US 8,569,351 B2 · Dual-acting benzyl triazole antihypertensive agents having angiotensin II type receptor antagonist activity and neprilysin-inhibition activity

Abstract

The invention is directed to compounds having the formula: wherein: Ar, X, R3, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Claims3

Dependent claims

A compound of formula IIIa:

wherein Ar is:
R1 is —COOR1a, where R1a is H or —C1-6alkyl;
R3 is —C1-10alkyl;
X is —CH2—NHC(O)—;
R5 is selected from —C0-3alkylene-SR5a and —C0-3alkylene-C(O)N(OH)H;
R5a is H or —C(O)C1-6alkyl;
R6 is selected from —C1-6alkyl and —C0-3alkylenearyl;
and R7 is H;
and pharmaceutically acceptable salts thereof.

6 more elements

Dependencies are inferred from the claim text.

Facts

Application

13/692,538Filed 3 Dec 2012 · division

Priority

24 Apr 2007

Published

US 2013/0096162 A118 Apr 2013

Granted

29 Oct 2013

Term ends

Not estimatedThe source records don’t support an estimate.

Classification31 codes

C07D 233/70
With hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals,…:…
A61K 31/415
Having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole: 1,2-Diazoles
A61K 31/4164
Having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole: 1,3-Diazoles
A61K 31/417
1,3-Diazoles: imidazole-alkylamines, e.g. histamine, phentolamine

Family

Application60/925,931Us provisional application · filed 24 Apr 2007

Application12/148,872Parent of this division · filed 23 Apr 2008

Application13/191,100Parent of this division · filed 26 Jul 2011

US 8,013,005 B2Parent of this division · filed 6 Sep 2011

Application13/531,057Parent of this division · filed 22 Jun 2012

US 8,236,846 B2Parent of this division · filed 7 Aug 2012

US 2013/0096162 A1Pre-grant publication · published 18 Apr 2013

US 8,349,875 B2Parent of this division

US 2008/0269305 A1Published application

US 2011/0281925 A1Published application

US 2012/0264752 A1Published application

US 8,569,351 B2This patent

From the US filing history. Foreign family members aren’t listed.

Dual-acting benzyl triazole antihypertensive agents having angiotensin II type receptor antagonist activity and neprilysin-inhibition activity

Life of this patent

Dual-acting benzyl triazole antihypertensive agents having angiotensin II type receptor antagonist activity and neprilysin-inhibition activity

Life of this patent

Abstract

Claims3