1418128-72-9

Upstream product

• 1418128-37-6 2-fluoro-4-(1-hydroxy-1-methyl-ethyl)-benzoic acid 
• 1418128-33-2 5-fluoro-2-methyl-3-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenylamine 
• 73183-34-3 bis(pinacol)diborane 
• 502496-33-5 1-bromo-5-fluoro-2-methyl-3-nitrobenzene 
• 314241-04-8 2-fluoro-terephthalic acid 4-methyl ester 
• 74733-25-8 methyl 3-fluoro-4-formylbenzoate 
• 193290-80-1 3-fluoro-4-formylbenzoic acid 
• 777074-51-8 4-(dibromomethyl)-3-fluorobenzoic acid 
• 350-28-7 3-fluoro-4-methyl-benzoic acid 

Relevant academic research and scientific papers

Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase

Bruton's tyrosine kinase (BTK), a cytoplasmic tyrosine kinase, plays a central role in immunity and is considered an attractive target for treating autoimmune diseases. The use of currently marketed covalent BTK inhibitors is limited to oncology indications based on their suboptimal kinase selectivity. We describe the discovery and preclinical profile of LOU064 (remibrutinib, 25), a potent, highly selective covalent BTK inhibitor. LOU064 exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for a best-in-class covalent BTK inhibitor for the treatment of autoimmune diseases. It demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis. LOU064 is currently being tested in phase 2 clinical studies for chronic spontaneous urticaria and Sjoegren's syndrome.

BIFUNCTIONAL DEGRADERS AND THEIR METHODS OF USE

Described herein are bifunctional degrader compounds, their various targets, their preparation, pharmaceutical compositions comprising them, and their use in the treatment of conditions, diseases, and disorders mediated by various target proteins.

N-(3-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PHENYL)BENZAMIDE DERIVATIVES

The invention relates to compounds of the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

NOVEL PYRROLO PYRIMIDINE DERIVATIVES

The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.