Patent ID: 6953788

Claim:
A compound of the formula wherein R 1 is C 1 -C 6 alkyl, a W—(CH 2 ) m — group, or a Q—Z—(CH 2 ) m — group wherein W is phthalimido; Z is a bond or is oxy, NR 6 , C(O)NR 6 , NR 6 C(O), NHC(O)NR 6 , OC(O)NR 6 , HNC(O)O, or SO 2 NR 6 ; Q is hydrogen, or a Y—(CH 2 ) n — group wherein Y is hydrogen, C 6 -C 10 aryl, a cyclic or bicyclic, aromatic assemblage of three to nine carbon atoms and from 1 to 3 nitrogen, oxygen, or sulfur atoms, —C(O)OR 6 , —N(R 6 ) 2 , morpholino, piperidino, pyrrolidino, or isoindolyl; R 2 is C 1 -C 4 alkyl, a —(CH 2 ) p —(C 3 -C 9 )heteroaryl group, or a —(CH 2 ) p —Ar 1 group wherein Ar 1 is phenyl or naphthyl optionally substituted with a substituent selected from the group consisting of halogen, C 1 -C 4 alkyl, —OR 7 , —N(R 6 ) 2 , SO 2 N(R 6 ) or —NO 2 ; R 3 is hydrogen, C 1 -C 6 alkyl, —CH 2 SCH 2 NHCOCH 3 , a —(CH 2 ) p —A group, a —(CH 2 ) m —B group or a —CH 2 —D—R 7 group wherein A is C 6 -C 10 aryl, C 3 -C 9 heteroaryl, or cyclohexyl; B is —N(R 7 ) 2 , guanidino, nitroguanidino, —C(O)OR 6 or —C(O)NR 6 ; and D is oxy or thio; R 4 is hydrogen or a —(CH 2 ) m —S(O) p X′(R 6 ) 2 group; R 5 is hydrogen, C 1 -C 6 alkyl or R 4 and R 5 taken together with the nitrogen atom to which they are attached form piperidino, pyrrolidino, or isoindolyl; R 6 is hydrogen or C 1 -C 6 alkyl; R 7 is hydrogen, C 1 -C 4 alkyl, or a —(CH 2 ) p —Ar 2 group wherein Ar 2 is phenyl or naphthyl optionally substituted with a substituent selected from the group consisting of halogen, C 1 -C 4 alkyl, —OR 7 , —N(R 6 ) 2 , SO 2 N(R 6 ) 2 or —NO 2 ; R 8 is hydrogen, —C(O)R 7 , a —C(O)—(CH 2 ) q —K group or a —S—G group, wherein K is selected from the group consisting of G is selected from the group consisting of R 9 and R 10 are each independently C 1 -C 4 alkyl or a —(CH 2 ) p —Ar 2 group; R 11 is —CF 3 , C 1 -C 10 alkyl or a —(CH 2 ) p —Ar 2 group; R 12 is hydrogen, C 1 -C 6 alkyl, —CH 2 CH 2 S(O) n CH 3 , or arylalkyl; R 13 is hydrogen, hydroxy, amino, C 1 -C 6 alkyl, N-methylamino, N,N-dimethylamino, —CO 2 R 17 or —OC(O)R 18 wherein R 17 is hydrogen, —CH 2 O—C(O)C(CH 3 ) 3 , C 1 -C 4 alkyl, a —(CH 2 ) p —Ar 2 group or diphenylmethyl and R 18 is hydrogen, C 1 -C 6 alkyl or phenyl; R 14 is 1 or 2 substituents independently chosen from the group consisting of hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, or halogen; R 15 is hydrogen, C 1 -C 6 alkyl or a —(CH 2 ) p —Ar 2 group; R 16 is hydrogen or C 1 -C 4 alkyl; V 1 is O, S, or NH; V 2 is N or CH; V 3 is a bond or —C(O)—; V 4 is —(CH 2 ) w′″ , O, S, NR 7 , or NC(O)R 11 ; X and X′ are each independently CH or N; m is an integer 2-4; n is zero or an integer 1-4; p is zero or an integer 1-2; q is zero or an integer 1-5; t is an integer 1-2; w is an integer 1-3; and w′ is zero or an integer 1; or a pharmaceutically acceptable salt, stereoisomer or hydrate thereof.