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Claims for Patent: 5,608,075

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Claims for Patent: 5,608,075

Title: Polymorphs of losartan and the process for the preparation of form II of losartan
Abstract:Polymorphic forms of Losartan (Formula I) ##STR1## and a process for the preparation of Form II of Losartan. Losartan is known to be useful in the treatment of hypertension.
Inventor(s): Campbell, Jr.; Gordon C. (Wilmington, DE), Dwivedi; Anil M. (Newark, DE), Levorse; Dorothy A. (South Amboy, NJ), McCauley; James A. (Bellemeade, NJ), Raghavan; Krishnaswamy S. (Wilmington, DE)
Assignee: Merck & Co., Inc. (Rahway, NJ) E. I. Du Pont de Nemours & Company (Wilmington, DE) The DuPont Merck Pharmaceutical Company (Wilmington, DE)
Application Number:08/371,937
Patent Claims: 1. Form I of Losartan characterized by an endothermal maximum of conversion at an extrapolated onset temperature of 229.5.degree. C. and an endothermal maximum of melting at an extrapolated onset temperature of 273.2.degree. C. when heated in an open pan in a differential scanning calorimetric cell at a rate of 10.degree. C./min under a nitrogen atmosphere and an X-ray powder diffraction pattern having X-ray powder diffraction angles: 7.24, 11.02, 14.16, 15.07, 18.46, 18.87, 26.53, 27.30, 29.15.

2. Form I of Losartan according to claim 1 further characterized by FTIR spectra from 1150 to 600 cm.sup.-1 and 1800 to 1150 cm.sup.-1 having spectral absorbances: 764, 713,886, 934, 953, 1358, 1340 cm.sup.-1.

3. Form I of Losartan according to claim 2 further characterized by solid state .sup.13 C CP/MAS NMR spectra of the upfield and downfield regions having .sup.13 C chemical shifts in parts per million as shown in the table below:

4. Form I of Losartan according to claim 3 further characterized by Raman spectra from 1100 to 600 cm.sup.-1 and 180 to 400 cm.sup.-1 having Raman spectral modes: 807, 819, 710, 760, 199, 227, 319, 340, 354 cm.sup.-1.

5. Form II of Losartan characterized by an endothermal maximum of melting at an extrapolated onset temperature of 273.2.degree. C. when heated in an open pan in a differential scanning calorimetric cell at a rate of 10.degree. C./min under a nitrogen atmosphere and an X-ray powder diffraction pattern having X-ray powder diffraction angles: 2.95, 6.95, 7.91, 12.61, 14.28, 18.98, 20.01, 21.63, 29.15.

6. Form H of Losartan according to claim 5 further characterized by FTIR spectra from 1150 to 600 cm.sup.-1 and 1800 to 1150 cm.sup.-1 having spectral absorbances: 754, 934, and 1357 cm.sup.-1.

7. Form II of Losartan according to claim 6 further characterized by solid state .sup.13 C CP/MAS NMR spectra of the upfield and downfield regions having .sup.13 C chemical shifts in parts per million as shown in the table below:

8. Form II of Losartan according to claim 7 further characterized by Raman spectra from 1100 to 600 cm.sup.-1 and 180 to 400 cm.sup.-1 having Raman spectral modes: 803, 763, 191, 316, 340 cm.sup.-1.

9. A process for the preparation of Form II of Losartan according to claim 5 which comprises heating Form I of Losartan to a temperature range of about 230.degree. to about 270.degree. C. at a rate of 10.degree. C./min.

10. The process of claim 9, wherein Form I of Losartan is heated in a differential scanning calorimetric cell in an open pan under a nitrogen atmosphere.

11. The process for the preparation of Form II of Losartan as recited in claim 10, which comprises heating Form I to a temperature of 255.degree. C .
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