537705-05-8

Upstream product

• 537705-06-9 3-(2-methyl-4-aminophenoxy)-6-methylpyridine 
• 16064-08-7 6-iodoquinazolin-4(3H)-one 
• 5326-47-6 2-amino-5-iodobenzoic acid 
• 13290-74-9 1-chloro-2-methyl-4-nitrobenzene 
• 16064-08-7 6-iodo-4-hydroxyquinazoline 
• 697299-78-8 2-methyl-5-(2-methyl-4-nitrophenoxy)pyridine 
• 1121-78-4 5-Hydroxy-2-methylpyridine 
• 98556-31-1 4-chloro-6-iodoquinazoline 

Downstream Products

• 537705-08-1 CP-724714 
• 383432-38-0 (E)-2-methoxy-N-(3-{4-[3-methyl-4-(6-methylpyridin-3-yloxy)phenylamino]quinazolin-6-yl}allyl)acetamide 
• 1260402-01-4 N-(4-(6-methylpyridin-3-yloxy)-3-methylphenyl)-6-(5-((4-methyl-1,4-azaphosphinan-1-yl)methyl)furan-2-yl)quinazolin-4-amine 
• 1260402-39-8 5-(4-(4-(6-methylpyridin-3-yloxy)-3-methylphenylamino)quinazolin-6-yl)furan-2-carbaldehyde 

Relevant academic research and scientific papers

Compounds capable of inhibiting ErbB/HDAC and preparation method thereof, and pharmaceutical composition comprising compounds and application thereof

The invention relates to compounds capable of inhibiting ErbB/HDAC and a preparation method thereof, and a pharmaceutical composition comprising the compounds and application thereof. The compounds are disclosed as Formula 1. The compounds or pharmaceutically acceptable salts, solvates, esters, acids, metabolites or prodrugs thereof, or the pharmaceutical composition comprising the compounds can be used for preparing ErbB kinases and HDAC activity inhibitors and also preparing ErbB-kinase/HDAC-activated mediated disease curatives.

Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy

By merging the critical pharmacophore of EGFR/HER2 and HDAC inhibitors into one compound, a novel series of EGFR, HER-2, and HDAC multitarget inhibitors were synthesized. Compounds 9a–l contained 4-anilinoquinazolines with C-6 triazole-linked long alkyl chains of hydroxamic acid and displayed excellent inhibition against these enzymes (compound 9d exhibited the best inhibitory potency on wild-type EGFR, HDAC1, and HDAC6 with IC50values 0.12 nM, 0.72 nM and 3.2 nM individually). Furthermore, compounds 9b and 9d potently inhibited proliferation of five human cancer cell lines (with IC50values between 0.49 and 8.76 μM). Further mechanistic study revealed that compound 9d also regulated the phosphorylation of EGFR and HER2 and histone H3 hyperacetylation on the cellular level and induced remarkable apoptosis in BT-474 cells. Therefore, our study suggested that a system network-based multi-target drug design strategy might provided an alternate drug design method, by taking into account the synergy effect of EGFR, HER-2 and HDAC.

[...] tyrosine kinase inhibitor and its preparation and application

The invention discloses a [...] tyrosine kinase inhibitor and its preparation and application, the tyrosine kinase inhibitor is [...] general formula (I) a compound represented by the formula, its various optical isomer or its pharmaceutically acceptable salt; in accordance with the preparation process of the preparation method of the conventional compounds. The [...] tyrosine kinase inhibitor on tyrosine kinase have a strong inhibiting activity, has excellent pharmacokin nature, the cardiovascular system has very good safety and can significantly inhibit the growth of tumors, can be used in the preparation of the treatment of tyrosine kinase-related disease.

Design, synthesis and biological evaluation of lapatinib derivatives as HER1/HER2 inhibitors

Five Lapatinib derivatives were designed by structurally modifying the side chain as well as the aniline substituent. The ELISA assay showed that the derivatives retained or even improved the inhibitory activity of Lapatinib against HER1/HER2. In vitro cy

PHOSPHORUS CONTAINING QUINAZOLINE COMPOUNDS AND METHODS OF USE

Disclosed are novel quinazoline derivatives containing phosphorus substitutions and methods for the treatment of hyperproliferative diseases (e.g. cancer) using the compounds. These compounds are type I receptor protein kinase inhibitors useful in treating disorders related to abnormal protein kinase activities such as cancer and inflammation in mammals. Also disclosed are pharmaceutical compositions containing the compounds, methods for the preparation of the compounds and their pharmaceutically acceptable salts.

Highly functionalised sulfur-based silica scavengers for the efficient removal of palladium species from active pharmaceutical ingredients

The use of multidentate sulfur-based silica scavengers 1,2, and 3 as highly effective adsorbents for the removal of precious metals, specifically palladium residues in this paper, from highly functionalised synthetic intermediates and APIs is described. The synthesis and purification of the polar and electron-rich reaction products, containing multiple functional groups, from palladium-catalysed removals of commonly used protecting groups such as benzyl, benzyloxycarbonyl, and allyloxycarbonyl and Sonogashira, Suzuki, Heck, and Buchwald-Hartwig coupling reactions is reported. The significant levels of residual palladium species, typically associated with these reaction products, are successfully and rapidly removed to below acceptable regulatory levels, of less than 5 ppm, by simple, unoptimised treatment with the designed silica scavengers at room temperature. Performance aspects, including broad solvent compatibility, excellent stability, and high metal affinity, combined with large-scale availability, ease of handling, and minimal loss of API make these silica scavengers particularly useful to process development groups.

Crystal forms of E-2-Methoxy-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide

Crystal forms of E-2-Methoxy-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide. A crystal form is useful in the synthesis of salts and complexes of E-2-Methoxy-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide. A crystal form also improves stability of tabletted or capsuled E-2-Methoxy-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide as a drug product.

COMPLEXES OF E-2-METHOXY-N-(3-{4-[3-METHYL-4-(6-METHYL-PYRIDIN-3-YLOXY)-PHENYLAMINO]-QUINAZOLIN-6-YL}-ALLYL)-ACETAMIDE, THEIR METHOD OF PRODUCTION, AND USE

The invention relates to complexes of E-2-Methoxy-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide having the following formula I: The invention also relates to pharmaceutical compositions containing the complexes of formula I. The invention further relates to methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above complexes and to methods of preparing the above complexes.