Patent ID: 6770640
Filing Date: 2004-08-03
Classification: C07D

Abstract:
A compound of the formula whereinR1 is selected from a group consisting of hydrogen, C1-C6 alkyl, â€”CH2SCH2NHCOCH3, â€”(CH2)pâ€”A, â€”(CH2)mâ€”B, and â€”CH2â€”Dâ€”R7; wherein A is selected from a group consisting of C6-C10 aryl, C3-C9 heteroaryl, or cyclohexyl; B is selected from a group consisting of â€”N(R7)2, guanidino, nitroguanidino, â€”C(O)OR6 and â€”C(O)NR6; D is selected from a group consisting of oxy and thio; R2 is selected from a group consisting of C1-C4 alkyl, â€”(CH2)pâ€”(C3-C9) heteroaryl, and â€”(CH2)pâ€”Ar1; wherein Ar1 is selected from the group consisting of phenyl and naphthyl optionally substituted with a substituent selected from the group consisting of halogen, C1-C4 alkyl, â€”OR6, â€”N(R6)2, â€”SO2N(R6)2 and â€”NO2; R3 is selected from a group consisting of Wâ€”(CH2)mâ€”, and Qâ€”Zâ€”(CH2)mâ€”; wherein W is phthalimido; Z is selected from the group consisting of â€”Oâ€”, â€”NR6â€”, â€”C(O)NR6â€”, â€”NR6C(O)â€”, â€”NHC(O)NR6â€”, â€”OC(O)NR6â€”, â€”HNC(O)Oâ€”, and â€”SO2NR6â€”; Q is selected from the group consisting of hydrogen, and Yâ€”(CH2)nâ€”; wherein Y is selected from the group consisting of hydrogen, C6-C10 aryl, C3-C9 heteroaryl, â€”C(O)OR6, â€”N(R6)2, morpholino, piperidino, pyrrolidino, and isoindolyl; R4 is selected from a group consisting of hydrogen, â€”C(O)R7, â€”C(O)â€”(CH2)qâ€”K and â€”Sâ€”G; wherein K is selected from the group consisting of G is selected from the group consisting of R6 is selected from the group consisting of hydrogen and C1-C6 alkyl; R7 is selected from the group consisting of hydrogen, C1-C4 alkyl, and â€”(CH2)pâ€”Ar2; wherein Ar2 is selected from the group consisting of phenyl and naphthyl optionally substituted with a substituent selected from the group consisting of halogen, C1-C4 alkyl, â€”OR6, â€”N(R6)2, â€”SO2N(R6)2 and â€”NO2; R9 and R10 are each independently selected from the group consisting of C1-C4 alkyl and â€”(CH2)pâ€”Ar2; R11 is selected from the group consisting of â€”CF3, C1-C10 alkyl and â€”(CH2)pâ€”Ar2; R12 is selected from the group consisting of hydrogen, C1-C6 alkyl, â€”CH2CH2S(O)pCH3, and arylalkyl; R13 is selected from the group consisting of hydrogen, hydroxy, amino, C1-C6 alkyl, N-methylamino, N,N-dimethylamino, â€”CO2R17 and â€”OC(O)R18; wherein R17 is selected from the group consisting of hydrogen, â€”C(O)C(CH3)3, C1-C4 alkyl, â€”(CH2)pâ€”Ar2, and diphenylmethyl; R18 is hydrogen, C1-C6 alkyl and phenyl; R14 is selected from the group consisting of 1 or 2 substituents independently chosen from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkoxy, and halogen; R15 is selected from the group consisting of hydrogen, C1-C6 alkyl and â€”(CH2)pâ€”Ar2; R16 is selected from the group consisting of hydrogen and C1-C4 alkyl; V1 is selected from the group consisting of â€”Oâ€”, â€”Sâ€”, and â€”NHâ€”; V2 is selected from the group consisting of â€”Nâ€” and â€”CHâ€”; V3 is selected from the group consisting of a bond and â€”C(O)â€”; V4 is selected from the group consisting of â€”(CH2)wâ€²â€”, â€”Oâ€”, â€”Sâ€”, â€”NR7â€”, and â€”NC(O)R11 â€”; Xâ€² is selected from the group consisting of â€”CHâ€” and â€”Nâ€”; m is an integer from 2-4; n is an integer from 0-4; p is an integer from 0-2; t is an integer from 1-2; w is an integer from 1-3; wâ€² is an integer from 0-1; or a pharmaceutically acceptable salt, stereoisomer or hydrate thereof.