24129-04-2

Usage

Uses

Used in Pharmaceutical Industry:
3-Bromomethyl-phthalic acid dimethyl ester is used as a building block for the synthesis of various pharmaceutical compounds, contributing to the development of new drugs and therapeutic agents.
Used in Agrochemical Industry:
In the agrochemical sector, 3-Bromomethyl-phthalic acid dimethyl ester serves as a key intermediate in the production of agrochemicals, aiding in the creation of effective pesticides and other agricultural chemicals.
Used in Organic Synthesis:
3-Bromomethyl-phthalic acid dimethyl ester is employed as a reagent in organic synthesis, facilitating the formation of a range of organic compounds for various applications.
Used in Dye and Pigment Manufacturing:
This chemical compound is utilized as an intermediate in the manufacturing process of dyes and pigments, playing a crucial role in the production of colorants for different industries.

Upstream product

• 37102-74-2 3-methylphthalic acid 
• 21483-46-5 dimethyl 3-methylbenzene-1,2-dicarboxylate 
• 131-11-3 phthalic acid dimethyl ester 
• 764-28-3 (E)-3,3'-(diazene-1,2-diyl)bis(2-methylpropanenitrile) 

Downstream Products

• 935269-24-2 3-azidomethyl-phthalic acid dimethyl ester 
• 1010100-31-8 3-[(t-butoxycarbonyl-methyl-amino)-methyl]-phthalic dimethyl ester 

Relevant academic research and scientific papers

BIFUNCTIONAL COMPOUNDS FOR THE TREATMENT OF CANCER

The invention provides bifunctional compounds of formula (I) or a pharmaceutically acceptable salt thereof. Formula (I). The compounds cause the degradation of SMARCA2 via the targeted ubiquination of SMARCA2 protein and subsequent proteasomal degradation and are thus useful for the treatment of cancer. The targeting ligand is of formula (TL).

Design and optimization of aspartate N-acetyltransferase inhibitors for the potential treatment of Canavan disease

Canavan disease is a fatal neurological disorder caused by defects in the metabolism of N-acetyl-L-aspartate (NAA). Recent work has shown that the devastating symptoms of this disorder are correlated with the elevated levels of NAA observed in these patients, caused as a consequence of the inability of mutated forms of aspartoacylase to adequately catalyze its breakdown. The membrane-associated enzyme responsible for the synthesis of NAA, aspartate N-acetyltransferase (ANAT), has recently been purified and examined (Wang et al., Prot Expr Purif. 2016;119:11). With the availability, for the first time, of a stable and soluble form of ANAT we can now report the identification of initial inhibitors against this biosynthetic enzyme, obtained from the screening of several focused compound libraries. Two core structures of these moderate binding compounds have subsequently been optimized, with the most potent inhibitors in these series possessing sub-micromolar inhibition constants (Kivalues) against ANAT. Slowing the production of NAA via the inhibition of ANAT will lower the elevated levels of this metabolite and can potentially serve as a treatment option to moderate the symptoms of Canavan disease.

POTENT PHTHALATE INHIBITORS OF ASPARTATE N-ACETYLTRANSFERASE AND SELECTIVE ASPARTATE PATHWAY INHIBITORS

Phthalate derivatives that are aspartate-P-semialdehyde dehydrogenase (ASADH) inhibitor compounds, aspartate N-acetyltransferase (ANAT) inhibitor compounds, or both, are described, as well as methods of making the same, and methods of using the same.

Elaboration of a fragment library hit produces potent and selective aspartate semialdehyde dehydrogenase inhibitors

Aspartate-β-semialdehyde dehydrogenase (ASADH) lies at the first branch point in the aspartate metabolic pathway which leads to the biosynthesis of several essential amino acids and some important metabolites. This pathway is crucial for many metabolic processes in plants and microbes like bacteria and fungi, but is absent in mammals. Therefore, the key microbial enzymes involved in this pathway are attractive potential targets for development of new antibiotics with novel modes of action. The ASADH enzyme family shares the same substrate binding and active site catalytic groups; however, the enzymes from representative bacterial and fungal species show different inhibition patterns when previously screened against low molecular weight inhibitors identified from fragment library screening. In the present study several approaches, including fragment based drug discovery (FBDD), inhibitor docking, kinetic, and structure-activity relationship (SAR) studies have been used to guide ASADH inhibitor development. Elaboration of a core structure identified by FBDD has led to the synthesis of low micromolar inhibitors of the target enzyme, with high selectivity introduced between the Gram-negative and Gram-positive orthologs of ASADH. This new set of structures open a novel direction for the development of inhibitors against this validated drug-target enzyme.

