cas 380894-77-9, Phosphonic acid, [[5-(3-fluorophenyl)-2-pyridinyl]Methyl]-, diethyl ester

Articles about 380894-77-9Total 7 be found

Discovery of Potent Orally Active Protease-Activated Receptor 1 (PAR1) Antagonists Based on Andrographolide
Protease-activated receptor-1 (PAR1), a G-protein-coupled receptor, plays a critical role in thrombin-mediated platelet aggregation. It is regarded as a promising antithrombosis target that is unlikely to result in bleeding. Here, we describe the synthesi
Liu, Jun,Sun, Bin,Zhao, Xiaoyu,Xing, Jie,Gao, Yanhui,Chang, Wenqiang,Ji, Jianbo,Zheng, Hongbo,Cui, Changyi,Ji, Aiguo,Lou, Hongxiang
p. 7166 - 7185
(2017/09/07)

Himbacine analogue preparation process for the preparation of intermediates (by machine translation)
The present invention provides a method for preparing intermediates of Himbacine analogs. The method provided by the present invention comprises: performing Suzuki reaction between 5-halo-2-hydroxymethyl pyridine and phenylboronic acid esters, reacting th
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(2016/10/07)

Discovery of octahydroindenes as PAR1 antagonists
Octahydroindene was identified as a novel scaffold for protease activated receptor 1 (PAR1) antagonists. Herein, the 2-position (C2) was explored for structure-activity relationship (SAR) studies. Compounds 14, 19, and 23b showed IC50 values of 1.3, 8.6, and 2.7 nM in a PAR1 radioligand binding assay, respectively, and their inhibitory activities on platelet activation were comparable to that of vorapaxar in a platelet rich plasma (PRP) aggregation assay. This series of compounds showed high potency and no significant cytotoxicity; however, the compounds were metabolically unstable in both human and rat liver microsomes. Current research efforts are focused on optimizing the compounds to improve metabolic stability and physicochemical properties as well as potency.
Lee, Sunkyung,Song, Jong-Hwan,Park, Chul Min,Kim, Jin-Seok,Jeong, Ji-Hye,Cho, Woo-Young,Lim, Dong-Chul
supporting information
p. 1054 - 1058
(2013/12/04)

[6+5] FUSED BICYCLES AS A THROMBIN ANTAGONIST, PROCESS FOR PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE BICYCLES
The present invention relates to the new [6+5] fused bicycle derivatives, pharmaceutically acceptable salts or isomers thereof, processes for preparing the same, and pharmaceutical compositions comprising the same. The [6+5] fused bicycle derivatives can antagonize the thrombin receptor and thus may be effectively used for the treatment and prevention of thrombus, platelet aggregation, atherosclerosis, restenosis, blood coagulation, hypertension, arrhythmia, angina pectoris, heart failure, inflammation and cancer when used alone or with other cardiovascular agents.
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Page/Page column 62-63

(2012/01/14)

Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate
This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.
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Page/Page column 13

(2008/06/13)

SYNTHESIS OF HIMBACINE ANALOGS
The present invention relates to an improved process for preparing imbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability,
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Page/Page column 30-31

(2008/06/13)

EXO- AND DIASTEREO- SELECTIVE SYNTHESES OF HIMBACINE ANALOGS
The application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught her
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Page/Page column 47-48

(2008/06/13)