A5020679786- Chronic Lymphocytic Leukemia Research
- Chronic Myeloid Leukemia Treatments
- Multiple Myeloma Research and Treatments
- Bone Metabolism and Diseases
- Free Radicals and Antioxidants
- Chemical Synthesis and Analysis
- Biochemical and Molecular Research
- Synthesis of Tetrazole Derivatives
- Chemical synthesis and alkaloids
- Immunodeficiency and Autoimmune Disorders
- Advanced Synthetic Organic Chemistry
- bioluminescence and chemiluminescence research
- Bone health and treatments
- Protein Tyrosine Phosphatases
- Bone and Dental Protein Studies
Biogen (United States)
2019-2024
Multiple sclerosis (MS) is a chronic disease with an underlying pathology characterized by inflammation-driven neuronal loss, axonal injury, and demyelination. Bruton's tyrosine kinase (BTK), nonreceptor member of the TEC family kinases, involved in regulation, migration, functional activation B cells myeloid periphery central nervous system (CNS), cell types which are deemed to contributing progression MS patients. Herein, we describe discovery BIIB129 (25), structurally distinct...
Multiple Sclerosis is a chronic autoimmune neurodegenerative disorder of the central nervous system (CNS) that characterized by inflammation, demyelination, and axonal injury leading to permeant disability. In early stage MS, inflammation primary driver disease progression. There remains an unmet need develop high efficacy therapies with superior safety profiles prevent processes Herein, we describe discovery BIIB091, structurally distinct orthosteric ATP competitive, reversible inhibitor...
Bruton's tyrosine kinase (BTK) plays a non-redundant signaling role downstream of the B-cell receptor (BCR) in B cells and receptors for Fc region immunoglobulins (FcR) myeloid cells. Here, we characterise BIIB091, novel, potent, selective reversible small-molecule inhibitor BTK.BIIB091 was evaluated vitro vivo preclinical models phase 1 clinical trial.In vitro, BIIB091 potently inhibited BTK-dependent proximal distal functional responses both with IC50s ranging from 3 to 106 nm, including...
An operationally simple protocol has been discovered that couples primary or secondary amines with N-aryl-substituted lactams to deliver differentiated diamines in moderate high yields. The process allows for the partial reduction of a lactam presence Cp2ZrHCl (Schwartz's reagent), followed by reductive amination between resulting hemiaminal and amine. These reactions can be telescoped one-pot fashion significantly simplify operation. scope substituted various ring sizes was demonstrated...