Patent ID: 6610707
Filing Date: 2003-08-26
Classification: A61P,C07D

Abstract:
A compound of the formula: or a pharmaceutically acceptable salt or solvate thereof, whereinR1 is triazolyl, isoxazolyl, oxadiazolyl, tetraazolyl, thiazolyl or thiadiazolyl, that is linked to the adjacent carbon atom by a ring carbon atom substituted by 1, 2 or 3 substituents each independently selected from C1-C6 alkyl, â€”X-aryl, X-het, â€”Xâ€”CO2R5 and â€”Xâ€”NR3R4 R2 is H, phenyl or C3-C7cycloalkyl, said phenyl or cycloalkyl being optionally benzo- or C3-C7cycloalkyl fused and optionally substituted, including in the benzo- or cycloalkyl-fused portion, by from 1 to 3 substituents each independently selected from C1-C6alkyl, C1-C6alkoxy, â€”OH, â€”(C1-C6alkylene) OH, halo and halo(C1-C6alkylene)â€”, or R2 is a 5-, 6- or 7-membered ring heterocyclic group containing either 1,2,3 or 4 nitrogen heteroatoms, or 1 oxygen or sulphur heteroatom and, optionally, 1 or 2 nitrogen heteroatoms, said heterocyclic group being saturated or partially or fully unsaturated, optionally benzo-fused and optionally substituted, including in the benzofused portion, by from 1 to 3 substituents each independently selected from C1-C6alkyl, C1-C6alkoxy, halo, halo(C1-C6alkylene- and â€”CO2R5, said R2 group being attached to W by by any mono- or bicyclic ring carbon atom or heteratom: R3 and R4 are either each independently selected from H, C1-C6alkyl C3-C6cycloalkyl and â€”(C1-C6alkylene)(C3-C6cycloalkyl), or, when taken together, represent unbranched C3-C6alkylene optionally containing 0 or NR5; R5 is H, C1-C6alkyl, C3-C6cycloalkyl, â€”(C1-C6alkyne)(C3-C6cycloalkyl) or â€”(C1-C6alkylene)aryl; A is unbranched C4 alkylene optionally substituted by C1-C6alkyl; W is a direct link, C1-C6alkylene or C2-C6alkenylene; X is direct link, C1-C6alkylene or (C0-C6alkylene)â€”Zâ€”(C0-C6alkylene)-; Y is SO2; Z is O, S, â€”CR5NR3R4â€”, â€”CR5NR5(CO2R5)â€”, â€”CR5(aryl1)â€”, â€”NR5â€”, â€”NR5CO2, â€”CONR5â€” or â€”NR5COâ€”; â€œarylâ€  is phenyl optionally substituted by from 1 to 3 substituents each independently selected from C1-C6alkyl, C1-C6alkoxy, â€”(C1-C6alkylene)(C1-C6alkoxy), halo, halo(C1-C6alkylene)â€”, â€”NR3R4, â€”(C1-C6alkylene)NR3R4, â€”(C1-C6alkylene)OH, â€”O(â€”C1-C6alkylene)NR3R4 and -alkylene)(phthalimido); â€œarylâ€  is phenyl optionally substituted by from 1 to 3 substituents each independently selected from C1-C6alkyl, C1-C6alkoxy, â€”(C1-C6alkylene)(C1-C6alkoxy), halo and halo(C1-C6alkylene)â€”; and â€œhetâ€  is a 5-, 6-, or 7-membered ring heterocyclic group containing either 1,2,3 or 4 nitrogen heteroatoms, or 1 oxygen or sulphur heteroatom and, optionally, 1 or 2 nitrogen heteratoms, said heterocyclic group being saturated or partially or fully unsaturated, or â€œhetâ€  is azetidinyl, said â€œhetâ€  being optionally substituted by from 1 to 3 substituted each independently selected from C1-C6alkyl, C1-C6alkoxy, C3-C7 cycloalkyl, â€”(C1-C6alkylene)(C1-C6alkoxy), (C1-C6alkylene)(C3-C7cycloaklyl), halo, halo(C1-C6alkylene)â€”, â€”NR3R4, â€”CO2R5, â€”(C1-C6alkylene)aryl and (C1-C6alkylene)NR3R4: with the provisos that (a) the heteroaryl group of R1 is not substituted by C0-C6alkylene)â€”Zâ€”(C0alkylene)(â€”OH or â€”C1-C4alkoxy or â€”CN or â€”NR3R4) when Z is O,S, â€”NR5â€”, â€”CONR5â€”.