1108745-25-0

Usage

Uses

Used in Pharmaceutical Research and Development:
5-(3,5-difluorobenzyl)-2-fluorobenzonitrile is utilized as a building block for the synthesis of various biologically active compounds. Its unique structure allows it to be a valuable component in the creation of new pharmaceuticals with potential therapeutic effects.
Used in Agrochemical Manufacturing:
In the agrochemical industry, 5-(3,5-difluorobenzyl)-2-fluorobenzonitrile serves as an intermediate in the production process. Its incorporation aids in the development of effective agrochemicals designed to protect crops and enhance agricultural productivity.
Used in Fine Chemicals Production:
5-(3,5-difluorobenzyl)-2-fluorobenzonitrile is also employed in the manufacturing of fine chemicals, where its specific properties contribute to the creation of high-quality specialty chemicals used in various applications, including fragrances, dyes, and other industrial chemicals.
Medicinal Chemistry Research:
Due to its potential biological activity, 5-(3,5-difluorobenzyl)-2-fluorobenzonitrile is a subject of interest in medicinal chemistry research. Scientists are exploring its properties to understand its possible role in the development of new drugs and therapeutic agents.
It is crucial to handle 5-(3,5-difluorobenzyl)-2-fluorobenzonitrile with care, as it may present health hazards and environmental concerns. Proper safety measures should be taken during its use to mitigate any potential risks.

Upstream product

• 1108745-07-8 5-[(3,5-difluoro-phenyl)-hydroxy-methyl]-2-fluoro-benzonitrile 
• 214210-21-6 3-cyano-4-fluorophenylboronic acid 
• 141776-91-2 1-bromomethyl-3,5-difluoro-benzene 

Downstream Products

• 1108745-36-3 5-[1-(3,5-difluoro-phenyl)-ethyl]-2-fluoro-benzonitrile 
• 1108745-30-7 5-(3,5-difluoro-benzyl)-1H-indazol-3-ylamine 
• 1108743-56-1 N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-nitrobenzamide 
• 1108743-64-1 N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-2-(2-methoxy-ethylamino)-4-(4-methyl-piperazin-1-yl)-benzamide 
• 1108743-61-8 N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-2-(3-methoxy-propylamino)-4-(4-methyl-piperazin-1-yl)-benzamide 
• 1108743-71-0 N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-2-(2-fluoro-ethylamino)-4-(4-methyl-piperazin-1-yl)-benzamide 
• 1108746-57-1 2-[(2-{[tert-butyl(dimethyl)silyl]oxy}ethyl)amino]-N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-benzamide 
• 1108744-32-6 N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-2-{[(1-methylazetidin-3-yl)methyl]amino}-4-(4-methylpiperazin-1-yl)benzamide 
• 1108743-70-9 2-benzylamino-N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-benzamide 
• 1108743-74-3 N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-phenylamino-benzamide 
• 1108743-66-3 2-cyclohexylamino-N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-benzamide 
• 1108744-24-6 N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-[(1-methylpiperidin-4-yl)amino]benzamide 
• 1108744-07-5 N₁ - [ 5 - ( 3 , 5-difluorobenzyl)-1H-indazol-3-yl]-N 4 - [ 2-(dimethylamino)ethyl]-N₄-methyl-2-(tetrahydro-2H-pyran-4-ylamino)benzene-1,4-dicarboxamide 
• 1108743-80-1 N-(5-(3,5-difluorobenzyl)-1H-indazol-3-yl)-4-(piperazin-1-yl)-2-((tetrahydro-2H-pyran-4-yl)amino) benzamide 

Relevant academic research and scientific papers

TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE

This disclosure relates to bivalent compounds (e.g., bi-functional small molecule compounds), compositions comprising one or more of the bivalent compounds, and to methods of use the bivalent compounds for the treatment of certain disease in a subject in need thereof. The disclosure also relates to methods for identifying such bivalent compounds.

MODIFIED PROTEINS AND PROTEIN DEGRADERS

Provided herein are compounds, pharmaceutical compositions, and methods for binding or degrading target proteins. Further provided herein are compounds having a DNA damage-binding protein 1 (DDB1) binding moiety. Some such embodiments include a linker. Some such embodiments include a target protein binding moiety. Further provided herein are ligand-DDB1 complexes. Further provided herein are in vivo modified DDB1 proteins.

TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE

Bivalent compounds, compositions comprising one or more of the bivalent compounds, and methods of use the bivalent compounds for the treatment of certain disease in a subject in need thereof are provided. Methods for identifying such bivalent compounds are provided, either.

Indazole compound for inhibiting kinase activity as well as composition and application thereof

The invention relates to an indazole compound for inhibiting kinase activity and relates to preparation and application of the indazole compound. Specifically, the invention discloses the indazole compound shown as a formula (I), or crystal forms, prodrugs, pharmaceutically acceptable salts, stereoisomers, tautomers, solvates or pharmaceutical compositions of hydrates of the indazole compound. Thecompound and the composition containing the compound, provided by the invention, have excellent inhibition performance on kinase protein, and also have better pharmacokinetics parameter characteristics at the same time; the medicine concentration of the compound in animals can be improved and the curative effect and safety of the medicine are improved. The formula (I) is shown in the description.

Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase responsible for the development of different tumor types. Despite the remarkable clinical activity of crizotinib (Xalkori), the first ALK inhibitor approved in 2011, the emergence of resistance mutations and of brain metastases frequently causes relapse in patients. Within our ALK drug discovery program, we identified compound 1, a novel 3-aminoindazole active on ALK in biochemical and in cellular assays. Its optimization led to compound 2 (entrectinib), a potent orally available ALK inhibitor active on ALK-dependent cell lines, efficiently penetrant the blood-brain barrier (BBB) in different animal species and highly efficacious in in vivo xenograft models. Moreover, entrectinib resulted to be strictly potent on the closely related tyrosine kinases ROS1 and TRKs recently found constitutively activated in several tumor types. Entrectinib is currently undergoing phase I/II clinical trial for the treatment of patients affected by ALK-, ROS1-, and TRK-positive tumors.

Highly efficient synthesis of 5-benzyl-3-aminoindazoles

A rapid and efficient procedure for the preparation of 5-benzyl-3-aminoindazoles 1 is reported. Key intermediates are fluoro-cyano diarylmethanes 2 which have been obtained by two different synthetic approaches. Benefits of these methods result from the u

SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS

Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.