US2019374498A1PendingUtilityA1

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

72
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 25/00A61P 27/06A61P 3/00A61P 25/06A61P 27/02A61P 3/04A61P 25/28A61P 13/12A61P 11/00A61P 13/02A61P 17/00C07D 257/04A61K 2300/00C07D 207/50A61K 31/216A61K 31/5415A61K 31/41A61K 45/06C07C 233/47A61K 31/4422
72
PatentIndex Score
0
Cited by
0
References
0
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
What is claimed is: 
     
         1 . A compound of formula [((S)-N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine) ((2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester)]Na 3 .xH 2 O, wherein 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, 2.75, 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 0.5x5. 
     
     
         6 . The compound according to  claim 5 , which is crystalline. 
     
     
         7 . The compound according to  claim 1 , wherein x is 0.5. 
     
     
         8 . The compound according to  claim 7 , which is crystalline. 
     
     
         9 . The compound according to  claim 1 , wherein x is 3. 
     
     
         10 . The compound according to  claim 9 , which is crystalline. 
     
     
         11 . The compound according to  claim 1 , which is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 1711, 1637, 1597, and 1401. 
     
     
         12 . The compound according to  claim 1 , which is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 2956, 1711, 1637, 1597, 1488, 1459, 1401, 1357, 1295, 1266, 1176, 1085, 1010, 942, 907, 862, 763, 742, 698, 533. 
     
     
         13 . The compound according to  claim 2 , which is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 1711, 1637, 1597, and 1401. 
     
     
         14 . The compound according to  claim 3 , which is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 1711, 1637, 1597, and 1401. 
     
     
         15 . The compound according to  claim 3 , characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 2956, 1711, 1637, 1597, 1488, 1459, 1401, 1357, 1295, 1266, 1176, 1085, 1010, 942, 907, 862, 763, 742, 698, 533. 
     
     
         16 . The compound according to  claim 4 , which is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 1711, 1637, 1597, and 1401. 
     
     
         17 . The compound according to  claim 5 , which is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 1711, 1637, 1597, and 1401. 
     
     
         18 . The compound according to  claim 5 , characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 2956, 1711, 1637, 1597, 1488, 1459, 1401, 1357, 1295, 1266, 1176, 1085, 1010, 942, 907, 862, 763, 742, 698, 533. 
     
     
         19 . The compound according to  claim 6 , which is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 1711, 1637, 1597, and 1401. 
     
     
         20 . The compound according to  claim 7 , which is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 1711, 1637, 1597, and 1401. 
     
     
         21 . The compound according to  claim 7 , characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 2956, 1711, 1637, 1597, 1488, 1459, 1401, 1357, 1295, 1266, 1176, 1085, 1010, 942, 907, 862, 763, 742, 698, 533. 
     
     
         22 . The compound according to  claim 8 , which is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 1711, 1637, 1597, and 1401. 
     
     
         23 . The compound according to  claim 9 , which is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 1711, 1637, 1597, and 1401. 
     
     
         24 . The compound according to  claim 9 , characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 2956, 1711, 1637, 1597, 1488, 1459, 1401, 1357, 1295, 1266, 1176, 1085, 1010, 942, 907, 862, 763, 742, 698, 533. 
     
     
         25 . The compound according to  claim 10 , which is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 1711, 1637, 1597, and 1401. 
     
     
         26 . A compound of formula [((S)-N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine)((2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester)]Na 3 .xH 2 O, wherein x is 2.5. 
     
     
         27 . The compound according to  claim 26 , which is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 1711, 1637, 1597, and 1401. 
     
     
         28 . The compound according to  claim 26 , characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having absorption bands expressed in reciprocal wave numbers (cm −1 )(±2 cm −1 ): 2956, 1711, 1637, 1597, 1488, 1459, 1401, 1357, 1295, 1266, 1176, 1085, 1010, 942, 907, 862, 763, 742, 698, 533.

Cited by (0)

No later patents cite this yet.

References (0)

No backward citations on record.