C07K5/06026

RILUZOLE PRODRUGS AND THEIR 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.

Tripeptide epoxy ketone protease inhibitors

Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): ##STR00001##
and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.

Difluoroketamide derivatives as HtrA1 inhibitors

The invention provides novel compounds having the general formula (I) ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 and R.sup.23 are as described herein, compositions including the compounds and methods of using the compounds.

PRODRUGS OF GLUTAMINE ANALOGS

The disclosure provides compounds having formula (I):

##STR00001##

and the pharmaceutically acceptable salts thereof, wherein R.sub.1, R.sub.2, R.sub.2′, and X are as defined as set firth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

NOVEL SELF-ASSEMBLED AMINO ACID SUPRAMOLECULAR POLYMER, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
20210236405 · 2021-08-05 ·

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.

Crystal of a caspase inhibitor

Disclosed herein a crystal structure of a caspase inhibitor, and more specifically a crystal structure of an (S)-3-((S)-2-(5-(2-chlorophenyl)isoxazole-3-formylamide)proponamide)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)valeric acid, a preparation method therefor, a crystal polymer, a pharmaceutical composition and uses thereof. The compound A of formula (I) disclosed herein exhibits high crystal structure stability, low hygroscopicity, and advantageously shows physical properties, safety and metabolic stability while having relatively high pharmaceutical value.

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.

RILUZOLE PRODRUGS AND THEIR 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.

Pyridazine Derivatives as SMARCA2/4 Degraders

The present invention provides pyridazine derivatives of formula (I), which are therapeutically useful as SMARCA2/4 degraders. These compounds are useful in the treatment and/or prevention of diseases or disorders dependent upon SMARCA2/4 in a mammal. The present invention also provides preparation of the compounds and pharmaceutical compositions of at least one of the pyridazine derivatives of formula (I) or a pharmaceutically acceptable salt, or a stereoisomer thereof.

##STR00001##

Cross-linkers and their uses

Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.