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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.
Afiliación
  • Follmann M; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Ackerstaff J; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Redlich G; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Wunder F; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Lang D; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Kern A; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Fey P; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Griebenow N; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Kroh W; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Becker-Pelster EM; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Kretschmer A; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Geiss V; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Li V; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Straub A; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Mittendorf J; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Jautelat R; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Schirok H; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Schlemmer KH; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Lustig K; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Gerisch M; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Knorr A; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Tinel H; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Mondritzki T; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Trübel H; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Sandner P; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
  • Stasch JP; Drug Discovery, Bayer AG , Aprather Weg 18a, 42113 Wuppertal, Germany.
J Med Chem ; 60(12): 5146-5161, 2017 06 22.
Article en En | MEDLINE | ID: mdl-28557445
ABSTRACT
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.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Pirimidinas / Relación Estructura-Actividad / Guanilil Ciclasa Soluble / Insuficiencia Cardíaca / Compuestos Heterocíclicos con 2 Anillos Límite: Animals / Humans / Male Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Alemania
Texto completo
Imprimir
XML
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Pirimidinas / Relación Estructura-Actividad / Guanilil Ciclasa Soluble / Insuficiencia Cardíaca / Compuestos Heterocíclicos con 2 Anillos Límite: Animals / Humans / Male Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Alemania