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1. (WO2011162300) CRYSTAL OF FUSED PYRIDINE COMPOUND SALT
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2011/162300    International Application No.:    PCT/JP2011/064291
Publication Date: 29.12.2011 International Filing Date: 22.06.2011
IPC:
C07D 471/04 (2006.01), A61K 9/14 (2006.01), A61K 9/16 (2006.01), A61K 9/20 (2006.01), A61K 9/48 (2006.01), A61K 31/437 (2006.01), A61P 9/10 (2006.01), A61P 11/06 (2006.01), A61P 17/04 (2006.01), A61P 17/06 (2006.01), A61P 19/02 (2006.01), A61P 29/00 (2006.01), A61P 35/00 (2006.01), A61P 35/02 (2006.01), A61P 37/02 (2006.01), A61P 37/06 (2006.01), A61P 37/08 (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).
KIKUCHI, Takashi [JP/JP]; (JP) (For US Only).
GATO, Katsuhiko [JP/JP]; (JP) (For US Only).
MUKOYOSHI, Koichiro [JP/JP]; (JP) (For US Only).
KITAMURA, Tsuyoshi [JP/JP]; (JP) (For US Only).
KAWAKAMI, Takeshi [JP/JP]; (JP) (For US Only).
YASUDA, Hironobu [JP/JP]; (JP) (For US Only)
Inventors: KIKUCHI, Takashi; (JP).
GATO, Katsuhiko; (JP).
MUKOYOSHI, Koichiro; (JP).
KITAMURA, Tsuyoshi; (JP).
KAWAKAMI, Takeshi; (JP).
YASUDA, Hironobu; (JP)
Agent: MORITA, Hiroshi; c/o Astellas Pharma Inc. Intellectual Property, 3-11, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411 (JP)
Priority Data:
2010-143226 23.06.2010 JP
Title (EN) CRYSTAL OF FUSED PYRIDINE COMPOUND SALT
(FR) CRISTAL D'UN SEL D'UN COMPOSÉ DE PYRIDINE FUSIONNÉ
(JA) 縮合ピリジン化合物塩の結晶
Abstract: front page image
(EN)Disclosed is a salt or crystal of a compound which is excellently stable in a solid state and useful as a starting material for the production of a pharmaceutical product. Specifically, a 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2- adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide succinic acid salt, a 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2- adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrobromic acid salt, a 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2- adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrochloride and crystals of the above-mentioned salts are useful for the production of a solid preparation, especially for the production of a solid dispersed preparation. In addition, a crystal of a hydrobromic acid salt is excellently stable in a solid state and useful as an active ingredient for the production of a pharmaceutical product.
(FR)L'invention concerne un sel ou un cristal d'un composé qui est remarquablement stable à l'état solide et utile en tant que matière première pour la fabrication d'un produit pharmaceutique. Spécifiquement, un sel de l'acide succinique de 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, un sel de l'acide bromhydrique de 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, un chlorhydrate de 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide et les cristaux des sels susmentionnés sont utiles pour la fabrication d'une préparation solide, notamment pour la fabrication d'une préparation solide dispersée. Par ailleurs, un cristal d'un sel de l'acide bromhydrique est remarquablement stable à l'état solide et utile en tant qu'ingrédient actif pour la fabrication d'un produit pharmaceutique.
(JA)【課題】優れた固体状態での安定性を有し、医薬品の製造原料として有用な化合物の塩もしくは結晶を提供する。 【解決手段】4-{[(1R,2s,3S,5s,7s)-5-ヒドロキシ-2-アダマンチル]アミノ}-1H-ピロロ[2,3-b]ピリジン-5-カルボキサミドコハク酸塩、4-{[(1R,2s,3S,5s,7s)-5-ヒドロキシ-2-アダマンチル]アミノ}-1H-ピロロ[2,3-b]ピリジン-5-カルボキサミド臭化水素酸塩、及び、4-{[(1R,2s,3S,5s,7s)-5-ヒドロキシ-2-アダマンチル]アミノ}-1H-ピロロ[2,3-b]ピリジン-5-カルボキサミド塩酸塩、並びにこれらの結晶は、固体製剤殊に固体分散体製剤の製造に有用である。また、臭化水素酸塩の結晶は、固体状態の安定性に優れ、医薬品の製造原体として有用である。
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)