1402004-16-3

Usage

Uses

Used in Pharmaceutical Industry:
7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydropyrido[2,1-c][1,4]oxazine-1,6-dione is used as a potential drug candidate for its diverse pharmacological activities, such as anticancer, antimicrobial, and anti-inflammatory properties. Its unique structure and therapeutic potential make it a valuable molecule for the development of new treatments in medicine.
Used in Oncology:
In the field of oncology, 7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydropyrido[2,1-c][1,4]oxazine-1,6-dione is used as an anticancer agent. Its potential to target and treat various types of cancer makes it a promising compound for further research and development in cancer therapy.
Used in Microbiology:
7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydropyrido[2,1-c][1,4]oxazine-1,6-dione is used as an antimicrobial agent, indicating its potential to combat various microbial infections. This property could be harnessed for the development of new antibiotics or antifungal agents.
Used in Inflammation Management:
As an anti-inflammatory agent, 7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydropyrido[2,1-c][1,4]oxazine-1,6-dione may be used in the treatment of various inflammatory conditions. Its potential to modulate inflammatory responses could lead to new therapeutic approaches for managing inflammation-related diseases.
Used in Neurological Disorders Treatment:
7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydropyrido[2,1-c][1,4]oxazine-1,6-dione is considered for use in the treatment of neurological disorders due to its potential neuroprotective and therapeutic effects. Further research could reveal its role in managing or treating conditions such as Alzheimer's, Parkinson's, or other neurodegenerative diseases.
Used in Cardiovascular Disease Management:
In the cardiovascular field, 7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydropyrido[2,1-c][1,4]oxazine-1,6-dione may be used for its potential to treat or manage cardiovascular diseases. Its pharmacological profile suggests it could contribute to the development of new therapies for heart conditions or vascular disorders.

Upstream product

• 106-93-4 ethylene dibromide 
• 1123194-97-7 N-(6-bromo-2-methoxypyridin-3-yl)-N-(2-oxopropyl)formamide 
• 1123194-96-6 N-(6-bromo-2-methoxypyridin-3-yl)-formamide 
• 89466-18-2 6-bromo-2-methoxy-pyridin-3-ylamine 
• 39856-57-0 2,6-dibromo-3-aminopyridine 
• 462-08-8 pyridin-3-ylamine 
• 822-36-6 4-methyl-1H-imidazole 
• 19621-92-2 2-oxo-1,2-dihydropyridine-6-carboxylic acid 
• 1123194-98-8 6-bromo-2-methoxy-3-(4-methyl-1H-imidazol-1-yl)pyridine 
• 1402003-83-1 5-(4-Methyl-1H-imidazol-1-yl)-6-oxo-1,6-dihydropyridine-2-carboxylic acid, hydrochloride salt 
• 1262197-81-8 methyl 6-methoxy-5-(4-methyl-1H-imidazol-1-yl)pyridine-2-carboxylate 

Downstream Products

• 1402002-76-9 2-[(2S)-1-{4-fluoro-2-[(2R)-1,1,1-trifluoropropan-2-yl]phenoxy}propan-2-yl]-7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione 
• 1402002-75-8 2-{(2S)-1-[4-chloro-2-(1,1,1-trifluoro-2-methylpropan-2-yl)phenoxy]propan-2-yl}-7-(4-methyl-1H-imidazol-1-yl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione 
• 1402004-28-7 N-{(2S)-1-[4-chloro-2-(1,1,1-trifluoro-2-methylpropan-2-yl)phenoxy]propan-2-yl}-1-(2-hydroxyethyl)-5-(4-methyl-1H-imidazol-1-yl)-6-oxo-1,6-dihydropyridine-2-carboxamide 
• 1587727-69-2 1-(2-hydroxyethyl)-5-(4-methyl-1H-imidazol-1-yl)-6-oxo-N-[(1S)-1-{(2S,5R)-5-[4-(trifluoromethyl)phenyl]tetrahydrofuran-2-yl}ethyl]-1,6-dihydropyridine-2-carboxamide 

Relevant academic research and scientific papers

1-CYANO-PYRROLIDINE DERIVATIVES AS DUB INHIBITORS

The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The novel compounds have formula (I): (Formula (I)) or are pharmaceutically acceptable salts thereof, wherein: R1a, R1b, R1c, R1d, R1e and R1f each independently represent hydrogen, optionally substituted C1-C6 alkyl or optionally substituted C3-C4 cycloalkyl, or R1b and R1c together form an optionally substituted C3-C6 cycloalkyl ring, or R1d and R1e together form an optionally substituted C3-C6 cycloalkyl ring; R2 represents hydrogen or optionally substituted C1-C6 alkyl; A represents an optionally further substituted 5 to 10 membered monocyclic or bicyclic heteroaryl, heterocyclyl or aryl ring; L represents a covalent bond or linker; B represents an optionally substituted 3 to 10 membered monocyclic or bicyclic heterocyclyl, heteroaryl, cycloalkyl or aryl ring; and when -A-L-B is at position x attachment to A is via a carbon ring atom of A, and either: A cannot be triazolopyridazinyl, triazolopyridinyl, imidazotriazinyl, imidazopyrazinyl or pyrrolopyrimidinyl; or B cannot be substituted with phenoxyl; or B cannot be cyclopentyl when L is an oxygen atom.

Synthesis of Pyridopyrazine-1,6-dione γ-Secretase Modulators via Selective 4-Methylimidazole N1-Buchwald Arylation

An efficient synthesis of pyridopyrazine-1,6-dione γ-secretase modulators (GSMs) is described. Our route features the construction of a crystalline lactone intermediate via a selective palladium-catalyzed 4-methylimidazole N1-arylation using the Buchwald Xantphos Pd G4 precatalyst, which does not require a preactivation step. The weak inorganic base KHCO3 was employed to minimize saponification of a particularly sensitive lactone substrate. Additional key transformations include DABAL-Me3-mediated lactone aminolysis and a mild TBD/ethyl trifluoroacetate mediated lactam ring closure to afford a representative GSM in high yield.

NOVEL BICYCLIC PYRIDINONES AS GAMMA-SECRETASE MODULATORS

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis,

Design of pyridopyrazine-1,6-dione γ-secretase modulators that align potency, MDR efflux ratio, and metabolic stability

Herein we describe the design and synthesis of a series of pyridopyrazine-1,6-dione γ-secretase modulators (GSMs) for Alzheimer's disease (AD) that achieve good alignment of potency, metabolic stability, and low MDR efflux ratios, while also maintaining favorable physicochemical properties. Specifically, incorporation of fluorine enabled design of metabolically less liable lipophilic alkyl substituents to increase potency without compromising the sp3-character. The lead compound 21 (PF-06442609) displayed a favorable rodent pharmacokinetic profile, and robust reductions of brain Aβ42 and Aβ40 were observed in a guinea pig time-course experiment.

Novel Bicyclic Pyridinones

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Novel Bicyclic Pyridinones

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.