1001345-80-7

Upstream product

• 67-56-1 methanol 
• 116465-48-6 2,5‐difluoro‐4‐nitrobenzoic acid 
• 924868-81-5 methyl 2,5-difluoro-4-nitrobenzoate 
• 124-41-4 sodium methylate 

Downstream Products

• 1001345-79-4 2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)-4-nitrobenzamide 
• 1001346-91-3 4-amino-2-fluoro-5-methoxy-benzoic acid 
• 1137867-66-3 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-2-fluoro-5-methoxy-benzoic acid 
• 1137868-52-0 TAK-960 
• 1022947-91-6 methyl 2-fluoro-5-methoxy-4-nitrobenzoate 
• 1351761-44-8 GNE-7915 
• 1018317-68-4 4-[(5-cyclopentyl-4-ethyl-2-methyl-3-oxo-2,4,5,7,9-pentazabicyclo[4.4.0]deca-6,8,10-trien-8-yl)amino]-2-fluoro-5-methoxy-N-(1-methyl-4-piperidyl)benzamide 
• 1018318-11-0 4-amino-N-(4-dimethylaminocyclohexyl)-2-fluoro-5-methoxy-benzamide 
• 1001347-08-5 4-amino-N-(1-ethyl-4-piperidyl)-2-fluoro-5-methoxy-benzamide 
• 1001347-29-0 4-amino-2-fluoro-5-methoxy-N-(2-pyrrolidin-1-ylethyl)benzamide 
• 1001346-90-2 4-amino-2-fluoro-5-methoxy-N-[(3R)-1-methylpyrrolidin-3-yl]benzamide 
• 1001345-78-3 4-amino-5-methoxy-2-fluoro-N-(1-methyl-piperidin-4-yl)-benzamide 
• 1214266-01-9 2-fluoro-5-methoxy-4-nitro-N-(4-oxocyclohexyl)benzamide 

Relevant academic research and scientific papers

The tale of proteolysis targeting chimeras (PROTACs) for Leucine-Rich Repeat Kinase 2 (LRRK2)

Here we present the rational design and synthetic methodologies towards proteolysis-targeting chimeras (PROTACs) for the recently-emerged target leucine-rich repeat kinase 2 (LRRK2). Two highly potent, selective, brain-penetrating kinase inhibitors were selected, and their structure was appropriately modified to assemble a cereblon-targeting PROTAC. Biological data show strong kinase inhibition and the ability of the synthesized compounds to enter the cells. However, data regarding the degradation of the target protein are inconclusive. The reasons for the inefficient degradation of the target are further discussed.

METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present invention can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

INDOLE CARBOXAMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS

The invention relates to indole carboxamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.

Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1)

Using structure-based drug design, we identified and optimized a novel series of pyrimidodiazepinone PLK1 inhibitors resulting in the selection of the development candidate TAK-960. TAK-960 is currently undergoing Phase I evaluation in adult patients with

POLO-LIKE KINASE INHIBITORS

Compounds of the following formula are provided for use with kinases: (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates use

NOVEL COMPOUNDS

There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.