443956-08-9

Usage

Uses

Used in Pharmaceutical Industry:
6-Bromo-2-nitro-pyridin-3-ol is used as a reagent for the synthesis of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors. These inhibitors serve as broad-spectrum antibacterial agents, targeting a wide range of bacterial pathogens and contributing to the development of new antibiotics to combat drug-resistant infections.
Used in Organic Synthesis:
6-Bromo-2-nitro-pyridin-3-ol also functions as a reagent for the preparation of α-styrylpyridines through palladium-catalyzed coupling of N-tosylhydrazones with halopyridines. This synthetic route allows for the creation of diverse α-styrylpyridine derivatives, which have been found to possess antitumor activity. This makes 6-Bromo-2-nitro-pyridin-3-ol a valuable intermediate in the development of potential cancer therapeutics.

InChI:InChI=1S/C5H3BrN2O3/c6-4-2-1-3(9)5(7-4)8(10)11/h1-2,9H

Upstream product

• 15128-82-2 3-hydroxy-2-nitropyridine 
• 916737-76-3 6-bromo-3-methoxy-2-nitropyridine 

Downstream Products

• 916737-76-3 6-bromo-3-methoxy-2-nitropyridine 
• 959992-61-1 6-bromo-3-(2-bromoethoxy)-2-nitropyridine 
• 443956-09-0 ethyl 2-(6-bromo-2-nitropyridin-3-yloxy)acetate 
• 934758-27-7 2-amino-6-bromo-3-hydroxypyridine 
• 887471-45-6 3-(benzyloxy)-6-bromo-2-nitropyridine 
• 959992-62-2 6-bromo-3,4-dihydro-2H-pyrido[3,2-b] [1,4]oxazine 
• 1303587-91-8 (2-((2,2-dimethyl-1,3-dioxolan-4-yl)methoxy)pyridin-4-yl)(6-(3-(trifluoromethyl)phenyl)-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methanone 
• 1303582-20-8 (2-(2,3-dihydroxypropoxy)pyridin-4-yl)(6-(3-(trifluoromethyl)phenyl)-2H-pyrido[3,2-b][l,4]oxazin-4(3H)-yl)methanone trifluoroacetate salt 
• 1303583-13-2 pyridin-3-yl 6-(3-(trifluoromethyl)phenyl)-2H-pyrido[3,2-b][1,4]oxazine-4(3H)-carboxylate 
• 1303587-79-2 6-(3-(trifluoromethyl)phenyl)-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazine 
• 1196153-28-2 6-bromo-2,2-dimethyl-2H,3H,4H-pyrido[3,2-b][1,4]oxazin-3-one 
• 1303588-12-6 2,2-dimethyl-6-(3-(trifluoromethyl)phenyl)-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazine 
• 1303583-09-6 2,2-dimethyl-N-(pyridin-4-yl)-6-(3-(trifluoromethyl)phenyl)-2H-pyrido[3,2-b][1,4]oxazine-4(3H)-carboxamide 
• 1303585-09-2 (S)-6-(3-(3-fluoropyrrolidin-1-yl)phenyl)-2,2-dimethyl-N-(5-methylpyridin-3-yl)-2H-pyrido[3,2-b][1,4]oxazine-4(3H)-carboxamide 

Relevant academic research and scientific papers

ANTI-BACTERIAL HETEROCYCLIC COMPOUNDS AND THEIR SYNTHESIS

The compounds of Formula I and Formula (B) are described herein along with their stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms, and pharmaceutically active

Design, synthesis and biological evaluation of 1,4-Diazobicylco[3.2.2]nonane derivatives as α7-Nicotinic acetylcholine receptor PET/CT imaging agents and agonists for Alzheimer's disease

