Patent ID: 6448397
Filing Date: 2002-09-10
Classification: A61P,C07D

Abstract:
A compound of formula I or a pharmaceutically acceptable salt thereof whereinR1 is (a) H, (b) halo, or (c) C1-6 alkyl; R2 is (c) H, (d) halo, (c) â€”OH, (d) â€”CN, (e) â€”CF3, (f) â€”O(C1-6)alkyl, (g) C1-6 alkyl, (h) C3-6 cycloalkyl, (i) â€”NR5R6, (k) â€”CONR5R6, (k) â€”SO2NR5R6, (l) â€”COOR7, or (m) phenyl, optionally substituted with halo, OH, O(C1-4) alkyl, or C1-6 alkyl; R3 is (a) â€”(CH2)mâ€”NR8R9 wherein the â€”(CH2)m â€” chain may be substituted with one or two C1-6 alkyl or C3-6 cycloalkyl; R4 is (a) aryl, or (b) heteroaryl; aryl is phenyl or naphthyl, optionally substituted with one or more R10; hetetoaryl is a radical of a five- or six-membered monocyclic aromatic ring having one or two heteroatoms each selected from the group consisting of oxygen, sulfur, and N(X), or a radical of a nine- or ten-membered ortho-fused bicyclic aromatic ring having one, two or three heteroatoms each selected from the group consisting of oxygen, sulfur, and N(X); wherein X is absent, H or C1-4 alkyl; wherein carbon atoms of heteroaryl may be substituted with one or more R10; R5 and R6 is independently (a) H, (b) C1-6 alkyl, or (c) C3-6 cycloalkyl; R7 is (a) H, (b) C1-6 alkyl, or (c) (C1-3 alkyl)-phenyl wherein phenyl may be substituted with R10; R8 and R9 is independently (a) H, (b) C1-6 alkyl, (c) C3-6 cycloalkyl, (d) C2-4 alkyl substituted with â€”OH, â€”O(C1-4 alkyl), â€”O(C1-4 alkyl)â€”NR11R12, or â€”CO2R5, (e) â€”CHO, with the proviso that only one of the R8 and R9 is CHO, the other one is hydrogen, (f) â€”(CH2)m-phenyl wherein the phenyl may be substituted with halo, or (g) R8 and R9 taken together with the nitrogen to which they are attached form a five-, six-, or seven-membered heterocyclic ring wherein the heterocyclic ring optionally has one to two additional heteroatoms selected from the group consisting of oxygen, sulfur and N(Y) and wherein the carbon atoms of the heterocyclic ring is optionally substituted with one or two R13; Y is absent or R14; R10 is (a) halo, (b) â€”OH, (c) â€”CN, (d) â€”CF3, (e) â€”O(C1-6)alkyl, (f) C1-6 alkyl, (g) C3-6 cycloalkyl, (h) â€”NR5R6, (i) â€”CONR5R6, (j) â€”SO2NR5R6, (k) â€”COOR7, or (l) phenyl, optionally substituted with halo, OH, O(C1-4) alkyl, or C1-6 alkyl; R11 and R12 is independently, (c) H, or (d) C1-4 alkyl; R13 is (a) C1-6 alkyl, (b) C3-6 cycloalkyl, (c) C2-4 alkyl substituted with â€”OH, â€”O(C1-4 alkyl), â€”O(C1-4 alkyl)â€”NR10R11, or â€”CO2R5, (d) â€”OH, or (e) oxo (&boxH;O); R14 is (a) H, (b) C1-6 alkyl, (c) C3-6 cycloalkyl, (d) C2-4 alkyl substituted with â€”OH, â€”O(C1-4 alkyl), â€”O(C1-4 alkyl)â€”NR10R11, or â€”CO2R5, (e) â€”COOR7, (f) â€”OH, or (g) oxo (&boxH;O); and m is 2, 3 or 4.