67036-14-0Relevant academic research and scientific papers
Prodrug compound and application ofprodrug compound in treatment of cancer
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Paragraph 0117-0118, (2021/03/06)
The present invention provides a compound indicated by a formula (I), pharmaceutically acceptable salts or esters thereof, a pharmaceutical composition of the compound, and application of the compoundand the pharmaceutical composition in the inhibition or regulation of the activity of tyrosine kinase and treating disease symptoms or symptoms including cancer mediated by tyrosine kinase.
PRODRUGS OF THE TYROSINE KINASE INHIBITOR FOR TREATING CANCER
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Paragraph 0078-0079, (2021/03/05)
There are provided compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, useful for inhibition or modulation of the activity of tyrosine kinases and treatment of disease states or conditions mediated by tyrosine kinases, including cancers. (I)
ONE STEP PROCESS FOR THE PREPARATION OF CAPECITABINE
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Page/Page column 20, (2011/09/30)
The present invention relates a one step process for the preparation of capecitabine and analogues thereof, such as galocitabine, sapacitabine, 5'-deoxy-5-fiuoro-N- [(cyclohexyloxy)carbonyl]cytidine, and N-[(heptyloxy)carbonyl]cytarabine.
14,15-Epoxyeicosa-5,8,11-trienoic acid (14,15-EET) surrogates containing epoxide bioisosteres: Influence upon vascular relaxation and soluble epoxide hydrolase inhibition
Falck,Kodela, Ravinder,Manne, Rajkumar,Atcha, Krishnam Raju,Puli, Narender,Dubasi, Narsimhaswamy,Manthati, Vijay L.,Capdevila, Jorge H.,Yi, Xiu-Yu,Goldman, Daniel H.,Morisseau, Christophe,Hammock, Bruce D.,Campbell, William B.
supporting information; experimental part, p. 5069 - 5075 (2010/03/04)
All-cis-14,15-epoxyeicosa-5,8,11-trienoic acid (14,15-EET) is a labile, vasodilatory eicosanoid generated from arachidonic acid by cytochrome P450 epoxygenases. A series of robust, partially saturated analogues containing epoxide bioisosteres were synthesized and evaluated for relaxation of precontracted bovine coronary artery rings and for in vitro inhibition of soluble epoxide hydrolase (sEH). Depending upon the bioisostere and its position along the carbon chain, varying levels of vascular relaxation and/or sEH inhibition were observed. For example, oxamide 16 and N-iPr-amide 20 were comparable (ED50 1.7 μM) to 14,15-EET as vasorelaxants but were approximately 10-35 times less potent as sEH inhibitors (IC50 59 and 19 μM, respectively); unsubstituted urea 12 showed useful activity in both assays (ED50 3.5 μM, IC50 16 nM). These data reveal differential structural parameters for the two pharmacophores that could assist the development of potent and specific in vivo drug candidates.
ARYLAMIDINE DERIVATIVE, SALT THEREOF AND ANTIFUNGAL CONTAINING THESE
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Page/Page column 27, (2008/06/13)
An arylamidine derivative represented by the general formula (wherein R 1 represents optionally protected or substituted amidino; and R 2 and R 3 are the same or different and each represents hydrogen or halogeno) or a salt of the derivative. The derivati
