89720-77-4

Usage

Uses

Used in Pharmaceutical Industry:
4-BROMO-1-BROMOMETHYL-2-CHLORO-BENZENE is used as a key intermediate in the synthesis of selective aldose reductase inhibitors. These inhibitors are important for the development of drugs that can treat diabetic complications, such as diabetic neuropathy, cataract, and retinopathy, by reducing the activity of aldose reductase, an enzyme involved in sugar metabolism.

Upstream product

• 185315-48-4 (4-bromo-2-chlorophenyl)methanol 
• 151-50-8 potassium cyanide 
• 185312-82-7 4-bromo-2-chlorobenzoic acid methyl ester 
• 59748-90-2 4-Bromo-2-chloro-benzoic Acid 
• 158435-41-7 4-bromo-2-chlorobenzaldehyde 
• 89794-02-5 4-bromo-2-chlorotoluene 

Downstream Products

• 67197-54-0 2-(4-bromo-2-chlorophenyl)acetonitrile 
• 932720-90-6 2-(benzhydrylidene-amino)-3-(4-bromo-2-chloro-phenyl)-1-(1,3-dihydro-isoindol-2-yl)-propan-1-one 
• 1213929-66-8 C₉H₉BrClNO₂ 
• 1432502-36-7 C₁₄H₁₇BrClNO₄ 
• 1432502-37-8 C₂₀H₂₃BrClNO₇ 
• 1432502-38-9 C₂₀H₂₅BrClNO₆ 
• 1432502-39-0 C₁₆H₁₉BrClNO₃ 
• 1432502-40-3 C₁₁H₁₁BrClNO 
• 1432502-41-4 C₁₆H₁₉BrClNO₂ 
• 1432502-42-5 C₁₆H₁₉BrClNO₃ 
• 1432502-43-6 C₁₁H₁₃BrClNO₃*ClH 
• 1432502-44-7 (2R,4R)-4-amino-5-(4-bromo-2-chlorophenyl)-2-hydroxypentanoic acid ethyl ester hydrochloride 
• 1428758-45-5 C₂₉H₂₉ClN₈O 
• 1330065-78-5 C₃₀H₃₀ClN₇OS 

Relevant academic research and scientific papers

HISTONE METHYLTRANSFERASE EZH2 INHIBITOR, PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF

The invention relates to a histone methyltransferase EZH2 inhibitor, a preparation method and pharmaceutical use thereof. In particular, the invention relates to a compound represented by the general formula (I), a preparation method thereof, a pharmaceut

An optimized synthesis of the potent and selective Pak1 inhibitor FRAX-1036

FRAX-1036 is a p21-activated kinase I inhibitor of significant interest to cancer biologists yet no commercial providers or detailed procedures are available. In this Letter, we chronicle the optimized synthesis of FRAX-1036, one of the most specific Pak1

SERINE/THREONINE KINASE INHIBITORS

Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.

Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pKa Polar Moiety

Signaling pathways intersecting with the p21-activated kinases (PAKs) play important roles in tumorigenesis and cancer progression. By recognizing that the limitations of FRAX1036 (1) were chiefly associated with the highly basic amine it contained, we devised a mitigation strategy to address several issues such as hERG activity. The 5-amino-1,3-dioxanyl moiety was identified as an effective means of reducing pKa and logP simultaneously. When positioned properly within the scaffold, this group conferred several benefits including potency, pharmacokinetics, and selectivity. Mouse xenograft PK/PD studies were carried out using an advanced compound, G-5555 (12), derived from this approach. These studies concluded that dose-dependent pathway modulation was achievable and paves the way for further in vivo investigations of PAK1 function in cancer and other diseases.

NEPRILYSIN INHIBITORS

In one aspect, the invention relates to compounds having the formula (I): where R1-R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

NEPRILYSIN INHIBITORS

In one aspect, the invention relates to compounds having the formula I: where R1-R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

2- PYRIDONE COMPOUND

PROBLEM TO BE SOLVED: To provide a compound that has excellent glucokinase (GK) activating action and is useful as a pharmaceutical. SOLUTION: The present invention provides a 2-pyridone compound represented by formula [1], and a tautomer or stereoisomer of the compound, or their pharmacologically acceptable salts, or their solvates (where R1 is RA-ZA-; RA is any of a carboxy group, a sulfo group or formula [5]). COPYRIGHT: (C)2016,JPOandINPIT

FATTY ACID SYNTHASE INHIBITORS

This invention relates to novel spirocyclic piperidines according to Formula (I) which are inhibitors of fatty acid synthase (FAS), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.

NEPRILYSIN INHIBITORS

In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

8-ETHYL-6-(ARYL)PYRIDO [2,3-D]PYRIMIDIN-7(8H) -ONES FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS AND CANCER

Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders or neurofibromatosis. Also described herein are methods of utilizing PAK inhibitors for the treatment of cancer.