US2019374497A1PendingUtilityA1

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

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Assignee: NOVARTIS AGPriority: Nov 9, 2005Filed: Jul 3, 2019Published: Dec 12, 2019
Est. expiryNov 9, 2025(expired)· nominal 20-yr term from priority
Inventors:Lili FengSven Erik GodtfredsenPaul Allen SuttonMahavir PrashadMichael John GirgisBin HuYugang LiuThomas J. BlacklockPiotr H. Karpinski
A61P 43/00A61P 9/14A61P 9/12A61P 9/10A61P 9/08A61P 9/06A61P 9/04A61P 9/00A61P 7/12A61P 5/42A61P 5/24A61P 3/10A61P 3/06A61P 25/28A61P 25/00A61P 3/00A61P 27/06A61P 3/04A61P 25/06A61P 27/02A61P 13/12A61P 13/02A61P 17/00A61P 11/00A61K 31/216A61K 31/4422A61K 45/06A61K 31/41C07D 257/04A61K 31/5415C07D 207/50C07C 233/47A61K 2300/00
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Claims

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.

Claims

exact text as granted — not AI-modified
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.

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