Abstract: The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.

Abstract: The invention relates to new formulations of compounds having activity against HCV-associated disorders, new combinations, new methods of treatment and their use in therapy.

Abstract: The invention relates to kinase ligands and polyligands. In particular, the invention relates to ligands, homopolyligands, and heteropolyligands that modulate protein kinase D (PKD) activity. The ligands and polyligands are utilized as research tools or as therapeutics. The invention includes linkage of the ligands and polyligands to cellular localization signals, epitope tags and/or reporters. The invention also includes polynucleotides encoding the ligands and polyligands.

Abstract: In particular, in alternative embodiments, the invention provides pharmaceutical compounds and formulations comprising a family of epoxyketone compounds, which include racemic mixtures or racemates, isomers, stereoisomers, diastereoisomers, derivatives and analogs, and methods for making and using them. In alternative embodiments, pharmaceutical compositions and formulations of the invention are administered to an individual in need thereof in an amount sufficient to treat, prevent, reverse and/or ameliorate an infection, disease or condition that can be ameliorated, treated, prevented or reversed by partially or completely inhibiting a chymotrypsin-like protease or a proteasome activity, including e.g.

Abstract: The present invention relates to methods, pharmaceutical compositions and kits for use in the treatment of Adult T-cell leukemia/lymphoma. More particularly, the present invention relates to a combination of an interferon, an arsenic compound and a reverse transcriptase inhibitor for the treatment of Adult T-cell leukemia/lymphoma.

Abstract: Anti-HIV peptides and methods of use are provided. In particular, these HIV inhibitory peptides are discovered based on the Antimicrobial Peptide Database.

Abstract: The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.

Abstract: Described is a method of fabricating biologically active, unnatural polypeptides. The method includes the steps of selecting a biologically active polypeptide or biologically active fragment thereof having an amino acid sequence comprising ?-amino acid residues, and fabricating a synthetic polypeptide that has an amino acid sequence that corresponds to the sequence of the biologically active polypeptide, but wherein about 14% to about 50% of the ?-amino acid residues found in the biologically active polypeptide or fragment of step (a) are replaced with ?-amino acid residues, and the ?-amino acid residues are distributed in a repeating pattern.

Abstract: A compound is provided which has a structure I: A-B-C and a method for administering the compound is also provided for use in the prophylaxis and/or treatment of a viral infection, and in particular for preventing and/or inhibiting viral replication, in which A is a quinoline or quinoline-like group, B is a sole amino acid or a peptide or polypeptide having a given amino acid sequence, and C is an O-phenoxy group. According to one embodiment, the compound is a protease inhibitor such as a caspase inhibitor, and the inhibitor can be Q-VD-OPh (N-(2-(quinolyl)valylaspartyl-(2,6-difluorophenoxy)methyl ketone), optionally in an O-methylated form. Antiviral compositions and kits are also provided.

Abstract: The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.

Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.

Abstract: Provided herein are methods or reactivating a latent Human Immunodeficiency Virus (HIV) infection in a cell. The methods comprise modulating a level of NF-?B activity in the cell by contacting the cell with an agent that produces a transient first increase in the level of NF-?B activity without a second delayed increase in NF-?B activity. Optionally, a second agent is used to prime the reactivation. Also provided herein is an isolated Massilia bacterium or population thereof capable of producing a HIV-1 reactivating factor (HRF). Also provided are methods of culturing the Massilia bacteria. Further provided are methods of reactivating a latent Human Immunodeficiency Virus-1 (HIV-1) infection in a subject comprising administering to the subject a HIV-1 reactivating factor produced by Massilia bacteria, optionally with a priming agent.

Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.

Abstract: The invention relates to a pharmaceutical composition for treating the human immunodeficiency virus (HIV) in humans, including three or four active principles selected as: a nucleoside reverse transcriptase inhibitor (NARTI) selected from lamivudine and emtricitabine; a nucleoside or nucleotide reverse transcriptase inhibitor (NARTI) selected from didanosine, abacavir and tenofovir; and the combination of ritonavir with a protease inhibitor (PI) selected from lopinavir, fosamprenavir, atazanavir and darunavir; or an non-nucleoside reverse transcriptase inhibitor (NNRTI) selected from efavirenz and etravirine; for daily administration to said human being one to four days per week.

