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1. (WO2006085692) CRYSTAL OF 4(3H)-QUINAZOLINONE DERIVATIVE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2006/085692    International Application No.:    PCT/JP2006/302900
Publication Date: 17.08.2006 International Filing Date: 13.02.2006
IPC:
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 (2006.01), A61P 25/36 (2006.01), A61P 43/00 (2006.01)
Applicants: BANYU PHARMACEUTICAL CO., LTD [JP/JP]; Kitanomaru Square 1-13-12, Kudankita Chiyoda-ku, Tokyo 102-8667 (JP) (For All Designated States Except US).
NAGASE, Tsuyoshi [JP/JP]; (JP) (For US Only).
SATO, Nagaaki [JP/JP]; (JP) (For US Only).
KANATANI, Akio [JP/JP]; (JP) (For US Only).
TOKITA, Shigeru [JP/JP]; (JP) (For US Only)
Inventors: NAGASE, Tsuyoshi; (JP).
SATO, Nagaaki; (JP).
KANATANI, Akio; (JP).
TOKITA, Shigeru; (JP)
Common
Representative:
BANYU PHARMACEUTICAL CO., LTD; Kitanomaru Square 1-13-12, Kudankita Chiyoda-ku, Tokyo 102-8667 (JP)
Priority Data:
2005-036659 14.02.2005 JP
Title (EN) CRYSTAL OF 4(3H)-QUINAZOLINONE DERIVATIVE
(FR) CRISTAL DE DERIVE DE LA 4(3H)-QUINAZOLINONE
(JA) 4(3H)-キナゾリノン誘導体の結晶
Abstract: front page image
(EN)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&thetas;±0.2°).
(FR)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&thetas; ± 0,2°).
(JA) 本発明は、ヒスタミンのヒスタミンH3受容体への結合に拮抗する作用又はヒスタミンH3受容体に有する恒常的活性を抑制する活性を有する物質を提供する。即ち、粉末X線回折において、回折角度(2θ±0.2°)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°及び39.0°にピークを有する、2−メチル−3−{4−[3−(1−ピロリジニル)プロポキシ]フェニル}−5−トリフルオロメチル−4(3H)−キナゾリノンのフォームI結晶が提供される。
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)