Patent classifications
C07K9/00
Antibiotic Compounds
Provided herein are lipidated glycopeptide compounds of formula (I); or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof. R.sub.1 is a lipid, R.sub.2 is —H or a lipid, and R.sub.3 and R.sub.4 are as defined herein. These compounds have antibiotic activity. Also provided are formulations comprising such compounds; as well as such compounds or formulations for use as a medicament. The compounds and formulations may also be used in the treatment of bacterial infection.
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CHIP SURFACE LINKER AND PREPARATION METHOD AND USE THEREFOR
The present invention relates to the field of biochips, and provides a chip surface linker and a preparation method and a use therefor. The chip surface linker is obtained by means of applying a direct current voltage to an aromatic amine bonding molecule in the presence of an acid and a nitrite to cause a reaction with a chip surface to form a bonding molecular group connected the chip surface, and then using a functional molecular for reaction and modification to add a functional molecular group containing a hydroxyl group and an ester group. The chip surface linker obtained in the present invention is able to bond more stably with a chip surface, being stable in hot water and basic conditions, and features relatively good electrical conductivity, stability during energization, and resistance to organic solvents required for nucleic acid synthesis, and is thus very advantageous for subsequent nucleic acid synthesis and other uses.
PCSK9 ANTAGONIST COMPOUNDS
Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof:
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where A, X, R.sup.1, and R.sup.2 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.
METHOD AND STRAINS FOR REDUCING BYPRODUCT SUCCINIC ACID IN FERMENTATION PROCESS OF L-MALIC ACID AND USE THEREOF
The disclosure discloses an Aspergillus niger engineered strain for reducing byproduct succinic acid in a fermentation process of L-malic acid. The Aspergillus niger engineered strain is an Aspergillus niger engineered strain in which fumaric acid reductase frdA and fumaric acid reductase flavoprotein subunit frdB are simultaneously knocked out. The disclosure provides an frdA and frdB gene double-knockout Aspergillus niger strain, and a method for greatly reducing byproduct succinic acid in a fermentation process of L-malic acid. By the disclosure, the byproduct succinic acid accumulated in a production process of malic acid through fermentation of Aspergillus niger is significantly reduced, a cost in a downstream separation and purification process of malic acid is decreased, and good strains are provided for producing malic acid via industrial fermentation.
THIRD GENERATION TUBULYSIN ANALOGUES AND PROCESS OF PREPARATION THEREOF
The present disclosure relates to a third generation tubulysin analogues and process of preparation thereof. The present disclosure also relates to a method of using these third generation tubulysin analogues for treatment of various diseases including cancer.
Muramyl Peptide Derivatives
The invention is directed to Muramyl Dipeptide (MDP) derivative compounds of structural Formula-VIII, a process for synthesis, intermediates used in the synthesis and use thereof:
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wherein, R can be a linear or branched alkyl, an aryl, a substituted aryl, or an alkoxy alkyl. These compounds possess excellent pharmacological properties, in particular immunomodulating properties for use as adjuvant in vaccine formulations. These compounds are particularly useful as adjuvants in vaccines.
Glycan markers as measure of disease state of hepatic diseases
The present invention is directed to developing a glycan markers capable of detecting a hepatic disease, and more specifically to developing a glycan marker indicating a hepatic disease-state. Furthermore, the present invention is also directed to developing a glycan marker capable of distinguishing hepatic disease-states with the progress of hepatocarcinoma. The present inventors identified, among the serum glycoproteins, glycopeptides and glycoproteins in which a glycan structure specifically changes due to a hepatic diseases including hepatocarcinoma and provide these as novel glycan markers (glycopeptide and glycoprotein) specific to hepatic disease-states.
Glycan markers as measure of disease state of hepatic diseases
The present invention is directed to developing a glycan markers capable of detecting a hepatic disease, and more specifically to developing a glycan marker indicating a hepatic disease-state. Furthermore, the present invention is also directed to developing a glycan marker capable of distinguishing hepatic disease-states with the progress of hepatocarcinoma. The present inventors identified, among the serum glycoproteins, glycopeptides and glycoproteins in which a glycan structure specifically changes due to a hepatic diseases including hepatocarcinoma and provide these as novel glycan markers (glycopeptide and glycoprotein) specific to hepatic disease-states.
Prevention of tissue ischemia and related methods
Provided herein are compositions for preventing, ameliorating, and/or reducing tissue ischemia and/or tissue damage due to ischemia, increasing blood vessel diameter, blood flow and tissue perfusion in the presence of vascular disease including peripheral vascular disease, atherosclerotic vascular disease, coronary artery disease, stroke and influencing other conditions, by suppressing CD47 and/or blocking TSP1 and/or CD47 activity or interaction. Influencing the interaction of CD47-TSP1 in blood vessels allows for control of blood vessel diameter and blood flow, and permits modification of blood pressure and cardiac function. Under conditions of decreased blood flow, for instance through injury or atherosclerosis, blocking TSP1-CD47 interaction allows blood vessels to dilate and increases blood flow, tissue perfusion and tissue survival.
Immunosuppression modulating compounds
The present invention provides immunosuppression compounds to inhibit the programmed cell death 1 (PD1) signalling pathway. The present invention further provides peptide based compositions for treatment of cancer or treatment of infections via immunopotentiation caused by inhibition of immunosuppressive signaling induced by PD-1, PD-L1, or PD-L2 and therapies using them, immunopotentiative substrates included as the active ingredient. Further, the invention provides an application of the compositions containing the peptide moieties for preventive and/or therapeutic agents for cancer, cancer metastasis, immunodeficiency, an infectious disease or the like and an application of peptide moieties as a testing or diagnostic agent or a research agent for such a disease.