1215868-94-2

Usage

Uses

Used in Pharmaceutical Research:
(S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine is used as a research compound for exploring its potential applications in the pharmaceutical industry. Its unique structure may allow it to interact with various biological targets, making it a candidate for the development of new drugs.
Used in Drug Design and Development:
In the field of drug design and development, (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine is utilized as a starting point for the creation of novel therapeutic agents. Its structural features may be optimized to enhance its interaction with specific biological targets, potentially leading to the development of more effective treatments for various diseases.
Used in Chemical Synthesis:
(S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine serves as a key intermediate in the synthesis of other complex organic molecules. Its unique structure can be further modified or used as a building block to create new compounds with specific applications in various industries, including pharmaceuticals, materials science, and agrochemicals.

Upstream product

• 1215865-50-1 3-bromo-7-iodo-5'H-spiro[chromeno[2,3-b]pyridin-5,4′-oxazol]-2′-amine 
• 1335218-37-5 5-bromo-2-(4-iodophenoxy)nicotinic acid 
• 1290541-27-3 3-ethynyl-3-methyloxetane 
• 1215867-42-7 (S)-3-bromo-7-(2-fluoropyridin-3-yl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine 
• 1215867-56-3 trimethyl((3-methyloxetan-3-yl)ethynyl)silane 
• 1335514-86-7 3-(2,2-dibromoethenyl)-3-methyloxetane 
• 99419-31-5 3-methyloxetane-3-carboxaldehyde 
• 3143-02-0 3-hydroxymethyl-3-methyloxethane 
• 1215865-55-6 (S)-3-bromo-7-iodo-5'H-spiro[chromeno[2,3-b]pyridine-5,4′-oxazol]-2′-amine 
• 1335218-38-6 3-bromo-7-iodo-5H-chromeno[2,3-b]pyridine-5-one 
• 29241-65-4 5-bromo-2-chloronicotinic acid 
• 540-38-5 p-Iodophenol 
• 1215868-93-1 (S)-2'-amino-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazole]-7-yl trifluoromethanesulfonate 
• 174669-73-9 (2-fluoro-pyridin-3-yl)boronic acid 

Relevant academic research and scientific papers

Inhibitors of β-site amyloid precursor protein cleaving enzyme (BACE1): Identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5′ H -spiro[chromeno[2,3- b ]pyridine-5,4′-oxazol]-2′-amine (AMG-8718)

We have previously shown that the aminooxazoline xanthene scaffold can generate potent and orally efficacious BACE1 inhibitors although certain of these compounds exhibited potential hERG liabilities. In this article, we describe 4-aza substitution on the xanthene core as a means to increase BACE1 potency while reducing hERG binding affinity. Further optimization of the P3 and P2′ side chains resulted in the identification of 42 (AMG-8718), a compound with a balanced profile of BACE1 potency, hERG binding affinity, and Pgp recognition. This compound produced robust and sustained reductions of CSF and brain Aβ levels in a rat pharmacodynamic model and exhibited significantly reduced potential for QTc elongation in a cardiovascular safety model.

SPIRO-TETRACYCLIC RING COMPOUNDS AS BETASECRETASE MODULATORS AND METHODS OF USE

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein A1, A2, A3, A4, A5, A6, T1, T2, W, X, Y and Z of Formula (I) are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula (I).