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Pub. No.:    WO/2017/199903    International Application No.:    PCT/JP2017/018165
Publication Date: 23.11.2017 International Filing Date: 15.05.2017
C07D 215/22 (2006.01), A61K 31/47 (2006.01), A61P 1/00 (2006.01), A61P 1/04 (2006.01), A61P 11/00 (2006.01), A61P 11/02 (2006.01), A61P 11/06 (2006.01), A61P 17/04 (2006.01), A61P 17/06 (2006.01)
Applicants: TEIJIN PHARMA LIMITED [JP/JP]; 2-1, Kasumigaseki 3-chome, Chiyoda-ku Tokyo 1000013 (JP)
Inventors: DALEY Donald John; (GB).
MONTANA John Gary; (GB).
HYND George; (GB).
TERAMOTO Mitsuru; (JP).
ITO Takahiro; (JP)
Agent: TAMEYAMA Taro; (JP)
Priority Data:
2016-097872 16.05.2016 JP
(JA) キノリン誘導体の結晶
Abstract: front page image
(EN)Crystals of [8-chloro-3-(4-chlorobenzyl)-4-difluoromethoxy- 2-ethylquinolin-5-yloxy]acetic acid L-lysine salt, i.e., a crystal A which has peaks at diffraction angles 2θ = 6.0°, 10.0°, 10.7°, 12.1°, 18.4°, 19.2° and 20.1° in powder X-ray diffraction spectra and a crystal B which has peaks at diffraction angles 2θ = 6.0°, 11.7°, 12.4°, 15.2°, 16.4°, 20.3° and 22.6° in powder X-ray diffraction spectra. These crystals are chemically stable and have excellent thermal stability and physical properties, and are therefore suitable as medicinal substances.
(FR)L'invention concerne des cristaux de sel de L-lysine d'acide [8-chloro-3-(4-chlorobenzyl)-4-difluorométhoxy-2-éthylquinolin-5-yloxy] acétique, c'est-à-dire un cristal A qui présente des pics à des angles de diffraction 2θ = 6,0°, 10,0°, 10,7°, 12,1°, 18,4°, 19,2° et 20,1° dans des spectres de diffraction des rayons X en poudre et un cristal B qui présente des pics à des angles de diffraction 2θ = 6,0°, 11,7°, 12,4°, 15,2°, 16,4°, 20,3° et 22,6° dans les spectres de diffraction des rayons X sur poudres. Ces cristaux sont chimiquement stables et présentent des propriétés physiques et de stabilité thermique excellentes, et sont par conséquent appropriés en tant que substances médicinales.
(JA)[8-クロロ-3-(4-クロロベンジル)-4-ジフルオロメトキシ-2-エチルキノリン-5-イルオキシ]酢酸 L-リシン塩の結晶であって、粉末X線回折スペクトルにおいて、回折角2θ=6.0°、10.0°、10.7°、12.1°、18.4°、19.2°、および20.1°にピークを有するそのA晶、ならびに回折角2θ=6.0°、11.7°、12.4°、15.2°、16.4°、20.3°、および22.6°にピークを有するそのB晶。これらの結晶は化学的に安定で、熱的安定性および物理的性質に優れ、医薬原薬として適している。
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG).
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)