81971-38-2

Usage

Uses

Used in Pharmaceutical Industry:
3-Bromo-1-methylpyridin-2(1H)-one is used as a building block in organic synthesis for the introduction of a pyridinone motif into various compounds. Its unique structure and reactivity make it suitable for the development of new pharmaceuticals with potential therapeutic applications.
Used in Agrochemical Industry:
In the agrochemical industry, 3-Bromo-1-methylpyridin-2(1H)-one serves as a key intermediate in the synthesis of various agrochemicals. Its ability to be incorporated into different molecular structures allows for the creation of new compounds with potential applications in crop protection and pest control.
Used as a Reagent in Chemical Reactions:
3-Bromo-1-methylpyridin-2(1H)-one is also utilized as a reagent in chemical reactions to introduce a methylpyridine group into molecules. This property makes it a valuable tool in the synthesis of complex organic compounds and contributes to the development of novel chemical entities with diverse applications.

Upstream product

• 13466-43-8 3-bromopyridin-2(1H)-one 
• 74-88-4 methyl iodide 
• 52200-48-3 3-bromo-2-chloropyridine 
• 13466-43-8 3-bromo-pyridin-2-ol 
• 142-08-5 2-Pyridone 
• 77-78-1 dimethyl sulfate 
• 694-85-9 1-methyl-2-pyridone 
• 626-55-1 3-Bromopyridine 

Downstream Products

• 284688-87-5 N-(3-methoxycarbonyladamant-1-ylcarbonyl)-(L)-4-(1'-methyl-2'-oxo-3'-pyridyl)phenylalanine methyl ester 
• 1184298-12-1 3-(3-benzylsulfanyl-2-ethyl-phenyl)-1-methyl-1H-pyridin-2-one 
• 1184298-17-6 3-(3-benzylsulfanyl-2-methoxy-phenyl)-1-methyl-1H-pyridin-2-one 
• 1093628-98-8 O-[tert-Butyl] N-[2-fluoro-4-(1-methyl-2-oxo-1,2-dihydropyridin-3-yl)phenyl]carbamate 
• 20538-40-3 1-methyl-3-phenyl-piperidin-2-one 
• 1184298-18-7 2-methoxy-3-(1-methyl-2-oxo-1 ,2-dihydro-pyridin-3-yl)-benzenesulfonyl chloride 
• 1184298-19-8 3-(5-chloro-1-methyl-2-oxo-1 ,2-dihydro-pyridin-3-yl)-2-methoxy-benzenesulfonyl chloride 
• 1184298-10-9 5-chloro-thiophene-2-carboxylic acid[(S)-2-[3-(5-chloro-1-methyl-2-oxo-1 ,2-dihydro-pyridin-3-yl)-2-ethyl-benzenesulfonylamino]-3-((S)-3-methyl-morpholin-4-yl)-3-oxo-propyl]-amide 
• 1184298-13-2 3-(5-chloro-1-methyl-2-oxo-1 ,2-dihydro-pyridin-3-yl)-2-ethyl-benzenesulfonyl chloride 
• 1394348-44-7 2-chloro-5-(1-methyl-2-oxo-1,2-dihydro-pyridin-3-ylamino)-benzoic acid methyl ester 
• 13180-21-7 1-methyl-3-phenylpyridin-2(1H)-one 
• 1349798-35-1 5-bromo-1-methyl-3-phenylpyridin-2(1H)-one 
• 1349798-30-6 C₂₆H₃₀N₂O₂ 
• 14529-54-5 3,5-dibromo-1-methyl-1H-pyridin-2-one 

Relevant academic research and scientific papers

Discovery and Optimization of Highly Selective Inhibitors of CDK5

Autosomal dominant polycystic kidney disease (ADPKD) is the most prevalent monogenic human disease, but to date, only one therapy (tolvaptan) is approved to treat kidney cysts in ADPKD patients. Cyclin-dependent kinase 5 (CDK5), an atypical member of the cyclin-dependent kinase family, has been implicated as a target for treating ADPKD. However, no compounds have been disclosed to date that selectively inhibit CDK5 while sparing the broader CDK family members. Herein, we report the discovery of CDK5 inhibitors, including GFB-12811, that are highly selective over the other tested kinases. In cellular assays, our compounds demonstrate CDK5 target engagement while avoiding anti-proliferative effects associated with inhibiting other CDKs. In addition, we show that the compounds in this series exhibit promising in vivo PK profiles, enabling their use as tool compounds for interrogating the role of CDK5 in ADPKD and other diseases.