N-METHYLAMINOMETHYL ISOINDOLE COMPOUNDS AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME

This invention relates to N-methylaminomethyl-isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: Design, synthesis, and biological activity

A novel series of 7-[1H-indol-2-yl]-2,3-dihydro-isoindol-1-ones designed to be inhibitors of VEGF-R2 kinase was synthesized and found to potently inhibit VEGF-R2 and Aurora-A kinases. The structure-based design, synthesis, and initial SAR of the series are discussed.

SUBSTITUTED DIHYDRO-ISOINDOLONES USEFUL IN TREATING KINASE DISORDERS

The present invention is directed to novel substituted dihydro-isoindolone compounds of formula (I): and forms thereof, wherein Ring A, X3, R1, R2, R3, R4 and R6 are as herein defined, and their synthesis and use as protein kinase inhibitors and interactions thereof.

CCK AND GASTRIN RECEPTOR LIGANDS

Compounds of formula (I) and their pharmaceutically active salts are gastrin and CCK receptor ligands, where Ar is a monocyclic aromatic group, R 1 is halo, amino, nitro, cyano, sulphamoyl, sulphonyl, trifluoromethyl, C 1 to C 3 alkyl, C 1 to C 3 alkylamino, C 1 to C 3 dialkylamino, phenyl, substituted phenyl, C 1 to C. sub.3 alkoxy, hydroxy, esterified hydroxy, C 1 to C 3 hydroxyalkyl, C 1 to C 3 alkylcarboxyamino, carboxy, esterified carboxy and amidated carboxy, m is 0, 1, 2, 3, or 4, provided that m is not more than 2 unless R 1 is exclusively halo, x+y=0 or 1, R 2 and R 4 independently are II, or C 1 to C 3 alkyl, R 3 is H or C 1 to C 15 hydrocarbyl, where one or more hydrogen atoms of die hydrocarbyl group may be replaced by a halogen atom, and where up to two of the carbon atoms may be replaced by a nitrogen, oxygen or sulphur atom, provided that R 3 does not contain a--O--O--group, R 5 is H or C 1 to C 3 alkyl, U is a cyclic moiety, selected from the group consisting of aryl, aromatic heterocyclic, non-aromatic heterocyclic, and cycloalkyl groups, where the aryl or aromatic group contains up to 3 substituents selected from the group consisting of halo, amino, nitro, cyano, sulphamoyl, sulphonyl, trifluoromethyl, C. sub.1 to C 3 alkyl, C 1 to C 3 alkylamino, C 1 to C 3 dialkylamino, phenyl, C 1 to C 3 alkoxy, hydroxy, esterified hydroxy, C 1 to C 3 hydroxyalkyl, C 1 to C 3 alkylcarboxyamino, carboxy, esterified carboxy and amidated carboxy, Z is a group of the formula (IIa) or (IIb) where R. sup.6 is H or C 1 to C. sub.3 alkyl, X is--CO 2 H, esterified carboxy, amidated carboxy, tetrazolyl, hydroxy, cyano, amidino,--CH 2 OH,--SO 2 NHCOR 7,--SONHCOR 7,--COR 7,--NHSO 2 R 7,--CONHSO 2 R. sup.7,--NHCOR 7 or--SO 2 NHR 8, where R. sup. 7 is C 1 to C 6, alkyl, C 1 to C 6 aryl or substituted aryl, and R 8 is--OH,--CN, C 1 to C 6 alkyl, C 1 to C. sub.6 haloalkyl, aryl or substituted aryl, Y is H or a group selected from those recited above for X, and a is 0, 1, or 2. STR1