| abstract |
Compounds of formula 1 and 1-1, n n n wherein R 1 is hydrogen, hydroxy, amino or halogen, R 2 is hydrogen, hydroxy, or halogen and R 3 is hydrogen (Formula 1) or R 1 is hydrogen and R 2 and R 3 taken together with the ethenylene group connecting them form phenyl, pyrrole, pyrroline, oxopyrroline, pyrazole, triazole, or imidazole (Formula 1-1), A is n n n R 4 R 5 are hydrogen, methyl, ethyl or halogen except that R 4 r 5 cannot both be hydrogen; and n 1) B is hydrogen, or lower alkyl; or n 2) B is n n n where R 6 R 7 R 8 and R 9 are independently hydrogen, hydroxy, aminosulfonyl, halogen, lower alkoxy, cyano, amino, lower alkyl, lower alkyl amino, or nitro; n or 3) B is n n n where R 10 is hydrogen, hydroxy, halogen, or lower alkyl and C is a five- or six- membered ring with 0 to 3 heteroatoms which heteroatoms are selected from nitrogen, oxygen, and sulfur, which ring may be unsubstituted or mono- or di- substituted with lower alkyl, cycloalkyl, amino, or substituted amino; n 4) B is n n n where X and Y are independently methylene or nitrogen; or n 5) B is n n n where at leat one of T, U, V, or W is nitrogen, and any of T, U, V or W which is carbon may be substituted with lower alkyl, lower alkyl amino, lower alkoxy, hydroxy, aminosulfonyl, halogen, cyano, amino, or nitro; or n 6) B is n n n where Y is carbon or nitrogen; n or n 7) B is a five-membered aromatic ring with 1 to 3 heteratoms selected from nitrogen, oxygen, and sulfur which ring may be unsubstituted or mono- or di-substituted with lower alkyl, cycloalky, trifluoroloweralkyl, amino, halogen, substituted amino, or which ring may be fused with a 5 or 6 membered aromatic ring containing 0 to 3 heteroatoms which heteroatoms are selected from nitrogen, oxygen, and sulfur; and pharmaceutically acceptable salts thereof, and related prodrugs, pharmaceutical compositions and methods of treatment, which compounds are useful for treating psoriasis. |