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1. WO2017199903 - CRYSTAL OF QUINOLINE DERIVATIVE

Publication Number WO/2017/199903
Publication Date 23.11.2017
International Application No. PCT/JP2017/018165
International Filing Date 15.05.2017
IPC
C07D 215/22 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
20Oxygen atoms
22attached in position 2 or 4
A61K 31/47 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
A61P 1/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 11/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 11/02 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
02Nasal agents, e.g. decongestants
CPC
A61K 31/47
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 11/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
02Nasal agents, e.g. decongestants
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
Applicants
  • 帝人ファーマ株式会社 TEIJIN PHARMA LIMITED [JP]/[JP] (JP)
  • PULMAGEN治療薬(喘息)リミテッド PULMAGEN THERAPEUTICS (ASTHMA) LIMITED [GB]/[GB] (AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BE, BF, BG, BH, BJ, BN, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CL, CM, CN, CO, CR, CU, CY, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IR, IS, IT, KE, KG, KH, KM, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, ME, MG, MK, ML, MN, MR, MT, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SI, SK, SL, SM, SN, ST, SV, SY, SZ, TD, TG, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW)
Inventors
  • ダリー ドナルド ジョーン DALEY Donald John
  • モンタナ ジョーン ゲイリー MONTANA John Gary
  • ハインド ジョージ HYND George
  • 寺本 満 TERAMOTO Mitsuru
  • 伊藤 孝浩 ITO Takahiro
Agents
  • 為山 太郎 TAMEYAMA Taro
Priority Data
2016-09787216.05.2016JP
Publication Language Japanese (ja)
Filing Language Japanese (JA)
Designated States
Title
(EN) CRYSTAL OF QUINOLINE DERIVATIVE
(FR) CRISTAL DE DÉRIVÉ DE QUINOLÉINE
(JA) キノリン誘導体の結晶
Abstract
(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。
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