Patent ID: 6576664
Filing Date: 2003-06-10
Classification: A61P,C07C,C07D

Abstract:
A compound of the formula II: or a pharmaceutically acceptable salt form or a steroisomer thereof, wherein:R1 is selected from: â€”CO2H, â€”C(O)NHOH, â€”C(O)NHOR7, â€”SH, and â€”CH2CO2R7; R2 is selected from the formula: Uâ€”Xâ€”Yâ€”Zâ€”Uaâ€”Xaâ€”Yaâ€”Za wherein:U 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; X is absent or selected from C1-10 alkylene, C2-10 alkenylene, and C2-10 alkynylene; Y is absent or selected from O, NRa, S(O)p, and C(O); Z is absent or selected from a C3-13 carbocyclic residue substituted with 0-5 Rb 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 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, and C2-10 alkynylene; Ya is absent or selected from O, NRa, S(O)p, and C(O); Za is selected from H, a C3-13 carbocyclic residue substituted with 0-5 Rc 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; Ra, at each occurrence, is independently selected from H, C1-4 alkyl, phenyl and benzyl; Raâ€², at each occurrence, is independently selected from H, C1-4 alkyl, phenyl and benzyl; alternatively, Ra and Raâ€² taken together with the nitrogen to which they are attached form a 5 or 6 membered ring containing from 0-1 additional heteroatoms selected from the group consisting of N, O, and S; Rb, at each occurrence, is independently selected from C1-6 alkyl, ORa, C1, F, Br, I, &boxH;O, CN, NO2, NRaRaâ€², C(O)Ra, C(O)ORa, C(O)NRaRaâ€², S(O)2NRaRaâ€², S(O)pRa, CF3, and CF2CF3; Rc, at each occurrence, is independently selected from C1-6 alkyl, ORa, Cl, F, Br, I, &boxH;O, CN, NO2, NRaRaâ€², C(O)Ra, C(O)ORa, C(O)NRaRaâ€², NRaS(O)2Raâ€², S(O)2NRaRaâ€², S(O)pRa, CF3, CF2CF3, and a 5-14 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S; R3 is selected from the formula: U1â€”X1â€”Y1â€”Z1â€”U1aâ€”X1aâ€”Y1aâ€”Z1a wherein:U1 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; X1 is absent or selected from C1-10 alkylene, C2-10 alkenylene, and C2-10 alkynylene; Y1 is absent or selected from O, NRa, S(O)p, and C(O); Z1 is absent or selected from a C3-13 carbocyclic residue substituted with 0-5 Rb and piperidinyl substituted with 0-5 Rb; U1a 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; X1a is absent or selected from C1-10 alkylene, C2-10 alkenylene, and C2-10 alkynylene; Y1a is absent or selected from O, NRa, S(O)p, and C(O); Z1a is selected from H, a C3-13 carbocyclic residue substituted with 0-5 Rc 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; Ra, at each occurrence, is independently selected from H, C1-4 alkyl, phenyl and benzyl; Raâ€², at each occurrence, is independently selected from H, C1-4 alkyl, phenyl and benzyl; alternatively, Ra and Raâ€² taken together with the nitrogen to which they are attached form a 5 or 6 membered ring containing from 0-1 additional heteroatoms selected from the group consisting of N, O, and S; Rb, at each occurrence, is independently selected from C1-6 alkyl, ORa, Cl, F, Br, I, &boxH;O, CN, NO2, NRaRaâ€², C(O)Ra, C(O)ORa, C(O)NRaRaâ€², S(O)2NRaRaâ€², S(O)pRa, CF3, and CF2CF3; Rc, at each occurrence, is independently selected from C1-6 alkyl, ORa, Cl, F, Br, I, &boxH;O, CN, NO2, NRaRaâ€², C(O)Ra, C(O)ORa, C(O)NRaRaâ€², NRaS(O)2Raâ€², S(O)2NRaRaâ€², S(O)pRa, CF3, CF2CF3, and a 5-14 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S; R5 is selected from: U2â€”X2â€”Y2â€”Z2â€”U2aâ€”X2aâ€”Y2aâ€”Z2a wherein:U2 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; X2 is absent or selected from C1-10 alkylene, C2-10 alkenylene, and C2-10 alkynylene; Y2 is absent or selected from O, NRa, S(O)p, and C(O); Z2 is absent or selected from a C3-13 carbocyclic residue substituted with 0-5 Rb 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 Rb; U2a 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; X2a is absent or selected from C1-10 alkylene, C2-10 alkenylene, and C2-10 alkynylene; Y2a is absent or selected from O, NRa, S(O)p, and C(O); Z2a is selected from H, a C3-13 carbocyclic residue substituted with 0-5 Rc 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; Ra, at each occurrence, is independently selected from H, C1-4 alkyl, phenyl and benzyl; Raâ€², at each occurrence, is independently selected from H, C1-4 alkyl, phenyl and benzyl; alternatively, Ra and Raâ€²taken together with the nitrogen to which they are attached form a 5 or 6 membered ring containing from 0-1 additional heteroatoms selected from the group consisting of N, O, and S; Rb, at each occurrence, is independently selected from C1-6 alkyl, ORa, Cl, F, Br, I, &boxH;O, CN, NO2, NRaRaâ€², C(O)Ra, C(O)ORa, C(O)NRaRaâ€², S(O)2NRaRaâ€², S(O)pRa, CF3, and CF2CF3; Rc, at each occurrence, is independently selected from C1-6 alkyl, ORa, Cl, F, Br, I, &boxH;O, CN, NO2, NRaRaâ€², C(O)Ra, C(O)ORa, C(O)NRaRaâ€², NRaS(O)2Raâ€², S(O)2NRaRaâ€², S(O)pRa, CF3, CF2CF3, and a 5-14 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S; R7 is selected from: C1-C10 alkyl, alkylaryl, and E is CH2 or CO.