Patent classifications
C07K5/0804
BRONCHIAL EMBOLIZATION MATERIAL
A material for endobronchial occlusion capable of repairing or replacing tissue is disclosed. The material contains a protein (A), wherein the protein (A) contains at least one of a polypeptide chain (Y) or a polypeptide chain (Y′), a total number of the polypeptide chain (Y) and the polypeptide chain (Y′) in the protein (A) is 1 to 100, the polypeptide chain (Y) is a polypeptide chain consisting of 2 to 200 tandem repeats of at least one amino acid sequence (X) among an amino acid sequence VPGVG, an amino acid sequence GVGVP 4, GPP, GAP, and an amino acid sequence GAHGPAGPK, the polypeptide chain (Y′) is a polypeptide chain in which each of a total of 5% or less of amino acids in the polypeptide chain (Y) is replaced by at least one of a lysine residue or an arginine residue, with a total number of the lysine and arginine residues being 1 to 100.
NOVEL MACROCYCLIC ANTIVIRAL AGENTS
The present invention discloses macrocyclic compounds of Formula (I), and pharmaceutically acceptable salts, thereof:
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which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.
Cyclic Peptide Compound Simulating Natural Product Structure, And Method For Preparation Thereof
Provided are a cyclic peptide compound simulating a natural product structure- and a method for preparation thereof. The method is: the compound of formula I, a divalent palladium catalyst, and a silver salt undergoing an intramolecular arylation in a solvent under heating and stirring to construct a cyclic peptide, to generate the compound of formula II, in which the arylation sites are diverse, and can be extended to the side chain γ-position methyl or methylene of the majority hydrophobic amino acids to perform intramolecular arylation, thus overcoming the previous defect of the restriction of the types of selectable amino acids, and effectively constructing a novel aromatic ring-supported cyclic peptide compound. The aromatic ring support structure can form a novel 3D structure similar to a natural product, and provide a very favorable support for the subsequent construction of a cyclic peptide molecular library and high-throughput drug screening.
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MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
HCV NS3 protease inhibitors
The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. ##STR00001##
Homo- and heterodimeric SMAC mimetic compounds as apoptosis inducers
The present invention relates to conformationally constrained homo- and heterodimeric mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
Compounds for the treatment and/or care of the skin and/or mucous membranes and their use in cosmetic or pharmaceutical compositions
Compounds of general formula (I): R.sub.i—W.sub.n—X.sub.m-AA.sub.i-AA.sub.2-AA.sub.3-AA.sub.4-AA.sub.5-AA.sub.6-Y.sub.p—Z.sub.q—R.sub.2 (I) their stereoisomers, mixtures thereof and/or their cosmetically or pharmaceutically acceptable salts, preparation processes, cosmetic and/or pharmaceutical compositions which contain them and their use in medicine, particularly in the treatment and/or prevention of pain, inflammation, itching, pigmentation disorders and angiogenic skin disorders, and in processes of treatment and/or care of the skin and/or mucous membranes.
HEPATITIS C VIRUS NS3/4A PROTEASE INHIBITORS
The invention provides novel classes of HCV therapeutics that are orally available, safe and effective HCV NS3/4A protease inhibitors and are less susceptible to drug resistance than existing therapeutics. The invention also relates to pharmaceutical composition of these compounds and methods of preparation and use thereof.
METHODS OF PREPARING CYTOTOXIC BENZODIAZEPINE DERIVATIVES
The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.
PEPTIDE INHIBITORS OF TIGHT JUNCTION PERMEABILITY
Novel compounds and methods for the inhibition of biological barrier permeability and for the inhibition of peptide translocation across biological barriers are identified. Assays for determining modulators of biological barrier permeability and for peptide translocation across biological barriers are provided. Methods for treating diseases relating to aberrant biological barrier permeability and peptide translocation across biological barriers are provided. Such diseases include celiac disease, necrotizing enterocolitis, diabetes, cancer, inflammatory bowel diseases, asthma, COPD, excessive or undesirable immune response, gluten sensitivity, gluten allergy, food allergy, rheumatoid arthritis, multiple sclerosis, immune-mediated or type 1 diabetes mellitus, systemic lupus erythematosus, psoriasis, scleroderma and autoimmune thyroid diseases.