Compounds containing s-n-valeryl-n-{[2'-(1h-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine and (2r,4s)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester moieties and cations

Patent metadata

Field	Value
Publication number	US-2019374497-A1
Application number	US-201916502811-A
Country	US
Kind code	A1
Filing date	Jul 3, 2019
Priority date	Nov 9, 2005
Publication date	Dec 12, 2019
Grant date	—

Abstract

A compound comprising of the angiotensin receptor antagonist (ARB) valsartan, the neutral endopeptidase inhibitor (NEPi) (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methylpentanoic acid ethyl ester and one or more monovalent cations such as Na + useful for the treatment of hypertension and/or heart failure.

First claim

1 . A compound comprising:
(i) ((S)—N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine); (ii) ((2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester); (iii) sodium cations; and (iv) H 2 O;
wherein 0<x<5 wherein the molar ratio of (i) to (ii) to (iii) to (iv) is 1:1:y:x, wherein y is 1 to 3 and 0<x<5.

2 . The compound according to claim 1 , which is crystalline.

3 . The compound according to claim 1 , wherein x is 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.25, 2.5, 2.75, 3, 3.25, 3.5, 3.75, 4, 4.25, 4.5, 4.75, or 5.

4 . The compound according to claim 3 , which is crystalline.

5 . The compound according to claim 1 , wherein 0.5<x<5.

6 . The compound according to claim 5 , which is crystalline.

7 . The compound according to claim 1 , wherein x is 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.25, 2.5, 2.75, or 3.

8 . The compound according to claim 7 , which is crystalline.

9 . The compound according to claim 1 , wherein 0.5<x<3.

10 . The compound according to claim 9 , which is crystalline.

11 . The compound according to claim 1 , wherein x is 0.5.

12 . The compound according to claim 11 , which is crystalline.

13 . The compound according to claim 1 , wherein x is 3.

14 . The compound according to claim 13 , which is crystalline.

15 . The compound according to claim 1 , wherein x is 2.5.

16 . The compound according to claim 15 , which is crystalline.

Assignees

• Novartis Ag

Inventors

• Feng Lili
• Godtfredsen Sven Erik
• Sutton Paul Allen
• Prashad Mahavir
• Girgis Michael J
• Hu Bin
• Liu Yugang
• Blacklock Thomas J
• Karpinski Piotr Henryk

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P9/14

  Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers · CPC title

• A61P9/12

  Antihypertensives · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P9/08

  Vasodilators for multiple indications · CPC title