858results about "Dipeptides" patented technology

Compounds of the formulaeLAn-Z-X—WwD and BZ-X—WwDwherein: D is a drug moiety; L is a ligand; B is a blocking group; A is an optional acyl unit; Z is an amino acid or a peptide residue; X is an aminobenzyl ether self-immolative spacer group; W is an optional second self-immolative group; n is an integer of 0 or 1; and w is an integer of 0 or 1, and compositions of said compounds with pharmaceutically acceptable carrier, diluent and / or excipient, and methods of delivery the drug D via the compounds.

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:

The present invention discloses the compound of Formula 3 as an inhibitor of HCV protease, as well as methods for preparing the compound. In another embodiment, the invention discloses pharmaceutical compositions comprising the compound as well as methods of using them to treat disorders associated with the HCV protease.

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.

The present invention relates to tripeptide compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. In particular, the present invention provides novel tripeptide analogs, pharmaceutical compositions containing such analogs and methods for using these analogs in the treatment of HCV infection.

The present invention relates to compounds of formula I:or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

Compounds of formula (I):wherein R1 is hydroxyl or sulfonamide derivative; R2 is t-butyl or —CH2—C(CH3)3 or —CH2-cyclopentyl; R3 is t-butyl or cyclohexyl and R4 is cyclobutyl, cyclopentyl or cyclohexyl; or a pharmaceutically acceptable salt thereof, are described as useful as inhibitor of the HCV NS3 protease.

The present invention provides stable compounds prepared from boronic acid and lyophilized compounds thereof of the formula (1): in which Z1 and Z2 are moieties derived from sugar. The invention also provides methods for preparing such compounds. Lyophilizing a mixture comprising a boronic acid compound and a moiety derived from sugar produces a stable composition that readily releases the boronic acid compound upon reconstitution in aqueous media.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

This invention relates generally to a fullerene nanotube composition. The fullerene nanotubes may be in the form of a felt, such as a bucky paper. Optionally, the fullerene nanotubes may be derivatized with one or more functional groups. Devices employing the fullerene nanotubes of this invention are also disclosed.

This invention features conjugates, compositions, methods of synthesis, and applications thereof, including folate derived conjugates of nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids and antisense nucleic acid molecules.

A novel class of compounds, known as peptide nucleic acids, bind complementary ssDNA and RNA strands more strongly than a corresponding DNA. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker.

The present invention relates to new compounds that act as specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I). Those compounds are represented by the general formula and the pharmaceutical salts thereof, in which R is an acyl-residue including urethane and peptide, or a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 carbocyclic, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, all of the above residues may be optionally substituted, or is H, AS is an amino acid or a peptide mimetic thereof. The amino acid is peptide bound with R and R' is a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 cycloalkenyl, C2-C9 heterocycloalkyl, C3-C9 heterocycloalkenyl, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, whereas the heterocycloalkyl, heterocycloalkenyl, heteroaryl, heterocyclic residue can have up to 6 hetero ring atoms, an amino acid or a peptide mimetic thereof, all of the above residues my be optionally substituted, or is H.

The present invention provides methods and compositions for modification and regulation of glucose and lipid metabolism, generally to reduce insulin resistance, hyperglycemia, hyperinsulinemia, obesity, hyperlipidemia, hyperlipoprotein-emia (such as chylomicrons, VLDL and LDL), and to regulate body fat and more generally lipid stores, and, more generally, for the improvement of metabolism disorders, especially those associated with diabetes, obesity and / or atherosclerosis.

The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

The present invention includes novel compounds and methods for preventing or treating diseases associated with and / or caused by overexpression and / or uncontrolled activation of a tyrosine kinase in a subject in need thereof. In certain embodiments, the compounds of the present invention comprise a tyrosine kinase inhibitor, a linker and a ubiquitin ligase binder. The methods of the present invention comprise administering to the subject an pharmaceutically effective amount of at least one compound of the invention.

The present invention provides compounds that inhibit Factor XIa and methods of preventing or treating undesired thrombosis by administering a compound of the invention to a mammal. The invention also provides three-dimensional structures of Factor XIa and methods for designing or selecting additional Factor XIa inhibitors using these structures.

A novel class of peptide nucleic acid monomers are synthesized having chirality in the backbone. Peptide nucleic acid oligomers are synthesized to incorporate these chiral monomers.

The present invention is directed to conjugated compounds comprising a folate, or an analog or derivative thereof, and an aziridinyl epothilone analog, as further described herein, and / or pharmaceutically-acceptable salts and / or solvates thereof, useful in the treatment of cancer or other folate-receptor associated conditions.

This invention features conjugates, compositions, methods of synthesis, and applications thereof, including folate derived conjugates of nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids and antisense nucleic acid molecules.

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.

The present invention provides compounds that inhibit Factor XIa and methods of preventing or treating undesired thrombosis by administering a compound of the invention to a mammal. The invention also provides three-dimensional structures of Factor XIa and methods for designing or selecting additional Factor XIa inhibitors using these structures.

Compounds of formula (I): wherein R1, R2, R3, R4, R5, Y, n and m are as defined herein. The compounds are useful as inhibitors of HCV NS3 protease.

Pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound with the formula: where the labeled substituents are as described herein.

This invention relates to a novel class of peptides having the Formula (I): which are useful as serine protease inhibitors, and more particularly as Hepatitis C virus(HCV) NS3 protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same in the treatment of HCV infection.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles