446852-65-9

Usage

Uses

Used in Organic Synthesis:
2-(2-BROMO-PYRIDIN-4-YL)-1-PYRIDIN-2-YL-ETHANONE is used as a building block in organic synthesis for the creation of more complex molecules. Its unique structure allows for the formation of various chemical entities that can be further explored for their potential applications.
Used in Medicinal Chemistry Research:
In the field of medicinal chemistry, 2-(2-BROMO-PYRIDIN-4-YL)-1-PYRIDIN-2-YL-ETHANONE is used as a starting material for the development of pharmaceuticals. Its biological activity is of interest for drug discovery efforts, as it may contribute to the design of new therapeutic agents.
Used in Pharmaceutical Development:
2-(2-BROMO-PYRIDIN-4-YL)-1-PYRIDIN-2-YL-ETHANONE is used as a key intermediate in the synthesis of pharmaceuticals. Its potential applications in this industry stem from its ability to be incorporated into molecules with therapeutic properties.
Used in Agrochemical Development:
Similarly, in the agrochemical industry, 2-(2-BROMO-PYRIDIN-4-YL)-1-PYRIDIN-2-YL-ETHANONE is used as a precursor in the development of agrochemicals. Its unique structure may contribute to the creation of new compounds with pesticidal or herbicidal properties.
It is crucial to handle 2-(2-BROMO-PYRIDIN-4-YL)-1-PYRIDIN-2-YL-ETHANONE with care due to its potential hazards, and to adhere to safe laboratory practices during its use in research and development.

Upstream product

• 4926-28-7 2-Bromo-4-picoline 
• 2524-52-9 ethyl-2-picolinate 

Downstream Products

• 446880-81-5 2-bromo-4-(3-(pyridine-2-yl)-1H-pyrazol-4-yl)pyridine 
• 1333492-76-4 1-methyl-4-(4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)pyridin-2-yl)piperazine 
• 1333492-75-3 2-(piperidin-1-yl)-4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)pyridine 
• 1333492-74-2 1-(4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)pyridin-2-yl)-1H-benzo[d]imidazole 
• 1333492-73-1 2-(1H-imidazol-1-yl)-4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)-pyridine 
• 1333492-72-0 2-(1H-pyrazol-1-yl)-4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)-pyridine 
• 1333492-71-9 4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)-2,2'-bipyridine 
• 1333492-70-8 6'-(4-methylpiperazin-1-yl)-4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)-2,3'-bipyridine 
• 1333492-69-5 N,N-dimethyl-3-((4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)-[2,3'-bipyridin]-6'-yl)-oxy)propan-1-amine 
• 1333492-68-4 8-(4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)pyridin-2-yl)quinoline 
• 1333492-67-3 2-(2-methoxyphenyl)-4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)pyridine 
• 1333492-66-2 2-(3-methoxyphenyl)-4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)pyridine 
• 1333492-65-1 2-(1-methyl-1H-pyrazol-4-yl)-4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)pyridine 
• 1333492-64-0 5-(4-(3-(pyridin-2-yl)-1-trityl-1H-pyrazol-4-yl)pyridin-2-yl)-pyrimidine 

Relevant academic research and scientific papers

ALK5 INHIBITOR CONJUGATES AND USES THEREOF

The present disclosure relates to targeted drug conjugates comprising ALK5 inhibitors and targeting moieties that direct the ALK5 inhibitors to cells involved in fibrosis and cancer, for example myofibroblasts, activated fibroblasts and transitioning fibr

Formulated and/or co-formulated liposome compositions containing TFGB antagonist prodrugs useful in the treatment of cancer and methods thereof

Formulated and/or co-formulated liposomes (LNP) and solid-lipid nanoparticles (SLNP) comprising TB Prodrugs and methods of making the LNPs and SLNPs are disclosed herein. The TB prodrug compositions comprise a drug moiety, a lipid moiety, and linkage unit

ANTIBODY-ALK5 INHIBITOR CONJUGATES AND THEIR USES

The present disclosure relates to antibody-drug conjugates comprising ALK5 inhibitors and their uses.

ANTIBODY-ALK5 INHIBITOR CONJUGATES AND THEIR USES

The present disclosure relates to antibody-drug conjugates comprising ALK5 inhibitors and their uses.

ANTIB0DY-ALK5 INHIBITOR CONJUGATES AND THEIR USES

The present disclosure relates to antibody-drug conjugates comprising ALK5 inhibitors and their uses.

2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-β1 and activin A signalling

Novel inhibitors of TGF-β1 and activin A signalling based on a 2-aryl-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridine pharmacophore have been synthesised. Compounds containing phenyl or aromatic nitrogen heterocycle substituents inhibited both types of signalling with HEK-293T cells in culture, with a selectivity preference for TGF-β1. Synthetic compounds containing pyridin-3-yl, pyrazol-4-yl, pyrazol-1-yl or 1H-imidazoyl-1-yl substituents exhibited structural and functional attributes suitable for further investigation related to the development of more potent TGF-β inhibitors.

Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N- (tetrahydro-2H-pyran-4-yl)benzamide (GW788388): A potent, selective, and orally active transforming growth factor-β type I receptor inhibitor

Inhibitors of transforming growth factor β (TGF-β) type I receptor (ALK5) offer a novel approach for the treatment of fibrotic diseases such as renal, hepatic, and pulmonary fibrosis. The optimization of a novel phenylpyridine pyrazole series (1a) led to the identification of potent, selective, and orally active ALK5 inhibitors. The cellular potency and pharmacokinetics profiles of these derivatives were improved and several compounds presented antifibrotic activity when orally administered to rats in an acute liver model of dimethylnitrosamine- (DMN-) induced expression of collagen IA1 mRNA, a major gene contributing to excessive extra cellular matrix deposit. One of the most potent ALK5 inhibitors identified in this chemical series, compound 13d (GW788388), reduced the expression of collagen IA1 by 80% at a dose of 1 mg/kg twice a day (b.i.d.). This compound significantly reduced the expression of collagen IA1 mRNA when administered orally at 10 mg/kg once a day (u.i.d.) in a model of puromycin aminonucleoside-induced renal fibrosis.

2-PHENYLPYRIDIN-4-YL DERIVATIVES AS ALK5 INHIBITORS

This invention relates to novel 2-phenylpyridin-4-yl heterocyclyl derivatives which are inhibitors of the transforming growth factor, ("TGF")-? signalling pathway, in particular, the phosphorylation of smad2 or smad3 by the TGF-β type I or activin-like kinase ("ALK")-5 receptor, methods for their preparation and their use in medicine, specifically in the treatment and prevention of a disease state mediated by this pathway.