Patent classifications
C07K5/06026
Self-assembled amino acid supramolecular polymer, preparation method therefor, and application thereof
Disclosed are a novel self-assembled amino acid supramolecular polymer, a preparation method therefor, and an application thereof. The self-assembled supramolecular polymer is N-lauroyl-L-alanyl-L-alanine or a salt thereof, and the salt thereof comprises sodium N-lauroyl-L-alanyl-L-alaninate and potassium N-lauroyl-L-alanyl-L-alaninate. The disclosed polymer is more effective at inhibiting bacteria and removing pesticides, and can be widely applied to the daily chemical, agricultural, and pharmaceutical industries. Further disclosed are three methods for preparing the compound. The methods produce products in high yields and are suitable for industrial production.
Amide compound having bet proteolysis-inducing action and medicinal application thereof
Provided are a compound superior in a cytotoxic action on cancer cells, an action inducing degradation of BET protein in cancer cells, and an inhibitory action on the binding of BET protein and acetylated histone, and useful as an anticancer agent, a BET protein degradation inducer or a BET protein inhibitor. A compound represented by the following formula (I) ##STR00001##
wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.
METHODS AND MATERIALS FOR MODULATING NRF2 PATHWAY
The present application provides methods and compounds of modulating Nrf2 pathway. Methods for treating cancer and neurodegenerative conditions are also provided.
LIVER TARGETING DRUG, PHARMACEUTICAL COMPOSITION AND USE THEREOF
Disclosed are a compound represented by formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition and use thereof. The compound has significant liver targeting characteristics, and can reduce the drug concentration in the circulating system while improving the efficacy, thereby reducing the toxic and side effects.
##STR00001##
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.
METHODS FOR TREATING COVID-19
The invention relates to methods for treating COVID-19 by targeting the inflammasome/caspase1/pyroptosis axis as a key inflammatory pathway. In particular, the invention relates to treating a patient infected with SARS-CoV-2 with an effective amount of one or more compounds that directly or indirectly inhibit one or more pathways of the inflammasome/caspase1/pyroptosis axis.
Therapeutics for the treatment of glaucoma
The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a K.sub.ATP channel to reduce an intraocular pressure.
THERAPEUTICS FOR THE TREATMENT OF GLAUCOMA
The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a K.sub.ATP channel to reduce an intraocular pressure.
FLUORESCENT PROBE FOR USE IN DETECTION OF BRAIN TUMOR
Provided is a novel fluorescent probe which can be used in a spray manner, has an outstandingly high sensitivity-specificity with instantaneousness, and enables detection of a brain tumor.
A fluorescent probe for detecting a brain tumor, including a compound of the following formula (I) or a salt thereof:
##STR00001##
wherein P1 represents an arginine residue, a histidine residue or a tyrosine residue, P2 represents a proline residue or a glycine residue, where P1 is linked to an adjacent N atom by forming an amide bond, and P2 is linked to P1 by forming an amide bond; R.sup.1 represents a hydrogen atom, or 1 to 4 identical or different substituents each independently selected from the group consisting of an optionally substituted alkyl group, a carboxyl group, an ester group, an alkoxy group, an amide group and an azide group; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently represent a hydrogen atom, a hydroxyl group, an optionally substituted alkyl group or a halogen atom; R.sup.8 and R.sup.9 each independently represent a hydrogen atom or an alkyl group;
X represents O, Si(R.sup.a)(R.sup.b), Ge(R.sup.a)(R.sup.b), Sn(R.sup.a)(R.sup.b), C(R.sup.a) (R.sup.b) or P(═O)(R.sup.a); R.sup.a and R.sup.b each independently represent a hydrogen atom, an alkyl group or an aryl group; and Y represents a C.sub.1-C.sub.3 alkylene group.
CATALYST FOR MANUFACTURING AMIDE COMPOUND, AND METHOD FOR MANUFACTURING AMIDE COMPOUND
The present invention provides a catalyst containing a Brønsted acid as a novel means capable of producing an amide compound by highly stereoselectively and/or highly efficiently causing an amidation reaction in a variety of substrates having a carboxylic ester group and an amino group.