40928-15-2

Upstream product

• 118-48-9 isatoic anhydride 
• 593-56-6 N-methoxylamine hydrochloride 
• 5344-90-1 2-Aminobenzyl alcohol 
• 67-62-9 O-Methylhydroxylamin 

Downstream Products

• 40928-18-5 2-amino-5-bromo-N-methoxybenzamide 
• 1184931-57-4 2-(5-bromo-2-chloro-pyridin-4-ylamino)-N-methoxy-benzamide 
• 1061358-81-3 2-(2-chloro-5-cyano-pyridin-4-ylamino)-N-methyl-benzamide 
• 1453199-51-3 2-(2-(5-amino-2-methoxyphenylamino)-5-chloropyrimidin-4-ylamino)-N-methoxybenzamide 
• 1453199-52-4 2-(2-(5-acrylamido-2-methoxyphenylamino)-5-chloropyrimidin-4-ylamino)-N-methoxybenzamide 
• 1453199-60-4 2-(5-chloro-2-(2-methoxy-5-(vinylsulfonamido)phenylamino)pyrimidin-4-ylamino)-Nmethoxybenzamide 
• 1453199-49-9 2-(5-chloro-2-(2-methoxy-5-nitrophenylamino)pyrimidin-4-ylamino)-N-methoxybenzamide 
• 1453199-48-8 2-((2,5-dichloropyrimidin-4-yl)amino)-N-methoxybenzamide 
• 1264037-81-1 2-(2-(trifluoromethyl)phenyl)quinazolin-4(3H)-one 
• 18818-41-2 2-(4-methylphenyl)-4(3H)-quinazolinone 
• 1152-07-4 2-(4-methoxyphenyl)-3H-quinazolin-4-one 
• 89860-51-5 2-(4-hydroxyphenyl)-4(3H)-quinazolinone 
• 1613113-57-7 2-(2,6-dichlorophenyl)quinazolin-4(3H)-one 
• 132982-03-7 2-(3¹,4¹-dimethoxyphenyl)quinazol-4-one 

Relevant academic research and scientific papers

SUBSTITUTED PYRIMIDINES, PHARMACEUTICAL COMPOSITIONS AND THERAPEUTIC METHODS THEREOF

The invention provide novel pyrimidine derivatives and analogs having inhibitory activities towards certain tyrosine kinases, e.g., Bruton's tyrosine kinase (Btk) and/or Focal adhesion kinase (FAK), extracellular signal-regulated kinase (ERK), pharmaceutical compositions thereof, and methods of treatment, reduction or prevention of certain diseases or conditions mediated by such by tyrosine kinases, e.g., cancers, tumors, fibrosis, inflammatory diseases, autoimmune diseases, diabetes, or immunologically mediated diseases.

Sustainable methine sources for the synthesis of heterocycles under metal- and peroxide-free conditions

Alcohols and ethers were identified as sustainable methine sources for synthesizing quinazolinone and benzimidazole derivatives using a combination of TsOH·H2O/O2 and appropriate bis-nucleophiles for the first time. Deuterium labeling studies clearly proved that the C2 hydrogen of the synthesized heterocycles came from the methine source. These unique reaction conditions were successfully applied to the synthesis of echinozolinone (2e′), 2f′ (a common precursor of rutaecarpine and (±) evodiamine), and dimedazole (6d). Notable features of this method include its low toxicity, use of commercial feedstocks as substrates, low cost, broad functional group tolerance and suitability for a wide range of bis-nucleophilic starting materials.

Focal adhesion kinase inhibitor and use

The invention belongs to the field of medicines, relates to a focal adhesion kinase inhibitor and use, in particular relates to a novel focal adhesion kinase inhibitor compound, or stereoisomers, geometric isomers, tautomers, oxynitrides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, further relates to the use of the compound and pharmaceutical compositions as medicines, in particular the use of the compound and pharmaceutical compositions in manufacture of medicines for treatment or prevention of cancer, pulmonary hypertension, and pathological angiogenesis-related diseases.

One-pot synthesis of quinazolinones from anthranilamides and aldehydes via p -toluenesulfonic acid catalyzed cyclocondensation and phenyliodine diacetate mediated oxidative dehydrogenation

A variety of 4(3H)-quinazolinones are synthesized conveniently in one pot from 2-aminobenzamides and aldehydes, via cyclization catalyzed by p-toluenesulfonic acid followed by oxidative dehydrogenation mediated by the hypervalent iodine compound phenyliodine diacetate [PhI(OAc)2, PIDA]. Highlights of the described method include the first synthesis of quinazolinones bearing an N-alkoxy substituent, a new application of phenyliodine diacetate as an efficient dehydrogenative oxidant, and mild reaction conditions. Georg Thieme Verlag Stuttgart, New York.

Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)

A novel series of small-molecule inhibitors has been developed to target the double mutant form of the epidermal growth factor receptor (EGFR) tyrosine kinase, which is resistant to treatment with gefitinib and erlotinib. Our reported compounds also show selectivity over wild-type EGFR. Guided by molecular modeling, this series was evolved to target a cysteine residue in the ATP binding site via covalent bond formation and demonstrates high levels of activity in cellular models of the double mutant form of EGFR. In addition, these compounds show significant activity against the activating mutations, which gefitinib and erlotinib target and inhibition of which gives rise to their observed clinical efficacy. A glutathione (GSH)-based assay was used to measure thiol reactivity toward the electrophilic functionality of the inhibitor series, enabling both the identification of a suitable reactivity window for their potency and the development of a reactivity quantitative structure-property relationship (QSPR) to support design.

Two-directional approach for the rapid synthesis of 2,4-bis-aminoaryl pyridine derivatives

We have developed two different approaches in parallel to rapidly access 2,4-bis aminoaryl pyridine compounds from a common starting material. The C-4/C-2 approach uses palladium-mediated coupling reactions to sequentially functionalize C-4 and then C-2. An alternative C-2/C-4 route uses a regioselective SNAr reaction to first substitute at C-2 then subsequently at C-4 by a palladium-mediated reaction. Both approaches have been used successfully to provide a range of 2,4-bis-aminoaryl pyridine compounds.

PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK

The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R11, R12, R13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.

PYRIDINE COMPOUNDS

The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.

ANILINOPYRIDINES AS INHIBITORS OF FAK

The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R4, Q, Z, r, and p are as defined herein. Compounds of the present invention are useful in the treatment of diseases associated with FAK overexpression, including proliferative diseases.