872091-85-5

Upstream product

• 68432-92-8 methyl 3-cyanomethylbenzoate 
• 74-88-4 methyl iodide 
• 67-56-1 methanol 
• 872091-00-4 3-(1-cyano-1-methylethyl)benzoic acid 
• 146257-39-8 2-<3-(carboxymethyl)phenyl>propionitrile 

Downstream Products

• 872091-38-8 N-[3-(8-chloro-4-oxo-4H-quinazolin-3-yl)-4-methylphenyl]-3-(1-cyano-1-methylethyl)benzamide 
• 872090-98-7 N-[3-(6-bromo-4-oxo-4H-quinazolin-3-yl)-4-methylphenyl]-3-(1-cyano-1-methylethyl)benzamide 
• 872091-24-2 N-[3-(7-bromo-4-oxo-4H-quinazolin-3-yl)-4-methylphenyl]-3-(1-cyano-1-methylethyl)benzamide 
• 951627-60-4 tert-butyl [3-(1-cyano-1-methylethyl)phenyl]carbamate 
• 915394-29-5 2-(3-aminophenyl)-2-methylpropanenitrile 
• 1351236-94-6 7-amino-N-(5-(3-(2-cyanopropan-2-yl)benzamido)-2-methylphenyl)-2-(ethylamino)thieno[2,3-b]pyrazine-6-carboxamide 

Relevant academic research and scientific papers

COMPOUNDS AND USES THEREOF

The present disclosure features compounds useful for the treatment of BAF complex-related disorders.

BIARYL AMIDE COMPOUNDS AS KINASE INHIBITORS

The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.

THIENO (2, 3B) PYRAZINE COMPOUNDS AS B-RAF INHIBITORS

The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer.

Design and synthesis of novel DFG-Out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffolds

To develop RAF/VEGFR2 inhibitors that bind to the inactive DFG-out conformation, we conducted structure-based drug design using the X-ray cocrystal structures of BRAF, starting from an imidazo[1,2-b]pyridazine derivative. We designed various [5,6]-fused bicyclic scaffolds (ring A, 1-6) possessing an anilide group that forms two hydrogen bond interactions with Cys532. Stabilizing the planarity of this anilide and the nitrogen atom on the six-membered ring of the scaffold was critical for enhancing BRAF inhibition. The selected [1,3]thiazolo[5,4-b]pyridine derivative 6d showed potent inhibitory activity in both BRAF and VEGFR2. Solid dispersion formulation of 6d (6d-SD) maximized its oral absorption in rats and showed significant suppression of ERK1/2 phosphorylation in an A375 melanoma xenograft model in rats by single administration. Tumor regression (T/C = -7.0%) in twice-daily repetitive studies at a dose of 50 mg/kg in rats confirmed that 6d is a promising RAF/VEGFR2 inhibitor showing potent anticancer activity.

THIENO (2, 3B) PYRAZINE COMPOUNDS AS B - RAF INHIBITORS

The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer.

HETEROCYCLIC COMPOUND AND USE THEREOF

Disclosed is a heterocyclic compound having a strong Raf inhibitory activity. Specifically disclosed is a compound represented by the formula (I), (II) or (III) below, or a salt thereof. (In the formulae, the symbols are as defined in the description.)

FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF

The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the specification, except a particular compound, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor or a cancer metastasis suppressor.

QUINAZOLINONE DERIVATIVES HAVING B-RAF INHIBITORY ACTIVITY

The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity

A series of amidoheteroaryl compounds were designed and synthesized as inhibitors of B-Raf kinase. Several compounds from the series show excellent potency in biochemical, phenotypic and mode of action cellular assays. Potent examples from the series have also demonstrated good plasma exposure following an oral dose in rodents and activity against the Ras-Raf pathway in tumor bearing mice.

CYCLYLAMINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity are disclosed. Specifically, a series of compounds of substituted or unsubstituted cyclylamine derivatives as shown in formulas (1).