15862-34-7

Usage

Chemical Properties

Yellow Solid

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

Upstream product

• 1072-97-5 5-bromo-2-pyridylamine 
• 6332-56-5 2-hydroxy-3-nitropyridine 
• 6945-68-2 5-bromo-3-nitro-pyridin-2-ylamine 
• 13466-38-1 5-bromopyridin-2(1H)-one 
• 13472-85-0 2-methoxy-5-bromopyridine 
• 13466-38-1 5-bromopyridin-2-ol 
• 7664-93-9 sulfuric acid 
• 7697-37-2 nitric acid 

Downstream Products

• 98786-86-8 5-bromo-2-hydroxy-3-aminopyridine 
• 67443-38-3 5-bromo-2-chloro-3-nitropyridine 
• 15862-37-0 2,5-dibromo-3-nitro-pyridine 
• 847777-33-7 5-bromo-3-nitropyridin-2-yl 4-methylbenzenesulfonate 
• 690265-69-1 5-(4-chloro-phenyl)-3-nitro-pyridin-2-ol 
• 153888-45-0 5-bromo-1-methyl-3-nitropyridine-2(1H)-one 
• 1086062-66-9 GS⁽²⁶⁴⁾K₂₁₅₈ 
• 1086063-46-8 N-(5-bromo-2-methoxypyridine-3-yl)-2,4-difluorobenzene sulfonyl chloride 
• 1360537-69-4 N-(5-bromo-2-methoxypyridin-3-yl)-4-fluoro-2-nitrobenzenesulfonamide 
• 152684-30-5 5-bromo-2-methoxy-3-nitropyridine 
• 588729-99-1 3-amino-5-bromo-2-chloropyridine 
• 1083326-21-9 N-(5-bromo-2-chloropyridin-3-yl )-2,4-difluorobenzenesulfonamide 
• 1400668-14-5 N-(5-bromo-2-chloropyridin-3-yl)-2,4-difluorobenzamide 
• 1178884-09-7 6-(dimethylamino)-2-(2-(hydroxymethyl)-3-(1-methyl-5-(5-(morpholine-4-carbonyl)pyridin-2-ylamino)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)-3,4-dihydroisoquinolin-1(2H)-one 

Relevant academic research and scientific papers

DOCK1-INHIBITING COMPOUND AND USE THEREOF

Provided is a compound that is usable as an active ingredient of an anticancer agent. Preferably provided is a compound that has DOCK1-inhibiting activity and exerts an anticancer effect based on the activity. A compound represented by the following formula (A) or a salt thereof: wherein X represents a carbon atom or a nitrogen atom; Y represents an oxygen atom, a hydroxy group, or a hydrocarbon group; R1 and R2 are different, and each represents a hydrogen atom or a group represented by the following formula (A-1): (wherein R6 represents a pyrrolidino group or a phenyl group, and n2 is 0 or 1) ; R3 represents -CO-R7 (wherein R7 is an alkoxy group, an alkyl group, or an alkylamino group), a 1,3-oxazole group, an alkylhydroxy group, a hydrogen atom, or an oxygen atom; R4 represents a hydrogen atom, an oxygen atom, or a hydrocarbon group in which one or more hydrogen atoms may be replaced by one or more substituents; R5 represents a halogen atom, a halogenated alkyl group, or a halogenated alkylthio group; and n1 is an integer of 0 to 5; and

Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors

Phosphoinositide 3-kinases (PI3Ks) are regarded as promising targets for treatment of various cancers due to their roles in regulating cell proliferation, differentiation, migration, and survival. Here we report our efforts to develop potent and orally bioavailable PI3K inhibitors for the treatment of cancers. The alkylsulfonamide-containing quinazoline derivatives A1–A18 significantly inhibited PI3Kα, and cell proliferation among HCT-116, MCF-7 and SU-DHL-6 cell lines. The optimal compound A1 displayed potent inhibitory activity against PI3Kα (IC50 = 4.5 nM), PI3Kβ (IC50 = 4.5 nM), PI3Kγ (IC50 = 4.5 nM), PI3Kδ (IC50 = 4.5 nM) and significantly inhibited the growth of HCT-116, MCF-7 and SU-DHL-6 cell lines with IC50 values of 0.82 μM, 0.99 μM and 0.19 μM, respectively. Western blot analysis demonstrated A1 significantly suppressed the phosphorylation of AKTS473 in a dose-dependent manner. Furthermore, A1 could markedly inhibit cancer growth at the dose of 25 mg/kg in nude mouse HCT-116 xenograft model in vivo without causing significant weight loss or toxicity.