COMPOUNDS AND METHODS FOR TREATING OXALATE-RELATED DISEASES

Disclosed herein are compounds and compositions for modulating glycolate oxidase, useful for treating oxalate-related diseases, such as hyperoxaluria, where modulating glycolate oxidase is expected to be therapeutic to a patent in need thereof. Methods of modulating glycolate oxidase activity in a human or animal subject are also provided.

SUBSTITUTED 1, 6-NAPHTHYRIDINE INHIBITORS OF CDK5

Disclosed are compounds having structural formula I, and related salts and pharmaceutical compositions. Also disclosed are therapeutic methods, e.g., of treating diseases and conditions such as kidney disease, kidney failure, kidney stones, or polycystic kidney disease, using the compounds of formula (I), and related salts and pharmaceutical compositions.

HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS

Aminopyrazine compounds as modulators of an adenosine receptor are provided. The compounds may find use as therapeutic agents for the treatment of diseases mediated through a G-protein-coupled receptor signaling pathway and may find particular use in oncology.

Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures

Target-based approaches toward new antimalarial treatments are highly valuable to prevent resistance development. We report several series of pyrazolopyran-based inhibitors targeting the enzyme serine hydroxymethyltransferase (SHMT), designed to improve microsomal metabolic stability and to identify suitable candidates for in vivo efficacy evaluation. The best ligands inhibited Plasmodium falciparum (Pf) and Arabidopsis thaliana (At) SHMT in target assays and PfNF54 strains in cell-based assays with values in the low nanomolar range (3.2-55 nM). A set of carboxylate derivatives demonstrated markedly improved in vitro metabolic stability (t1/2 > 2 h). A selected ligand showed significant in vivo efficacy with 73% of parasitemia reduction in a mouse model. Five new cocrystal structures with PvSHMT were solved at 2.3-2.6 ? resolution, revealing a unique water-mediated interaction with Tyr63 at the end of the para-Aminobenzoate channel. They also displayed the high degree of conformational flexibility of the Cys364-loop lining this channel.

C3-CARBON LINKED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN DEGRADATION

This invention provides Degronimers that have carbon-linked E3 Ubiquitin Ligase targeting moieties (Degrons), which can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.

Discovery of 1,3-Diaryl-pyridones as Potent VEGFR-2 Inhibitors: Design, Synthesis, and Biological Evaluation

In this study, we described the design, synthesis, and biological evaluation of 1,3-diaryl-pyridones as vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. The 1,3-diaryl-pyridones were synthesized via Chan-Lam and Suzuki coupling reactions. Two representative compounds, 17 and 35h, displayed excellent enzymatic inhibitory activities, with IC50 values of 3.5 and 3.0 nm, respectively. Furthermore, compounds 17 and 35h blocked the tube formation and suppressed the VEGF-induced phosphorylation of VEGFR-2 and downstream extracellular signal-regulated kinases (Erk) in human umbilical vein endothelial cells (HUVECs) at 10 nm concentration. The docking simulation showed that compound 17 bound well into the active site of VEGFR-2 via two hydrogen bonds and hydrophobic interactions.

HETEROCYCLIC COMPOUND

The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the f

PYRROLOPYRROLONE DERIVATIVES AND THEIR USE AS BET INHIBITORS

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Asymmetric Homogeneous Hydrogenation of 2-Pyridones

An asymmetric homogeneous hydrogenation of 2(1H)-pyridones has been developed, using a ruthenium complex bearing two chiral N-heterocyclic carbene (NHC) ligands. To the best of our knowledge, the presented reaction is the first example of a homogeneous asymmetric conversion of 2-pyridones into the corresponding enantioenriched 2-piperidones.