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US 12,473,268 B2Granted
Solid state forms of Blarcamesine salts
AssigneeAssia Chemical Industries Ltd.
InventorsPolina Lapido, Jenny Goldshtein
Life of this patent
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Abstract
The present disclosure encompasses a novel solid state form of Blarcamesine and salts thereof, processes for preparation thereof, and pharmaceutical compositions thereof.
Claims18
A crystalline form of Blarcamesine HBr designated Form A, which is characterized by data selected from one or more of the following:
- (a) an XRPD pattern having peaks at 6.4, 13.9, 19.2, 20.3 and 21.5 degrees 2-theta±0.2 degrees 2-theta;
- (b) an XRPD pattern substantially as depicted in FIG. 1;
- (c) an XRPD pattern having peaks at 6.4, 13.9, 19.2, 20.3 and 21.5 degrees 2-theta #0.2 degrees 2-theta, and also having one, two, three, four or five additional peaks selected from 11.6, 13.1, 16.1, 22.3 or 23.2 degrees two theta±0.2 degrees two theta;
- (d) an X-ray powder diffraction pattern having peaks at 6.4, 11.6, 13.1, 13.9, 16.1, 19.2, 20.3, 21.5, 22.3 and 23.2 degrees 2-theta±0.2 degrees 2-theta;
- (e) an X-ray powder diffraction pattern having peaks at 6.4, 11.6, 12.6, 13.1, 13.9, 16.1, 19.2, 20.3, 21.5, 22.3, 23.2, 25.4, 26.0, 27.5 and 29.0 degrees 2-theta±0.2 degrees 2-theta;
- (f) a solid state 13C NMR spectrum with characteristic peaks at 143.7, 127.1, 59.0, 50.7 and 43.5 ppm±0.2 ppm;
- (g) a solid state 13C NMR spectrum having the following chemical shift absolute differences from reference peak at 146.7 ppm±1 ppm:
- 3.0, 19.6, 87.7, 96.0 and 103.2 ppm±0.1 ppm;
- (h) a solid state 13C NMR spectrum substantially as depicted in FIG. 3, 4 or 5;
- and
- (i) combinations of these data.
8 more elements
A crystalline form of Blarcamesine HBr designated Form B, which is characterized by data selected from one or more of the following:
- (a) an XRPD pattern having peaks at 7.9, 10.2, 11.9, 15.9 and 21.1 degrees 2-theta±0.2 degrees 2-theta;
- (b) an XRPD pattern substantially as depicted in FIG. 7;
- (c) an XRPD pattern having peaks at 7.9, 10.2, 11.9, 15.9 and 21.1 degrees 2-theta±0.2 degrees 2-theta, and also having one, two, three, four or five additional peaks selected from 13.1, 16.9, 17.9, 20.4 or 23.8 degrees two theta±0.2 degrees two theta;
- (d) an X-ray powder diffraction pattern having peaks at 7.9, 10.2, 11.9, 13.1, 15.9, 16.9, 17.9, 20.4, 21.1 and 23.8 degrees 2-theta±0.2 degrees 2-theta;
- (e) an X-ray powder diffraction pattern having peaks at 7.9, 10.2, 11.9, 13.1, 15.9, 16.4, 16.9, 17.9, 19.6, 20.0, 20.4, 21.1, 23.8, 24.3, 25.2, 25.5 and 26.3 degrees 2-theta±0.2 degrees 2-theta;
- (f) a solid state 13C NMR spectrum with characteristic peaks at 144.8, 134.8, 47.0, 46.5 and 42.7 ppm±0.2 ppm;
- (g) a solid state 13C NMR spectrum having the following chemical shift absolute differences from reference peak at 148.9 ppm #1 ppm:
- 4.1, 14.1, 101.9, 102.4 and 106.2 ppm±0.1 ppm;
- (h) a solid state 13C NMR spectrum substantially as depicted in FIG. 9, 10 or 11;
- and
- (i) combinations of these data.
8 more elements
Dependencies are inferred from the claim text.