Patent ID: 6620810
Filing Date: 2003-09-16
Classification: A61P,C07D

Abstract:
A compound of formula I: or a pharmnaceutically acceptable salt thereof wherein,R1 is (a) Cl, (b) Br, (c) CN, (d) NO2, or (e) F; R2 is (a) H, (b) R5, (c) NR7R8, (d) SO2R9, or (e) OR9; R3 is (a) H, (b) halo, (c) aryl, (d) S(O)mR6, (e) (C&boxH;O)R6, (f) (C&boxH;O)OR9, (g) cyano, (h) het, wherein said het is bound via a carbon atom, (i) OR10, (j) Ohet, (k) NR7R8 (l) SR10, (m) Shet, (n) NHCOR12, (o) NHSO2R12, or (p) C1-7alkyl which may be partially unsaturated and optionally substituted by one or more substituents of the group R11, OR13, SR10, SR13, NR7R8, halo, (C&boxH;O)C1-7alkyl, or SOmR9; R4 is (a) H, (b) halo, (c) C 1-4alkyl, or (d) R4 together with R3 form a carbocyclic or het, either of which may be optionally substituted by NR7R8, by C1-7alkyl which may be optionally substituted by OR14, or by het, wherein said het is bound via a carbon atom; R5 is (a) (CH2CH2O)iR10, (b) het, wherein said het is bound via a carbon atom, (c) aryl, (d) C1-7alkyl which may be partially unsaturated and is optionally substituted by one or more substituents selected from a group consisting of NR7R8, R11, SOmR9, and OC2-4alkyl which may be further substituted by het, OR10, or NR7R8, or (e) C3-8cycloalkyl which may be partially unsaturated and optionally substituted by one or more substituents selected from a group consisting of R11, NR7R8, SOmR9, and C1-7alkyl optionally substituted by R11, NR7R8, or SOmR9; R6 is (a) C1-7alkyl, (b) NR7R8, (c) aryl, or (d) het, wherein said het is bound via a carbon atom; R7 and R8 are independently (a) H, (b) aryl, (c) C1-7alkyl which may be partially unsaturated and is optionally substituted by one or more substituents selected from a group consisting of NR10R10, R11, SOmR9, CONR10R10, or halo, or, (d) R7 and R8 together with the nitrogen to which they are attached form a het; R9 is (a) aryl, (b) het, (c) C3-8cycloalkyl, or (d) C1-7alkyl which may be partially unsaturated and is optionally substituted by one or more substituents selected from a group consisting of NR10R10, R11, SH, CONR10R10, or halo; R10 is (a) H, or (b) C1-7alkyl optionally substituted by OH; R11 is (a) OR10, (b) Ohet, (c) Oaryl, (d) CO2R10, (e) het, (f) aryl, or (g) CN; R12 is (a) H, (b) het, (c) aryl, (d) C3-8cycloalkyl, or (e) C1-7alkyl optionally substituted by NR7R8 or R11; R13 is (a) (P&boxH;O)(OR14)2, (b) CO(CH2)nCON(CH3)â€”(CH2)nSO3âˆ’M+, (c) an amino acid, (d) C(&boxH;O)aryl, or (e) C(&boxH;O)C1-7alkyl optionally substituted by NR7R8, aryl, het, CO2H, or O(CH2)nCO2R14); R14 is (a) H, or (b) C1-7alkyl; each i is independently 2, 3, or 4; each n is independently 1, 2, 3, 4 or 5; each m is independently 0, 1, or 2; and M is sodium, potassium, or lithium; wherein any aryl is optionally substituted with one or more substituents selected from the group consisting of halo, OH, cyano, CO2R14, CF3, C1-6alkoxy, and C1-6 alkyl which maybe further substituted by one to three SR14, NR14R14, OR14, het, and CO2R14; and wherein any het is optionally substituted with one or more substituents selected from the group consisting of halo, OH, cyano, phenyl, CO2R14, CF3, C1-6alkoxy, oxo, oxime, and C1-6alkyl which maybe further substituted by one to three SR14, NR14R14, OR14, and CO2R14.