IP Library Granted Patent US 7,834,042
Granted Patent B2
US 7,834,042 · App. 12/312,225 · Granted Nov 16, 2010

Angiotensin II receptor antagonists

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Quick Facts
Patent No.
US 7,834,042
App. No.
12/312,225
Granted
Nov 16, 2010
Kind
B2
Abstract

A compound having the structure (Formula I), wherein Y is —Y 1 —Y 2 —Y 3 —Y 4 —Y 5 —; Y 1 is C(O) or C(R 1 R 2 ); Y 2 is O, C(O), P(O)(OH) or CH 2 , provided that when Y 1 is C(O), Y 2 is not C(O); R 1 is selected from the group consisting of hydrogen and C 1-4 alkyl; R 2 is selected from the pup consisting of hydrogen, C 1-4 alkyl, and —OC(O)C 1-4 alkyl; Y 3 is O, C(O) or CH 2 , provided that when Y 2 is C(O), then Y 3 is not C(O), and further provided that when Y 2 is O, then Y 3 is not O; Y 4 is O or CH 2 or is absent, provided that when Y 3 is O, then Y 4 is not O; Y5 is —(CH 2 ) 1-2 —(X) 0-1 —(CH 2 ) 0-1 — or is absent; X is —O— or —CR 3 R 4 —; and R 3 and R 4 are independently selected from the group consisting of hydrogen and C 1 -C 4 alkyl; or a pharmaceutically acceptable salt thereof, which is useful for treating hypertension.

Claims (27)

1. A compound having the structure

wherein

Y is —Y 1 —Y 2 —Y 3 —Y 4 —Y 5 —;

Y 1 is C(O) or C(R 1 R 2 );

Y 2 is O, C(O), P(O)(OH) or CH 2 , provided that when Y 1 is C(O), Y 2 is not C(O);

R 1 is selected from the group consisting of hydrogen and C 1-4 alkyl;

R 2 is selected from the group consisting of hydrogen, C 1-4 alkyl, and —OC(O)C 1-4 alkyl;

Y 3 is O, C(O) or CH 2 , provided that when Y 2 is C(O), then Y 3 is not C(O), and further provided that when Y 2 is O, then Y 3 is not O;

Y 4 is O or CH 2 or is absent, provided that when Y 3 is O, then Y 4 is not O;

Y 5 is —(CH 2 ) 1-2 —(X) 0-1 —(CH 2 ) 0-1 — or is absent;

X is —O— or —CR 3 R 4 —; and

R 3 and R 4 are independently selected from the group consisting of hydrogen and C 1 -C 4 alkyl;

or a pharmaceutically acceptable salt thereof.

2. A compound of claim 1 , wherein Y 1 is C(O).

3. A compound of claim 1 , wherein Y 2 is CH 2 .

4. A compound of claim 1 , wherein Y 3 is CH 2 .

5. A compound of claim 1 , wherein Y 4 is CH 2 .

6. A compound of claim 1 , wherein Y 5 is absent.

7. A compound having the structure

or a pharmaceutically acceptable salt or hydrate thereof.

8. A compound of claim 7 having the structure

or a pharmaceutically acceptable salt or hydrate thereof.

9. A compound of claim 7 having the structure

or a pharmaceutically acceptable salt or hydrate thereof.

10. A pharmaceutical composition comprising a compound of claim 7 and a pharmaceutically acceptable carrier.

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

12. 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 (3)
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 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 1, 2010
From: SEBHAT, IYASSU K.; LO, MICHAEL MAN-CHU; NARGUND, RAVI P.; ALI, AMJAD
To: MERCK SHARP & DOHME CORP.
Reel/Frame 024922/0934 →