereof with a pharmaceutically acceptable acid or base,wherein:aryl being understood to mean phenyl or naphthyl optionally containing one or more, identical or different, substituents selected from hydroxy, halogen, carboxy, nitro, amino, linear or branched (C1-C6) lkylamino, di(C1-C6) alkylamino, wherein each alkyl moiety may be linear or branched, linear or branched (C1-C6) alkoxy, linear or branched (C1-C6)acyl and linear or branched (C1-C6)alkyl-carbonyloxy, and optical isomers thereof.