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Pub. No.:    WO/2011/016528    International Application No.:    PCT/JP2010/063315
Publication Date: 10.02.2011 International Filing Date: 05.08.2010
C07D 401/14 (2006.01), A61K 31/4184 (2006.01), A61K 31/437 (2006.01), A61K 31/4439 (2006.01), A61K 31/444 (2006.01), A61K 31/454 (2006.01), A61K 31/4709 (2006.01), A61K 31/496 (2006.01), A61K 31/501 (2006.01), A61K 31/5377 (2006.01), A61P 35/00 (2006.01), A61P 35/02 (2006.01), A61P 43/00 (2006.01), C07D 403/14 (2006.01), C07D 405/14 (2006.01), C07D 409/14 (2006.01), C07D 413/14 (2006.01), C07D 417/14 (2006.01), C07D 471/04 (2006.01), C07D 491/056 (2006.01)
Applicants: CHUGAI SEIYAKU KABUSHIKI KAISHA [JP/JP]; 5-1, Ukima 5-chome, Kita-ku, Tokyo 1158543 (JP) (For All Designated States Except US).
F.HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124, Basel, CH4070 (CH) (For All Designated States Except US).
TAKA, Naoki [JP/JP]; (JP) (For US Only).
OHMORI, Masayuki [JP/JP]; (JP) (For US Only).
TAKAMI, Kyoko [JP/JP]; (JP) (For US Only).
MATSUSHITA, Masayuki [JP/JP]; (JP) (For US Only).
HAYASE, Tadakatsu [JP/JP]; (JP) (For US Only).
HYODO, Ikumi [JP/JP]; (JP) (For US Only).
KOCHI, Masami [JP/JP]; (JP) (For US Only).
NISHII, Hiroki [JP/JP]; (JP) (For US Only).
EBIIKE, Hirosato [JP/JP]; (JP) (For US Only).
NAKANISHI, Yoshito [JP/JP]; (JP) (For US Only).
MIO, Toshiyuki [JP/JP]; (JP) (For US Only).
WANG, Lisha [CN/CN]; (CN) (For US Only).
ZHAO, Weili [CN/CN]; (CN) (For US Only)
Inventors: TAKA, Naoki; (JP).
OHMORI, Masayuki; (JP).
TAKAMI, Kyoko; (JP).
MATSUSHITA, Masayuki; (JP).
HAYASE, Tadakatsu; (JP).
HYODO, Ikumi; (JP).
KOCHI, Masami; (JP).
NISHII, Hiroki; (JP).
EBIIKE, Hirosato; (JP).
NAKANISHI, Yoshito; (JP).
MIO, Toshiyuki; (JP).
WANG, Lisha; (CN).
ZHAO, Weili; (CN)
Agent: SHIMIZU, Hatsushi; Kantetsu Tsukuba Bldg. 6F, 1-1-1, Oroshi-machi, Tsuchiura-shi, Ibaraki 3000847 (JP)
Priority Data:
2009-184822 07.08.2009 JP
(JA) アミノピラゾール誘導体
Abstract: front page image
(EN)A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like 1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.)
(FR)Cette invention concerne un composé représenté par la formule (I) ou un sel pharmacologiquement acceptable de celui-ci, capable d'inhiber une kinase de la famille des FGFR (récepteurs du facteur de croissance fibroblastique) dans des tissus cancéreux. (Dans la formule, A représente un groupe hétéroaryle de 5 à 10 chaînons, ou un groupe aryle C6-10 ; R1 et R2 représentent indépendamment H, OH, X, CN, NO2, un groupe halogénoalkyle C1-4, un groupe alkyle C1-6, ou autre 1 et R2 formant ensemble un groupe hétérocyclyle de 3 à 10 chaînons (substitué) ou un groupe hétéroaryle de 5 à 10 chaînons (substitué)> ; R3 représente H, un groupe alkyle C1-5, un groupe aryle C6-10, ou un groupe halogénoalkyle C1-4 ; et R4 représente H, X, un groupe alkyle C1-3, un groupe halogénoalkyle C1-4, OH, CN, NO2, ou autre).
(JA) 本発明は、線維芽細胞増殖因子受容体(FGFR)ファミリーキナーゼを癌組織内で阻害することができる、下記式(I)で表される化合物またはその薬理学的に許容される塩である。 A :5-10 員ヘテロアリール,C6-10 アリール R1,2:H,OH,X,CN,NO2,C1-4 ハロアルキル,C1-6 アルキル 等 <共に(置換)3-10 員ヘテロシクリル,(置換)5-10 員ヘテロアリールを形成してもよい> R3:H,C1-5 アルキル,C6-10 アリールC1-5 アルキル,C1-4 ハロアルキル R4:H,X,C1-3 アルキル,C1-4 ハロアルキル,OH,CN,NO2
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, 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)