Patent ID: 7625892

Claim:
A pharmaceutical composition comprising as active principle at least one among the 3-aza-bicyclo[3.2.1]octane derivatives of general formula (I), or mixtures thereof wherein: R 1 is H, R 2 is selected from the group consisting of H, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, cycloalkyl, aryl, arylC 1-8 alkyl, heterocycleC 1-8 alkyl, aminoC 1-8 alkyl, aminoaryl, C 1-8 alkyloxyaryl, hydroxyaryl, hydroxyC 1-8 alkyl, carboxyC 1-8 alkyl, methyloxycarbonylC 1-8 alkyl, carboxyaryl, carboalkyloxyaryl, alkylcarbamoylaryl and -(side chains of amino acids), or R 3 is selected from the group consisting of H, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, cycloalkyl, aryl, arylC 1-8 alkyl, heterocycleC 1-8 alkyl, RR′NC 1-8 alkyl, RR′Naryl, RO—C 1-8 alkyl, RO(O)C—C 1-8 alkyl, R(O)C—C 1-8 alkyl, RC(O)O—C 1-8 alkyl, RC(O)N(R)C 1-8 alkyl, RO-aryl, RO(O)C-aryl, R(O)C-aryl RC(O)O-aryl, RC(O)N(R)aryl, —CH(amino acid side-chain)CO 2 R, —CH(amino acid side-chain)C(O)NR, —CH(CO 2 R)— amino acid side-chain, CH(CONRR′)— amino acid side-chain, Fmoc, Boc and Cbz, R 4 , and R 5 , equal or different amongst each other, are selected from the group consisting of H, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkinyl, cycloalkyl, aryl, heterocycle, arylC 1-8 alkyl and heterocycleC 1-8 alkyl, R 6 is selected from the group consisting of H, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, cycloalkyl, aryl, arylC 1-8 alkyl, heterocycle, heterocycleC 1-8 alkyl; —C(O)R, —C(O)OR, —C(O)NRR′, CH 2 OR, CH 2 NRR′, —C(O)NH—CH(amino acid side-chain)C(O)OR, CH 2 NR-Fmoc, CH 2 NR-Boc and CH 2 NR—CBz, R and R′, equal or different between each other, are selected from the group consisting of H, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, cycloalkyl, aryl, heterocycle, arylC 1-8 alkyl; heterocycleC 1-8 alkyl; protecting group, —C(O)CH-(amino acid side-chain)-NHT, —NH—CH(amino acid side-chain)COOT and —CH(amino acid side-chain)COOT, where T is selected from between H and C 1-8 alkyl; X is O, α is a double bond, Y and Z, equal or different from each other, are selected from the group consisting of O, S, SO, SO 2 and N—R, wherein R is as above defined; Q is selected from the group consisting of C═O, CH 2 , CO—NH—CH (amino acid side-chain)-CO, CONR(CH 2 ) n CO, CONR—C 2-8 alkenyl-CO C(O)O(CH 2 )CO, CH 2 OC(O)(CH 2 )CO, and CH 2 NRC(O)(CH 2 ) n CO, wherein n is comprised between 2 and 6, and R is as above defined, Q′ is selected from the group consisting of C(O)OCH 2 , C(O)NRCH 2 , CH 2 OC(O), CH 2 NRC(O), CONR(CH 2 ) n NRCO, CONR—C 2-8 alkenyl-NRCO, C(O)O(CH 2 ) n NRCO, CONR(CH 2 ) n OC(O), CH 2 OC(O)(CH 2 ) n OC(O)CH 2 , CH 2 NRC(O)(CH 2 ) n NRC(O)CH 2 , CH 2 OC(O)(CH 2 ) n NRC(O)CH 2 , CH 2 NRC(O)(CH 2 ) n OC(O)CH 2 , CH 2 NR(CH 2 ) n NRCH 2 , CH 2 O(CH 2 ) n OCH 2 , CH 2 O(CH 2 ) n NRCH 2 , and CH 2 NR(CH 2 ) n OCH 2 , wherein n is comprised between 2 and 6, and R is as above defined, and where the groups alkyl, alkenyl, alkynyl, cycloalkyl, aryl and the heterocyclic groups above reported, are possibly substituted; and a pharmaceutically acceptable excipient or diluent.