853908-81-3

Usage

Uses

Used in Organic Synthesis:
6-bromo-4-chloro-7-fluoro-3-nitroquinoline is used as a building block for the synthesis of various organic compounds. Its unique combination of halogen and nitro substituents allows for versatile chemical reactions and modifications, making it a valuable component in the development of new organic molecules.
Used in Pharmaceutical Research:
In the pharmaceutical industry, 6-bromo-4-chloro-7-fluoro-3-nitroquinoline is utilized as a starting material for the development of new drugs. Its potential biological activities, such as antibacterial and antifungal properties, make it a promising candidate for the creation of novel therapeutic agents.
Used in Medicinal Research:
6-bromo-4-chloro-7-fluoro-3-nitroquinoline is employed as a valuable tool in medicinal research. Its unique functional groups enable it to be used in the study of various biological activities and interactions, contributing to the advancement of medical knowledge and the development of new treatments.

Upstream product

• 143945-65-7 2-amino-4-fluoro-5-bromobenzoic acid 
• 1656989-76-2 6-bromo-7-fluoro-3-nitroquinolin-4-ol 

Relevant academic research and scientific papers

Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action

Mutations in MEK1/2 have been described as a resistance mechanism to BRAF/MEK inhibitor treatment. We report the discovery of a novel ATP-competitive MEK1/2 inhibitor with efficacy in wildtype (WT) and mutant MEK12 models. Starting from a HTS hit, we obtained selective, cellularly active compounds that showed equipotent inhibition of WT MEK1/2 and a panel of MEK1/2 mutant cell lines. Using a structure-based approach, the optimization addressed the liabilities by systematic analysis of molecular matched pairs (MMPs) and ligand conformation. Addition of only three heavy atoms to early tool compound 6 removed Cyp3A4 liabilities and increased the cellular potency by 100-fold, while reducing log P by 5 units. Profiling of MAP855, compound 30, in pharmacokinetic-pharmacodynamic and efficacy studies in BRAF-mutant models showed comparable efficacy to clinical MEK1/2 inhibitors. Compound 30 is a novel highly potent and selective MEK1/2 kinase inhibitor with equipotent inhibition of WT and mutant MEK1/2, whose drug-like properties allow further investigation in the mutant MEK setting upon BRAF/MEK therapy.

DUAL ATM AND DNA-PK INHIBITORS FOR USE IN ANTI-TUMOR THERAPY

Provided herein are compounds of the Formula (I), (II), and (III), as well as pharmaceutically acceptable salts thereof, wherein the substituents are those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of oncologic diseases.

COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK

The present invention relates to compounds of formula I: in which n, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a pro

COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK

The present invention relates to compounds of formula I in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.

COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK

The present invention relates to compounds of formula I: in which n, Y, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention fur

COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK

The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.

IMIDAZOQUINOLINES AS LIPID KINASE INHIBITORS

The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment of an inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease.

1H-IMIDAZOQUINOLINE DERIVATIVES AS PROTEIN KINASE INHIBITORS

The invention relates to imidazoquinolines of formula (I) for use in the treatment of protein kinase dependent diseases; pharmaceutical preparations comprinsing an imidazoquinoline, especially for the treatment of a pretein kinase dependent disease; novel imidazoquinolines; and a process for the preparation of the novel imidazoquinilines.