IP Library Granted Patent US 8,106,034
Granted Patent B2
US 8,106,034 · App. 12/864,448 · Granted Jan 31, 2012

Angiotensin II receptor antagonists

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Quick Facts
Patent No.
US 8,106,034
App. No.
12/864,448
Granted
Jan 31, 2012
Kind
B2
Abstract

A compound having the structure wherein R is an angiotensin receptor blocking group Y is —(CR 1 R 20 ) 1-7 R 5 , or —C(O)(CR 1 R 20 ) 1-7 R 5 ; R 1 and R 20 are independently selected from the group consisting of hydrogen or C 1-4 alkyl; R 5 is —O—N═N(O)—NR 3 R 4 ; and R 3 and R 4 are independently selected from the group consisting of —CH 2 CH 2 OH, —CH 2 CH 2 OCH 3 , —C 1-4 alkyl, unsubstituted or substituted C 1-6 alkenyl, unsubstituted or substituted morpholino, amino, unsubstituted or substituted benzyl, unsubstituted or substituted phenyl, unsubstituted or substituted arylC 1-4 alkyl, or R 3 and R 4 together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, which is useful for treating hypertension.

Claims (20)

1. A compound having the general formula:

wherein R is

Y is —(CR 1 R 20 ) 1-7 R 5 , or —C(O)(CR 1 R 20 ) 1-7 R 5 ;

R 1 and R 20 are independently selected from the group consisting of hydrogen or C 1-4 alkyl;

R 5 is —O—N═N(O)—NR 3 R 4 ;

R 3 and R 4 together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of

Q is selected from the group consisting of S, O and NR 6 ;

R 6 , R 8 and R 9 are independently selected from the group consisting of hydrogen and unsubstituted or substituted C 1-6 alkyl;

R 12 and R 13 are independently selected from the group consisting of —OH, —CH 2 OH, —CH 2 CH 2 OH, —COOH, and —CH 2 COOH;

or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof.

2. A compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is H or CH 3 .

3. A compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 3 and R 4 , together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of

4. A compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 8 and R 9 are hydrogen.

5. A compound of claim 1 , or a pharmaceutically acceptable salt thereof, selected from the group consisting of

6. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

7. A pharmaceutical composition comprising a compound of claim 1 , a diuretic, and a pharmaceutically acceptable carrier.

8. A method for treating hypertension in a patient which comprises administering to the patient a therapeutically effective amount of the composition of claim 6 .

9. A pharmaceutical composition comprising a compound of claim 5 and a pharmaceutically acceptable carrier.

10. A pharmaceutical composition comprising a compound of claim 5 , a diuretic, and a pharmaceutically acceptable carrier.

11. A method for treating hypertension in a patient which comprises administering to the patient a therapeutically effective amount of the composition of claim 10 .

Assignments (2)
CHANGE OF NAME Recorded Aug 29, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028866/0511 →
MERGER Recorded Aug 27, 2012
From: MERCK SHARP & DOHME CORP.
To: SCHERING CORPORATION
Reel/Frame 028850/0515 →