169124-35-0

Upstream product

• 100-26-5 Pyridine-2,5-dicarboxylic acid 
• 1679-64-7 Monomethyl terephthalate 
• 881-86-7 dimethyl 2,5-pyridine dicarboxylate 
• 17874-79-2 pyridine-2,5-dicarboxylic acid 5-methyl ester 

Downstream Products

• 153559-92-3 methyl 6-[(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)carbonyl]nicotinate 
• 845830-76-4 6-((S)-1-Hydroxymethyl-2-phenyl-ethylcarbamoyl)-nicotinic acid methyl ester 
• 870450-03-6 6-[(S)-2-(4-Benzyloxy-phenyl)-1-hydroxymethyl-ethylcarbamoyl]-nicotinic acid methyl ester 
• 870450-04-7 6-[(S)-2-(4-Benzyloxy-phenyl)-1-methanesulfonyloxymethyl-ethylcarbamoyl]-nicotinic acid methyl ester 
• 845830-78-6 6-((S)-4-Benzyl-4,5-dihydro-oxazol-2-yl)-nicotinic acid methyl ester 
• 845830-79-7 6-((S)-4-Benzyl-4,5-dihydro-oxazol-2-yl)-nicotinic acid 
• 845830-77-5 6-((S)-1-Methanesulfonyloxymethyl-2-phenyl-ethylcarbamoyl)-nicotinic acid methyl ester 
• 845830-80-0 6-((S)-4-Benzyl-4,5-dihydro-oxazol-2-yl)-nicotinic acid 2-tritylsulfanyl-ethyl ester 
• 153559-44-5 methyl 6-[(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)ethenyl]nicotinate 
• 153559-76-3 6-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopropyl)nicotinic acid 
• 153559-50-3 methyl 6-<1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopropyl>nicotinate 
• 861905-71-7 methyl 6-[(4-bromo-2-fluorophenyl)carbonyl]-3-pyridinecarboxylate 
• 305448-82-2 methyl 6-{N-[4-(1-hydroxy-1-methyl-2-{[(methylethyl)sulfonyl]amino}ethyl)phenyl]carbamoyl}pyridine-3-carboxylate 
• 1344702-60-8 C₅₇H₅₂N₁₄O₁₁S₆ 

Relevant academic research and scientific papers

A highly selective colorimetric chemosensor for cobalt(ii) ions based on a tripodal amide ligand

A tripodal amide based ligand, tris-{(2-carbamoyl-5-carbomethoxy-pyridine)- 2-ethyl}amine (H3L, 1), was synthesized and structurally characterized by single crystal X-ray diffraction. Investigation of the cation recognition behavior showed that the ligand has selective colorimetric sensing properties for cobalt(ii) ions by an obvious color change from colorless to yellow. To investigate the sensing mechanism of H3L for Co 2+ ions, UV-vis absorption spectroscopy and single-crystal structural analysis were performed. The mixture of the ligand and cobalt(ii) ions displayed selective colorimetric sensing properties for weak acid anions, such as CO32-, Ac-, HCO3-, SO32-, and PO43-. Detailed 1H NMR experiments revealed that the basicity of the anions played an important role in the intensity of the interaction between the ligand and anions. The structures of compounds CoL (2), Co-Ac-HL (3), H4L- NO3 (4), and H4L-ClO4 (5) were also determined by single crystal diffraction studies. This journal is the Partner Organisations 2014.

DNA-Encoded Libraries: Hydrazide as a Pluripotent Precursor for On-DNA Synthesis of Various Azole Derivatives

DNA-encoded combinatorial chemical library (DEL) technology, an approach that combines the power of genetics and chemistry, has emerged as an invaluable tool in drug discovery. Skeletal diversity plays a fundamental importance in DEL applications, and relies heavily on novel DNA-compatible chemical reactions. We report herein a phylogenic chemical transformation strategy using DNA-conjugated benzoyl hydrazine as a common versatile precursor in azole chemical expansion of DELs. DNA-compatible reactions deriving from the common benzoyl hydrazine precursor showed excellent functional group tolerance with exceptional efficiency in the synthesis of various azoles, including oxadiazoles, thiadiazoles, and triazoles, under mild reaction conditions. The phylogenic chemical transformation strategy provides DELs a facile way to expand into various unique chemical spaces with privileged scaffolds and pharmacophores.

Rh-Catalyzed Annulative Insertion of Terminal Olefin onto Pyridines via a C-H Activation Strategy Using Ethenesulfonyl Fluoride as Ethylene Provider

A Rh(III)-catalyzed annulative insertion of ethylene onto picolinamides was achieved, providing a portal to a class of unique pyridine-containing molecules bearing a terminal olefin moiety for diversification. Application of this method for modification of Sorafenib was also accomplished.

Heterocyclic phosphodiesterase inhibitor and uses thereof

The present invention belongs to the technical field of medicine, and particularly relates to a heterocyclic phosphodiesterase inhibitor compound represented by a formula (I), or a pharmaceutically acceptable salt and a stereoisomer thereof, and a pharmaceutical preparation, a pharmaceutical composition and applications of the compound, wherein R1, R2, R3, R4, ring A, m and n are defined in the specification. According to the present invention, the compound can be used for preparing drugs for treatment or prevention of diseases associated with PDE9 kinase.

ARYL HYDROCARBON RECEPTOR MODULATORS AND USES THEREOF

Provided are compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, stereoisomers, tautomers, isotopically labeled derivatives, polymorphs, and prodrugs thereof, wherein X1-X4, RX, RC, RB, n, and Ring A are as defined herein. The compounds may be aryl hydrocarbon receptor agonists or partial aryl hydrocarbon receptor agonists. Also provided are pharmaceutical compositions comprising a compound of Formula (I) and methods of using such compounds for treating diseases and conditions related to the activity of an aryl hydrocarbon receptor, such as, for example, inflammatory diseases, autoimmune diseases, metabolic disorders, and proliferative diseases.

SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS AS RXR AGONISTS

The present invention relates to certain substituted bicyclic compounds that are agonists of RXR and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders.

NOVEL COMPOUNDS

Disclosed are novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.

Rhodium(III)-catalyzed oxidative olefination of picolinamides: Convenient synthesis of 3-alkenylpicolinamides

A rhodium(III)-catalyzed selective olefination of picolinamide derivatives has been developed. The reaction shows high regioselectivity, low catalyst loading (0.5 mol%), high yield and good functional group tolerance, providing a convenient strategy for the synthesis of 3-alkenylpicolinamides.

Synthesis and structure-activity relationships of novel, potent, orally active hypoxia-inducible factor-1 inhibitors

Hypoxia-inducible factor-1 (HIF-1) is the chief transcription factor regulating hypoxia-driven gene expression. HIF-1 overexpression is associated with poor prognosis in several cancers and therefore represents an attractive target for novel antitumor agents. We explored small molecule inhibitors of the HIF-1 pathway. Using high-throughput-screening, we identified benzanilide compound 1 (IC50= 560 nM) as a seed. Subsequent extensive derivatization led to the discovery of compounds 43a and 51d, with anti-HIF-1 activities in vitro (IC50= 21 and 0.47 nM, respectively), and in vivo. Additionally, 43a (12.5-100 mg/kg) also displayed in vivo anti-tumor efficacy, without influencing body weight.

THERAPEUTIC COMPOUNDS

The invention provides compounds of formulae (I), (II), (III), and (IV): and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers and Alzheimer's disease.