943995-32-2

Usage

Uses

Used in Pharmaceutical Industry:
2-chloro-6H,7H,8H-pyrimido[5,4-b][1,4]oxazin-7-one is used as a general reagent in pharmaceutical syntheses for its ability to facilitate the creation of a wide range of pharmaceutical agents. Its unique structure allows for versatile chemical reactions, enabling the synthesis of various drug molecules with potential therapeutic applications.
In the pharmaceutical industry, 2-chloro-6H,7H,8H-pyrimido [5,4-b][1,4]oxazin-7-one is particularly valuable for its role in the synthesis of novel drug candidates, which can be further optimized for improved efficacy, safety, and pharmacokinetic properties. By serving as a key intermediate in the synthesis of these agents, 2-chloro-6H,7H,8H-pyrimido[5,4-b][1,4]oxazin-7-one contributes to the advancement of new treatments for various diseases and conditions.

Upstream product

• 943995-31-1 4-amino-2-chloropyrimidin-5-ol 
• 79-04-9 chloroacetyl chloride 
• 105-36-2 ethyl bromoacetate 
• 99979-77-8 2-chloro-5-methoxypyrimidin-4-amine 

Downstream Products

• 1349829-86-2 2-((2R,5R)-2-methyl-5-phenylmorpholino)-6H-pyrimido[5,4-b][1,4]oxazin-7(8H)-one 

Relevant academic research and scientific papers

Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists

A novel series of morpholine-based nonsteroidal mineralocorticoid receptor antagonists is reported. Starting from a pyrrolidine HTS hit 9 that possessed modest potency but excellect selectivity versus related nuclear hormone receptors, a series of libraries led to identification of morpholine lead 10. After further optimization, cis disubstituted morpholine 22 was discovered, which showed a 45-fold boost in binding affinity and corresponding functional potency compared to 13. While 22 had high clearance in rat, it provided sufficient exposure at high doses to favorably assess in vivo efficacy (increased urinary Na+/K+ ratio) and safety. In contrast to rat, the dog and human MetID and PK profiles of 22 were adequate, suggesting that it could be suitable as a potential clinical asset.

FUSED IMIDAZOLE AND PYRAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY

A series of substituted benzimidazole, imidazo[1,2-a]pyridine and pyrazolo[1,5-a]pyridine derivatives, and analogues thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

MORPHOLINE COMPOUNDS

Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.