Patent ID: 6610704
Filing Date: 2003-08-26
Classification: A61P,C07D

Abstract:
A compound of formula I (or a pharmaceutically acceptable salt thereof) whereinA3, A4, A5 and A6, together with the two carbons to which they are attached, complete a substituted heteroaromatic ring in which one of A3, A4, A5 and A6 is N, and each of the others is CR3, CR4, CR5 or CR6, respectively; wherein each of R3, R4, R5 and R6 is independently hydrogen or methyl, or one of R3, R4, R5 and R6 attached to a carbon which is not bonded to an N-atom is chloro and the others are hydrogen; wherein L1 is â€”NHâ€”COâ€”, â€”COâ€”NHâ€” or â€”CH2â€”NHâ€” such that â€”L1â€”Q1 is â€”NHâ€”COâ€”Q1â€”COâ€”NHâ€”Q1 or â€”CH2â€”NHâ€”Q1; Q1 is phenyl, in which the phenyl may bear one, two or three substituents at the 3-, 4- or 5-position(s) independently selected from halo, cyano, carbamoyl, aminomethyl, methyl, methoxy, difluoromethoxy, hydroxymethyl, formyl, vinyl, amino, hydroxy and 3,4-methylenedioxy; and in addition the phenyl may bear a 2-chloro or 2-fluoro substituent; or â€”COâ€”Q1 is cyclopentenylcarbonyl or cyclohexenylcarbonyl; R2 is â€”NHâ€”CH2â€”Q2 in which Q2 is Q2A wherein Q2A (showing the â€”CH2â€” to which it is attached) is â€ƒin which R2A is hydrogen, t-butyl, methylsulfonyl, â€”CHRyRz, â€”CHRwRx, or 4-pyridinyl (which is unsubstituted or bears a substituent Rv at the 2- or 3-position) wherein Rv is methyl, hydroxymethyl, {(1-2C)alkoxy}carbonyl; cyano, carbamoyl, thiocarbamoyl, or N-hydroxyamidino; each of Rw and Rx independently is hydrogen or (1-3C) normal alkyl; or â€”CHRwRx is 2-indanyl or (showing the nitrogen to which it is attached) is â€ƒin which T is a single bond or methylene and U is methylene, ethylene, oxy, â€”S(O)qâ€” (wherein q is 0, 1 or 2) or imino (which may bear a methyl substituent), or T is ethan-1,1-diyl and U is a single bond or methylene; Ry is hydrogen or methyl; and Rz is isopropyl, t-butyl, (3-6C)cycloalkyl, phenyl (which is unsubstituted or bears one or more substituents independently selected from halo, methyl, methoxy and hydroxy), 4-quinolinyl or heteroaryl (which heteroaryl is a 5-membered aromatic ring which includes one to four heteroatoms selected from sulfur, oxygen and nitrogen or is a 6-membered aromatic ring which includes one to three nitrogen atoms, wherein the heteroaryl is attached at carbon and may bear one or more methyl substituents on carbon or nitrogen); and wherein halo is fluoro, chloro, bromo or iodo; (1-2C)alkyl is methyl or ethyl; (1-3C) normal alkyl is methyl, ethyl or propyl; and (3-6C)cycloalkyl is cyclopropyl, cyclobutyl, cyclopenytyl or cyclohexyl.