| abstract |
The present application describes new lactams and their derivatives of Formula I) or its salt acceptable for pharmaceutical or stereoisomer use, where A is selected from COR5, -CO2H, CH2CO2H, -C02R6, -CONHOH, -CONHOR5, CONHOR6, NHRa -N (OH ) COR5, -SH, -CH2SH, -SO2NHRa, SN2H2Ra, PO (OH) 2, and PO (OH) NHRa; elanillo B is a 4-8 membered cyclic amide that contains between 0 - 3 additional heteroatoms selected from O, NRa and S (O) p, 0-1 additional carbonyl groups and 0 - 1 double ligatures, R1 is selected from U-X - Y -Z - Ua, Xa, Ya, Za where U is absent or selected from: O, NRa, C (O), C (O) O, OC (O), C (O) NRa, NRa C ( O), OC (O) O, OC (O) NRa, NRaC (O) O, NRaC (O) NRa, S (O) p, S (O) pNRa, NRaS (O) p and NRaSO2NRa; X is absent or selected from H, C1-10 alkylene, C2-10 alkenylene, C2-10 alkynylene; Y is absent or is selected from H, O, NRa, S (O) p, C (O); Z is absent or selected from H, a C3-13 carbocyclic residue substituted with 0-5 Rb and a 5-14 membered heterocyclic system containing 1-4 heteroatoms selected from the group consisting of N, O and S substituted with 0-5 Rb; Ua is absent or is selected from: O, NRa, C (O), C (O) O, OC (O), C (O) NRa, NRaC (O), OC (O) O, OC (O) NRa , NRaC (O) O, NRaC (O) NRa, S (O) p, S (O) pNRa, NRaS (O) p and NRaSO2NRa; Xa is absent or selected from C1-10 alkylene, C2-10 alkenylene, C2-10 alkynylene; Ua is absent or is selected from O, NR exp.a, S (O) p, and C (O): Za se selects between H, a C3-13 carbocyclic residue, substituted with 0-5Rcy and a 5-14 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O and S substituted with 0-5 Rc; R2 is selected from H, Q, C1-10 alkylene-Q, C2-10 alkenylene Q, C2-10 alkynylene-Q, (CRR) r. or (CRR) r, -Q (CRR) r, NRa (CRR) r - Q, (CRR) rNRa (CRR) r -Q, (CRR) r, -Q, (CRR) rNRa C (O) (CRR ), -Q (CRR) r, C (O) NRa (CRR) r - Q, (CRR) r C (O) (CRR) r - Q, (CRR) r, C (O) or (CRR) r - Q |