6401-02-1Relevant academic research and scientific papers
Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure
Follmann, Markus,Ackerstaff, Jens,Redlich, Gorden,Wunder, Frank,Lang, Dieter,Kern, Armin,Fey, Peter,Griebenow, Nils,Kroh, Walter,Becker-Pelster, Eva-Maria,Kretschmer, Axel,Geiss, Volker,Li, Volkhart,Straub, Alexander,Mittendorf, Joachim,Jautelat, Rolf,Schirok, Hartmut,Schlemmer, Karl-Heinz,Lustig, Klemens,Gerisch, Michael,Knorr, Andreas,Tinel, Hanna,Mondritzki, Thomas,Trübel, Hubert,Sandner, Peter,Stasch, Johannes-Peter
, p. 5146 - 5161 (2017/06/28)
The first-in-class soluble guanylate cyclase (sGC) stimulator riociguat was recently introduced as a novel treatment option for pulmonary hypertension. Despite its outstanding pharmacological profile, application of riociguat in other cardiovascular indications is limited by its short half-life, necessitating a three times daily dosing regimen. In our efforts to further optimize the compound class, we have uncovered interesting structure-Activity relationships and were able to decrease oxidative metabolism significantly. These studies resulting in the discovery of once daily sGC stimulator vericiguat (compound 24, BAY 1021189), currently in phase 3 trials for chronic heart failure, are now reported.
Process for preparing substituted 5-fluoro-1H-pyrazolopyridines
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Paragraph 0160; 0161; 0162, (2013/06/26)
The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for tr
METHODS OF MAKING FLUORINATED ETHERS, FLUORINATED ETHERS, AND USES THEREOF
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Page/Page column 4-5, (2010/05/13)
A method of making a fluorinated ether includes combining, in a polar aprotic solvent: a fluorinated alcohol represented by the formula X—Rf1CH2OH, and a fluorinated sulfonate ester represented by the formula Rf2CH2OS(═O)2Rf3, and base; and obtaining a fluorinated ether represented by the formula Y—Rf1CH2OCH2Rf2—Y. Rf1 is selected from perfluorinated C1-C10 alkylene groups having from 1 to 10 carbon atoms and partially fluorinated C1-C10 alkylene groups, and derivatives thereof having catenated heteroatom(s). X represents H, F, or an HOCH2— group. Rf2 is selected from perfluorinated C1-C10 alkyl groups and partially fluorinated C1-C10 alkyl groups, and derivatives thereof having catenated heteroatom(s). Rf3 is a C1-C4 alkyl group. Y represents H, F, or an Rf2CH2OCH2— group. A variant method, useful for preparing symmetric fluorinated ethers, is also disclosed. The present disclosure also provides fluorinated ethers preparable according to the methods. Use of fluorinated ethers in various applications is also disclosed.
METHOD FOR PRODUCTION OF FLUOROALYKYLFLUOROALKANE-SULFONATE
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Page/Page column 10-11; 13, (2008/06/13)
PROBLEM TO BE SOLVED: To provide a method for simply producing, under more moderate condition than heretofore, a fluoroalkylfluoroalkane-sulfonate useful as an intermediate for medicines or agrochemicals and as a reagent for introducing a fluorine-containing group. SOLUTION: The fluoroalkyl fluoroalkane-sulfonate is produced by reacting a perfluoroalkanesulfonyl halide with a fluorine-containing alcohol in the presence of a base. In this case, an organic solvent is not used but water coexists as a solvent. It is particularly preferable that a reaction temperature is ≥-10°C but ≤40°C and water content is ≥0.2 g and ≤5 g per 1 g of the fluorine-containing alcohol. According to this method, for example, 2,2,2-trifluoroethyltrifluoromethane-sulfonate or 2,2,3,3-tetrafluoropropyltrifluoromethane-sulfonate can efficiently be produced, and the discharge amount of waste materials can remarkably be reduced. COPYRIGHT: (C)2006,JPOandNCIPI
NITRILE COMPOUND AND ITS USE IN PEST CONTROL
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Page/Page column 123, (2010/02/12)
The present invention provides a nitrile compound represented by the formula (I): wherein R represents C1-C4 fluoroalkyl, Q represents halogen, C1-C11 alkyl optionally substituted with halogen, C2-C6 alkenyl group optionally substituted with halogen, C2-C6 alkynyl optionally substituted with halogen, C3-C7 cycloalkyl optionally substituted with halogen or (C3-C7 cycloalkyl optionally substituted with halogen)C1-C4 alkyl, which has excellent control effect against pests.
