405174-97-2

Usage

Uses

Used in Pharmaceutical Industry:
3-Bromo-2-pyridinecarboxaldehyde is used as a key intermediate for the synthesis of various pharmaceuticals, contributing to the development of new drugs and medicinal compounds. Its reactivity allows for the creation of a wide range of pyridine-based molecules with potential therapeutic applications.
Used in Agrochemical Industry:
In the agrochemical sector, 3-Bromo-2-pyridinecarboxaldehyde is utilized as a building block in the synthesis of agrochemicals, such as pesticides and herbicides. Its role in creating effective and targeted compounds helps to improve crop protection and yield.
Used in Fine Chemicals Production:
3-Bromo-2-pyridinecarboxaldehyde is employed as a reagent in the production of fine chemicals, where its high reactivity is leveraged to produce specialty chemicals used in various industries, including fragrances, dyes, and coatings.
Used in Dyes and Pigments Industry:
3-Bromo-2-pyridinecarboxaldehyde is used as a crucial component in the manufacturing process of dyes and pigments, where its chemical properties contribute to the color intensity and stability of the final products.

InChI:InChI=1/C6H4BrNO/c7-5-2-1-3-8-6(5)4-9/h1-4H

Upstream product

• 30683-23-9 3-bromopicolinic acid 
• 13534-89-9 2,3-dibromopyridine 
• 68-12-2 N,N-dimethyl-formamide 
• 626-55-1 3-Bromopyridine 
• 867353-49-9 3-bromo-N-methoxy-N-methylpyridine-2-carboxamide 
• 38749-79-0 3-bromo-2-picoline 

Downstream Products

• 1248738-01-3 N-[(3-bromo-2-pyridinyl)methyl]-5-isoquinolinamine 
• 1318073-01-6 ethyl 3-(3-bromopyridin-2-yl)-5-methylisoxazole-4-carboxylate 
• 17288-32-3 1H-pyrrolo[3,2-b]pyridine-2-carboxylic acid ethyl ester 
• 1620580-05-3 1'-benzyl-7-methoxy-7H-spiro[furo[3,4-b]pyridine-5,4'-piperidine] 
• 1620580-10-0 C₂₀H₂₆N₂O₃ 
• 1620580-09-7 3-bromopyridine-2-carbaldehyde dimethyl acetal 
• 98491-40-8 3-ethyl-2-pyridinecarboxaldehyde 

Relevant academic research and scientific papers

Design, synthesis and characterization of HIV-1 ca-targeting small molecules: Conformational restriction of PF74

Small molecules targeting the PF74 binding site of the HIV-1 capsid protein (CA) confer potent and mechanistically unique antiviral activities. Structural modifications of PF74 could further the understanding of ligand binding modes, diversify ligand chemical classes, and allow identification of new variants with balanced antiviral activity and metabolic stability. In the current work, we designed and synthesized three series of PF74-like analogs featuring conformational constraints at the aniline terminus or the phenylalanine carboxamide moiety, and characterized them using a biophysical thermal shift assay (TSA), cell-based antiviral and cytotoxicity assays, and in vitro metabolic stability assays in human and mouse liver microsomes. These studies showed that the two series with the phenylalanine carboxamide moiety replaced by a pyridine or imidazole ring can provide viable hits. Subsequent SAR identified an improved analog 15 which effectively inhibited HIV-1 (EC50 = 0.31 μM), strongly stabilized CA hexamer (?Tm = 8.7?C), and exhibited substantially enhanced metabolic stability (t1/2 = 27 min for 15 vs. 0.7 min for PF74). Metabolic profiles from the microsomal stability assay also indicate that blocking the C5 position of the indole ring could lead to increased resistance to oxidative metabolism.

Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead

Covalent inhibitors of wild-type HIV-1 reverse transcriptase (CRTIs) are reported. Three compounds derived from catechol diether non-nucleoside inhibitors (NNRTIs) with addition of a fluorosulfate warhead are demonstrated to covalently modify Tyr181 of HIV-RT. X-ray crystal structures for complexes of the CRTIs with the enzyme are provided, which fully demonstrate the covalent attachment, and confirmation is provided by appropriate mass shifts in ESI-TOF mass spectra. The three CRTIs and six noncovalent analogues are found to be potent inhibitors with both IC50 values for in vitro inhibition of WT RT and EC50 values for cytopathic protection of HIV-1-infected human T-cells in the 5-320 nM range.

HISTONE ACETYLTRANSFERASE (HAT) INHIBITOR AND USE THEREOF

The present invention relates to a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising the same, and use thereof in the treatment of various HAT-related diseases or conditions.

COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF 1H-PYRAZOLO[4,3-B]PYRIDINES

The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound useful in the treatment of a neurodegenerative disorder and their combined use as a medicament, in particular for the treatment of neurodegenerative and/or cognitive disorders.

1H-PYRAZOLO[4,3-B]PYRIDINES AS PDE1 INHIBITORS

The present invention provides 1H-pyrazolo[4,3-b]pyridines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF 1H-PYRAZOLO[4,3-B]PYRIDINES

The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound which compound is useful in the treatment of a psychiatric disorder and their combined use as a medicament, in particular for the treatment of psychiatric and/or cognitive disorders.

Discovery of TRPM8 Antagonist (S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine

Transient-receptor-potential melastatin 8 (TRPM8), the predominant mammalian cold-temperature thermosensor, is a nonselective cation channel expressed in a subpopulation of sensory neurons in the peripheral nervous system, including nerve circuitry implicated in migraine pathogenesis: the trigeminal and pterygopalatine ganglia. Genomewide association studies have identified an association between TRPM8 and reduced risk of migraine. This disclosure focuses on medicinal-chemistry efforts to improve the druglike properties of initial leads, particularly removal of CYP3A4-induction liability and improvement of pharmacokinetic properties. A novel series of biarylmethanamide TRPM8 antagonists was developed, and a subset of leads were evaluated in preclinical toxicology studies to identify a clinical candidate with an acceptable preclinical safety profile leading to clinical candidate AMG 333, a potent and highly selective antagonist of TRPM8 that was evaluated in human clinical trials.

1H-PYRAZOLO[4,3-B]PYRIDINES AS PDE1 INHIBITORS

The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

Multi-substituted amine compound and its preparation and use (by machine translation)

The invention belongs to the field of medical technology, in particular, the present invention provides the following formula I shown multi-substituted amine compound or its isomer or its pharmaceutically acceptable salt, ester, prodrug or hydrate, its pharmaceutical composition, preparation method thereof and its use in the preparation of medicine for treating aids in use. The compound or pharmaceutical composition containing the compound can be used as an inhibitor for inhibiting HIV integrase with LEDGF/p75 between protein - protein interaction and HIV integrase dimerization, then can be used for the treatment of aids. . (by machine translation)