US 2013/0296353 A1Published application

Crystalline pharmaceutically active ingredients

AssigneeEGIS Gyogyszergyar Nyilvanosan Mukodo Reszvenytar- sasag

InventorsImre Markovits, Ferenc Jurak, Gyorgyi Kovanyine Lax, Csaba Hamori, Balazs Havasi, Eva Sipos, Balazs Volk, Zsolt Runge, Krisztina Fodorne Kocsmar, Gyula Lukacs, Katalin Kataine Fadgyas, Monika Mezovari

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Abstract

The present invention is related to crystalline forms of rosuvastatin zinc (2:1) salt. The polymorphs are suitable for use as pharmaceutically active ingredients in the treatment of the diseases of the lipid metabolism including hypercholesterolemia, hyperlipidemia, dyslipidemia or atherosclerosis.

Claims24

Dependent claims

A crystalline Form V rosuvastatin zinc (2:1) salt [hemizinc salt of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S)-dihydroxy-hept-6-enoic acid] of Formula (I)

which has
X-ray diffraction lines measured by CuKα radiation at the following diffraction angle 2Θ (±0.2° 2Θ):
4.746 degrees;
or
X-ray diffraction lines measured by CuKα radiation at the following diffraction angles 2Θ (±0.2° 2Θ):
4.746 and 15.371 degrees;
or
a powder X-ray diffractogram of FIG. 1;
or
the following X-ray diffraction lines measured by the CuKα radiation:
2Θ [°]
d-value [Å]
Relative intensity [%]
4.764
18.5324
100.0
5.873
15.0352
20.9
8.941
9.8823
11.1
9.547
9.2561
12.5
10.960
8.0664
20.7
11.773
7.5111
19.0
12.224
7.2347
20.6
12.870
6.8733
8.8
13.118
6.7438
21.1
13.979
6.3303
13.9
14.401
6.1454
9.8
15.371
5.7599
61.6
15.997
5.5359
13.2
16.357
5.4148
10.4
16.852
5.2570
8.0
17.641
5.0235
6.9
17.995
4.9256
29.6
18.783
4.7206
5.8
19.394
4.5733
31.9
19.977
4.4411
9.2
20.741
4.2792
5.1
20.959
4.2352
4.6
21.700
4.0922
12.3
22.263
3.9899
17.5
22.736
3.9080
9.7
23.367
3.8038
14.9
23.659
3.7575
12.9
24.235
3.6695
29.8
24.716
3.5992
10.5
25.245
3.5250
19.3
26.034
3.4199
9.5
26.485
3.3627
8.0
27.028
3.2964
12.9
28.016
3.1824
8.3
28.667
3.1115
8.0
29.662
3.0093
8.6
30.967
2.8854
9.2
32.668
2.7390
6.9
33.032
2.7096
8.0
33.342
2.6851
7.2
33.989
2.6355
5.6
34.452
2.6011
6.8

136 more elements

A crystalline Form III rosuvastatin zinc (2:1) salt [hemizinc salt of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S)-dihydroxy-hept-6-enoic acid] of Formula (I)

which has
X-ray diffraction line measured by CuKα radiation at the following diffraction angles 2Θ (±0.2° 2Θ):
18.961 degrees;
or
X-ray diffraction lines measured by CuKα radiation at the following diffraction angles 2Θ (±0.2° 2Θ):
6.259, 13.414 and 18.961 degrees;
or
X-ray diffraction lines measured by CuKα radiation at the following diffraction angles 2Θ (±0.2° 2Θ):
6.259, 10.982, 13.414, 16.401, 18.600, 18.961, 19.409, 20.462 and 22.302 degrees;
or
X-ray diffraction lines measured by CuKα radiation at the following diffraction angles 2Θ (±0.2° 2Θ):
6.259, 9.400, 10.982, 13.414, 15.480, 16.401, 16.623, 16.926, 18.338, 18.600, 18.961, 19.409, 20.462, 21.846, 22.302, 22.779, 23.232, 26.451, 27.178, 27.603, 31.311 and 31.861 degrees;
or
a powder X-ray diffractogram of FIG. 2 measured by CuKα radiation;
or
characteristic reflexions in a powder X-ray diffractogram measured by CuKα radiation according to the following table:
Relative
Intensity
2Θ
d (Å)
(%)
6.259
14.11083
90.2
9.400
9.40131
36
10.982
8.04997
62.4
11.318
7.81202
15.4
12.565
7.03939
12.1
13.414
6.59524
92.8
14.437
6.13017
5.4
14.806
5.97820
19.6
15.48
5.71948
20.5
15.776
5.61288
18.7
16.059
5.51479
15.4
16.401
5.40024
50.1
16.623
5.32865
44.8
16.926
5.23406
43.6
17.572
5.04319
15.4
17.894
4.95294
15.4
18.338
4.83405
48.9
18.600
4.76648
50.4
18.961
4.67672
100
19.409
4.56959
58.2
20.462
4.33695
53.2
21.383
4.15201
12.6
21.846
4.06507
47.1
22.302
3.98297
58.1
22.779
3.90066
39.5
23.232
3.82568
35.6
24.055
3.69663
10.4
24.690
3.60288
17.4
25.388
3.50540
16.9
26.451
3.36697
33.9
27.178
3.27846
22.5
27.603
3.22900
20.6
28.472
3.13240
16.2
29.938
2.98221
14.8
30.180
2.95883
16.7
31.311
2.85449
21.8
31.861
2.80646
25.7
32.695
2.73674
14.6
33.177
2.39812
13.2
34.134
2.62459
8

138 more elements

Dependencies are inferred from the claim text.

Facts

Application: 13/885,509Filed 16 Nov 2011
Priority: HU P10 0061616 Nov 2010
Published: 7 Nov 2013
Term ends: Not estimatedThe source records don’t support an estimate.

Classification5 codes

C07D 239/42
One oxygen, sulfur or nitrogen atom: one nitrogen atom
A61P 3/06
Drugs for disorders of the metabolism: antihyperlipidemics
A61P 9/10
Drugs for disorders of the cardiovascular system: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary…
C07D
Heterocyclic compounds

Family

US 9,321,733 B2Related patent
US 2013/0296353 A1This patent

From the US filing history. Foreign family members aren’t listed.

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