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Relevant academic research and scientific papers

FERROPTOSIS INHIBITORS–DIARYLAMINE PARA-ACETAMIDES

Provided are compounds that inhibit ferroptosis activity, or modulate or inhibit a disease associated with ferroptosis dysregulation, such as neuropathy, ischemia reperfusion injury, acute kidney failure and cancer, including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE

Bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof.

Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases

Autoreactive B cell-derived antibodies form immune complexes that likely play a pathogenic role in autoimmune diseases. In systemic lupus erythematosus (SLE), these antibodies bind Fc receptors on myeloid cells and induce proinflammatory cytokine producti

A Facile Synthesis of Ligands for the von Hippel-Lindau E3 Ligase

The proteolysis-targeting chimeras (PROTACs) have become an integral part of different stages of drug discovery. This growing field, therefore, benefits from advancements in all segments of the design of these compounds. Herein, an efficient and optimized synthetic protocol to various von Hippel-Lindau (VHL) ligands is presented, which enables easy access to multigram quantities of these essential PROTAC building blocks. Moreover, the elaborated synthesis represents a straightforward approach to further explore the chemical space of VHL ligands.

INHIBITING AGENTS FOR BRUTON'S TYROSINE KINASE

Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, and methods for their use and production.

Process Development and Large-Scale Synthesis of BTK Inhibitor BIIB068

Chemical process development efforts leading to multikilogram production of BIIB068 hemiadipate are discussed. Process optimization resulted in (1) removal of transition metal from the process, (2) a streamlined process with significantly improved overall

N-(CYANO-SUBSTITUTED BENZYL OR PYRIDINYLMETHYL)-3-HYDROXYPICOLINAMIDE DERIVATIVES USEFUL AS HIF PROLYL HYDROXYLASE INHIBITORS

Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R3, R4 R5, R6, R7, R8, R9, X1 and X2 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with PHD.

INHIBITING AGENTS FOR BRUTON'S TYROSINE KINASE

Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, methods for use as Bruton's tyrosine kinase and methods of production.

ADIPATE FORMS AND COMPOSITIONS OF BIARYL INHIBITORS OF BRUTON'S TYROSINE KINASE

The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.

FORMS AND COMPOSITIONS OF BIARYL INHIBITORS OF BRUTON'S TYROSINE KINASE

The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.