134517-34-3Relevant articles and documents
QUINAZOLINE COMPOUNDS AND THE USE THEREOF IN THE TREATMENT OF CANCER
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Paragraph 00165, (2021/08/13)
The present disclosure relates generally to a class of quinazoline compounds, compositions containing the same and the therapeutic use of the compounds in the treatment of cancer.
Evaluation of quinazoline analogues as glucocerebrosidase inhibitors with chaperone activity
Marugan, Juan J.,Zheng, Wei,Motabar, Omid,Southall, Noel,Goldin, Ehud,Westbroek, Wendy,Stubblefield, Barbara K.,Sidransky, Ellen,Aungst, Ronald A.,Lea, Wendy A.,Simeonov, Anton,Leister, William,Austin, Christopher P.
experimental part, p. 1033 - 1058 (2011/04/25)
Gaucher disease is a lysosomal storage disorder (LSD) caused by deficiency in the enzyme glucocerebrosidase (GC). Small molecule chaperones of protein folding and translocation have been proposed as a promising therapeutic approach to this LSD. Most small molecule chaperones described in the literature contain an iminosugar scaffold. Here we present the discovery and evaluation of a new series of GC inhibitors with a quinazoline core. We demonstrate that this series can improve the translocation of GC to the lysosome in patient-derived cells. To optimize this chemical series, systematic synthetic modifications were performed and the SAR was evaluated and compared using three different readouts of compound activity: enzymatic inhibition, enzyme thermostabilization, and lysosomal translocation of GC.
Heterocyclic compounds and their preparation and use
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, (2008/06/13)
New imidazoquinazoline compounds having the general formula STR1 wherein A together with the α-marked carbon atom and the β-marked nitrogen atom is one of the groups STR2 wherein R4, R5, R6 and R7 independently are hydrogen, halogen C1-6 -alkyl, aryl or aralkyl R1 is STR3 cyano or CO2 R8, wherein R8 is hydrogen, C1-6 -alkyl or C3-7 -cycloalkyl, trifluoromethyl or C1-6 -alkoxymethyl, R2 and R3 independently are hydrogen, halogen, CN, C1-6 -alkyl, C2-6 -alkenyl, C2-6 -alkynyl, trifluoromethyl, C1-6 -alkoxy, dialkylaminoalkoxy, aralkoxy, aryloxy which may be substituted with halogen or alkoxy, a cyclic amino group, or NR9 R10, wherein R9 and R10 independently are hydrogen or C1-6 -alkyl. The compounds are useful in psychopharmaceutical preparations as anticonvusants, anxiolytics, hypnotics, antipsychotics, antiemetics, or in improving the cognitive function of the brain of mammals.