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1. (WO2013058361) CRYSTALS OF ANDROGEN RECEPTOR ANTAGONIST COMPOUND
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2013/058361    International Application No.:    PCT/JP2012/077091
Publication Date: 25.04.2013 International Filing Date: 19.10.2012
IPC:
C07D 403/12 (2006.01), A61K 31/506 (2006.01), A61P 5/28 (2006.01), A61P 13/08 (2006.01), A61P 35/00 (2006.01)
Applicants: ASTELLAS PHARMA INC. [JP/JP]; 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411 (JP)
Inventors: NAKAMURA, Takashi; (JP).
OKAMOTO, Takumi; (JP).
HIRAKURA, Yutaka; (JP).
YAMAZAKI, Kouji; (JP).
KAKEFUDA, Akio; (JP).
YAMASHITA, Hiroyuki; (JP)
Agent: MORITA, Hiroshi; c/o Astellas Pharma Inc. Intellectual Property, 3-11, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411 (JP)
Priority Data:
2011-231273 21.10.2011 JP
Title (EN) CRYSTALS OF ANDROGEN RECEPTOR ANTAGONIST COMPOUND
(FR) CRISTAUX DE COMPOSÉ ANTAGONISTE DE RÉCEPTEUR D'ANDROGÈNE
(JA) アンドロゲン受容体拮抗化合物の結晶
Abstract: front page image
(EN)[Problem] To provide the following: crystals suitable for industrialization as the starting drug of a pharmaceutical product, having excellent activity as an androgen receptor (AR) antagonist compound and formed of (2R,5S)-4-(3-chloro-4-cyanophenyl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-dimethylpiperazine-1-carboxamide, or a salt thereof, or a hydrate of the same; a pharmaceutical composition containing the crystals as an active ingredient; and the pharmaceutical composition, which is an AR antagonist. [Solution]Provided are A01-shaped crystals of a monohydrate, A01-shaped crystals of a hydrochloride, A01-shaped crystals of a hydrobromate, and A01-shaped crystals of a methanesulfonylic acid salt of (2R,5S)-4-(3-chloro-4-cyanophenyl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-dimethylpiperazine-1-carboxamide, wherein the crystals have a specific shape.
(FR)La présente invention concerne des cristaux appropriés pour l'industrialisation en tant que médicament de départ d'un produit pharmaceutique, présentant une excellente activité en tant que composé antagoniste de récepteur d'androgène (RA) et formé de (2R,5S)-4-(3-chloro-4-cyanophényl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-diméthylpipérazine-1-carboxamide ou d'un sel de celui-ci ou de son hydrate; une composition pharmaceutique contenant les cristaux en tant que principe actif; et la composition pharmaceutique, qui est un antagoniste de RA. L'invention concerne des cristaux sous forme A01 d'un monohydrate, des cristaux sous forme A01 d'un chlorhydrate, des cristaux sous forme A01 d'un bromhydrate et des cristaux sous forme A01 d'un sel d'acide méthanesulfonylique de (2R,5S)-4-(3-chloro-4-cyanophényl)-N-(2-cyclopropylpyrimidin-5-yl)-2,5-diméthylpipérazine-1-carboxamide, les cristaux présentant une forme spécifique.
(JA)【課題】アンドロゲン受容体(AR)拮抗化合物として優れた活性を有する、(2R,5S)-4-(3-クロロ-4-シアノフェニル)-N-(2-シクロプロピルピリミジン-5-イル)-2,5-ジメチルピペラジン-1-カルボキサミド又はその塩、或いはそれらの溶媒和物の、医薬品の原薬として工業化に適する結晶、当該結晶を有効成分として含有する医薬組成物、並びにAR拮抗薬である当該医薬組成物を提供する。 【解決手段】(2R,5S)-4-(3-クロロ-4-シアノフェニル)-N-(2-シクロプロピルピリミジン-5-イル)-2,5-ジメチルピペラジン-1-カルボキサミドの、ある特定の結晶形を有する、一水和物のA01形結晶、塩酸塩のA01形結晶、臭化水素酸塩のA01形結晶、及びメタンスルホニル酸塩のA01形結晶を提供する。
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, 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, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, 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, 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, ML, MR, NE, SN, TD, TG).
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)