1350653-30-3Relevant articles and documents
PROCESS FOR PREPARING METHYL {4,6-DIAMINO-2-[5-FLUORO-1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRIDIN-3-YL]PYRIMIDIN-5-YL}CARBAMATE
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, (2022/01/05)
The present application relates to a novel and efficient process with high yield for preparing methyl {4,6- diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate of the formula (I) in the crystalline form of modification I, wherein the x-ray diffractogram of the compound of the formula (I) in modification I exhibits peak maxima of the 2 theta angle at 5.9, 6.9, 22.7, in very high purity which is significantly more cost-effective than the process known from the art and can be performed in customary pilot- and production plant-equipment (stirred tank/devices for isolation).
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.
USE OF STIMULATORS AND ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE FOR TREATING SICKLE-CELL ANEMIA AND CONSERVING BLOOD SUBSTITUTES
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Paragraph 0151-0155, (2013/06/28)
The present invention relates to the novel use of stimulators and activators of soluble guanylate cyclase for the treatment of sickle cell anemia and for the preservation of blood substitutes. The present invention furthermore relates to the use of stimulators and activators of soluble guanylate cyclase in combination with PDE5 inhibitors for the treatment of sickle cell anemia and for the preservation of blood substitutes.