Patent ID: 6335358
Filing Date: 2002-01-01
Classification: A61K,A61P,C07D,C12N

Abstract:
A pharmaceutical composition comprising a compound having the following formula wherein Z1 is O, S, SO2, NH, or NRa, Ra being C1-6 alkyl; X1 is O, S, CH2, two singly bonded H, CH(Rb) in the E or Z configuration, or C(Rb) (Rc) in the E or Z configuration, each of Rb and Rc, independently, being C1-6 alkyl, C6-12 aryl, C3-8 cycloalkyl, C3-8 heteroaryl, C3-8 heterocyclic radical, or halogen, provided that when Z1 is SO2, X1 is two singly bonded H; Z2 is CHR1 in the (R) or (S) configuration, R1 being H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, hydroxyl, halogen, a side chain of a naturally occurring &agr;-amino acid, ORd, SRd, or NRdRe (each of Rd and Re, independently, being H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, or C2-5 alkynyl); Z3 is O, S, NH, or NRj, wherein Rj is C1-6 alkyl; X2 is O or S; and A1 is H, the side chain of any naturally occurring &agr;-amino acid, or is of the following formula, â€”(CH2)mâ€”Yâ€”(CH2)nâ€”R3X3 â€ƒwherein Y is O, S, C&boxH;O, C&boxH;S, â€”(CH&boxH;CH)â€”, vinylidene, â€”CH&boxH;NORh, â€”CH&boxH;NNRiRiâ€², sulfonyl, methylene, CHX4 in the (R) or (S) configuration, or deleted, X4 being halogen, methyl, halomethyl, ORh, SRh, NRiRiâ€², â€”NRi(ORh), or â€”NRi(NRiRiâ€²), wherein Rh is selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, and C2-6 alkynyl, and each of Ri and Riâ€², independently is selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-10 acyl; m is 0, 1, 2, or 3, and n is 0, 1, 2, or 3; and R3 is straight chain or branched C1-8 alkylidene, straight chain or branched C1-8 alkylene, C3-10 cycloalkylidene, C3-10 cycloalkylene, phenylene, C6-14 arylalkylidene, C6-14 arylalkylene, or deleted, and X3 is H, hydroxyl, thiol, carboxyl, amino, halogen, (C1-6 alkyl)oxycarbonyl, (C7-14 arylalkyl)-oxycarbonyl, or C6-14 aryl; or R3 and X3 taken together are the side chain of any naturally occurring &agr;-amino acid; and a pharmaceutically acceptable carrier.