85953-31-7

Usage

Uses

Used in Pharmaceutical Industry:
2-Bromo-4-fluoro-5-nitrobenzoic acid methyl ester is used as a key intermediate in the synthesis of quinoxaline derivatives, which are known as phosphodiesterase 9 (PDE9) inhibitors. PDE9 inhibitors are a class of compounds that have potential therapeutic applications in treating various diseases, including neurological disorders and cognitive impairments, by modulating the levels of cyclic guanosine monophosphate (cGMP) in cells.
In the preparation of quinoxaline derivatives, 2-bromo-4-fluoro-5-nitrobenzoic acid methyl ester serves as a valuable building block, allowing for the development of novel PDE9 inhibitors with improved potency, selectivity, and pharmacokinetic properties. This makes it an important compound for medicinal chemistry research and drug discovery efforts aimed at identifying new treatments for various medical conditions.

Upstream product

• 653-92-9 methyl 2-bromo-4-fluorobenzoate 
• 1006-41-3 2-bromo-4-fluorobenzoic acid 
• 67-56-1 methanol 
• 1036389-83-9 2-bromo-4-fluoro-5-nitrobenzoic acid 

Downstream Products

• 1036389-90-8 6-amino-5-fluoro-isoindolin-1-one 

Relevant academic research and scientific papers

IRAK DEGRADERS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same. The compounds include an IRAK binding moiety capable of binding to IRAK4 and a degradation inducing moiety (DIM). The DIM could be DTM a ligase binding moiety (LBM) or lysine mimetic. The compounds could be useful as IRAK protein kinase inhibitors and applied to IRAK mediated disorders.

ASK1 INHIBITOR COMPOUNDS AND USES THEREOF

Described herein are compounds, including pharmaceutically acceptable salts, solvates, metabolites, prodrugs thereof, methods of making such compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat non

cGAS ANTAGONIST COMPOUNDS

Disclosed are novel compounds of Formula (I) that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.

Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors

Inhibitors of Factor VIIa (FVIIa), a serine protease in the clotting cascade, have shown strong antithrombotic efficacy in preclinical thrombosis models with minimal bleeding liabilities. Discovery of potent, orally active FVIIa inhibitors has been largely unsuccessful because known chemotypes have required a highly basic group in the S1 binding pocket for high affinity. A recently reported fragment screening effort resulted in the discovery of a neutral heterocycle, 7-chloro-3,4-dihydroisoquinolin-1(2H)-one, that binds in the S1 pocket of FVIIa and can be incorporated into a phenylglycine FVIIa inhibitor. Optimization of this P1 binding group led to the first series of neutral, permeable FVIIa inhibitors with low nanomolar potency.

Sulfo-imidazole-diketone and imidazole-diketone compound and applications thereof

The invention discloses a sulfo-imidazole-diketone and imidazole-diketone compound and applications thereof. The invention provides the formula (I) compound (please see the specification) or pharmaceutical salt, solvate, prodrug, stereoisomer, tautomer and metabolite thereof, wherein X, Y, Z, R1, R2, R3 and A are defined in the formula. The invention further provides a preparing method for the compound and applications of the compound serving as an androgen receptor antagonist to treating diseases related to an androgen receptor, such as prostatic cancer, prostatic hyperplasia, acne, feather-loss disorder, hair hyperplasia, breast cancer and poor male sexual function.

A kind of diaryl hydanto?n derivatives, its preparation method, pharmaceutical composition and application

Provided are a compound as represented by formula I, or pharmaceutically acceptable salt, solvate, precursor drug, stereoisomer, tautomer, polymorph or metabolite thereof, pharmaceutical composition containing same, and uses thereof in the preparation of drugs for treating androgen receptor related diseases.

BICYCLIC LACTAM FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS

The present invention provides novel bicyclic lactams derivatives, and analogues thereof, of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, B, C, W, Y, Z1, Z2, Z3, Z4, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.

MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS

The present invention relates generally to novel macrocycles of Formula (I) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.

Bicyclic pyrazole compounds as antibacterial agents

Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.

Tetrahydrophthalimides, and their production and use

A compound of the formula: STR1 wherein X is a chlorine atom or a bromine atom, which is useful as a herbicide.