Patent classifications
C07K5/06104
Prodrugs of riluzole and their method of use
Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.
SUGAR-DIPEPTIDE CONJUGATES AS FLAVOR MOLECULES
The present invention relates to compounds of formula (I) and compositions comprising them for use in enhancing umami taste and/or saltiness of a food product.
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SITE-SPECIFIC CHEMOENZYMATIC PROTEIN MODIFICATIONS
The present invention relates to methods and reagents for use in site-selective modification of proteins having lysine residues with functionalized peptides using a chemoenzymatic microbial transglutaminase-mediated reaction. The functionalized proteins may be used for study or therapeutic uses.
GEMINOID LIPOPEPTIDE COMPOUNDS AND THEIR USES
Disclosed are geminoid peptide-like compound according to Formula (I): R.sup.1C(=0)-Z.sub.nNR.sup.3R.sup.2 in which R.sup.1 and R.sup.2 are each independently saturated, partly saturated or unsaturated, straight, branched or cyclic alkyl chains, wherein R.sup.1 has a number of C atoms of 11 or more, preferably 11 to 19, and R.sup.2 has a number of C atoms of 12 or more, preferably 12 to 20; R3 is hydrogen or C.sub.1-C-.sub.6 alkyl; n is an integer from 1-15; each Z independently is an amino acid residue, wherein Z.sub.n comprises an N-terminus attached to C(=0) and a C-terminus that is attached to NR.sup.3, for use as a medicament.
Cyclopolyphosphazenes, Related Methods of Preparation and Methods of Use
Disclosed herein are cyclopolyphosphazenes of formula I:
##STR00001##
methods for the preparation thereof and uses thereof in adjuvant compositions.
SILANE-CONTAINING CONDENSED CYCLIC DIPEPTIDE COMPOUND, PRODUCTION METHOD THEREFOR, AND METHOD FOR PRODUCING POLYPEPTIDE COMPOUND USING SAME
The present invention provides, as a novel compound that can be utilized for efficient synthesis or the like of a polypeptide comprising various amino acids, a silane-containing condensed cyclic dipeptide compound represented by formula (A).
##STR00001##
In formula (A), each of R.sup.11, R.sup.12, R.sup.13, R.sup.21, and R.sup.22 independently represents a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a nitro group, a cyano group, or a thiol group, or a monovalent aliphatic hydrocarbon group, aromatic hydrocarbon group, or heterocyclic group that may have one or more substituents; and each of R.sup.a1 and R.sup.a2 independently represents a monovalent aliphatic hydrocarbon group or aromatic hydrocarbon group that may have one or more substituents
NMDA ANTAGONIST PRODRUGS
Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them.
Azaindoline compounds as granzyme B inhibitors
Azaindoline compounds as granzyme B inhibitors, compositions that include the compounds, and methods for using the compounds. Methods for treating cutaneous scleroderma, epidermolysis bullosa, radiation dermatitis, alopecia areata, and discoid lupus erythematosus are provided.
AZA-PEPTIDE ALDEHYDES AND KETONES
The present disclosure relates to compositions for inhibiting proteases, methods for synthesizing the compositions, and methods of using the disclosed protease inhibitors. Aspects of the invention include aza-peptide aldehyde and ketone compositions that inhibit proteases. The disclosed compounds, pharmaceutically acceptable salts, pharmaceutically acceptable derivatives, prodrugs, or combinations thereof can be used to treat disease or pathological conditions related to the activity of proteases associated with a specific disease or condition.
Matriptase inhibitors and uses thereof against orthomyxoviridae infections
The present invention provides matriptase inhibitors and compositions for treating and preventing orthomyxovirus infections such as flue infections. The present invention also provides novel compounds, compositions, methods of use, uses and kits thereof for inhibiting matriptase. Such compounds are useful for treating and prevention orthomyxovirus infections, such as flu infections, and for inhibiting tumor growth, progression and/or metastasis.