IP Library › Granted Patent US 9,487,506
Granted Patent B2
US 9,487,506 · App. 14/110,441 · Granted Nov 8, 2016

Mineralocorticoid receptor antagonists

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Quick Facts
Patent No.
US 9,487,506
App. No.
14/110,441
Granted
Nov 8, 2016
Kind
B2
Abstract

Compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases are disclosed. Processes for preparing compounds of the Formula (I), use of the compounds for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and pharmaceutical compositions which comprise compounds of the Formula (I) are disclosed.

Claims (31)

1. A compound selected from

3-(4-Chloro-2-fluorobenzyl)-1H-indazole and 3-(4-Chloro-2-fluorobenzyl)-7-ethyl-1H-indazole;

N-{3-[1-(4-Chloro-2-fluorophenyl)-3-cyanopropyl]-1H-indazol-7-yl}methanesulfonamide;

4-(4-Chloro-2-fluorophenyl)-4-(7-pyridin-3-yl-1H-indazol-3-yl)butanenitrile;

4-(4-Chloro-2-fluorophenyl)-4-(7-pyridin-4-yl-1H-indazol-3-yl)butanenitrile;

N-{3-[1-(4-Chloro-2-fluorophenyl)-4-hydroxybutyl]-1H-indazol-7-yl}methanesulfonamide;

N-{3-[1-(4-Chloro-2-fluorophenyl)-2-cyanoethyl]-1H-indazol-7-yl}methanesulfonamide;

N-{3-[1-(4-Chloro-2-fluorophenyl)-3-cyanopropyl]-1H-indazol-7-yl}cyclopropanesulfonamide;

N-{3-[1-(4-Chloro-2-fluorophenyl)-3-(3-methyl-1,2,4-oxadiazol-5-yl)propyl]-1H-indazol-7-yl}methanesulfonamide;

N-{3-[1-(4-Chloro-2-fluorophenyl)-4-oxopentyl]-1H-indazol-7-yl}methanesulfonamide;

N-{3-[1-(4-Chloro-2-fluorophenyl)-4-hydroxy-4-methylpentyl]-1H-indazol-7-yl}methanesulfonamide;

N-{3-[1-(4-Chloro-2-fluorophenyl)-4-hydroxy-4-ethylhexyl]-1H-indazol-7-yl}methanesulfonamide;

4-(4-Chloro-2-fluorophenyl)-4-(1H-indazol-3-yl)butanenitrile;

4-(4-Chloro-2-fluorophenyl)-4-(1-methyl-1H-indazol-3-yl)butanenitrile;

4-(4-Chloro-2-fluorophenyl)-4-(1-ethyl-1H-indazol-3-yl)butanenitrile;

4-(4-Chloro-2-fluorophenyl)-4-(1-propyl-1H-indazol-3-yl)butanenitrile;

4-(1-Benzyl-1H-indazol-3-yl)-4-(4-chloro-2-fluorophenyl)butanenitrile;

Methyl {3-[1-(4-chloro-2-fluorophenyl)-3-cyanopropyl]-1H-indazol-1-yl}acetate;

tert-Butyl {3-[1-(4-chloro-2-fluorophenyl)-3-cyanopropyl]-1H-indazol-1-yl}acetate;

Methyl 3-{3-[1-(4-chloro-2-fluorophenyl)-3-cyanopropyl]-1H-indazol-1-yl}propanoate;

4-(4-Chloro-2-fluorophenyl)-4-{1-[(methylsulfanyl)methyl]-1H-indazol-3-yl}butanenitrile;

4-(4-Chloro-2-fluorophenyl)-4-[1-(cyanomethyl)-1H-indazol-3-yl]butanenitrile;

4-(4-Chloro-2-fluorophenyl)-4-[1-(2-methoxyethyl)-1H-indazol-3-yl]butanenitrile;

tert-Butyl {3-[1-(4-chlorophenyl)-1-methylethyl]-1H-indazol-1-yl}acetate;

Methyl {3-[1-(4-chlorophenyl)-1-ethylpropyl]-1H-indazol-1-yl}acetate;

Methyl [3-(4-chlorobenzyl)-1H-indazol-1-yl]acetate; and

3-(4-Chlorobenzyl)-1-benzyl-1H-indazole;

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprised of the compound of claim 1 and a pharmaceutically acceptable carrier.

3. The pharmaceutical composition of claim 2 comprising one or more pharmaceutically active agents in addition to the compound of claim 1 .

4. A method for antagonizing aldosterone receptor (MR) and increasing aldosterone levels comprising administering an amount efficacious therefore of the compound of claim 1 .

Assignments (1)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →