26156-48-9

Usage

Chemical Properties

Colorless liquid or solid

InChI:InChI=1/C7H6BrNO2/c1-11-7(10)5-2-3-9-6(8)4-5/h2-4H,1H3

Upstream product

• 186581-53-3 diazomethane 
• 66572-56-3 2-bromoisonicotinic acid 
• 67-56-1 methanol 
• 74-88-4 methyl iodide 

Downstream Products

• 29849-15-8 2-bromoisonicotinic acid hydrazide 
• 860369-93-3 2-bromoisonicotinic acid methyl ester N-oxide 
• 118289-16-0 (2-bromopyridin-4-yl)methanol 
• 4634-14-4 2-phenylisonicotinic acid methyl ester 
• 94413-64-6 2-Cyano-4-carbomethoxypyridine 
• 2639418-00-9 methyl 2-(dimethylphosphoryl)isonicotinate 
• 1508339-39-6 2-(dimethylphosphoryl)isonicotinic acid 
• 1240618-14-7 2-ethynylisonicotinic acid 
• 66572-56-3 2-bromoisonicotinic acid 
• 1214384-41-4 C₁₁H₈N₂O₂ 

Relevant academic research and scientific papers

Design and synthesis of non-symmetric phenylpyridine type ligands. Experimental and theoretical studies of their corresponding iridium complexes

In this work three non-symmetric phenylpyridine type ligands, L1, L2 and L3, were designed, and their corresponding Iridium complexes, C1, C2 and C3, synthetized, in order to understand the effect of ligand asymmetry on the properties of the complexes, and to explore their potentiality in devices. The complexes were structurally characterized by NMR experiments and by X-ray Diffraction, and physicochemically by technics as UV/Vis and cyclic voltammetry. Theoretical DFT calculations of the energy and electronic density of the frontier orbitals of the complexes under study were also performed. The energy of the HOMO and LUMO correlated well with the experimental electrochemical data, and supported the understanding of the processes observed.

Discovery of a new class of JMJD6 inhibitors and structure–activity relationship study

JmjC domain-containing protein 6 (JMJD6) has been thought as a potential target for various diseases particularly cancer. However, few selective JMJD6 inhibitors have been reported. In this investigation, molecular docking and biological activity evaluation were performed to retrieve new JMJD6 inhibitors, which led to the identification of a hit compound, J2. Further structural optimization and structure–activity relationship (SAR) analysis towards J2 were carried out, which gave a new potent JMJD6 inhibitor, 7p. This compound showed an IC50 value of 0.681 μM against JMJD6, but displayed no activity against other tested JmjC domain-containing protein family members, indicating good selectivity (>100 fold). Collectively, this investigation offers a selective JMJD6 inhibitor, which could be taken as a lead compound for subsequent drug discovery targeting JMJD6.

RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.

POLYSUBUNIT OPIOID PRODRUGS RESISTANT TO OVERDOSE AND ABUSE

The invention provides compositions and methods for the treatment or prevention of pain. Compositions provided are resistant to overdose and abuse. Compositions provided comprise two or more different molecules, where each molecule comprises at least one GI enzyme-labile opioid agonist releasing subunit comprising an opioid agonist that is covalently linked to at least one GI enzyme inhibitor subunit.

POLYSUBUNIT OPIOID PRODRUGS RESISTANT TO OVERDOSE AND ABUSE

The invention provides compositions and methods for the treatment or prevention of pain. The invention provides constructs whereby hydrolysis of the construct by a specified gastrointestinal enzyme directly, or indirectly, releases an opioid when taken orally as prescribed. The gastrointestinal enzyme mediated release of opioid from constructs of the invention is designed to be attenuated in vivo via a saturation or inhibition mechanism when overdoses are ingested. The invention further provides constructs that are highly resistant to oral overdose, chemical tampering, and abuse via non-oral routes of administration.

INDAZOLYL THIADIAZOLAMINES AND RELATED COMPOUNDS FOR INHIBITION OF RHO-ASSOCIATED PROTEIN KINASE AND THE TREATMENT OF DISEASE

The invention provides indazolyl thiadiazolamines and related compounds, pharmaceutical compositions, methods of inhibiting Rho-associated protein kinase, and methods of treating inflammatory disorders, immune disorders, fibrotic disorders, and other medical disorders using such compounds. An exemplary indazolyl thiadiazolamine compound is an N-(5-[5-[(1H4ndazol-5-yl)amino]-1,3,4-thiadiazol-2-yl]pyridin-3-yl)acetamide compound.

TETRAHYDROISOQUINOLINE DERIVED PRMT5-INHIBITORS

A compound of formula (I) wherein: R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.

Active agent prodrugs with heterocyclic linkers

The embodiments provide prodrug compounds of Formulae I-XVII. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XVII that provides controlled release of an active agent. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an active agent from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

N1-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS

The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions there-of; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal

N2-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS

The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal.