Patent ID: 6610731
Filing Date: 2003-08-26
Classification: C07D

Abstract:
A compound of formula I: or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein; A is â€”CONHOH; ring B is a 4 membered cyclic amide; R1 is â€”Zâ€”Uaâ€”Xaâ€”Yaâ€”Za; Z is phenylene substituted with 0-5 Rb; Ua is absent or is selected from: O, NRa, C(O)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; 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 and substituted with 0-5 Rc; R2 is amino or methyl; R, at each occurrence, is independently selected from H, CH3, CH2CH3, CH&boxH;CH2, CH&boxH;CH3, and CH2CH&boxH;CH2; Râ€², at each occurrence, is independently selected from H, CH3, CH2CH3, and CH(CH3)2; R3 is selected from Q, C1-10 alkylene-Q, C2-10 alkenylene-Q, C2-10 alkynylene-Q, (CRRâ€²)râ€²O(CRRâ€²)râ€”Q, (CRRâ€²)râ€²NRa(CRRâ€²)râ€”Q, (CRRâ€²)rC(O)(CRRâ€²)râ€”Q, (CRRâ€²)rC(O)O(CRRâ€²)râ€”Q, (CRRâ€²)râ€²OC(O)(CRRâ€²)râ€”Q, (CRRâ€²)rC(O)NRa(CRRâ€²)râ€”Q, (CRRâ€²)râ€²NRaC(O)(CRRâ€²)râ€”Q, (CRRâ€²)râ€²OC(O)O(CRRâ€²)râ€”Q, (CRRâ€²)râ€²OC(O)NRa(CRRâ€²)râ€”Q, (CRRâ€²)râ€²NRaC(O)O(CRRâ€²)râ€”Q, (CRRâ€²)râ€²NRaC(O)NRa(CRRâ€²)râ€”Q, (CRRâ€²)râ€²S(O)p(CRRâ€²)râ€”Q, (CRRâ€²)râ€²SO2NRa(CRRâ€²)râ€”Q, (CRRâ€²)râ€²NRaSO2(CRRâ€²)râ€”Q, (CRRâ€²)râ€²NRaSO2NRa(CRRâ€²)râ€”Q, (CRRâ€²)râ€²NRaC(O)(CRRâ€²)râ€³NHQ, (CRRâ€²)râ€²NRaC(O)(CRRâ€²)rNHC(O)ORa, and (CRRâ€²)râ€²NRaC(O)(CRRâ€²)rNHC(O)(CRRâ€²)rNHC(O)ORa, provided that R3 is other than H; Q is selected from H, a C3-13carbocyclic 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 and substituted with 0-5 Rb; R4 is H; 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; Raâ€³, at each occurrence, is independently selected from H, C1-4 alkyl, benzyl, C3-7 carbocyclic residue, or a 5 to 6 membered heteroaromatic ring containing 1-4 heteroatoms. selected from the group consisting of N, O, and S; 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)Raâ€³, 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, NRaC(O)NRaRaâ€², S(O)2NRaRaâ€², S(O)pRa, CF3, CF2CF3, â€”CH(&boxH;NOH), â€”C(&boxH;NOH)CH3, (CRRâ€²)sO(CRRâ€²)sâ€²Rd, (CRRâ€²)sS(O)p(CRRâ€²)sâ€²Rd, (CRRâ€²)sNRa(CRRâ€²)sâ€²Rd, phenyl, and a 5-14 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S; Rd, at each occurrence, is independently selected from phenyl substituted with 0-3 Rb, biphenyl substituted with 0-2 Rb, naphthyl substituted with 0-3 Rb and a 5-10 membered heteroaryl system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S and substituted with 0-3 Rb; p, at each occurrence, is selected from 0, 1, and 2; r, at each occurrence, is selected from 0, 1, 2, 3, 4, and 5; râ€², at each occurrence, is selected from 0, 1, 2, 3, 4, and 5; râ€³, at each occurrence, is selected from 1, 2, and 3; s, at each occurrence, is selected from 0, 1, 2, and 3; and, sâ€², at each occurrence, is selected from 0, 1, 2, and 3.