Abstract: Macrocyclic peptides are disclosed having the general formula: wherein R3, R?3, R4, R6, R?, X, Q and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: The present invention relates to a process for the stereoselective enzymatic reduction of 1-halo-2-oxo-3-(protected)amino-4-substituted-butanes utilizing certain species of Rhodococcus and Brevibacterium. The product 1-halo-2-hydroxy-3-(protected)amino-4-substituted-butanes, which are useful as intermediates in the synthesis of compounds that are inhibitors of ACE, renin and HIV proteases, are obtained in high yield and, particularly, in very high diastereomeric purity. The process is advantageously highly selective for the (3S,2R) enantiomer of the product.

Abstract: This invention provides compounds of Formula I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.

Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with sulfonylureido piperazine derivatives of Formula I. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. wherein: Z is Q is selected from the group consisting of: —W— is — represents a carbon-carbon bond or does not exist; and A is NR13R14.

Abstract: The invention comprises novel azaindole intermediate compounds useful in the preparation of compounds of the class of azaindole piperazine diamide derivatives, composition thereof and their use as anti-viral agents, and particularly for treating HIV infection.

Abstract: The invention comprises substituted indole, azaindole and related heterocyclic amidopiperazine derivatives of general Formula I wherein: Q is —may represent a bond; A is selected from the group consisting of C1-6alkoxy, C1-6alkyl, C3-7cycloalkyl, phenyl, and heteroaryl; wherein said heteroaryl may be monocyclic or bicyclic and may be comprised of three to eleven atoms selected from the group consisting of C, N, NR9, O, and S, and wherein each ring of said phenyl and heteroaryl is optionally substituted with one to five same or different substituents selected from the group consisting of R19-R23; T is U is NR7, O, or S; V is C(H)kR1, O or N(R7′)k; W is CR3 or NR10; X is CR4 or NR10; Y is CR5 or NR10; Z is CR6 or NR10; k is 0 or 1; and m, n, and p are each independently 0, 1, or 2 provided that the sum of m, n, and p must equal 1 or 2; compositions thereof and their use as antiviral agents, particularly for treating HIV infection.

Abstract: The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel bicyclic diamide compounds that are neuroprotective and/or neurotrophic agents (i.e. compounds capable of stimulating growth or proliferation of nervous tissue) and that bind to immunophilins such as FKBP12 and inhibit their rotamase activity. This invention also relates to pharmaceutical compositions comprising these compounds.

Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.

Abstract: The present invention concerns novel taxane derivatives, their use as antitumor agents, and pharmaceutical formulations. The invention claims compounds of formula I and the use of compounds of formula I or pharmaceutical salts thereof as oral drugs for the treatment of human or veterinary disease. in which: R is phenyl, isopropyl, or tert butyl; R1 is —C(O)Rz in which Rz is (CH3)3CO—, (CH3)3CCH2—, CH3(CH2)3O—, cyclobutyl-, cyclohexyloxy, or (2-furyl); R2 is CH3C(O)O—.

Abstract: The novel crystalline bis hydrochloride monohydrate salt having the formula and pharmaceutical dosage forms thereof is provided having use in the treatment of respiratory syncytial viral infection.

Abstract: This invention relates to a method of treating human immunodeficiency virus (HIV) infection in a mammal comprising administering to the mammal a therapeutically effective amount of a combination of: (i) at least one cytotoxic agent and (ii) at least one non-nucleoside reverse transcriptase HIV inhibitor (NNRTI). This invention also relates to a method of treating chronic viral infections comprising administering to the mammal a therapeutically effective amount of a combination of: (i) at least one cytotoxic agent and (ii) at least one antiviral agent.

Abstract: The invention comprises compounds of the class of azaindole piperazine diamide derivatives, compositions thereof and their use as anti-viral agents, and particularly for treating HIV infection.

Abstract: The invention comprises substituted indoleoxoacetic piperazine derivatives of general Formula I, compositions thereof and their use as antiviral agents, and particularly for treating HIV infection.

Abstract: The present invention concerns antiviral compounds, their compositions, and use in the treatment of viral infections. More particularly, the invention provides benzimidazolone derivatives for the treatment of respiratory syncytial virus infection.

Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides imidazopyridine and imidazopyrimidine derivatives (Formula I) for the treatment of respiratory syncytial virus infection.

Abstract: The invention comprises compounds of the class of azaindole piperazine diamide derivatives, compositions thereof and their use as anti-viral agents, and particularly for treating HIV infection.

Abstract: The present invention concerns antitumor compounds. More particularly, the invention provides novel taxane derivatives, pharmaceutical compositions thereof, and their use as antitumor agents.

Abstract: The present invention concerns novel 7-deoxy taxane derivatives their use as antitumor agents, and pharmaceutical formulations.

Abstract: Fermentation of Nocardia sp. ATCC-202099 in the presence of a halogen- or hydroxy-substituted tryptophan precursor yields a novel corresponding halogen- or hydroxy-substituted nocathiacin compound which has broad spectrum antibiotic activity against Gram-positive bacteria and has in vivo efficacy in animals.

Abstract: Disclosed are novel pradimicin compounds which possess antifungal activity and, preferably, improved water solubility. The compounds of the invention are prepared by modifying the 4′-amino or 4′-alkylamino moieties of known pradimicin compounds.