Stable crystal form of tipiracil hydrochloride and crystallization method for the same
DC
First Claim
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1. Crystal Form I of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting powder X-ray peaks at two or more angles selected from the group consisting of 11.6°
- , 17.2°
, 17.8°
, 23.3°
, 27.1°
, and 29.3°
as a diffraction angle (2θ
±
0.2°
), and having a purity of at least 90% by mass.
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Abstract
Crystal Form I of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting powder X-ray peaks at two or more angles selected from the group consisting of 11.6°, 17.2°, 17.8°, 23.3°, 27.1°, and 29.3° as a diffraction angle (2θ±0.2°).
5 Citations
16 Claims
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1. Crystal Form I of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting powder X-ray peaks at two or more angles selected from the group consisting of 11.6°
- , 17.2°
, 17.8°
, 23.3°
, 27.1°
, and 29.3°
as a diffraction angle (2θ
±
0.2°
), and having a purity of at least 90% by mass. - View Dependent Claims (6, 7, 10, 11, 12, 13, 14, 15, 16)
- , 17.2°
-
2. Crystal Form I of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting peaks at three or more angles of 11.6°
- , 17.2°
, 17.8°
, 23.3°
, 27.1°
, and 29.3°
as a diffraction angle (2θ
±
0.2°
), and having a purity of at least 90% by mass.
- , 17.2°
-
3. Crystal Form I of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting peaks at angles of 11.6°
- , 17.2°
, 17.8°
, 23.3°
, 27.1°
, and 29.3°
as a diffraction angle (2θ
±
0.2°
), and having a purity of at least 90% by mass.
- , 17.2°
-
4. Crystal Form I of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting an endothermic peak determined by thermogravimetry-differential thermal analysis at a temperature of around 262°
- C., exhibiting powder X-ray peaks at two or more angles selected from the group consisting of 11.6°
, 17.2°
, 17.8°
, 23.3°
, 27.1°
, and 29.3°
as a diffraction angle (2θ
±
0.2°
), and having a purity of at least 90% by mass.
- C., exhibiting powder X-ray peaks at two or more angles selected from the group consisting of 11.6°
-
5. Crystal Form I of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride which exhibits powder X-ray peaks at two or more angles selected from the group consisting of 11.6°
- , 17.2°
, 17.8°
, 23.3°
, 27.1°
, and 29.3°
as a diffraction angle (2θ
±
0.2°
), has a purity of at least 90% by mass, and shows, in single-crystal analysis, the following crystal data;Crystal system;
monoclinic systemSpace group;
P21/n (No.
14)Lattice constant; a=11.6006 (9) Å b=10.3106 (11) Å c=10.3036 (10) Å α
=90°β
=101.951 (7)°γ
=90°Unit lattice volume;
1205.7 (2) Å
3.
- , 17.2°
-
8. Crystal Form I of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride after 6-month stability test at 40°
- C., exhibiting powder X-ray peaks at two or more angles selected from the group consisting of 11.6°
, 17.2°
, 17.8°
, 23.3°
, 27.1°
, and 29.3°
as a diffraction angle (2θ
±
0.2°
), and having a purity of at least 90% by mass. - View Dependent Claims (9)
- C., exhibiting powder X-ray peaks at two or more angles selected from the group consisting of 11.6°
Specification
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Litigation Data
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Current AssigneeTaiho Pharmaceutical Company Limited (Otsuka Holdings Company Limited)
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Original AssigneeTaiho Pharmaceutical Company Limited (Otsuka Holdings Company Limited)
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InventorsKazuno, Hideki, Mutsumi, Tomonobu
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Primary Examiner(s)Heyer, Dennis
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Application NumberUS15/969,434Publication NumberTime in Patent Office545 DaysField of SearchNoneUS Class CurrentCPC Class CodesA61P 35/00 Antineoplastic agentsA61P 43/00 Drugs for specific purposes...C07B 2200/13 Crystalline forms, e.g. pol...C07D 403/06 linked by a carbon chain co...
