Stimulators and/or activators of soluble guanylate cyclase (sgc) in combination with an inhibitor of neutral endopeptidase (nep inhibitor) and/or an angiotensin aii antagonist and the use thereof

Patent metadata

Field	Value
Publication number	US-2019125709-A1
Application number	US-201615746624-A
Country	US
Kind code	A1
Filing date	Jul 15, 2016
Priority date	Jul 23, 2015
Publication date	May 2, 2019
Grant date	—

Abstract

The present invention relates to stimulators and activators of soluble guanylate cyclase in combination with an inhibitor of neutral endopeptidase and/or angiotensin AII antagonists and the use thereof for the treatment and/or prophylaxis of cardiovascular disorders, for example heart failure with preserved ejection fraction or heart failure with reduced ejection fraction, renal disorders, for example chronic kidney failure, urological disorders, lung disorders, disorders of the central nervous system, for regulation of cerebral perfusion, for example in the event of vascular cerebral states of dementia, for the treatment and/or prophylaxis of fibrotic disorders and other disease symptoms (e.g. end organ damage affecting the brain, kidney or heart).

First claim

1 . A combination comprising an sGC stimulator, sacubitril and/or an angiotensin AII antagonist and also in each case the salts, solvates and solvates of the salts thereof.

2 . The combination as claimed in claim 1 comprising an sGC stimulator, sacubitril and/or valsartan and also in each case the salts, solvates and solvates of the salts thereof.

3 . The combination as claimed in claim 1 comprising an sGC stimulator and LCZ696 and also in each case the salts, solvates and solvates of the salts thereof.

4 . The combination as claimed in claim 1 for preparing a medicament for the treatment and/or prophylaxis of cardiovascular disorders, renal disorders, lung disorders, and also for the treatment and/or prophylaxis of fibrotic disorders.

5 . A medicament comprising a combination as claimed in claim 1 in combination with an inert, non-toxic, pharmaceutically suitable excipient.

6 . The medicament comprising a combination as claimed in claim 1 in combination with one or more further active ingredients selected from the group consisting of ACE inhibitors, renin inhibitors, beta blockers, acetylsalicylic acid, diuretics, calcium antagonists, statins, digitalis (digoxin) derivatives, calcium sensitizers, nitrates and antithrombotics.

7 . The medicament comprising a combination as claimed in claim 1 for the treatment and/or prophylaxis of cardiovascular disorders, renal disorders, lung disorders, and also for the treatment and/or prophylaxis of fibrotic disorders.

8 . A method for the treatment and/or prophylaxis of cardiovascular disorders, renal disorders, lung disorders, and fibrotic disorders, in humans and animals comprising administering a therapeutically effective amount of the combination of claim 1 to a human or animal in need thereof.

9 . A kit comprising a pharmaceutical composition comprising an sGC stimulator and a pharmaceutical composition comprising an angiotensin AII antagonist and N-(3-carboxy-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-2R-methylbutanoic acid or the esters thereof.

10 . The kit as claimed in claim 9 comprising a pharmaceutical composition comprising an sGC stimulator and a pharmaceutical composition comprising valsartan and N-(3-carboxy-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-2R-methylbutanoic acid or an ester thereof.

11 . The kit as claimed in claim 9 comprising a pharmaceutical composition comprising an sGC stimulator and a pharmaceutical composition comprising trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3′-methyl-2′-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate] hemipentahydrate.

12 . A method for the treatment and/or prophylaxis of cardiovascular disorders, renal disorders, lung disorders, and fibrotic disorders in humans and animals comprising administering a therapeutically effective amount of a combination having as components an sGC stimulator, sacubitril and/or an angiotensin AII antagonist and also in each case the salts, solvates and solvates of the salts thereof to a human or animal in need thereof; wherein the components are administered together or successively.

13 . The method of claim 12 , wherein the components are administered successively and each component is present in a separate unit dosage form from the other components.

Assignees

• Bayer Pharma AG

Inventors

• Marquardt Tobias
• Follmann Markus
• Stasch Johannes-Peter

Classifications

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P7/10

  Antioedematous agents; Diuretics · CPC title

• A61P7/02

  Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors · CPC title

• A61P3/06

  Antihyperlipidemics · CPC title

• A61P9/04

  Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure · CPC title