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Claims for Patent: 8,877,938

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Claims for Patent: 8,877,938

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 compound of an angiotensin receptor antagonist (ARB), a neutral endopeptidase inhibitor (NEPi) and one or more monovalent cations are useful for the treatment of hypertension and/or heart failure. ARB includes S--N-valeryl-N-{[2'-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-v- aline in the anion form, NEPi includes (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester in the anion form and cation includes monovalent cations such as Na.sup.+. The compound includes trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propi- onate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-4'-ylmeth- yl}amino)butyrate] hemipentahydrate.
Inventor(s): Feng; Lili (Pine Brook, NJ), Godtfredsen; Sven Erik (Chatham, NJ), Hu; Bin (Green Brook, NJ), Liu; Yugang (Bridgewater, NJ), Karpinski; Piotr (Lincoln Park, NJ), Sutton; Paul Allen (Parsippany, NJ), Prashad; Mahavir (Montville, NJ), Girgis; Michael J. (Montville, NJ), Blacklock; Thomas J. (Clark, NJ)
Assignee: Novartis Pharmaceuticals Corporation (East Hanover, NJ)
Application Number:11/722,360
Patent Claims: 1. Trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propi- onate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5-ylate)biphenyl-4'-ylmeth- yl}amino)butyrate] hemipentahydrate in crystalline form.

2. The compound of claim 1 having the sum formula C.sub.48H.sub.55N.sub.6O.sub.8Na.sub.3 .circle-solid. 2.5 H.sub.2O and being in the form of an asymmetric unit comprising six C.sub.48H.sub.55N.sub.6O.sub.8Na.sub.3 .circle-solid. 2.5 H.sub.2O formula units.

3. The compound of claim 1 characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having the following absorption bands expressed in reciprocal wave numbers (cm.sup.-1)(.+-.2 cm.sup.-1): 1711 (st), 1637 (st), 1597 (st) and 1401 (st).

4. The compound of claim 3 characterized by an Attenuated Total Reflection Fourier Transform Infrared (ATR-FTIR) spectrum having the following absorption bands expressed in reciprocal wave numbers (cm.sup.-1)(.+-.2 cm.sup.-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).

5. The compound of claim 1 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).

6. The compound of claim 1 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.] 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.

7. The compound of claim 1 in the form of a monoclinic unit cell, wherein its cell content comprises twelve formula units of C.sub.48H.sub.55N.sub.6O.sub.8Na.sub.3 .circle-solid. 2.5 H.sub.2O.

8. The compound of claim 7 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.

9. The compound of claim 7 wherein the monoclinic unit cell has a P2i space group.

10. The compound of claim 1 characterized by TABLE-US-00005 sum formula C.sub.48H.sub.55N.sub.6O.sub.8Na.sub.3.cndot.2.5H.sub.2O molecular mass 957.99 crystal colour colourless crystal shape tabular: hexagonal crystal system monoclinic space group P2.sub.1 Cell parameters a = 20.344 .ANG. b = 42.018 .ANG. c = 20.374 .ANG. .alpha. = 90.degree. .beta. = 119.29.degree. .gamma. = 90.degree. volume of unit cell 15190.03 .ANG..sup.3 Z (the number of asymmetric 2 units in the unit cell) calculated density 1.26845 g/cm3.

11. A pharmaceutical composition comprising an effective amount of the compound of claim 1 and at least one pharmaceutically acceptable additive.

12. The pharmaceutical composition of claim 10 further comprising a therapeutic agent selected from an anti-diabetic, a hypolipidemic agent, an anti-obesity agent and an anti-hypertensive agent.

13. The pharmaceutical composition of claim 11 wherein the therapeutic agent is amlodipine besylate.

14. The pharmaceutical composition of claim 11, wherein the therapeutic agent is hydrochlorothiazide.
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