Patent ID: 6673793
Filing Date: 2004-01-06
Classification: A61P,C07D

Abstract:
A compound of formula I or a pharmaceutically acceptable salt, racemate, solvate, tautomer, optical isomer or prodrug derivative thereof wherein:each X is independently O or S; Y is Cl, F, Br, CN or NO2; R1, R2, R3 and R4 are independently a) hydrogen, b) N3, c) CN, d) fluoro, e) trifluoromethyl, f) aryl, g) het, h) C1-8 alkyl, optionally substituted with R6 or OR7, or i) R1 and R2 or R3 and R4 together with the carbon to which they are attached form C3-8cycloalkyl or het; R5 is C1-8alkyl, which may be partially unsaturated and optionally substituted with one to three N3, halo, CN, R6 or R7; R6 is a) aryl, b) het, c) SOiR8, d) OR8, e) C(&boxH;O)OR8, f) C(&boxH;O)R8, or g) NR8R9; R7 is a) P(&boxH;O)(OR10)2, b) CO(CH2)jCON(CH3)(CH2)kSO3âˆ’M+, c) an amino acid, d) C(&boxH;O)C1-6alkyl, optionally substituted by NR10R10, or e) CO(CH2)nCO2H; R8 and R9 are independently a) hydrogen, b) C3-8cycloalkyl, c) aryl, d) het, or e) C1-8alkyl which is further optionally substituted with one or more aryl, het, halo, CN, CO2R10, SOiR10, OR10, NR10R10, CF3, or C3-8cycloalkyl; R10 is a) H or b) C1-8alkyl, optionally substituted with OH or OC1-4alkyl; R11 and R12 are independently a) hydrogen b) halo, c) NO2, d) CN, e) R6, f) SOiNR8R9, or g) C1-8alkyl, which may be partially unsaturated and optionally substituted with one to three N3, halo, CN, R6 or OR7; aryl is a phenyl radical, optionally fused with a saturated or unsaturated carbocyclic or heterocyclic ring; at each occurrence, aryl may be substituted with one or more halo, CN, CO2R10, SOiR10, OR10, NR10R10, CF3, C3-8cycloalkyl, or C1-4alkyl wherein C1-4alkyl is optionally substituted with OR10; het is a four- (4), five- (5), six- (6), or seven- (7) membered saturated or unsaturated heterocyclic ring having 1, 2, or 3 heteroatoms selected from the group consisting of O, S, and NW, wherein W is hydrogen, C1-4alkyl, C(&boxH;O)OC1-4alkyl or absent, wherein het is optionally fused with a benzene ring, a carbcyclic or a heterocyclic ring; at each occurrence, het may be substituted with one or more halo, CN, CO2R10, SOiR10, OR10, NR10R10, C1-4alkyl, CF3, C3-8cycloalkyl, or oxo; at each occurrence, a cycloalkyl may be substituted with C1-4alkyl, OR10, oxo, or a spiro fused het;i is 0, 1 or 2; j is 1, 2, 3, 4, 5, or 6; k is 1, 2, 3, 4, 5, or 6; n is 1, 2, 3, 4, 5, or 6; M is sodium, potassium, or lithium; and with the following provisos:a) at least one of R1, R2, R3 and R4 is other than hydrogen; b) where R1, R2, R3 and R4 are independently C1-8 alkyl, at least one of the alkyl groups is substituted with R6 or OR7.