Crystal of 4(3h)-quinazolinone derivative

Details Crystal of 4(3h)-quinazolinone derivative Crystal of 4(3h)-quinazolinone derivative

C - Chemistry, Metallurgy

07

D

C07D 239/91 (2006.01) A61K 31/517 (2006.01) A61K 45/00 (2006.01) A61P 1/16 (2006.01) A61P 3/04 (2006.01) A61P 3/06 (2006.01) A61P 3/10 (2006.01) A61P 3/12 (2006.01) A61P 5/00 (2006.01) A61P 9/04 (2006.01) A61P 9/10 (2006.01) A61P 9/12 (2006.01) A61P 13/12 (2006.01) A61P 19/06 (2006.01) A61P 25/02 (2006.01) A61P 25/08 (2006.01) A61P 25/14 (2006.01) A61P 25/16 (2006.01) A61P 25/18 (2006.01) A61P 25/20 (2006.01) A61P 25/22 (2006.01) A61P 25/24 (2006.01) A61P 25/28 (2006.01) A61P 25/30 (2006.01) A61P 25/32 (200

Patent

CA 2597541

A substance that has a potency antagonistic to coupling of histamine with histamine H3 receptor or a potency of inhibiting the constant activity of histamine H3 receptor. There is provided a form I crystal of 2-methyl-3-{4-[3- (1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone that in the powder X-ray diffractometry, has peaks at 6.4~, 9.7~, 10.2~, 12.9~, 14.2~, 14.7~, 16.0~, 16.3~, 16.8~, 17.6~, 19.5~, 20.3~, 20.6~, 21.2~, 21.8~, 22.1~, 22.4~, 22.6~, 24.0~, 24.3~, 24.9~, 25.7~, 25.9~, 26.5~, 26.7~, 27.4~, 29.1~, 29.4~, 32.3~ and 39.0~ diffraction angles (2.theta.~0.2~).

La substance de l~invention possède une capacité antagoniste vis-à-vis du couplage de l~histamine avec le récepteur H3 de l~histamine, ou une capacité d~inhibition de l~activité permanente dudit récepteur. L~invention concerne un cristal de forme (I) de la 2-méthyl-3-{4-[3-(1-pyrrolidinyl)propoxy]phényl}-5-trifluorométhyl-4(3H)-quinazolinone, lequel cristal, lorsqu~il est soumis à diffractométrie X à l~état de poudre, produit des pics aux angles de diffraction suivants : 6,4°, 9,7°, 10,2°, 12,9°, 14,2°, 14,7°, 16,0°, 16,3°, 16,8°, 17,6°, 19,5°, 20,3°, 20,6°, 21,2°, 21,8°, 22,1°, 22,4°, 22,6°, 24,0°, 24,3°, 24,9°, 25,7°, 25,9°, 26,5°, 26,7°, 27,4°, 29,1°, 29,4°, 32,3° et 39,0° (2.theta. ± 0,2°).

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