58539-65-4

Usage

Uses

Used in Pharmaceutical Industry:
3-Pyridinecarboxamide,2-methyl-(9CI) is used as a JAK inhibitor for the treatment of autoimmune diseases and cancer. Its application as a JAK inhibitor is due to its ability to modulate the JAK/STAT signaling pathway, which plays a crucial role in the pathogenesis of various autoimmune and inflammatory conditions, as well as in the development and progression of cancer.
3-Pyridinecarboxamide,2-methyl-(9CI)'s effectiveness in treating these conditions is attributed to its ability to inhibit the activation of JAK proteins, which are key mediators of cellular responses to various cytokines and growth factors. By blocking the JAK/STAT pathway, 3-Pyridinecarboxamide,2-methyl-(9CI) can potentially reduce inflammation, suppress the immune system, and inhibit tumor growth, making it a promising candidate for the development of novel therapeutics in the treatment of autoimmune diseases and cancer.

InChI:InChI=1/C7H8N2O/c1-5-6(7(8)10)3-2-4-9-5/h2-4H,1H3,(H2,8,10)

Upstream product

• 1721-26-2 ethyl 2-methyl nicotinate 
• 65719-09-7 methyl 2-methylnicotinate 
• 3222-56-8 2-methylnicotinic acid 
• 124-38-9 carbon dioxide 
• 530-62-1 1,1'-carbonyldiimidazole 
• 169229-06-5 2-methylnicotinoyl chloride 
• 1055970-47-2 2-methylnicotinic acid imidazolide 
• 110-86-1 pyridine 

Downstream Products

• 1721-23-9 2-methyl-nicotinonitrile 
• 23616-31-1 1,6-naphthyridine-5(6H)-one 
• 91999-48-3 2-Methyl-1-(2',6'-Dichlorobenzyl)-1,4-dihydronicotinamide 
• 58539-64-3 ((2-methylpyridin-3-yl)methyl)amine 
• 1590403-10-3 C₂₁H₁₆F₄N₂O₂ 
• 1590403-06-7 C₁₉H₁₃F₃N₄O₂ 
• 1590403-04-5 C₂₁H₁₂F₄N₂O₂ 
• 1590409-70-3 C₁₅H₈BrF₃N₂O₂ 
• 1044871-97-7 C₂₃H₂₀N₂O₂ 
• 167709-12-8 1-benzyl-2,4-dimethyl-1,4-dihydronicotinamide 
• 114174-69-5 1-benzyl-2-methyl-1,4-dihydronicotinamide 
• 177662-71-4 2-methyl-3-[1-[4-[[2-(trimethylsilyl)-ethyl]sulfonyl]phenyl]-4-(trifluoromethyl)-1H-imidazol-2-yl]pyridine 
• 177660-94-5 4-[2-(2-methyl-pyridin-3-yl)-4-trifluoromethyl-imidazol-1-yl]-benzenesulfonamide 
• 177660-93-4 2-methyl-3-[1-[4-(methylsulfonyl)phenyl]-4-(trifluoromethyl)-1H-imidazol-2-yl]pyridine 

Relevant academic research and scientific papers

ANTI-FIBROTIC PYRIDINONES

This application relates to polycyclic compounds with a pyridinone or pyridinone derivative core including, substituted pyridinones, 5,6- and 6,6- bicyclic heterocycles and substituted pyridine-thiones. This application also discloses methods of preparing these polycyclic compounds, pharmaceutical compositions and medicaments comprising said compounds and methods to treat, prevent or diagnose diseases, disorders or conditions associated with fibrosis.

ANTI-FIBROTIC PYRIDINONES

Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.

TREATMENT OF DISEASES BY EPIGENETIC REGULATION

The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis.

Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2

As part of an effort to identify novel selective modulators of sirtuins, we synthesized and tested several isosteres and constrained analogues of nicotinamide. Biological data suggest that compound 2 is selective for Sirt3 over Sirt1 and Sirt2.

COMPOUNDS FOR THE PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASES

The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.

PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF COMPLEX DISEASES AND THEIR DELIVERY BY INSERTABLE MEDICAL DEVICES

The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.

NEW COMPOUNDS III

The present invention relates to new compounds [Chemical formula should be inserted here. Please see paper copy] (I) or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, ph

Ready access to 7,8-dihydro- and 1,2,3,4-tetrahydro-1,6-naphthyridine-5(6H) -ones from simple pyridine precursors

Short pathways are described for the synthesis of a representative example of each of the 7,8-dihydro- and 1,2,3,4-tetrahydro-1,6-naphthyridine-5(6H)-one ring systems from simple pyridine precursors. An attempted synthesis of the related 4,6-dihydro-1,6-naphthyridin-5(1H)-one ring system from a common intermediate was unsuccessful.

A process for the preparation of 4-[2-(aryl or heterocyclo)-1H-imidazol-1-yl]benzenesulfonamides

A process to make a compound of the formula or a pharmaceutically acceptable salt thereof is disclosed wherein R3 is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, heteroaralkyl, acyl, cyano, alkaxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclocarbonyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkylaminocarbonylalkyl, heteroarylalkoxyalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, aralkoxy, aralkylthio, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, arylthio, aryloxy, aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl; wherein R4 is a radical selected from hydrido, alkyl and halo; and wherein R2 is selected from aryl and heterocyclo, wherein R2 is optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfonyl, aminosulfonyl, halo, alkylthio, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, alkoxyalkyl, haloalkoxy, amino, alkylamino, arylamino and nitro; ???said method comprising the steps of forming a (protected sulfonyl)benzenamine, treating said (protected sulfonyl)benzenamine first with a base and then with a nitrile to form an amidine, treating said amidine with a haloketone derivative in the presence of a base to form a hydroxyimidazole, forming a (protected sulfonylphenyl) imidazole by dehydrating said hydroxyimidazole, and forming said compounds by deprotecting said (protected sulfonylphenyl)imidazole.

Selective cyclooxygenase-2 inhibitors: Heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents

A series of heteroaryl modified 1,2-diarylimidazoles has been synthesized and found to be potent and highly selective (1000-9000-fold) inhibitors of the human COX-2.3-Pyridyl derived COX-2 selective inhibitor (25) exhibited excellent activity in acute (carrageenan induced paw edema, ED50 = 5.4 mg/kg) and chronic (adjuvant induced arthritis, ED50 = 0.25 mg/kg) models of inflammation. The relatively long half-life of 25 in rat and dog prompted investigation of the pyridyl and other heteroaromatic systems containing potential metabolic functionalities. A number of substituted pyridyl and thiazole containing compounds (e.g., 44, 46, 54, 76, and 78) demonstrated excellent oral activity in every efficacy model evaluated. Several orally active diarylimidazoles exhibited desirable pharmacokinetics profiles and showed no GI toxicity in the rat up to 100 mg/kg in both acute and chronic models. The paper describes facile and practical syntheses of the targeted diarylimidazoles. The structure-activity relationships and antiinflammatory properties of a series of diarylimidazoles are discussed.