888327-27-3Relevant academic research and scientific papers
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-HETEROCYCLIC SUBSTITUTED CARBOXYLIC ACID DERIVATIVES AND THE USE THEREOF
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, (2011/02/26)
The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS PPAR MODULATORS FOR THE TREATMENT OF NON-ALCOHOLIC STEATOHEPATITIS
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Page/Page column 15, (2008/12/07)
Disclosed herein are new methods of treatment of non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and other fibrotic diseases of the liver in a subject by modulating PPARδ with sulfonyl-substituted bicyclic compounds and co
METHODS FOR THE MODULATION OF CRP BY THE SELECTIVE MODULATION OF PPAR DELTA
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Page/Page column 12, (2010/11/29)
The present invention discloses methods to reduce C-reactive protein (CRP) in patients in need thereof comprising the selective modulation of PPARδ.
Salts of Modulators Of PPAR and Methods of Treating Metabolic Disorders
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Page/Page column 12, (2010/11/26)
Salt forms of potent modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
METHODS FOR THE UPREGULATION OF GLUT4 VIA MODULATION OF PPAR DELTA IN ADIPOSE TISSUE AND FOR THE TREATMENT OF DISEASE
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Page/Page column 14, (2010/11/28)
The present invention is directed to novel compositions and their application as pharmaceuticals for the treatment of disease. Methods of upregulation of GLUT4 via activation of peroxisome proliferator activated receptor delta activity in the adipose tiss
SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS MODULATORS OF PPAR
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, (2015/10/07)
Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
