| abstract |
Bis-aminomethylcarbonyl protease inhibitors are provided, comprising a compound of the formula (I): R1 and R2 are independently H or C1-6 alkyl, as long as R1 and R2 are not both C1-6 alkyl; formula ( II) R3 is chosen from the group formed by CH2CH (CH3) 2, CH2CH2CH3, CH3CH = CH2 or CH2Ph; R4 is chosen from the group consisting of: C0-6 alkyl; N-piperizine; N-tetrahydroisoquinoline; C0-6 alkyl substituted with phenyl, thiophene, benzothiazole, 2-, 3-, 4-, 5-, 6-or 7-quinoline, naphthyl, 1- (7-nitro-2, 1, 3-benzoxadiazol-4- il) -L-prolyl, (C0-6) alkyl pyrazole, N-Cbz-2- (N, N-dimethylamino) ethylglycyl-, N-methylpyrrole, benzoxazole, benzyloxy, C1-6 alkoxy; 2, 3, or 4-pyridinyloxy; adamantyl, thieno [3,2-b] thiophene; phenyl; thiophene; benzothiophene; benozofuran; benzothiazole; 2-, 3-, 4-, 5-, 6- or 7-quinoline; naphthyl; and benzoxazole, each independently substituted with one or more of the groups C1-6 alkyl, halogen, nitro, cyano, hydroxy, C1-6 alkoxy, trifluoromethyl, carboxy, carboxy-C1-6 alkyl ester, alkyl ( C0-6) 2N-C0-6 alkyl, (C0-6) alkyl 2N-C0-6 alkoxy, N- (C0-C6) -N-piperizine, N- (N-alkyl (C0-C6) N-piperidine ) -4-(C0-6) -amine, (C0-6) 2N-(C0-6) -amine, N-morpholino-C0-6 alkyl, N-morpholino-C0-6 alkyl, N -morpholino-C0-6 alkoxy, phenyl, thiophene, benzothiazole, 2, 3, 4, 5, 6 or 7-quinoline, naphthyl, (C0-6) alkyl pyrazole, N-methyl-pyrrole, benzoxazole; benzyloxysubstituted with one or more (C1-6) alkyl, halogen, nitro, cyano, hydroxy, (C1-6) alkoxy, trifluoromethyl, carboxyl, carboxy (C1-6) alkyl ester, phenyl, thiophene, bentiazole, 2, 3, 4, 5 groups or 7 quinolein, naphthyl, (C0-6) alkyl pyrazole, N-methyl-pyrrole, and benzoxazole; and pyrazine; pyrimidine; 2,7-dimethylpyrazolo [1,5a] pyrimidine and 4,7-dimethylpyrazolo [5,1-c ] [1,2,4] -triazine R6 is chosen from the group formed by phenyl and phenyl substituted with C0-6 alkyl, N-piperidine, benzofuran; or 2,3 or 4 pyridine; Q is formula (III) in which R7 is selected from the group consisting of phenyl and phenyl substituted with (C0-C6) alkyl, N-piperidine, benzofuran; or 2, 3 or 4 pyridine; R8 is chosen from the group consisting of H, CH2Ch (CH3) 2, CH2CH2CH3 and CH2CH = CH2, CH2Ph, when R9 is H; or R8 and R9 |