1192040-12-2

Upstream product

• 78239-71-1 3-bromo-4-fluorobenzyl bromide 
• 1192040-06-4 tert-butyl 1-[3-(benzylamino)-4-fluorobenzyl]cyclopropanecarboxylate 
• 1192040-00-8 tert-butyl 1-(3-bromo-4-fluorobenzyl)cyclopropanecarboxylate 
• 87661-20-9 tert-butyl cyclopropanecarboxylate 

Downstream Products

• 1380604-83-0 tert-Butyl 1-(5-amino-2-chloro-4-fluorobenzyl)cyclopropanecarboxylate 
• 1380606-01-8 tert-butyl 1-(3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}-4-fluorobenzyl)cyclopropanecarboxylate 
• 1380606-49-4 tert-butyl 1-[3-(2S)-(2-{[4-((E)-2-cyanovinyl)phenyl]-2-cyclopentylacetyl}amino)-4-fluorobenzyl]cyclopropanecarboxylate 
• 1380605-62-8 (+/-)-tert-butyl 1-(3-{[2-(4-bromophenyl)-2-cyclopentylacetyl]amino}-4-fluorobenzyl)cyclopropanecarboxylate 

Relevant academic research and scientific papers

Discovery of the Soluble Guanylate Cyclase Activator Runcaciguat (BAY 1101042)

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.

N-[3-(2-CARBOXYETHYL)PHENYL]PIPERIDIN-1-YLACETAMIDE DERIVATIVES AND USE THEREOF AS ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE

The present application relates to novel substituted 2-(piperidin-1-yl)acetamide derivatives, to processes for preparation thereof, to the use thereof for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of cardiovascular diseases.

Substituted 1-benzylcycloalkylcarboxylic acids and the use thereof

The present application relates to novel substituted 1-benzylcycloalkylcarboxylic acid derivatives, 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.

OXO-HETEROCYCLIC SUBSTITUTED CARBOXYLIC ACID DERIVATIVES AND THE USE THEREOF

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.