The present application provides bifunctional compounds of Formula (X): ##STR00001##
or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for protein kinases. The present application also relates to methods for the targeted degradation of one or more protein kinases through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to one or more protein kinases which can be utilized in the treatment of disorders modulated by protein kinases.

A pharmaceutical formulation including an immediate release layer and an extended release layer according to the present disclosure has a biphasic dissolution profile, such that it is possible to quickly reach an effective plasma concentration of cibenzoline at the early stage, and the effective plasma concentration may be continuously maintained at the late stage. Therefore, the medicinal effect of cibenzoline may be maintained only by an administration of a single formulation once a day.

Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative, and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.

Treatment of NAFLD and NASH by therapy with MBX-8025 or an MBX-8025 salt.

Treatment of NAFLD and NASH by therapy with MBX-8025 or an MBX-8025 salt.

Methods of treating human papillomavirus (HPV)-induced conditions, HPV-induced lesions, or HPV-infected cells. The method involves administering one or more artemisinin-related compounds and one or more histone deacetylase (HDAC) inhibitors. In addition, treatment regimens involving the use of artemisinin-related compounds and HDAC inhibitors, and kits comprising pharmaceutical compositions of artemisinin-related compounds and HDAC inhibitors.

An immunosuppressant having the structure of formula (I), and a preparation method therefor and the use thereof are provided. The series of compounds can be widely used in the preparation of drugs for preventing and/or treating cancers or tumors, immune-related diseases and disorders, communicable diseases, infectious diseases or metabolic diseases mediated by PD-1/PD-L1 signal pathways, which drugs are expected to be developed into a new generation of PD-1/PD-L1 inhibitors.

##STR00001##

Disclosed herein are cyclic thiol prodrugs, and pharmaceutical compositions thereof. The prodrugs and pharmaceutical compositions thereof may be used to treat or prevent medical disorders such as, for example, cystinuria, cystinosis, cancer, neurodegenerative disease, Parkinson’s disease, Huntington’s disease, malaria, nonalcoholic fatty liver disease, radiation poisoning, arsenic poisoning, radioprotection, Wilson’s disease or rheumatoid arthritis.

Provided herein are injectable, thermoresponsive hydrogels that are liquid at room temperature, provide a carrier material, and gel at body temperature to allow for controlled release. In particular, PPCN-based hydrogels are provided with therapeutic agents (e.g., drugs, ions, etc.) incorporated within or appended thereto, and methods of preparation and use thereof, for example, for the promotion of bone formation/repair and/or the treatment of bone diseases.

The present invention is directed to a combination therapy involving a type II anti-CD20 antibody and a selective Bcl-2 inhibitor for the treatment of a patient suffering from cancer, particularly, a CD20-expressing cancer.