IP Library Granted Patent US 7,960,387
Granted Patent B2
US 7,960,387 · App. 10/545,453 · Granted Jun 14, 2011

2-(3-phenyl-2-piperazinyl-3,4-dihydroquinazolin-4-yl)acetic acids as antiviral agents, especially against cytomegaloviruses

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Quick Facts
Patent No.
US 7,960,387
App. No.
10/545,453
Granted
Jun 14, 2011
Kind
B2
Abstract

The invention relates to dihydroquinazolines and methods for the production thereof, the use thereof in the treatment and/or prophylaxis of diseases, in addition to the use thereof in the production of medicaments in the treatment and/or prophylaxis of diseases, especially for use as anti-viral agents, especially against cytomegalo viruses.

Claims (30)

1. A medicament comprising a compound of formula (I), or a salt, or a solvate, or a solvate of a salt thereof,

in which

Ar represents aryl which may be substituted by 1 to 3 substituents, where the substituents are selected independently of one another from the group consisting of alkyl, alkoxy, formyl, carboxyl, alkylcarbonyl, alkoxycarbonyl, trifluoromethyl, halogen, cyano, hydroxyl, amino, alkylamino, aminocarbonyl and nitro,

where alkyl may be substituted by 1 to 3 substituents, where the substituents are selected independently of one another from the group consisting of halogen, amino, alkylamino, hydroxyl and aryl,

or two of the substituents on the aryl radical together with the carbon atoms to which they are attached form a 1,3-dioxolane, a cyclopentane ring or a cyclohexane ring, and any third substituent present is selected independently therefrom from the group mentioned,

R 1 represents hydrogen, alkyl, alkoxy, cyano, halogen, nitro or trifluoromethyl,

R 2 represents hydrogen, alkyl, alkoxy, cyano, halogen, nitro or trifluoromethyl,

R 3 represents alkyl, alkoxy, cyano, halogen, nitro or trifluoromethyl

or

one of the radicals R 1 , R 2 and R 3 represents hydrogen, alkyl, alkoxy, cyano, halogen, nitro or trifluoromethyl and the other two together with the carbon atoms to which they are attached form a 1,3-dioxolane, a cyclopentane ring or a cyclohexane ring,

R 4 represents hydrogen or alkyl,

R 5 represents hydrogen or alkyl,

or

the radicals R 4 and R 5 are attached to carbon atoms directly opposing each other in the piperazine ring and form a methylene bridge which is optionally substituted by 1 or 2 methyl groups, in combination with a further active compound.

2. The medicament according to claim 1 , wherein the further active compound is an antiviral active compound.

3. The medicament according to claim 2 , wherein the antiviral active compound is gancyclovir or acyclovir.

4. A method of controlling viral infections in humans and animals, said method comprising administering an antivirally effective amount of a medicament comprising a compound of formula (I) or a salt, or a solvate, or a solvate of a salt thereof,

in which

Ar represents aryl which may be substituted by 1 to 3 substituents, where the substituents are selected independently of one another from the group consisting of alkyl, alkoxy, formyl, carboxyl, alkylcarbonyl, alkoxycarbonyl, trifluoromethyl, halogen, cyano, hydroxyl, amino, alkylamino, aminocarbonyl and nitro,

where alkyl may be substituted by 1 to 3 substituents, where the substituents are selected independently of one another from the group consisting of halogen, amino, alkylamino, hydroxyl and aryl,

or two of the substituents on the aryl radical together with the carbon atoms to which they are attached form a 1,3-dioxolane, a cyclopentane ring or a cyclohexane ring, and any third substituent present is selected independently therefrom from the group mentioned,

R 1 represents hydrogen, alkyl, alkoxy, cyano, halogen, nitro or trifluoromethyl,

R 2 represents hydrogen, alkyl, alkoxy, cyano, halogen, nitro or trifluoromethyl,

R 3 represents alkyl, alkoxy, cyano, halogen, nitro or trifluoromethyl

or

one of the radicals R 1 , R 2 and R 3 represents hydrogen, alkyl, alkoxy, cyano, halogen, nitro or trifluoromethyl and the other two together with the carbon atoms to which they are attached form a 1,3-dioxolane, a cyclopentane ring or a cyclohexane ring,

R 4 represents hydrogen or alkyl,

R 5 represents hydrogen or alkyl,

or

the radicals R 4 and R 5 are attached to carbon atoms directly opposing each other in the piperazine ring and form a methylene bridge which is optionally substituted by 1 or 2 methyl groups, in combination with a further active compound.

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 4, 2018
From: BAYER INTELLECTUAL PROPERTY GMBH
To: AICURIS ANTI-INFECTIVE CURES GMBH
Reel/Frame 045714/0272 →
CHANGE OF NAME Recorded Apr 12, 2013
From: BAYER SCHERING PHARMA AG
To: BAYER PHARMA AKTIENGESELLSCHAFT
Reel/Frame 030202/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2013
From: BAYER PHARMA AKTIENGESELLSCHAFT
To: BAYER INTELLECTUAL PROPERTY GMBH
Reel/Frame 029908/0437 →
MERGER Recorded Jan 12, 2010
From: BAYER HEALTHCARE AG
To: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
Reel/Frame 023769/0122 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2006
From: WUNBERG, TOBIAS; BAUMEISTER, JUDITH; BETZ, ULRICH; JESKE, MARIO; KLEYMANN, GERALD; LAMPE, THOMAS; NIKOLIC, SUSANNE; REEFSCHLAGER, JURGEN; SCHOHE-LOOP, RUDOLF; SUBMEIER, FRANK; ZIMMERMANN, HOLGER; GROSSER, ROLF; HENNINGER, KERSTIN; HEWLETT, GUY; KELDENICH, JORG; KRAMER, THOMAS; NELL, PETER; LIN, TSE-I
To: BAYER HEALTHCARE AG
Reel/Frame 018083/0493 →