Patent ID: 6498255
Filing Date: 2002-12-24
Classification: A61K,C07D

Abstract:
A compound of the formula wherein R1 and R2 are independently selected from hydrogen, (C1-C6)alkoxy, benzyloxy, phenoxy, hydroxy, phenyl, benzyl, halo, nitro, cyano, COR5, â€”COOR5, â€”CONHR5, â€”NR5R6, â€”NR5COR6, â€”OCONR5R6, â€”NHCOOR5, (C1-C6)alkyl optionally substituted with from 1 to 3 fluorine atoms; SOpCH2-phenyl or SOp(C1-C6)alkyl, wherein p is 0, 1 or 2; pyridylmethyloxy or thienyl-methyloxy; 2-oxazolyl, 2-thiazolyl and benzenesulfonamide; wherein the phenyl moieties of said phenoxy, benzyloxy, phenyl, benzyl and benzenesulfonamide groups, the pyridyl and thienyl moieties of said pyridylmethyloxy or thienylmethyloxy and the oxazolyl and thiazolyl moieties of said 2-oxaxolyl and 2-thiazolyl may optionally be substituted with 1 or 2 substituents independently selected from halo, (C1-C4)alkyl, trifluoromethyl, (C1-C4)alkoxy, cyano, nitro and hydroxy;or R1 and R2, when attached to adjacent carbon atoms and when X is oxygen, sulfur or NR4 wherein R4 is hydrogen or (C1-C4 alkyl) may form, together with the carbon atoms to which they are attached, a group of the formula â€ƒwherein J is oxygen, sulfur or NR4, â€œaâ€  is 1 or 2, R3 is hydrogen or (C1-C6)alkyl and Q is oxygen, sulfur, NH, CHCH3, C(CH3)2, â€”CH&boxH;CHâ€”, or (CH2)l wherein l is an integer from 1 to 3; R5 and R6 are each independently selected from hydrogen, (C1-C6)alkyl, phenyl or benzyl, wherein the phenyl moieties of said phenyl and benzyl may optionally be substituted with 1 or 2 substituents independently selected from fluoro, chloro, bromo, iodo, (C1-C4)alkyl, trifluoromethyl, (C1-C4)alkoxy, cyano, nitro and hydroxy, or NR5R6 together form a 4 to 8 membered ring wherein one atom of the ring is nitrogen and the others are carbon, oxygen or nitrogen, or NR5COR6 together form a 4 to 8 membered cyclic lactam ring; L is phenyl, phenyl-(C1-C6)alkyl, cinnamyl or pyridylmethyl, wherein the phenyl moieties of said phenyl and phenyl-(C1-C6)alkyl may optionally be substituted with 1-3 substituents independently selected from (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C4)alkoxycarbonyl, (C1-C4)alkylcarbonyl â€”OCONR5R6, â€”NHCOOR5 or halo; or L is a group of the formula wherein b is an integer from 1 to 4, R13 and R14 are independently selected from hydrogen, (C1-C4)alkyl, halo and phenyl, E and F are independently selected from â€”CHâ€” and nitrogen, and G is oxygen, sulfur or NR4 wherein R4 is defined as above, with the proviso that when E and F are both nitrogen, one of R13 and R14 is absent; and R7 and R8 are independently selected from hydrogen, (C1-C6)alkyl, (C1-C6)alkoxycarbonyl, (C1-C6)alkylcarbonyl and (C1-C6)alkoxy, with the proviso that said (C1-C6)alkoxy is not attached to a carbon that is adjacent to a nitrogen; and Yâ€² is â€”CH&boxH;CHâ€”(CH2)nâ€” wherein n is an integer from 0 to 3.