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Details for Patent: 9,388,134

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Details for Patent: 9,388,134

Title: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
Abstract: A method for treatment of a cardiovascular or renal condition or disease with a specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi.
Inventor(s): Feng; Lili (Pine Brook, NJ), Godtfredsen; Sven Erik (Chatham, NJ), Sutton; Paul Allen (Parsippany, NJ), Prashad; Mahavir (Montville, NJ), Girgis; Michael J. (Montville, NJ), Hu; Bin (Green Brook, NJ), Liu; Yugang (Bridgewater, NJ), Blacklock; Thomas J. (East Hanover, NJ), Karpinski; Piotr Henryk (Lincoln Park, NJ)
Assignee: NOVARTIS, AG (Basel, CH)
Filing Date:Jun 23, 2014
Application Number:14/311,788
Claims:1. A method for treatment of a cardiovascular condition or disease, wherein the cardiovascular condition or disease is heart failure or hypertension, in a patient in need thereof comprising administering to the patient a therapeutically effective amount of trisodium[3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbam- oyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-- 4'-ylmethyl}amino)butyrate]hemipentahydrate.

2. The method according to claim 1, wherein the heart failure is chronic heart failure.

3. The method according to claim 1, wherein the condition or disease is hypertension.

4. The method according to claim 1, wherein the compound trisodium[3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbam- oyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-- 4'-ylmethyl}amino)butyrate]hemipentahydrate is administered in the form of a pharmaceutical composition.

5. The method according to claim 1, wherein the compound trisodium[3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbam- oyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-- 4'-ylmethyl}amino)butyrate]hemipentahydrate is in the crystalline form.

6. The method according to claim 5, wherein the compound trisodium[3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbam- oyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-- 4'-ylmethyl}amino)butyrate]hemipentahydrate is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having the following absorption bands expressed in reciprocal wave numbers (cm-1)(.+-.2 cm-1): 1711 (st), 1637 (st), 1597 (st) and 1401 (st).

7. The method according to claim 5, wherein the compound trisodium[3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbam- oyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-- 4'-ylmethyl}amino)butyrate]hemipentahydrate is characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having the following absorption bands expressed in reciprocal wave numbers (cm-1)(.+-.2 cm-1): 2956 (w), 1711 (st), 1637 (st), 1597 (st), 1488 (w), 1459 (m), 1401 (st), 1357 (w), 1295 (m), 1266 (m), 1176 (w), 1085 (m), 1010 (w), 942(w), 907 (w), 862 (w), 763 (st), 742 (m), 698 (m), 533 (st).

8. The method according to claim 5, wherein the compound trisodium[3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbam- oyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-- 4'-ylmethyl}amino)butyrate]hemipentahydrate is characterized by an X-ray powder diffraction pattern taken with a Scintag XDS2000 powder diffractometer comprising the following interlattice plane intervals: d in [.ANG.] (.+-.0.1 .ANG.): 21.2(s), 17.0(w), 7.1(s), 5.2(w), 4.7(w), 4.6(w), 4.2(w), 3.5(w), 3.3(w).

9. The method according to claim 5, wherein the compound trisodium[3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbam- oyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-- 4'-ylmethyl}amino)butyrate]hemipentahydrate is characterized by an X-ray powder diffraction pattern taken with a Scintag XDS2000 powder diffractometer comprising the following interlattice plane intervals, 2.theta. in [.degree.]) (.+-.0.2.degree.) 4.5, 5.5, 5.6, 9.9, 12.8, 15.7, 17.0, 17.1, 17.2, 18.3, 18.5, 19.8, 21.5, 21.7, 23.2, 23.3, 24.9, 25.3, 27.4, 27.9, 28.0, 30.2.

10. The method according to claim 5, wherein the compound trisodium[3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbam- oyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-- 4'-ylmethyl}amino)butyrate]hemipentahydrate is in the form of a monoclinic unit cell, wherein its cell content comprises twelve formula units of C48H55N6O8Na3.2.5H2O.

11. The method according to claim 10, wherein the compound trisodium[3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbam- oyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-- 4'-ylmethyl}amino)butyrate]hemipentahydrate is in the form of a monoclinic unit cell, wherein the cell content of the monoclinic unit cell comprises two asymmetric units on two-fold positions.

12. The method according to claim 10, wherein the monoclinic unit cell has a P2i space group.

13. The method according to claim 5, wherein the compound trisodium[3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbam- oyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-- 4'-ylmethyl}amino)butyrate]hemipentahydrate is characterized by sum formula C48H55N6O8Na3.2.5H2O molecular mass 957.99 crystal colour colourless crystal shape tabular: hexagonal crystal system monoclinic space group P21 Cell parameters a=20.344 .ANG. b=42.018 .ANG. c=20.374 .ANG. .alpha.=90 0 .beta.=119.29 .gamma.=90 o volume of unit cell 15190.03 .ANG.3 Z (the number of asymmetric units in the unit cell) 2 calculated density 1.26845 g/cm3.

14. The method according to claim 5, wherein the compound trisodium[3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbam- oyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-- 4'-ylmethyl}amino)butyrate]hemipentahydrate has the sum formula C48H55N6O8Na3.2.5H2O and is in the form of an asymmetric unit comprising six C48H55N6O8Na3.2.5H2O formula units.

15. The method according to claim 5, wherein the compound trisodium[3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbam- oyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-- 4'-ylmethyl}amino)butyrate]hemipentahydrate is characterized by an X-ray powder diffraction pattern taken with a Scintag XDS2000 powder diffractometer comprising the following interlattice plane intervals, 2e in [.degree. ]) (.+-.0.2.degree.) 4.5, 5.6, 12.8, 17.0, 17.2, 19.8, 21.5, 27.4.
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