808793-73-9

Upstream product

• 367-21-5 3-chloro-4-fluorophenylamine 
• 692059-26-0 4-chloro-6-(2-chloroethoxy)-7-methoxyquinazoline 
• 1188906-91-3 6-(2-chloroethoxy)-4-hydroxy-7-methoxyquinazoline 
• 1188906-90-2 methyl 2-amino-5-(2-chloroethoxy)-4-methoxybenzoate 
• 1188906-89-9 methyl 5-(2-chloroethoxy)-4-methoxy-2-nitrobenzoate 
• 895244-45-8 methyl 3-(2-chloroethoxy)-4-methoxybenzoate 
• 1176169-43-9 C₁₀H₁₁ClO₄ 
• 165121-44-8 3-(2-chloroethoxy)-4-methoxybenzaldehyde 
• 621-59-0 isovanillin 
• 16670-48-7 2-chloroethyl benzenesulfonate 
• 184475-71-6 4-(3-chloro-4-fluorophenylamino)-6-hydroxy-7-methoxyquinazoline 

Downstream Products

• 1445861-29-9 4-(3'-chloro-4'-fluorophenylamino)-6-[2-(2-oxa-6-azaspiro[3.3]heptane-6-yl)oxethyl]-7-methoxyquinazoline 
• 1456070-09-9 C₂₂H₂₂ClFN₄O₃ 
• 1456070-10-2 C₂₂H₂₂ClFN₄O₂S 
• 1456070-11-3 C₂₂H₂₂ClFN₄O₄S 
• 1456070-12-4 C₂₀H₂₀ClFN₄O₃ 
• 1456070-13-5 C₂₁H₂₂ClFN₄O₃ 

Relevant academic research and scientific papers

Quinazoline-1-deoxynojirimycin hybrids as high active dual inhibitors of EGFR and α-glucosidase

A series of novel quinazoline-1-deoxynojirimycin hybrids were designed, synthesized and evaluated for their inhibitory activities against two drug target enzymes, epidermal growth factor receptor (EGFR) tyrosine kinase and α-glucosidase. Some synthesized compounds exhibited significantly inhibitory activities against the tested enzymes. Comparing with reference compounds gefitinib and lapatinib, compounds 7d, 8d, 9b and 9d showed higher inhibitory activities against EGFR (IC50: 1.79–10.71 nM). Meanwhile the inhibitory activities of 7d, 8d and 9c against α-glucosidase (IC50 = 0.14, 0.09 and 0.25 μM, respectively) were obvious higher than that of miglitol (IC50 = 2.43 μM), a clinical using α-glucosidase inhibitor. Interestingly, compound 9d as a dual inhibitor showed high inhibitory activity to EGFRwt tyrosine kinase (IC50 = 1.79 nM), also to α-glucosidase (IC50 = 0.39 μM). The work could be very useful starting point for developing a new series of enzyme inhibitors targeting EGFR and/or α-glucosidase.

Four-membered heterocycles-containing 4-anilino-quinazoline derivatives as epidermal growth factor receptor (EGFR) kinase inhibitors

We report herein the design and synthesis of novel azaspirocycle or azetidine substituted 4-anilinoquinazoline derivatives. The EGFR inhibitory activities and in vitro antitumor potency of these newly synthesized compounds against two lung cancer cell lines HCC827 and A549 were evaluated. Most of the target compounds possess good inhibitory potency. In particular, compounds 21g with 2-oxa-6-azaspiro[3.4]octane substituent was found to possess higher EGFR inhibitory activities and similar antitumor potency comparing to the lead compound gefitinib with improved water solubility.

BICYCLIC HETEROCYCLES, DRUGS CONTAINING SAID COMPOUNDS, THE USE THEREOF AND METHOD FOR PREPARING THE SAME

The invention relates to the bicyclic heterocycles of general formula (I), wherein R, R, R, R, X and n are defined as in claim 1, to their tautomers, stereoisomers, mixtures and salts thereof, especially the physiologically acceptable salts thereof with inorganic or organic acids. The inventive compounds have valuable pharmacological properties, especially they inhibit tyrosinkinase-mediated signal transduction. The invention also relates to the use of said compounds for treating diseases, especially tumor diseases and benign prostatic hyperplasia (BPH), diseases of the lung and respiratory tracts, and to the production of these compounds.