# US 11,439,628 B2 · Use of non-steroidal mineralocorticoid receptor antagonists alone or in combination for the treatment of muscular or neuromuscular diseases

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- Number: US 11,439,628 B2
- Document ID: US11439628B2
- Status: Granted
- Kind: B2
- Application number: 17/051,923
- Filed: 2019-05-10
- Published: 2021-04-29
- Granted: 2022-09-13
- Earliest claimed: 2018-05-11
- Assignees: Bayer Aktiengesellschaft
- Applicants: Bayer Aktiengesellschaft
- Inventors: Peter Sandner; Peter Kolkhof; Ilka Mathar; Stefanie Breitenstein
- Web page: https://patentgrep.com/patent/US11439628B2

## CPC

- A61K 31/4375: the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 21/04: for myasthenia gravis
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to non-steriodal mineralocorticoid receptor (MR) and the pharmacology of mineralocorticoid receptor antagonists (MR Antagonists, MRAs). In particular, the invention relates to the use of MRAs alone and in combination preferably in combination with sGC stimulators and/or sGC activators for preparation of medicaments for the prevention and/or treatment of muscular or neuromuscular diseases, especially for the treatment of Duchenne Muscular Dystrophy (DMD).

## Claims

### Claim 1

A method for the treatment and/or prevention of Duchenne muscular dystrophy in a human or animal comprising administering a therapeutically effective amount of a non-steroidal mineralocorticoid receptor antagonist that is (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1, 6-naphthyridine-3-carboxamide according to formula (I)
or a pharmaceutically acceptable salt thereof to a human or animal in need thereof.

### Claim 2 (depends on 1)

The method of claim 1, further comprising administering to the human or animal an additional therapeutic agent that is an sGC stimulator.

### Claim 3 (depends on 2)

The method of claim 2, wherein the sGC stimulator is selected from the group consisting of
methyl 4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl(methyl)carbamate,
methyl {4,6-diamino-245-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-yl]pyrimidin-5-yl}carbamate,
3-(4-amino-5-cyclopropylpyrimidin-2-yl)-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine and
1, 1,1,3,3,3-hexafluoro-2-[({5-fluoro-2-[(2-fluorobenzyl)-5-(1,2-oxazol-3-yl)-1H-pyrazol-3-yl]-4-pyrimidinyl}amino)methyl]-2-propanol
or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 2)

The method of claim 2, wherein the sGC stimulator is 3-(4-amino-5-cyclopropylpyrimidin-2-yl)-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine or a pharmaceutically acceptable salt thereof.

### Claim 5 (depends on 1)

The method of claim 1, wherein the non-steroidal mineralocorticoid receptor antagonist is administered at a dose of 5 to 40 mg once daily to a child having a body weight of approximately 70 to 80 kg.

### Claim 6 (depends on 5)

The method of claim 5, wherein the non-steroidal mineralocorticoid receptor antagonist is administered at a dose of 10 to 20 mg once daily.

### Claim 7 (depends on 2)

The method of claim 2, wherein the non-steroidal mineralocorticoid receptor antagonist is administered at a dose of 5 to 40 mg once daily to a child having a body weight of approximately 70 to 80 kg.

### Claim 8 (depends on 7)

The method of claim 7, wherein the non-steroidal mineralocorticoid receptor antagonist is administered at a dose of 10 to 20 mg once daily.