IP Library Granted Patent US 8,329,716
Granted Patent B2
US 8,329,716 · App. 11/547,975 · Granted Dec 11, 2012

Hetaryloxy-substituted phenylamino pyrimidines as Rho kinase inhibitors

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Quick Facts
Patent No.
US 8,329,716
App. No.
11/547,975
Granted
Dec 11, 2012
Kind
B2
Abstract

The invention relates to hetaryloxy-substituted phenylaminopyrimidines, to a process for their preparation and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases in humans and animals, in particular cardiovascular disorders.

Claims (26)

1. A compound of the formula (I)

in which

R 1 represents chlorine, cyano, methyl, ethyl, hydroxyethyl, methoxyethyl or cyclopropyl,

R 2 represents hydrogen or fluorine, and

R 3 represents hydrogen, chlorine, trifluoromethyl or pentafluoroethyl, or a salt thereof.

2. The compound as claimed in claim 1 ,

in which

R 1 represents chlorine, cyano, methyl, ethyl, hydroxyethyl, methoxyethyl or cyclopropyl,

R 2 represents hydrogen or fluorine, and

R 3 represents hydrogen, chlorine or trifluoromethyl, or a salt thereof.

3. The compound as claimed in claim 1 ,

in which

R 1 represents cyano, methyl or hydroxyethyl,

R 2 represents hydrogen or fluorine, and

R 3 represents chlorine or trifluoromethyl,

or a salt thereof.

4. A process for preparing a compound of the formula (I) as defined in claim 1 , characterized in that

a compound of the formula (II)

in which

R 1 and R 2 are as defined in claim 1 is reacted with a compound of the formula (III)

in which

R 3 is as defined in claim 1 .

5. A method for the treatment of erectile dysfunction comprising administering an effective amount of a compound of the formula (I) as defined in claim 1 .

6. A method for the treatment of hypertension, comprising administering an effective amount of a compound of the formula (I) as defined in claim 1 .

7. A pharmaceutical composition, comprising a compound of the formula (I) as defined in claim 1 in combination with a further active compound.

8. A pharmaceutical composition comprising a compound of the formula (I) as defined in claim 1 in combination with an inert nontoxic pharmaceutically acceptable auxiliary.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2013
From: BAYER PHARMA AKTIENGESELLSCHAFT
To: BAYER INTELLECTUAL PROPERTY GMBH
Reel/Frame 029904/0996 →
MERGER Recorded Jan 12, 2010
From: BAYER HEALTHCARE AG
To: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
Reel/Frame 023769/0122 →