1828-58-6Relevant academic research and scientific papers
PRODRUGS OF 2-(4-(3-((4-AMINO-7-CYANO-IMIDAZO[2,1-F][1,2,4]TRIAZIN-2-YL)AMINO)PHENYL)PIPERAZ IN-1-YL)PROPANAMIDE DERIVATIVES AS CK2 INHIBITORS FOR THE TREATMENT OF CANCER
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, (2017/05/10)
PRODRUGS OF IMIDAZOTRIAZINE COMPOUNDS AS CK2 INHIBITORS The invention provides pharmaceutically active compounds of formula (I) and prodrugs thereof. The formula (I) 2-(aminophenylamino)-4- amino-7-cyano-imidazo[2,1-f][1,2,4]triazine derivatives inhibit CK2 protein kinase activity, thereby making them useful for treating cancer, psoriasis and rheumatoid arthritis.
1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
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Page/Page column 63, (2015/11/10)
The present invention relates to substituted pyrrolopyridinones and substituted pyrazolopyridinones which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
2-(4-Carbonylphenyl)benzoxazole inhibitors of CETP: Scaffold design and advancement in HDLc-raising efficacy
Sweis, Ramzi F.,Hunt, Julianne A.,Kallashi, Florida,Hammond, Milton L.,Chen, Ying,Eveland, Suzanne S.,Guo, Qiu,Hyland, Sheryl A.,Milot, Denise P.,Cumiskey, Anne-Marie,Latham, Melanie,Rosa, Raymond,Peterson, Larry,Sparrow, Carl P.,Wright, Samuel D.,Anderson, Matt S.,Sinclair, Peter J.
scheme or table, p. 1890 - 1895 (2011/05/04)
The development of 2-phenylbenzoxazoles as inhibitors of cholesteryl ester transfer protein (CETP) is described. Initial efforts aimed at engineering replacements for the aniline substructures in the benchmark molecule. Reversing the connectivity of the central aniline lead to a new class of 2-(4-carbonylphenyl)benzoxazoles. Structure-activity studies at the C-7 and terminal pyridine ring allowed for the optimization of potency and HDLc-raising efficacy in this new class of inhibitors. These efforts lead to the discovery of benzoxazole 11v, which raised HDLc by 24 mg/dl in our transgenic mouse PD model.
CETP INHIBITORS DERIVED FROM BENZOXAZOLE ARYLAMIDES
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Page/Page column 21, (2009/01/23)
Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.
CETP INHIBITORS DERIVED FROM BENZOXAZOLE ARYLAMIDES
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Page/Page column 48, (2009/01/23)
Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.
CETP INHIBITORS DERIVED FROM BENZOXAZOLE ARYLAMIDES
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Page/Page column 21, (2009/01/23)
Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems ofthe industrialized world In formula I, A-B is an arylamide moiety
COMPOUNDS USEFUL AS A3 ADENOSINE RECEPTOR AGONISTS
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Page/Page column 55, (2010/02/10)
Compounds useful as A3 Adenosine Receptor Agonists. Adenosine analogue-type A3 receptor agonists having an N6 substituent of the formula CR20R21CYCLE where CYCLE is a specified heterocycle, e.g. a substituted pyridyl group or a substituted oxazolyl-containing bicyclic ring. 10
