508241-14-3

Usage

Uses

As the provided materials do not specify any particular applications for Pyrazino[2,1-c][1,4]oxazine, octahydro-, (9aR)(9CI), it is not possible to list specific uses for Pyrazino[2,1-c][1,4]oxazine, octahydro-, (9aR)- (9CI) based on the information given. However, given its classification as an oxazine and the presence of a heterocyclic ring structure, it may be explored for potential applications in the following industries:
Used in Pharmaceutical Industry:
Pyrazino[2,1-c][1,4]oxazine, octahydro-, (9aR)(9CI) could be used as a pharmaceutical compound for [specific application reason], pending further research into its biological activity and therapeutic potential.
Used in Agrochemical Industry:
In the agrochemical industry, Pyrazino[2,1-c][1,4]oxazine, octahydro-, (9aR)(9CI) might be utilized as an agrochemical compound for [specific application reason], contingent upon its effectiveness and safety in agricultural settings.
Used in Materials Science:
Pyrazino[2,1-c][1,4]oxazine, octahydro-, (9aR)(9CI) could potentially be employed in materials science as a component in the development of new materials with [specific application reason], based on its chemical properties and structural characteristics.

Upstream product

• 930783-26-9 (R)-hexahydropyrazino[2,1-c][1,4]oxazin-4-one 
• 1147422-39-6 (R)-4-(2-chloroacetyl)-3-(hydroxymethyl)piperazine-1-carboxylic acid tert-butyl ester 
• 1147422-40-9 (R)-4-oxohexahydropyrazino[2,1-c][1,4]oxazine-8-carboxylic acid tert-butyl ester 
• 1217444-84-2 (R)-4-N-Boc-2-hydroxymethyl-piperazine hydrochloride 
• 1383427-89-1 C₇H₁₂N₂O₂*ClH 
• 278788-66-2 (R)-tert-butyl 3-(hydroxymethyl)piperazine-1-carboxylate 

Downstream Products

• 508236-08-6 8-[(6R)-1,8-diaza-4-oxabicyclo[4.4.0]decan-8-ylmethyl]-5-(3,4-dimethoxybenzylamino)-2-(2-furyl)[1,2,4]triazolo[1,5-c]pyrimidine 

Relevant academic research and scientific papers

Novel lead generation of an anti-tuberculosis agent active against non-replicating mycobacteria: Exploring hybridization of pyrazinamide with multiple fragments

The key to shortening tuberculosis (TB) drug regimen lies in eliminating the reservoir of non-replicating persistent (NRP) Mycobacterium tuberculosis (Mtb). Pyrazinamide (PZA) is the only known drug used as part of a combination therapy that is believed to kill NRP Mtb and achieve sterilization. PZA is active only under low pH screening conditions. Screening and identification of NRP-active anti-TB compounds are severely limited because compounds are usually inactive under regular assay conditions. In an effort to design novel NRP-active anti-TB compounds, we used pyrazinamide as a core and hybridized it with the fragments derived from marketed drugs. One of these designs, compound 8, was a hybrid with fluoroquinolone. This compound exhibited >10 fold improvement in NRP activity under low pH condition as compared to pyrazinamide and a modest activity (0.8 log10 kill) under nutritionally starved NRP condition. Furthermore, compound 8 was active against fluoroquinolone-resistant strains and did not show any activity in a DNA supercoiling assay (gyrase inhibition), suggesting that its mechanism of action is not that of the parent fluoroquinolone. These results provide a novel avenue in the exploration of new chemotypes that are active against non-replicating Mtb.

BICYCLIC RING SYSTEM SUBSTITUTED AMIDE FUNCTIONALISED PHENOLS AS MEDICAMENTS

This invention relates to bicyclic ring system substituted amide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.

BICYCLIC RING SYSTEM SUBSTITUTED SULFONAMIDE FUNCTIONALISED PHENOLS AS MEDICAMENTS

This invention relates to bicyclic ring system substituted sulfonamide functionalized phenols of general formula (1), their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.

BICYCLIC RING SYSTEM SUBSTITUTED SULFONAMIDE FUNCTIONALISED PHENOLS AS MEDICAMENTS

This invention relates to bicyclic ring system substituted sulfonamide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.

BICYCLIC RING SYSTEM SUBSTITUTED AMIDE FUNCTIONALISED PHENOLS AS MEDICAMENTS

This invention relates to bicyclic ring system substituted amide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds

Discovery of novel PI3-Kinase δ specific inhibitors for the treatment of rheumatoid arthritis: Taming CYP3A4 time-dependent inhibition

PI3Kδis a lipid kinase and a member of a larger family of enzymes, PI3K class IA(α, β, δ) and IB (γ), which catalyze the phosphorylation of PIP2 to PIP3. PI3Kδ is mainly expressed in leukocytes, where it plays a critical, nonredundant role in B cell receptor mediated signaling and provides an attractive opportunity to treat diseases where B cell activity is essential, e.g., rheumatoid arthritis. We report the discovery of novel, potent, and selective PI3Kδinhibitors and describe a structural hypothesis for isoform (α, β γ?) selectivity gained from interactions in the affinity pocket. The critical component of our initial pharmacophore for isoform selectivity was strongly associated with CYP3A4 time-dependent inhibition (TDI). We describe a variety of strategies and methods for monitoring and attenuating TDI. Ultimately, a structure-based design approach was employed to identify a suitable structural replacement for further optimization.

THIENOPYRIMIDIENE DERIVATIVES AS PI3K INHIBITORS

Thienopyrimidines of formula (I) wherein W and R1 to R4 are as defined in the claims, and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PI3 kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.

PURINE DERIVATIVES USEFUL AS PI3 KINASE INHIBITORS

This invention provides a compound which is a purine of formula (Ia) or (Ib): and the pharmaceutically acceptable salts thereof that are inhibitors of PI3K and a selective for the p110δ isoform, which is a class Ia PI3 kinase, over other class Ia PI3 kinases and over class Ib kinases. The compounds may be used to treat diseases and disorders arisi from abnormal cell growth, function or behaviour associated with PI3 kinase such as cance immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.