178990-43-7Relevant academic research and scientific papers
Quinazoline, Quinoline Derivatives and Their Use as EGFR Kinase Inhibitors
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Paragraph 0283-0286, (2018/12/01)
The present invention relates to quinazoline, a quinoline derivative, and a use thereof as an epidermal growth factor receptor (EGFR) kinase inhibitor. A pharmaceutical composition comprising the quinazoline represented by chemical formula 1, the quinoline derivative, or a respective pharmaceutically acceptable salt thereof, inhibits EGFR (del E746-A750/T790M/C797S) kinase, and thus is able to treat diseases related to EGFR (del E746-A750/T790M/C797S) such as non-small-cell lung cancer.COPYRIGHT KIPO 2018
AMINO-ETHYL-AMINO-ARYL (AEAA) COMPOUNDS AND THEIR USE
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Page/Page column 136; 138, (2009/10/06)
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain amino-ethyl-amino-aryl (AEAA) compounds which, inter alia, inhibit protein kinase D (PKD) (e.g., PKD1, PKD2, PKD3). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PKD, and in the treatment of diseases and conditions that are mediated by PKD, that are ameliorated by the inhibition of PKD, etc., including proliferative conditions such as cancer, etc.
THERAPEUTIC OXY-PHENYL-ARYL COMPOUNDS AND THEIR USE
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Page/Page column 125, (2009/05/28)
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.
Oxadiazoles as bioisosteric transformations of carboxylic functionalities. II
Andersen,Lundt,Jorgensen,Braestrup
, p. 417 - 425 (2007/10/03)
In order to improve the in vivo efficacy of a series of known benzodiazepine receptor (BZR) ligands, 1-(2-phenyl-4-quinolinyl)-4-piperidinecarboxamides, a series of analogs has been prepared in which the amide group of these ligands has been replaced by a 1,2,4-oxadiazole moiety or converted to other carboxylic isosters such as esters or nitriles. An increase in the in vivo efficacy was observed for some of the compounds prepared in this investigation compared to the parent carboxamide derivatives.
