930783-26-9

Usage

Uses

Used in Pharmaceutical Applications:
(R)-hexahydropyrazino[2,1-c][1,4]oxazin-4-one is used as a potential drug candidate for various medical conditions due to its structural features and possible interactions with biological molecules. Its complex molecular structure allows for the exploration of its efficacy in treating different health issues.
Used in Medicinal Chemistry Research:
(R)-hexahydropyrazino[2,1-c][1,4]oxazin-4-one is used as a building block for the synthesis of other bioactive compounds in the field of medicinal chemistry. Its unique properties and potential interactions with biological molecules make it an interesting target for the development of novel therapeutic agents.
Used in Drug Development:
(R)-hexahydropyrazino[2,1-c][1,4]oxazin-4-one is utilized in the development of new drugs, as its complex molecular structure and potential pharmaceutical applications make it a valuable compound for further research and exploration in the pharmaceutical industry.

Upstream product

• 1147422-40-9 (R)-4-oxohexahydropyrazino[2,1-c][1,4]oxazine-8-carboxylic acid tert-butyl ester 
• 278788-66-2 (R)-tert-butyl 3-(hydroxymethyl)piperazine-1-carboxylate 
• 1147422-39-6 (R)-4-(2-chloroacetyl)-3-(hydroxymethyl)piperazine-1-carboxylic acid tert-butyl ester 

Downstream Products

• 508241-14-3 (R)-octahydropiperazine[2,1-c][1,4]oxazine 

Relevant academic research and scientific papers

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.

NOVEL AZETIDINE COMPOUNDS USEFUL IN THE TREATMENT OF FUNCTIONAL GASTROINTESTINAL DISORDERS, IBS AND FUNCTIONAL DYSPEPSIA

The present invention relates to new azetidine compounds, to pharmaceutical compositions cotaining them and the use of said compounds in in the treatment of functional gastrointestinal disorders, IBS and functional dyspepsia. The compounds are neurokinin