Patent ID: 6593361
Filing Date: 2003-07-15
Classification: A61K

Abstract:
A method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with one or more said adenomas a non-toxic therapeutically effective amount of compound of formula III or a pharmaceutically acceptable salt thereof wherein:R1 is selected from the group consisting of (a) S(O)2CH3, (b) S(O)2NH2, (c) S(O)2NHC(O)CF3, (d) S(O)(NH)CH3, (e) S(O)(NH)NH2, (f) S(O)(NH)NHC(O)CF3, R2 is selected from the group consisting of (a) C3, C4, C5, C6, and C7, cycloalkyl, (b) mono-, di- or tri-substituted phenyl wherein the substituent is selected from the group consisting of (1) hydrogen, (2) halo, (3) C1-6alkoxy, (4) C1-6alkylthio, (5) CN, (6) CF3, (7) C1-6alkyl, (8) N3, (9) â€”CO2H, (10) â€”CO2â€”C1-4alkyl, (11) â€”C(H)(R6)â€”OH, (12) â€”C(H)(R6)â€”Oâ€”C1-4alkyl, and (13) â€”C1-6alkyl-CO2H; (c) mono-, di- or tri-substituted heteroaryl wherein the heteroaryl is a monocyclic aromatic ring of 5 atoms, said ring having one hetero atom which is S, O, or N, and optionally 1, 2, or 3 additional N atoms; or â€ƒthe heteroaryl is a monocyclic ring of 6 atoms, said ring having one hetero atom which is N, and optionally 1, 2 or 3 additional N atoms; said substituents are selected from the group consisting of (1) hydrogen, (2) halo, including fluoro, chloro, bromo and iodo, (3) C1-6alkyl, (4) C1-6alkoxy, (5) C1-6alkylthio, (6) CN, (7) CF3, (8) N3, (9) â€”C(H)(R6)â€”OH, (10) â€”C(H)(R6)â€”Oâ€”C1-4alkyl; R5 and R5â€² are each hydrogen, R6 is selected from the group consisting of (a) hydrogen, (b) C1-6alkyl.