US2004029813A1PendingUtilityA1
Novel $g(beta crystalline form of perindopril tert-butylamine salt, preparation method, and pharmaceutical compositions containing same
Priority: Jul 6, 2000Filed: Jul 6, 2001Published: Feb 12, 2004
Est. expiryJul 6, 2020(expired)· nominal 20-yr term from priority
A61P 9/00A61P 9/12A61P 9/10A61P 9/04A61P 43/00A61P 7/10A61P 13/02C07D 209/42A61K 31/404
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Claims
Abstract
β crystalline form of the compound of formula (I): characterised by its powder X-ray diffraction diagram. Medicaments.
Claims
exact text as granted — not AI-modified1 . β Crystalline Form of the Compound of Formula (I):
characterised by the following powder x-ray diffraction diagram measured using a diffractometer (copper anticathode) and expressed in terms of inter-planar distance d, Bragg's angle 2 theta, intensity and relative intensity (expressed as a percentage with respect to the most intense ray):
Angle 2 theta
Inter-planar
Relative intensity
(°)
distance d (Å)
Intensity
(%)
5.169
17.08
523
16.5
8.379
10.54
1001
31.5
9.350
9.45
3175
100
14.746
6.00
236
7.4
15.411
5.74
753
23.7
15.931
5.56
279
8.8
16.711
5.30
113
3.6
18.161
4.88
122
3.8
20.564
4.32
1198
37.7
21.285
4.17
330
10.4
21.781
4.08
317
10
22.632
3.93
190
6
23.308
3.81
133
4.2
23.797
3.74
427
13.4
24.276
3.66
118
3.7
25.190
3.53
92
2.9
25.924
3.43
251
7.9
26.646
3.34
250
7.9
27.620
3.23
96
3
28.306
3.15
133
4.2
2 . Process for the preparation of the β crystalline form of the compound of formula (1) according to claim 1 , characterised in that a solution of perindopril tert-butylamine salt in dichloromethane is heated at reflux, the solution is then cooled to 0° C. and the solid obtained is collected by filtration.
3 . Process for the preparation of the β crystalline form of the compound of formula (I) according to claim 1 , characterised in that a solution of perindopril tert-butylamine salt in ethyl acetate is heated at reflux, the solution is rapidly cooled to 5° C. and the solid obtained is then collected by filtration.
4 . Process according to either claim 2 or claim 3 , characterised in tat the compound of formula (I) obtained by the preparation process described in patent specification EP 0 308 341 is used.
5 . Process according to claim 2 , characterised in that the concentration of the compound of formula (I) in the dichloromethane is from 100 to 200 g/litre.
6 . Process according to claim 3 , characterised in that the concentration of the compound of formula (I) in the ethyl acetate is from 70 to 90 g/litre.
7 . Pharmaceutical composition comprising as active ingredient the compound according to claim 1 , in combination with one or more pharmaceutically acceptable, inert, non-toxic carriers.
8 . Pharmaceutical composition according to claim 7 for use in the manufacture of medicaments for use as inhibitors of angiotensin I converting enzyme.
9 . Pharmaceutical composition according to claim 8 for use in the manufacture of medicaments for use in the treatment of cardiovascular diseases.
10 . Pharmaceutical composition according to any one of claims 7 to 9 , characterised in that it also comprises a diuretic.
11 . Pharmaceutical composition according to claim 10 , characterised in tat the diuretic is indapamide.Join the waitlist — get patent alerts
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