IP Library Granted Patent US 7,880,014
Granted Patent B2
US 7,880,014 · App. 12/000,247 · Granted Feb 1, 2011

Angiotensin II receptor antagonists

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Quick Facts
Patent No.
US 7,880,014
App. No.
12/000,247
Granted
Feb 1, 2011
Kind
B2
Abstract

A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is -Y 1 -Y 2 -Y 3 -Y 4 -Y 5 -; Y 1 is C(R 1 R 2 ); 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 2 is O or CH 2 ; Y 3 is C(O) or CH 2 ; Y 4 is O or CH 2 ; 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 or hydrate thereof, which is useful for treating hypertension.

Claims (11)

1. A compound having the following formula:

or a pharmaceutically acceptable salt of the compound.

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

1-[({[(5R)-5,6-bis(nitrooxy)hexyl]oxy}carbonyl)oxy]ethyl 2-butyl-4-chloro-1-{[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylate—Diastereomer A, and

1-[({[(5R)-5,6-bis(nitrooxy)hexyl]oxy}carbonyl)oxy]ethyl 2-butyl-4-chloro-1-{[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylate—Diastereomer B.

3. A compound of claim 2 , or a pharmaceutically acceptable salt thereof, which is

1-[({[(5R)-5,6-bis(nitrooxy)hexyl]oxy}carbonyl)oxy]ethyl 2-butyl-4-chloro-1-{[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylate—Diastereomer A.

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

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

6. A pharmaceutical composition comprising a compound of claim 3 and a pharmaceutically acceptable carrier.

7. A pharmaceutical composition comprising a compound of claim 3 , a diuretic, and a pharmaceutically acceptable carrier.

Assignments (4)
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 Dec 9, 2010
From: SEBHAT, IYASSU K.; LO, MICHAEL MAN-CHU; NARGUND, RAVI P.; ALI, AMJAD; FRANKLIN, CHRISTOPHER; ALMIRANTE, NICOLETTA; STEFANINI, SILVIA; STORONI, LAURA
To: MERCK SHARP & DOHME CORP.; NICOX S.A.
Reel/Frame 025482/0776 →
CHANGE OF NAME Recorded Jan 26, 2010
From: MERCK & CO., INC.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 023906/0803 →