Abstract: Macrocylic compounds having inhibitory activity on the replication of the hepatitis C virus (HCV) of the general formula (I) X is N, CH and where X bears a double bond it is C; R1a and R1b are hydrogen, C3-7cycloalkyl, aryl, Het, C1-6alkoxy, C1-6alkyl optionally substituted with halo, C1-6alkoxy, cyano, polyhaloC1-6alkoxy, C3-7cycloalkyl, aryl, or with Het; or R1a and R1b together with the nitrogen to which they are attached form a 4 to 6 membered heterocyclic ring which may be optionally substituted; Het being a heterocyclic ring; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—CO—, —O—C(?O)—NR5a— or —O—C(?O)—NR5a—C1-4alkanediyl-; n is 3, 4, 5, or 6; p is 1, or 2; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl, amino, mono- or diC1-6alkylamino; R4 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system

Abstract: This invention relates to grassystatins A, B and C, and their isolated or purified forms. The compounds of the invention are useful as aspartic protease, gamma secretase, or metalloprotease inhibitors. Methods of using the compounds and compositions thereof are also disclosed.

Abstract: The invention relates to compounds which are polysulfated oligosaccharide derivatives having activity as inhibitors of heparan sulfate-binding proteins and inhibitors of the enzyme heparanase; methods for the preparation of the compounds; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment, lowering of blood triglyceride levels and inhibition of cardiovascular disease of a mammalian subject.

Abstract: The invention relates to (among other things) protease inhibitors containing both a water-soluble, non-peptidic oligomer and a lipophilic moiety-containing residue. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over protease inhibitor compounds lacking the water-soluble, non-peptidic oligomer and a lipophilic moiety-containing residue.

Abstract: The present invention relates to a protein which has the capacity to bind to and inhibit the viral uracil DNA glycosylase (UDG) enzyme and its use as a therapeutic agent; in particular, as an antiviral agent.

Abstract: The invention relates to non-proteolysable oligopeptides that inhibit glycoprotein 41 of the AIDS virus. More specifically, the invention relates to the identification of oligopeptides, particularly hexapeptides, (D), (L) or mixed, preferably D-hexapeptides, which inhibit the binding of a retrovirus to a target cell, thereby providing novel therapies against infection from the human immunodeficiency virus (HIV). The invention also relates to the use of said D-hexapeptides in the form of single components or complex mixtures as prophylactic or therapeutic agents for retroviral infections, especially human immunodeficiency virus type 1 (HIV-1).

Abstract: The present invention relates to compounds, in particular, dual antagonists comprising a nucleoside reverse transcriptase inhibitor (NRTI) or a nucleoside competititive reverse transcriptase inhibitor and a non-nucleoside reverse transcriptase inhibitor (NNRTI), linked together using a chemical linker, which may be used to inhibit HIV (HIV-1) reverse transcriptase and in the treatment of HIV infections, more severe cases of HIV infections, including ARC and AIDS, including reducing the likelihood of these infections and disease states.

Abstract: The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.

Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: The present invention includes methods of treatment and compositions for treating diseases related to the activity of a histone deacetylase in a subject by administering to the subject an effective amount of a modified FK228 compound comprising an amino acid conjugate which constitutes an amino thiol, a hydroxy thiol, a dithiol, or a hydroxamic acid, instead of a hydroxy-mercapto-heptenoic acid moiety in FK228.

Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: The present invention relates to methods of increasing bone formation in patient suffering from a wasting disorder by orally or intranasally administering a pharmaceutically effective amount of a leptin peptide and a pharmaceutically acceptable carrier, wherein the leptin peptide increases serum osteocalcin levels.

Abstract: Disclosed is a process for preparing a compound of formula (I) by protecting the secondary amide nitrogen atom in the compound of formula (III) to obtain (IV) wherein PGN is a suitable nitrogen protecting group, ring-closing the compound of formula (IV) by cyclizing it in the presence of a suitable catalyst in a suitable organic solvent to obtain (V), and then deprotecting the resulting compound of formula (V) to obtain (I), as outlined in the following scheme. The compounds of formula (I) are active agents for the treatment of hepatitis C viral (HCV) infections or are intermediates useful for the preparation of anti-HCV agents.

Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

Abstract: A process for the synthesis of bisfuran intermediates of formula (0) useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed. Furthermore disclosed is a HIV protease inhibitor of formula (IV) as well as various intermediates thereof.

Abstract: The present invention provides a method for providing alpha-1 antitrypsin (?1-AT) to a subject, in particular a method for treating or preventing a disorder or disease associated with ?1-AT deficiency in the subject, wherein the method comprises providing, subcutaneously, a therapeutically or prophylactically effective amount of ?1-AT to the subject. Also provided is a composition and article of manufacture comprising ?1-AT, in particular a formulation suitable for subcutaneous administration of ?1-AT.