Patent ID: 6610729
Filing Date: 2003-08-26
Classification: A61P,C07C,C07D

Abstract:
A hydroxamic acid compound of the formula (I): whereinX is hydrogen or hydroxy-protecting group; R1 is hydrogen, alkyl, arylalkyl, heteroarylthioalkyl, arylthioalkyl, alkylthioalkyl, arylalkylthioalkyl, phthalimidoalkyl, alkenyl, or â€”(CH2)lâ€”A wherein l is an integer of 1 to 4 and A is a 5- or 6-membered N-heterocycle (a) which is bonded by N atom, (b) which optionally has at least one atom selected from N, O and S as an additional heteroatom at a position not adjacent to the bonded N atom, (c) in which one or both C atom(s) adjacent to said bonded N atom is(are) substituted by oxo, and (d) which is benzo-fused, or one or more other C atom(s) is(are) substituted by lower alkyl or oxo, and/or a different N atom is optionally substituted by lower alkyl or phenyl; R2 is hydrogen, alkyl, arylalkyl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl or aryl; R3 is hydrogen, alkyl or a group of the formula wherein Q1 is an aromatic hydrocarbon ring or an aromatic heterocycle, m is an integer of 0 to 3, and R13 is hydrogen, halogen, hydroxy, nitro, cyano, trifluoromethyl, lower alkyl, alkoxy, alkylthio, formyl, acyloxy, phenyl, arylalkyl, carboxy, â€”COORa wherein Ra is lower alkyl, arylalkyl or aryl, carbamoyl, guanidino, hydroxysulfonyloxy, sulfo, arylalkyloxyalkyl or a group selected from wherein n and q are the same or different and each is an integer of 1 to 5, r is an integer of 0 to 2, R14 and R15 are the same or different and each is hydrogen, alkyl, arylalkyl, heteroarylalkyl or aryl, or R14 and R15 may form, together with the adjacent nitrogen atom, an optionally substituted heterocycle, R16 is aryl, heteroaryl, hydroxysulfonyloxy or sulfo and R17 is hydroxy, hydroxysulfonyloxy, sulfo or carboxy; and Y is a group of the formula wherein Q2 is an aromatic heterocycle, and R18 is hydrogen, halogen, hydroxy, nitro, cyano, trifluoromethyl, lower alkyl, alkoxy, alkylthio, formyl, acyloxy, phenyl, arylalkyl, carboxy, â€”COORa wherein Ra is lower alkyl, arylalkyl or aryl, carbamoyl, guanidino, hydroxysulfonyloxy, sulfo, arylalkyloxyalkyl or a group selected from wherein s and t are the same or different and each is an integer of 1 to 5, u is an integer of 0 to 2, R19 and R20 are the same or different and each is hydrogen, alkyl, arylalkyl, heteroarylalkyl or aryl, or R19 and R20 may form, together with the adjacent nitrogen atom, an optionally substituted heterocycle, R21 is aryl, heteroaryl, hydroxysulfonyloxy, sulfo or carboxy, and R22 is hydroxy, hydroxysulfonyloxy, sulfo or carboxy; provided thatwhen (i) R3 is a group other than a group of the formula (A) wherein Q1 is a benzene ring, m is an integer of 0 to 3, and R13 is guanidino, hydroxysulfonyloxy, sulfo or a group selected from wherein n is an integer of 1 to 5, r is an integer of 0 to 2, R14 and R15 are the same or different and each is hydrogen, alkyl, arylalkyl, heteroarylalkyl or aryl, or R14 and R15 may form, together with the adjacent nitrogen atom, an optionally substituted heterocycle, and R16 is hydroxysulfonyloxy or sulfo, then (ii) Y should be a group of the formula (B) wherein Q2 is a furan ring, and R18 is arylalkyloxyalkyl or a group selected from wherein s and t are the same or different and each is an integer of 1 to 5, u is an integer of 0 to 2, R19 and R20 are the same or different and each is hydrogen, alkyl, arylalkyl, heteroaryl or aryl, or R19 and R20 may form, together with the adjacent nitrogen atom, an optionally substituted heterocycle, and R22 is hydroxy, hydroxysulfonyloxy, sulfo or carboxy, wherein the aforementioned arylalkyl, heteroarylthioalkyl, arylthioalkyl, arylalkylthioalkyl, phthalimidoalkyl, aryl, heteroaryl and heteroarylalkyl may have a substituent, or a pharmacologically acceptable salt thereof.