- PROCESS FOR THE PREPARATION OF METHYL 4,6-DIAMINO-2-[1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRIDIN-3-YL]-5-PYRIMIDINYL(METHYL)CARBAMATE AND ITS POLYMORPHS THEREOF
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The present invention relates to an improved process for the preparation of methyl 4,6-diamino-2-[ 1-(2-fluorobenzyl)-1 H -pyrazolo[3,4-b )pyridin-3 -yl]-5-pyrimidinyl(methyl)carbamatecompound of formula-1 and its polymorphs thereof, represented by the fo
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Page/Page column 15-16
(2018/06/12)
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- Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure
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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.
- 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
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p. 5146 - 5161
(2017/06/28)
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- The preparation method of the west leo gua (by machine translation)
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The invention discloses a method for preparation of west leo gua, its to 1 - (2 - fluorobenzyl) - 1 H - pyrazolo [3, 4 - b] pyridine - 3 - carboxamidine hydrochloride as the raw material, via the four-step reaction 2 - [1 - (2 - fluorobenzyl) - 1 H - pyra
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Paragraph 0062; 0063; 0064; 0065; 0066-0069; 0074; 0075
(2017/10/05)
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- PROCESS FOR THE PREPARATION OF METHYL 4,6-DIAMINO-2-[L-(2-FHIOROBENZVR)-LH-PYRAZOLO I3,4-BLPVRIDIN-3-VN-5-PYRIMIDINYL(METHVL)CARBAMATE AND ITS POLYMORPHS THEREOF
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The present invention relates to process for the preparation of methyl 4,6-diamino-2-[1-(2-fluorobenzyl)-lH-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl(methyl)carbamate and its polymorphs thereof compound of formula-1, represented by the following structur
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Page/Page column 34; 37; 38
(2017/03/08)
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- Method for compounding riociguat intermediate
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The invention discloses a method for compounding riociguat intermediate, firstly 1-(2-fluorine benzyl) 1H-pyrazolo [3, 4-b] pyridine-3-formamidine hydrochloride are used as starting materials, and 2-[1-(2-fluorine benzyl)-1 H- pyrazolo [3, 4-b] pyridine-3-yl]-4, 5, 6-pyrimidine triamine of the riociguat intermediate are prepared by catalyzing and hydrogenating in normal pressure through a catalyst. The method for compounding the riociguat intermediate is mild in reaction conditions, prevents using a high pressure reaction kettle, reduces process demands to equipment, enables product purity to be bigger than 99.0% at last, and is suitable for commercial process.
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Paragraph 0020
(2017/03/08)
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- Novel Combination Containing a Stimulator of Soluble Guanylate Cyclase and a Lipid-Lowering Substance
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A combination product which comprises as pharmaceutically active ingredients at least one active ingredient component A and at least one active ingredient component B, where active ingredient component A is a direct soluble guanylate cyclase stimulator of
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Page/Page column 5; 10
(2010/11/28)
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- Novel sulfonamide-substituted pyrazolopyridine derivatives
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The invention relates to novel pyrazolopyridine derivatives of formula (I) wherein R1 represents H, Cl or NH2, and R2 and R3 form; together with the heteroatoms to which they are bonded, a five to six-membered heterocycle which can be saturated or partially unsaturated, can optionally contain at least one other heteroatom from the group N, O, S and can be optionally substituted. The invention also relates to salts, isomers and hydrates of said derivatives, in the form of stimulators of soluble guanylate cyclase and as agents for treating cardiovascular diseases, hypertonia, thrombo-embolic diseases and ischaemia, sexual dysfunction, inflammations, and diseases of the central nervous system.
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- Metabolites of orally active NO-independent pyrazolopyridine stimulators of soluble guanylate cyclase.
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The pyrazolopyridine stimulators of soluble guanylate cyclase BAY 41-2272 and 41-8543 were oxidised in rats and dogs at their 5-pyrimidinyl-cyclopropyl and -morpholino residue. These metabolites activate the soluble guanylate cyclase, induce vasoelaxation and thereby may contribute to the in vivo activity of BAY 41-2272 and BAY 41-8543.
- Straub, Alexander,Benet-Buckholz, Jordi,Froede, Rita,Kern, Armin,Kohlsdorfer, Christian,Schmitt, Peter,Schwarz, Thomas,Siefert, Hans Martin,Stasch, Johannes Peter
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p. 1711 - 1717
(2007/10/03)
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