摘要:
The invention provides compounds of formula I, II, and III as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of formula I, II, and III are useful as anti-viral agents and/or as anti-cancer agents.
摘要:
The invention provides methods for treating hepatitis C viral infections and related viral infections, as well as compounds and compositions that are useful for treating such infections.
摘要:
Compounds represented by the formula: Wherein A is —(CH2)n—R, —CH═CH2, —CH2—CH═CH2, —O—(CH2)n—R, —CH(OH)CH3, —CH(OH)—CH2OH, —CH2—CH(OH)CH3, —CH2—CH(OH)—CH2OH, —CH(OH)—CH(OH)—CH3; R is H, OH, F, N3, NH2, CO2H, SH, alkyl, S-alkyl, O-acyl, CONH2, CONH-alkyl; Z and Z′ independently is OR′, OR2, O—(CH2)n—O-alkyl or aminoacids and esters thereof; R1 and R2 independently is H, alkyl, aryl, pivaloyloxymethyl, phthalyl or substituted phthalyl, C(R3)2OC(O) X (R4)a, R3 is —H, C1-C12 alkyl, C5-C12 aryl, C2-C12 alkenyl, C2-C12 alkynyl, C7-C12 alkenylaryl, C7-C12 alkynylaryl, or C6-C12 alkaryl, any of which is unsubstituted or is substituted with 1 or 2 halo, cyano, azido, nitro, or —OR5; R4 is —H, C1-C12 alkyl, C5-C12 aryl, C2-C12 alkenyl, C2-C12 alkynyl, C7-C12 alkenylaryl, C7-C12 alkynylaryl, or C6-C12 alkaryl, any of which is unsubstituted or is substituted with 1 or 2 halo, cyano, azido, nitro, —N(R6)2 or —OR5; R5 is C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl or C5-C12 aryl; provided that at least one R4 is not H; and a is 1 when X is CH2, or direct bond, or 1 or 2 when X is N with the proviso that when a is 2 and X is N, (a) two N-linked R groups can be taken together to form a carbocyclic or oxygen containing heterocycle, (b) one N-linked R4 additionally can be —OR5 or (c) both N-linked R4 groups can be —H; R6 is H or C1-C8 alkyl; R7 is selected from H, alkyl, alkenyl, alkynyl, aryl, acyloxyalkyl, and pivaloyloxyalkyl; n is 1-3; Y is O, S or NH; W is O or S; B is selected from the group consisting of adenine, guanine, and modified purines are provided.
摘要:
Compounds represented by the formula: , and pharmaceutically acceptable salts thereof and prodrugs thereof; wherein R1 is H, CH3, C2H5, C3H7 R2 is H, CH3, C2H5, C3H7, CH═CH2, CH2—OH, CH2F, CF3 R′2 is H, OH, NH2, NH-alkyl, F, N3, OCH3, O—C(O)CH(NH2)alkyl R3 is H, CH3, C2H5, C3H7 R′3 is H, OH, NH2, NH-alkyl, F, N3, OCH3, O—C(O)CH(NH2)alkyl R4 is H, CH3, C2H5, C3H7 At least one of R2, R3, or R4 has to be other than H, when X═NH in B R6 is H, CH3, C2H5, R7 is selected from H, alkyl, alkenyl, aryl, acyloxyalkyl, and pivaloyloxyalkyl, aminoacids, CH2CH2SC(O)alkyl; and B is represented by the following structure: X is independently NR6, O, S, R8 and R9 independently is H, NH2, OH, SH, F, Cl, Br, I, aryl, heterocycle, alkyl, alkene, alkyne, S-alkyl, S-aryl, S(O)-alkyl, SO2-alkyl, SO2NH2, SO2NH-alkyl, SO2NH-aryl, NH-alkyl, NH-aryl, N(alkyl)2, N(aryl)2, O-alkyl, O-aryl, O-heterocycle, NH-(CH2)n-aryl, NH—C(O)-alkyl, NH—C(O)-aryl are useful for inhibiting viral RNA polymerases and treating patients suffering from diseases caused by various RNA viruses.
摘要:
Two syntheses are provided; one for the preparation of (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol, and other for the preparation of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol. (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is prepared using the achiral ylide prepared from benzylamine instead of phenethylamine (Scheme 3) which provides a crystalline intermediate. The synthesis of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is achieved from (S)-diethylmalate as described in Scheme 4. A process for preparing camphor sultam is also provided.
摘要:
The invention provides compounds of Formula I: as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of Formula (I) are useful as anti-viral agents and/or as anti-cancer agents.
摘要:
The invention provides compounds of Formula I: as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of Formula (I) are useful as anti-viral agents and/or as anti-cancer agents.
摘要:
The invention provides compounds of Formula I: as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of Formula (I) are useful as anti-viral agents and/or as anti-cancer agents.