529508-58-5Relevant articles and documents
Hetero-aromatic compound and its use in medicine
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Paragraph 0908; 0913-0916; 1489; 1492-1495, (2019/07/04)
The invention provides a hetero-aromatic compound or a stereisomer, geometric isomer, tautomer, despinner, nitrogen oxide, hydrate, solvate, metabolite, metabolism precursor and pharmaceutically acceptable salt or prodrug thereof, which is used for treating proliferative diseases. The invention also discloses a pharmaceutical composition containing the compound and an application of the compound or pharmaceutical composition thereof in preparation of a medicine for treating proliferative diseases.
QUINAZOLINE COMPOUNDS
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Page/Page column 11, (2012/01/14)
Provided are certain quinazoline compounds, compositions thereof and methods of use thereof. These quinazoline compound can effectively inhibit the overexpression and/or overactivity of epidermal growth factor receptor (EGFR).
QUINAZOLINE COMPOUNDS
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Page/Page column 10-11, (2012/01/14)
Provided are certain quinazoline compounds, compositions thereof and methods of use thereof. These quinazoline compounds can effectively inhibit the overexpression and/or overactivity of epidermal growth factor receptor (EGFR).
PHOSPHORUS CONTAINING QUINAZOLINE COMPOUNDS AND METHODS OF USE
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Page/Page column 63, (2011/02/24)
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.
Synthesis and cytotoxic activity of 2,5-disubstituted pyrimido[5,4-c] quinoline derivatives
Zhang, Fan,Zhai, Xin,Chen, Li Juan,Qi, Jian Guo,Cui, Bo,Gu, Yu Cheng,Gong, Ping
scheme or table, p. 1277 - 1280 (2012/01/06)
A series of 2,5-disubstituted pyrimido[5,4-c]quinoline derivatives were synthesized and their cytotoxic activity against H460, HT-29 and MDA-MB-231 cell lines was evaluated in vitro. It was found that most of the tested compounds especially compound 17, s
Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H- indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epide
Gavai, Ashvinikumar V.,Fink, Brian E.,Fairfax, David J.,Martin, Gregory S.,Rossiter, Lana M.,Holst, Christian L.,Kim, Soong-Hoon,Leavitt, Kenneth J.,Mastalerz, Harold,Han, Wen-Ching,Norris, Derek,Goyal, Bindu,Swaminathan, Shankar,Patel, Bharat,Mathur, Arvind,Vyas, Dolatrai M.,Tokarski, John S.,Chiang, Yu,Oppenheimer, Simone,Hongjian, Zhang,Marathe, Punit,Fargnoli, Joseph,Lee, Francis Y.,Wong, Tai W.,Vite, Gregory D.
supporting information; experimental part, p. 6527 - 6530 (2010/03/26)
Structure-activity relationships in a series of 4-[1H-indazol-5-ylamino] pyrrolo[2,1-f][1,2,4]triazine-6-carbamates identified dual human epidermal growth factor receptor (HER)1/HER2 kinase inhibitors with excellent biochemical potency and kinase selectiv
Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors
Waterson, Alex G.,Petrov, Kimberly G.,Hornberger, Keith R.,Hubbard, Robert D.,Sammond, Douglas M.,Smith, Stephon C.,Dickson, Hamilton D.,Caferro, Thomas R.,Hinkle, Kevin W.,Stevens, Kirk L.,Dickerson, Scott H.,Rusnak, David W.,Spehar, Glenn M.,Wood, Edgar R.,Griffin, Robert J.,Uehling, David E.
scheme or table, p. 1332 - 1336 (2009/11/30)
Aniline 'headgroups' were synthesized and incorporated into an alkynyl thienopyrimidine series of EGFR and ErbB-2 inhibitors. Potent inhibition of enzyme activity and cellular proliferation was observed. In certain instances, protein binding was reduced a
4- (IH-INDAZOL-S-YL-AMINO)-QUINAZOLINE COMPOUNDS AS ERBB RECEPTOR TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER
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Page/Page column 89, (2008/06/13)
A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blood
NOVEL HETEROCYCLES
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Page/Page column 104-105, (2010/10/20)
The invention relates to novel heterocycles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.
BENZOTHIENO’2,3-D! PYRIMIDINE COMPOUNDS AS INHIBITORS OF TYROSINE KINASE ACTIVITIES OF THE EPIDERMAL GROWTH FACTOR RECEPTORS (EGFRS) FOR THE TREATMENT OF HYPERPROLIFERATIVE DISEASES
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Page/Page column 42-43, (2010/11/08)
This invention relates to novel compounds of formula (I) and processes for their preparation, their use for of treating diseases, particularly hyperproliferative diseases such as cancer, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly hyperproliferative diseases such as cancer. Wherein m is 0, 1 or 2; R3 is *-O(CH2)n AR, wherein Ar is phenyl, thienyl, furyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, pyridyl, pyrimidyl od pyridazinyl, wherein Ar can optionally be substituted.