摘要:
.beta.-Lactams having a substituted hydroxymethylene group at the position .alpha. to the lactam carbonyl group are prepared by reaction of an .alpha.-halo-.beta.-lactam with zinc or zinc amalgam in an anhydrous aprotic medium to produce an intermediate which in situ reacts with an appropriate aldehyde or ketone.Also described are noval penicillins and cephalosporins having useful antibacterial activity.
摘要:
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要:
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要:
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要:
The present invention is directed to certain diaryl amide compounds as NS3-Serine protease inhibitors of hepatitis C virus. A particularly preferred compound is of the formula:
摘要:
A process for producing compounds of the formula: is disclosed. The compound of formula 1.0 is produced by: (1) separating the atropisomers of to obtain the atropisomers (2) heating the atropisomer of formula 2.0B at a suitable temperature in a suitable solvent to obtain a mixture of atropisomers of formulas 2.0A and 2.0B; (3) separating the atropisomers of formulas 2.0A and 2.0B of step (2); and (4) reducing the atropisomer of formula 2.0A to obtain a compound of formula 1.0. Preferably, R1 is Br, R2 is Cl and R3 is Br. Also disclosed is the (+)-atropisomer of formula 2.0 wherein R1 is Br, R2 is Cl and R3 is Br.
摘要:
Ribavirin derivatives represented by formula I wherein at least one of R2, R3 or R5 is a straight or branched chain polyalkylene oxide polymer conjugate, and pharmaceutical compositions containing them as well as their use to treat patients having susceptible viral infections, alone and in combination with a therapeutically effective amount of interferon-alpha are disclosed.
摘要:
A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two groups convertible in vivo into hydroxy moieties, (e.g., a polyether ester, amino acid ester or phosphate ester) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.
摘要:
This invention relates to tri- and tetra-substituted-oxetanes, e.g. (.+-.)-cis- and (.+-.)-trans-2-[(4-(4-isopropylpiperazin-1-yl)phenoxy)methyl]-4-(2,4-dihalophenyl)-4-[1H-1,2,4-triazol-1-yl)-methyl]oxetane and tri- and tetra-substituted-tetrahydrofurans, e.g. (.+-.)-cis- and (.+-.)-trans-1-[4-[[2-(2,4-dihalophenyl)tetrahydro-2-[(1H-azol-1-yl)methyl]-5-furanylmethoxy]phenyl]-4-yl-1-substituted piperazine-3-one and related derivatives which exhibit antifungal and antiallergy activities, pharmaceutical composition thereof, methods of their use in treating or preventing susceptible fungal infections and allergic reactions in a host including warm-blooded animals such as humans.
摘要:
The disclosed invention is compounds represented by the formulaZ--X--Q--Y--W, IZ--X--Q--Y--W'--Y--Q--X--Z IIand pharmaceutically acceptable acid addition salts and quarternary amine salts thereof, whereinZ is phenyl, naphthyl or adamantyl; substituted phenyl wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, methylsulfonyl, isoxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, loweralkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl; 5 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen and one carbon in the ring, wherein the substituents are one or more of carboxyl, hydroxymethyl, loweralkyl, loweralkylcarbonyl or aryl lower alkyl; or tertiary butyl;X and Y are each independently a bond, -O-, ##STR1## Q is a divalent substituted or unsubstituted straight or branched chain lower alkanediyl, -lower alkanedinyl- cycloalkanediyl- lower alkanediyl-, lower alkendiyl, lower alkynediyl, phenylene, tetrahydrofurandiyl or tetrahydropyrandiyl;W is a monovalent substituted or unsubstituted aromatic heterocyclic single or fused ring containing from 5 to 10 ring atoms, at least one hetero atom of which is a nitrogen atom, wherein the substituents are hydroxy, amino, carbamoyl, carboxyl, nitrile, nitro, oxo, lower alkoxy carbonyl, halogen, sulfamyl, lower alkyl, lower alkylthio, lower alkoxy, hydroxyloweralkyl, lower alkoxycarbonylloweralkyl, amino loweralkyl, carboxyloweralkyl, guanidino, thioureido, lower alkylsulfonylamino, aminocarbonylloweralkyl, allyloxycarbonylmethyl or carbamoyloxylowralkyl; andW' is divalent W.The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.