IP Library Granted Patent US 9,168,249
Granted Patent B2
US 9,168,249 · App. 14/613,367 · Granted Oct 27, 2015

Substituted dihydropyrazolones for treating cardiovascular and hematological diseases

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Quick Facts
Patent No.
US 9,168,249
App. No.
14/613,367
Granted
Oct 27, 2015
Kind
B2
Abstract

The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.

Claims (20)

1. A method of treatment of a cardiovascular disease, cardiac insufficiency, anemia, a chronic kidney disease or renal insufficiency comprising administering to a human or animal in need thereof an active amount of a compound of formula (I)

in which

R 1 represents a heteroaryl group of the formula

wherein

* denotes the linkage point with the dihydropyrazolone ring

and

R 4 denotes hydrogen, fluorine, chlorine, bromine, cyano, (C 1 -C 4 )-alkyl, trifluoromethyl, hydroxymethyl, (C 1 -C 4 )-alkoxy, trifluoromethoxy, hydroxycarbonyl or (C 1 -C 4 )-alkoxycarbonyl,

R 2 represents a heteroaryl group of the formula

wherein

# denotes the linkage point with the dihydropyrazolone ring

and

R 6 , R 6A and R 6B are identical or different and independently of one another denote hydrogen or a substituent chosen from the series consisting of fluorine, chlorine, bromine, cyano, (C 1 -C 6 )-alkyl, trifluoromethyl, hydroxyl, (C 1 -C 6 )-alkoxy, trifluoromethoxy, amino, mono-(C 1 -C 4 )-alkylamino, di-(C 1 -C 4 )-alkylamino, hydroxycarbonyl, (C 1 -C 4 )-alkoxycarbonyl and 4- to 6-membered heterocycloalkyl, wherein

 (C 1 -C 6 )-alkyl in its turn can be substituted by hydroxyl, (C 1 -C 4 )-alkoxy or amino

 and

 4- to 6-membered heterocycloalkyl in its turn can be substituted once or twice in an identical or different manner by fluorine, cyano, (C 1 -C 4 )-alkyl, trifluoromethyl, hydroxyl, (C 1 -C 4 )-alkoxy, oxo, amino, mono-(C 1 -C 4 )-alkylamino, di-(C 1 -C 4 )-alkylamino, hydroxycarbonyl and/or (C 1 -C 4 )-alkoxycarbonyl,

and

R 3 represents hydrogen,

and their salts, solvates and solvates of the salts.

2. The method of treatment of claim 1 , wherein the compound of formula (I) is 2-[5-(Hydroxymethyl)pyridin-2-yl]-4-[4-(trifluoromethyl)-1H-imidazol-1-yl]-1,2-dihydro-3H-pyrazol-3-one having the following formula

and its salts, solvates and solvates of the salts.

Assignments (1)
CHANGE OF ADDRESS Recorded Jun 12, 2023
From: BAYER INTELLECTUAL PROPERTY GMBH
To: BAYER INTELLECTUAL PROPERTY GMBH
Reel/Frame 064021/0344 →