Patent ID: 6740654
Filing Date: 2004-05-25
Classification: A61P,C07D

Abstract:
A compound of formula (1): whereinHet is a bicyclic fused ring heteroaromatic group; g is zero or the integer 1, 2, 3 or 4; Each R16, which may be the same or different, is an atom or group â€”L3(Alk2)tL4(R4)u, L3 and L4, which may be the same or different, are each a covalent bond or a linker atom or group â€”Oâ€”, â€”Sâ€”, â€”C(O)â€”, â€”C(O)Oâ€”, â€”OC(O)â€”, â€”C(S)â€”, â€”S(O)â€”, â€”S(O)2â€”, â€”N(R8)â€”, â€”N(R8)Oâ€”, â€”N(R8)Nâ€”, â€”CON(R)8)â€”, â€”OC(O)N(R8)â€”, â€”CSN(R8)â€”, â€”N(R8)COâ€”, â€”N(R8)C(O)Oâ€”, â€”N(R8)CSâ€”, â€”S(O)2N(R8)â€”, â€”N(R8)S(O)2â€”, â€”N(R8)CON(R8)â€”, â€”N(R8)CSN(R8)â€”, or â€”N(R8)SO2N(R8)â€”, R8 is a hydrogen atom or an optionally substituted C1-6alkyl group, t is zero or the integer 1, u is an integer 1, 2 or 3, Alk2 is an aliphatic or heteroaliphatic chain, and R4 is a hydrogen or halogen atom or a group selected from an optionally substituted C1-6alkyl or C3-8 cycloalkyl group, â€”OR5 (where R5 is a hydrogen atom, an optionally substituted C1-6alkyl or C3-8 cycloalkyl group), â€”SR5, â€”NR5R6 (where R6 is as just defined for R5 and may be the same or different), â€”NO2, â€”CN, â€”CO2R5, â€”SO3H, â€”SOR5, SO2R5, â€”SO3R5, â€”OCO2R5, â€”CONR5R6, â€”OCONR5R6, â€”CSNR5R6, â€”COR5, â€”OCOR5, â€”N(R5)COR6, â€”N(R5)CSR6, â€”SO2N(R5)(R6), â€”N(R5)SO2R6, â€”N(R5)CON(R6)(R7), (where R7 is a hydrogen atom, an optionally substituted C1-6alkyl or C3-8cycloalkyl group), â€”N(R5)CSN(R6)(R7) or â€”N(R5)SO2N(R6)(R7), provided that when t is zero and each of L3 and L4 is a covalent bond then u is the integer 1 and R4 is other than a hydrogen atom; L2 is a covalent bond or an atom or group â€”Oâ€”, â€”Sâ€”, â€”C(O)â€”, â€”C(S)â€”, â€”S(O)â€”, â€”S(O)2, â€”N(R8)â€” or â€”C(R8)(R8a)â€” (where R8a is an atom or group as defined for R8 and may be the same or different); Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain in which R is a carboxylic acid (â€”CO2H), a carboxylic acid ester, a carboxylic acid amide, or a carboxylic acid biostere;R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group â€”Oâ€”, â€”Sâ€”, â€”C(O)â€”, â€”C(O)Oâ€”, â€”OC(O)â€”, â€”C(S)â€”, â€”S(O)â€”, â€”S(O)2â€”, â€”N(R8)â€”, â€”N(R8)Oâ€”, â€”N(R8)Nâ€”, â€”CON(R8)â€”, â€”OC(O)N(R8)â€”, â€”CSN(R8)â€”, â€”N(R8)COâ€”, â€”N(R8)C(O)Oâ€”, â€”N(R8)CSâ€”, â€”S(O)2N(R8)â€”, â€”N(R8)S(O)2â€”, â€”N(R8)CON(R8)â€”, â€”N(R8)CSN(R8)â€”, or â€”N(R8)SO2N(R8)â€”; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, C3-10cycloaliphatic, C3-10heterocycloaliphatic, C7-10polycycloaliphatic, C7-10heteropolycycloaliphatic, aromatic or heteroaromatic group, wherein said heteroaliphatic, C3-10heterocycloaliphatic, and C7-10heteropolycycloaliphatic groups contain one, two, three, or four heteroatoms or heteroatom-containing groups as defined for L3 and L4, which may be the same or different; provided that Het is not a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl group; and the salts and N-oxides thereof.