New Pyridinones and Isoquinolinones as Inhibitors of the Bromodomain BRD9

The present invention encompasses compounds of general formula (I) wherein the groups R1 to R9, X1 and X2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, e.g. cancer, pharmaceutical preparations containing such compounds and their uses as a medicament.

New tetracyclic 1,4-oxazepines constructed via practically simple tandem condensation strategy from readily available synthons

A streamlined synthetic methodology towards novel tetracyclic 1,4-oxazepines from readily available precursors is described. The compounds, designed as more soluble version of the earlier described, poorly soluble dibenzo[b,f][1,4]oxazepines, were obtained in high yields and as a single regioisomer as a result of three tandem chemical events - nucleophilic aromatic substitution, Smiles rearrangement and denitrocyclization.

HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF

Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

SULFONYL BENZIMIDAZOLE DERIVATIVES

This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R1, R2 ,R3, R4, R5, m and n are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, GERD, constipation, diarrhea, functional gastrointestinal disorders, irritable bowel syndrome, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, COPD, cryptogenic fibrosing alveolitis and bronchitis.

Sulfonyl benzimidazole derivatives

This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, GERD, constipation, diarrhea, functional gastrointestinal disorders, irritable bowel syndrome, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, COPD, cryptogenic fibrosing alveolitis and bronchitis.

Condensation of 2,3-pyridinediamines with acetonylacetone

The reaction of 2,3-pyridinediamine 1a and its 5-bromo analogue 1b, independently, with acetonylacetone leads to the formation of 1:1 condensation products irrespective of the molar ratios employed.'The condensation products have been assigned 2-amino 2a and 5-bromo-2-amino-3 (2',5'-dimethylpyrrolyl)pyridine 2b structures. Authentic chemical evidence is given in support of the claim for these structures ruling out the equally probable alternative structure 3 for these compounds. Attempted studies on the reactivity of the latter compounds towards electrophilic reagents such as acetic arthydride, benzoyl chloride, and arylsulphonyl chlorides have been described.

3-fluoropyridines, process for their preparation, and their use in liquid-crystal mixtures

A 3-fluoropyridine of the formula (I) STR1 in which the symbols have the following meanings: R1 and R2, independently of one another, are, for example, H or straight-chain or branched alkyl, A1, A2, A3 and A4 are identical or different and are, for example, 1,4-phenylene, pyrazine-2,5-diyl or trans-1,4-cyclohexylene, M1, M2, M3 and M4 are identical or different and are, for example, --O-- or --CO--O--, R3, R4, R6 and R7, independently of one another are, for example, H or straight-chain or branched alkyl, M5 is for example, --O--CO-- or a single bond, k, l, m, n, o, p, q and r are zero or one, with the proviso that the sum k+m+p+r is less than 4 and greater than zero, can advantageously be employed as a component in ferroelectric liquid-crystal mixtures.

2-(3-AMINO-5-HALO-2-PYRIDYLALKYLAMINO)-PYRIMIDONES USEFUL AS HISTAMINE H1-ANTAGONISTS

The invention describes 5-halo-3-amino-2-pyridyl derivatives which are useful as histamine H 1-antagonists. Particular compounds described are 2-4-(5-bromo-3-aminopyrid-2-yl)butylamino!-5-(6-methylpyrid-3-ylmethyl)-4-pyr imidone and 2-4-(5-bromo-3-aminopyrid-2-yl)butylamino!-5-(N-oxopyrid-4-ylmethyl)-4-pyrimi done.