- Hetero-aromatic compound and its use in medicine
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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.
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Paragraph 0908; 0913-0916; 1489; 1492-1495
(2019/07/04)
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- QUINAZOLINE COMPOUNDS
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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).
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Page/Page column 11
(2012/01/14)
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- QUINAZOLINE COMPOUNDS
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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).
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Page/Page column 10-11
(2012/01/14)
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- Synthesis and cytotoxic activity of 2,5-disubstituted pyrimido[5,4-c] quinoline derivatives
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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
- Zhang, Fan,Zhai, Xin,Chen, Li Juan,Qi, Jian Guo,Cui, Bo,Gu, Yu Cheng,Gong, Ping
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scheme or table
p. 1277 - 1280
(2012/01/06)
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- PHOSPHORUS CONTAINING QUINAZOLINE COMPOUNDS AND METHODS OF USE
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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.
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Page/Page column 63
(2011/02/24)
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- Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors
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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
- 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.
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scheme or table
p. 1332 - 1336
(2009/11/30)
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- 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
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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
- 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.
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supporting information; experimental part
p. 6527 - 6530
(2010/03/26)
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- 4- (IH-INDAZOL-S-YL-AMINO)-QUINAZOLINE COMPOUNDS AS ERBB RECEPTOR TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER
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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
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Page/Page column 89
(2008/06/13)
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- NOVEL HETEROCYCLES
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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.
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Page/Page column 104-105
(2010/10/20)
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- THIA-TETRAAZAACENAPHTHYLENE KINASE INHIBITORS
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The present invention is directed to novel thia-tetraazaacenaphthylene compounds of Formula (I): and pharmaceutically acceptable forms thereof and their synthesis and use as inhibitors of ATP-protein kinase interactions.
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Page/Page column 96
(2008/06/13)
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- 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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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.
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Page/Page column 42-43
(2010/11/08)
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- SYNTHETIC PROCESS
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The present invention provides a process for preparing compounds of formula (I) ["insert chemical structure here"](I)or a pharmaceutically acceptable salt thereof. The compounds prepared by the process of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
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Page/Page column 32-33
(2008/06/13)
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- Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitors
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Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases in mammals are also disclosed.
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Page/Page column 12-13
(2008/06/13)
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- C-5 Modified indazolylpyrrolotriazines
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The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
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