157312-16-8Relevant articles and documents
Discovery of the Soluble Guanylate Cyclase Activator Runcaciguat (BAY 1101042)
Hahn, Michael G.,Lampe, Thomas,El Sheikh, Sherif,Griebenow, Nils,Woltering, Elisabeth,Schlemmer, Karl-Heinz,Dietz, Lisa,Gerisch, Michael,Wunder, Frank,Becker-Pelster, Eva-Maria,Mondritzki, Thomas,Tinel, Hanna,Knorr, Andreas,Kern, Armin,Lang, Dieter,Hueser, Joerg,Schomber, Tibor,Benardeau, Agnes,Eitner, Frank,Truebel, Hubert,Mittendorf, Joachim,Kumar, Vijay,Van Den Akker, Focco,Schaefer, Martina,Geiss, Volker,Sandner, Peter,Stasch, Johannes-Peter
, p. 5323 - 5344 (2021/05/06)
Herein we describe the discovery, mode of action, and preclinical characterization of the soluble guanylate cyclase (sGC) activator runcaciguat. The sGC enzyme, via the formation of cyclic guanosine monophoshphate, is a key regulator of body and tissue homeostasis. sGC activators with their unique mode of action are activating the oxidized and heme-free and therefore NO-unresponsive form of sGC, which is formed under oxidative stress. The first generation of sGC activators like cinaciguat or ataciguat exhibited limitations and were discontinued. We overcame limitations of first-generation sGC activators and identified a new chemical class via high-throughput screening. The investigation of the structure-activity relationship allowed to improve potency and multiple solubility, permeability, metabolism, and drug-drug interactions parameters. This program resulted in the discovery of the oral sGC activator runcaciguat (compound 45, BAY 1101042). Runcaciguat is currently investigated in clinical phase 2 studies for the treatment of patients with chronic kidney disease and nonproliferative diabetic retinopathy.
OXO-HETEROCYCLICALLY SUBSTITUTED ALKYL CARBOXYLIC ACIDS AND USE THEREOF
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Page/Page column 23, (2012/02/06)
The present application relates to novel alkylcarboxylic acids having an oxo-substituted azaheterocyclic partial structure, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
Arylacetamides and their use as medicaments
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, (2008/06/13)
The new arylacetamides are obtained by first converting appropriately substituted arylacetic acids into the acetyl chlorides and then converting these into the amides using the appropriate amines. The new arylacetamides can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.