710348-95-1

Upstream product

• 73183-34-3 bis(pinacol)diborane 
• 134168-97-1 3-bromo-5-fluoroaniline 
• 710348-94-0 2-(3-fluoro-5-nitrophenyl)-4,4,5,5-tetramethyl[1,3,2]dioxaborolane 
• 807620-95-7 N-(3-bromo-5-fluorophenyl)acetamide 
• 1435-51-4 1,3-dibromo-5-fluorobenzene 

Downstream Products

• 807620-97-9 2-{2-[3-fluoro-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl]-2H-tetrazol-5-yl}-pyridine 

Relevant academic research and scientific papers

MACROCYCLIC RIP2-KINASE INHIBITORS

The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of RIP2-kinase, and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of RIP2-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.

INDOLIZINE DERIVATIVES AS PHOSHOINOSITIDE 3-KINASES INHIBITORS

Compounds of formula (I), defined herein, inhibit phosphoinositide 3-kinases (PI3K) and are useful for the treatment of disorders associated with PI3K enzymes.

TRICYCLIC STEROID HORMONE NUCLEAR RECEPTOR MODULATORS

The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula (I): or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula (I), including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula (I).

3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: A highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist

Structure-activity relationship studies performed around 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile for the purposes of developing novel mGlu5 receptor antagonists are described. Synthesis of a series of four-ring tetrazoles led to the discovery of 3-[3-fluoro-5-(5-pyridin-2-yl- 2H-tetrazol-2-yl)phenyl]-4-methylpyridine (26), a highly potent, brain penetrant, tetrazole-based mGlu5 receptor antagonist. Structure-activity relationship studies performed around 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2- yl)benzonitrile for the purpose of developing novel mGlu5 receptor antagonists are described. Synthesis of a series of four-ring tetrazoles led to the discovery of 3-[3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4- methylpyridine, a highly potent, brain penetrant, azole-based mGlu5 receptor antagonist.