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Pub. No.:    WO/2011/145548    International Application No.:    PCT/JP2011/061156
Publication Date: 24.11.2011 International Filing Date: 16.05.2011
C07D 401/12 (2006.01), A61K 31/53 (2006.01), A61P 35/00 (2006.01), A61P 43/00 (2006.01)
Applicants: Astellas Pharma Inc. [JP/JP]; 3-11, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411 (JP) (For All Designated States Except US).
SHIMADA, Itsuro [JP/JP]; (JP) (For US Only).
HIRAKURA, Yutaka [JP/JP]; (JP) (For US Only).
YAMAZAKI, Kouji [JP/JP]; (JP) (For US Only).
TAKEGUCHI, Kazuhiro [JP/JP]; (JP) (For US Only).
UEDA, Norihiro [JP/JP]; (JP) (For US Only)
Inventors: SHIMADA, Itsuro; (JP).
HIRAKURA, Yutaka; (JP).
YAMAZAKI, Kouji; (JP).
TAKEGUCHI, Kazuhiro; (JP).
UEDA, Norihiro; (JP)
Agent: MORITA, Hiroshi; c/o Astellas Pharma Inc. Intellectual Property, 3-11, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411 (JP)
Priority Data:
2010-114265 18.05.2010 JP
(JA) ジ(アリールアミノ)アリール化合物の結晶
Abstract: front page image
(EN)Provided are crystals of compound A which have properties suitable for industrial production. As the results of intensive studies to provide crystals of compound A having an inhibitory activity on the kinase activity of an EML4-ALK fusion protein and a mutant EGFR protein, crystals of compound A were found. Moreover, it was found that A04 type crystals of compound A, from among the aforesaid crystals of compound A, unexpectedly have preferred properties as a bulk drug.
(FR)L'invention concerne des cristaux d'un composé A qui possèdent des propriétés adaptées à une production industrielle. Des cristaux d'un composé A ont été trouvés comme résultats d'études approfondies pour fournir des cristaux d'un composé A ayant une activité inhibitrice sur l'activité kinase d'une protéine de fusion EML4-ALK et d'une protéine mutante EGFR. En outre, il a été trouvé que des cristaux de type A04 d'un composé A, parmi les cristaux susmentionnés d'un composé A, possèdent, de manière inattendue, des propriétés privilégiées comme un médicament en vrac.
(JA)【課題】工業的生産において好適な性質を有する化合物Aの結晶を提供する。 【解決手段】本発明者等は、EML4-ALK融合タンパク及び変異EGFRタンパクのキナーゼ活性の阻害活性を有する化合物Aの結晶の提供に関し鋭意研究した結果、化合物Aの結晶を見出した。さらには、これらの化合物Aの結晶のうち、意外にも、本発明の化合物AのA04型結晶が、医薬品原薬として好適な性質を有することを知見して、発明を完成した。
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, 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, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, 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, ML, MR, NE, SN, TD, TG).
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)