Patent classifications
C07K9/006
PCSK9 antagonist compounds
Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof: ##STR00001##
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.
PCSK9 ANTAGONIST COMPOUNDS
Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof:
##STR00001##
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.
INHIBITOR USING PLANT CYCLOPEPTIDE AS EFFECTIVE COMPONENT FOR LIPID METABOLIC ABNORMALITIES IN CANCER CELLS AND USES THEREOF
The present disclosure discloses an inhibitor for abnormal lipid metabolism of tumor cells with a plant cyclopeptide as an effective component, and discloses application of the inhibitor to preparation of drugs for inhibiting abnormal lipid metabolism of the tumor cells, which specifically can be applied to preparation of drugs for treating and preventing abnormal lipid metabolism related cancers including liver cancer, colon cancer, rectal cancer and prostatic cancer. The inhibitor for abnormal lipid metabolism of the cells of the present disclosure can effectively inhibit abnormal lipid metabolism of the tumor cells. Its effective component, the plant cyclopeptide, is wide in source and mature in extraction technology. The inhibitor has diversified dosage forms and medication ways and has a wide clinical application prospect.
PCSK9 ANTAGONIST COMPOUNDS
Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof:
##STR00001##
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.
CYCLIC COMPOUND HAVING SELECTIVE KRAS INHIBITORY EFFECT ON HRAS AND NRAS
Cyclic compounds that selectively inhibit KRAS were found. Moreover, cyclic compounds were found to interact with an amino acid residue specific to KRAS.
Glycopeptide compound or pharmaceutical salt thereof and method for preparing same, and pharmaceutical compositions and applications thereof
The present invention provides a glycopeptide compound or pharmaceutically acceptable salt thereof as shown in Formula (I) or (II), and a method for preparing same, and pharmaceutical compositions and applications thereof, wherein the definition of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 is the same as that of the specification. The glycopeptide compound of the present invention has in-vitro antibacterial activity and has important significance for development of new antibacterial agents. ##STR00001##
Isolation, identification, and uses of antifungal compounds
In one aspect, the invention relates to isolated compounds useful as antifungal agents, for example, compounds having a structure represented by a formula: wherein R.sup.1 is hydrogen or hydroxyl; wherein R.sup.2 is hydrogen, a-xylose or -xylose; and wherein R.sup.3 and R.sup.4 are each hydrogen or together oxygen, or a pharmaceutically acceptable salt thereof; methods of isolating and purifying same; pharmaceutical compositions comprising same; agricultural compositions comprising same; and methods of treating and/or preventing fungal infections using same. In one aspect, R.sup.2 is not hydrogen or -xylose when R.sup.1 is hydroxyl and R.sup.3 and R.sup.4 are together oxygen. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
PCSK9 antagonist compounds
Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof: ##STR00001##
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.
Cyclodecapeptide compounds for use as drugs
The invention relates to novel cyclodecapeptide compounds having formula (I) for use as drugs and, more specifically, for use in the diagnosis, prevention and/or treatment of neurodegenerative diseases, such as Wilson's disease and Alzheimer's disease, and for use in the diagnosis, prevention and/or treatment of poisoning with metal ions, such as copper and mercury ions. The invention also relates to pharmaceutical compositions comprising at least one compound having formula (I) as an active principle. ##STR00001##
CYCLIC COMPOUND HAVING SELECTIVE KRAS INHIBITORY EFFECT ON HRAS AND NRAS
Cyclic compounds that selectively inhibit KRAS were found. Moreover, cyclic compounds were found to interact with an amino acid residue specific to KRAS.