859282-11-4

Usage

Uses

Used in Pharmaceutical Industry:
Benzoic acid, 4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)is used as a metabolite in the pharmaceutical industry for the development and study of flumatinib, a tyrosine kinase inhibitor. Flumatinib is prescribed for the treatment of gastrointestinal stromal tumors (GIST) and other cancer types. The presence of this metabolite helps researchers understand the drug's metabolism and potential side effects, as well as to optimize its therapeutic efficacy and safety profile.

Upstream product

• 161622-14-6 4-bromo-3-(trifluoromethyl)benzoic acid 
• 463355-64-8 4-bromo-3-trifluoromethyl-benzoic acid ethyl ester 
• 1262215-68-8 4-formyl-3-trifluoromethyl-benzoic acid ethyl ester 
• 109-01-3 1-methyl-piperazine 
• 863248-28-6 4-(bromomethyl)-3-(trifluoromethyl)benzoic acid methyl ester 
• 896160-80-8 4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylbenzoic acid methyl ester 
• 116419-94-4 4-methyl-3-(trifluoromethyl)benzoic acid methyl ester 
• 859213-39-1 4-(bromomethyl)-3-(trifluoromethyl)benzoic acid 
• 859027-01-3 4-bromomethyl-3-trifluoromethyl-benzoic acid ethyl ester 
• 859026-99-6 4-methyl-3-trifluoromethyl-benzoic acid ethyl ester 
• 261952-01-6 4-methyl-3-(trifluoromethyl)benzoic acid 
• 859027-00-2 4-(4-methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-benzoic acid ethyl ester 

Downstream Products

• 1616689-31-6 2-acetyl-1H-pyrrolo[2,3-b]pyridine-5-carboxylic acid {2-methyl-5-[4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylbenzoylamino]-phenyl}-amide 
• 1616689-85-0 5-[(tert-butoxycarbonyl-{3-[4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylbenzoylamino]-benzyl}-amino)-methyl]-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid methyl ester 
• 1616689-47-4 5-({3-[4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylbenzoylamino]-benzylamino}-methyl)-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid methyl ester 
• 1616689-51-0 5-(2-{3-[4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylbenzoylamino]-phenyl}-ethylamino)-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid methyl ester 
• 1616689-53-2 5-[2-(3-{[4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylbenzoylamino]-methyl}-phenyl)-ethyl]-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid methyl ester 
• 1616670-36-0 5-{2-chloro-5-[4-(4-methylpiperazin-1-ylmethyl)-3-trifluoromethylbenzoylamino]-benzylamino}-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid methyl ester 

Relevant academic research and scientific papers

ISOQUINOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF DISEASES

The present invention discloses compounds according to Formula (I) wherein R1, R2, R3, L1, L2, and L3 are as defined herein. The present invention relates to compounds inhibiting discoidin domain receptors (DDRs), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of fibrotic diseases, inflammatory diseases, respiratory diseases, autoimmune diseases, metabolic diseases, cardiovascular diseases, and/or proliferative diseases by administering a compound of the invention.

Discovery of a highly potent kinase inhibitor capable of overcoming multiple imatinib-resistant ABL mutants for chronic myeloid leukemia (CML)

As the critical driving force for chronic myeloid leukemia (CML), BCR gene fused ABL kinase has been extensively explored as a validated target of drug discovery. Although imatinib has achieved tremendous success as the first-line treatment for CML, the l

Evaluation of carbon-11 labeled 5-(1-methyl-1H-pyrazol-4-yl)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)nicotinamide as PET tracer for imaging of CSF-1R expression in the brain

Pharmacological targeting of tumor associated macrophages and microglia in the tumor microenvironment is a novel therapeutic strategy in the treatment of glioblastoma multiforme. As such, the colony stimulating factor-1 receptor (CSF-1R) has been identified as a druggable target. However, no validated companion diagnostic marker for these therapies exists to date. Towards development of a CSF-1R PET tracer, a set of six compounds based on recently reported CSF-1R inhibitor 5-(1-methyl-1H-pyrazol-4-yl)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)nicotinamide (Compound 5) was designed, synthesized and evaluated in vitro for potency and selectivity. The highest affinity for CSF-1R was found for compound 5 (IC50: 2.7 nM). Subsequent radiosynthesis of [11C]5 was achieved in 2.0 ± 0.2% yield (decay corrected to start of synthesis) by carbon-11 carbon monoxide aminocarbonylation in 40 min after end of bombardment. In vitro autoradiography with [11C]5 on rat brain sections demonstrated high specific binding, but also strong off-target binding. Ex vivo, only intact tracer was observed in blood plasma at 90 min post injection in healthy rats. PET scanning results demonstrated negligible brain uptake under baseline conditions and this brain uptake did not increase by blocking of efflux transporters using Tariquidar. To conclude, [11C]5 was successfully synthesized and evaluated in healthy rats. However, the inability of [11C]5 to cross the blood-brain-barrier excludes its use for imaging of CSF-1R expression in the brain.

NOVEL IMIDAZOPYRIDINE DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING CANCER

The present invention relates to a novel imidazopyridine derivative, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient for preventing or treating cancer. The novel imidazopyridine derivative acco

Synthetic method of intermediate of flumatinib mesylate

The invention discloses a synthetic method of an intermediate of flumatinib mesylate, and particularly relates to a preparation method of a key intermediate for synthesizing flumatinib mesylate. The initial raw material 4-methyl-3-trifluoro-methyl methyl

A novel structure of the kinase inhibitors

The invention provides compounds of a novel kinase inhibitor as shown in the formula (I) or pharmaceutically acceptable salts, solvates, esters, acids, metabolites, combination drugs or prodrugs thereof. The compounds independently combines with at least

3-ACETYLENYL-PYRAZOLE-PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USES THEREOF

The present invention relates to the field of chemical and medicine, more particularly, 3-ethynylpyrazolopyrimidine derivatives and their preparation methods and uses. The invention provides a 3-ethynylpyrazolopyrimidine derivative, and the structure is shown in formula I. The present invention also provides preparation methods and use of 3-ethynylpyrazolopyrimidine derivatives, comprising the compounds and derivatives, and their pharmaceutical compositions for the use of the treatment and prevention of tumors.

1H-1,8- NAPHTHYRIDIN-2ONES AS ANTI PROLIFERATIVE COMPOUNDS

The present invention relates to novel antiproliferative1H-1, 8-naphthyridin-2-ones of the general formula (I) or pharmaceutically acceptable salts thereof: In which the variable groups are as defined herein, and their preparation and use in therapeutic treatment of disorders related to inhibition of tyrosine kinases in warm blooded animals. The compounds can overcome imatinib induced drug resistance.

AZAINDOLE DERIVATIVES AS INHIBITORS OF PROTEIN KINASES

The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus a

PROTEIN KINASE INHIBITORS

The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus also includes the preparation of compounds of formula (I), their uses, in particular in the inhibition of protein kinases which are implicated for example in numerous diseases such as cancers or immune system disorders.