α7-Nicotinic acetylcholine receptor (α7-nAChR) agonists are promising therapeutic drug candidates for treating the cognitive impairment associated with Alzheimer's disease (AD). Thus, a novel class of derivatives of 1,4-diazobicylco[3.2.2]nonane has been synthesized and evaluated as α7-nAChR ligands. Five of them displayed high binding affinity (Ki = 0.001–25 nM). In particular, the Ki of 14 was 0.0069 nM, which is superior to that of the most potent ligand that was previously reported by an order of magnitude. Four of them had high selectivity for α7-nAChRs over α4β2-nAChRs and no significant hERG (human ether-a-go-go-related gene) inhibition. Their agonist activity was also discussed preliminarily. One of the compounds, 15 (Ki = 2.98 ± 1.41 nM), was further radiolabeled with 18F to afford [18F]15 for PET imaging, which exhibited high initial brain uptake (11.60 ± 0.14%ID/g at 15 min post injection), brain/blood value (9.57 at 30 min post injection), specific labeling of α7-nAChRs and fast clearance from the brain. Blocking studies demonstrated that [18F]15 was α7-nAChR selective. In addition, micro-PET/CT imaging in normal rats further indicated that [18F]15 had obvious accumulation in the brain. Therefore, [18F]15 was proved to be a potential PET radiotracer for α7-nAChR imaging.

COMPOUNDS AND THEIR METHODS OF USE

The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.

ORGANIC COMPOUND FOR OPTOELECTRONIC DEVICE AND ORGANIC OPTOELECTRONIC DEVICE AND DISPLAY DEVICE

The present invention relates to a compound for an organic optoelectronic device represented by chemical formula 1, an organic optoelectronic device applying the same and a display device including the organic optoelectronic device. The detailed content with respect to the chemical formula 1 are the same as defined in the specification. The compound can provide an organic optoelectronic device having high efficiency, long lifespan, etc.COPYRIGHT KIPO 2017

FORMULATIONS FOR 2-HETEROARYL SUBSTITUTED BENZOFURANS

Processes and compositions for 2-heteroaryl substituted benzofuran derivatives are described. The 2-heteroaryl substituted benzofuran derivatives may be suitable for preparing radiolabeled 2-heteroaryl substituted benzofuran derivatives for imaging amyloid deposits in living patients.

BRIDGED PIPERIDINE DERIVATIVES

The present invention relates to a compound of formula (I), wherein Het Ar is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, or lower alkoxy; R2 is lower alkyl substituted by halogen, -CH2-C3-6-cycloalkyl, substituted by one or two substituents, selected from lower alkyl substituted by halogen or halogen, or is lower alkenyl substituted by halogen; R3 is hydrogen, lower alkyl substituted by halogen, lower alkyl, halogen, C3-6-cycloalkyl or lower alkyl substituted by hydroxy; n is 1 or 2; for n = 2, R1 can be independent to each other; Y is CH or N; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.

Ligand compound of alpha7 nicotinic acetylcholine receptor and application of ligand compound

The embodiment of the invention provides a ligand compound of an alpha7 nicotinic acetylcholine receptor, the ligand compound has one of the following general formulas: wherein (1) X and R1 are shown in the description, and R7 is halogen; (2) R2 is hydrogen, and R3 is halogen or amino; or R3 is hydrogen, and R2 is halogen or amino; (3) R6 is hydrogen, and R4 and R5 are synthesized into a compound shown in the description; or R4 is hydrogen, and R5 and R6 are synthesized into a compound shown in the description; R8 is halogen; and (4) Y is nitrogen or carbon, Z is shown in the description, and R9 and R10 are respectively halogens. The provided ligand compound is an excellent ligand compound of the alpha7 nicotinic acetylcholine receptor. After being chemically marked radioactively, the provided ligand compound of the alpha7 nicotinic acetylcholine receptor can serve as a PET photographic developer.

HETEROCYCLIC COMPOUNDS USEFUL AS ANTI-BACTERIAL AGENTS AND METHOD FOR PRODUCTION

The present disclosure relates to compounds of Formula I, its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms thereof and pharmaceutical compositions containing them as the active ingredient which can be used as medicaments. The aforementioned substances can also be used in the manufacture of medicaments for treatment, prevention or suppression of diseases, and conditions mediated by microbes. The present disclosure also relates to the synthesis.and characterization of aforementioned substances.

MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR

The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, R3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

Modulators of Cystic Fibrosis Transmembrane Conductance Regulator

The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, R3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.