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1. (WO2017090699) PHARMACEUTICAL COMPOSITION FOR IMMUNOACTIVATION AND/OR PHARMACEUTICAL COMPOSITION FOR CANCER IMMUNOTHERAPY, CONTAINING PYRAZINE CARBOXAMIDE AS ACTIVE INGREDIENT
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/090699 International Application No.: PCT/JP2016/084885
Publication Date: 01.06.2017 International Filing Date: 25.11.2016
IPC:
A61K 31/497 (2006.01) ,A61P 35/00 (2006.01) ,A61P 37/04 (2006.01) ,A61P 43/00 (2006.01) ,C12N 15/09 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4965
Non-condensed pyrazines
497
containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
02
Immunomodulators
04
Immunostimulants
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43
Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15
Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09
Recombinant DNA-technology
Applicants:
アステラス製薬株式会社 ASTELLAS PHARMA INC. [JP/JP]; 東京都中央区日本橋本町二丁目5番1号 5-1, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411, JP
Inventors:
小長井 智史 KONAGAI, Satoshi; JP
吉田 卓 YOSHIDA, Taku; JP
辻本 晋 TSUJIMOTO, Susumu; JP
Agent:
森平 浩一郎 MORIHIRA, Koichiro; JP
矢野 恵美子 YANO, Emiko; JP
鈴木 ▲頼▼子 SUZUKI, Yoriko; JP
濱井 康丞 HAMAI, Kousuke; JP
寺内 輝和 TERAUCHI, Terukazu; JP
飯室 加奈 IIMURO, Kana; JP
影山 路人 KAGEYAMA, Michihito; JP
川濱 周弥 KAWAHAMA, Shuya; JP
鎌田 啓明 KAMADA, Hiroaki; JP
Priority Data:
2015-23164327.11.2015JP
Title (EN) PHARMACEUTICAL COMPOSITION FOR IMMUNOACTIVATION AND/OR PHARMACEUTICAL COMPOSITION FOR CANCER IMMUNOTHERAPY, CONTAINING PYRAZINE CARBOXAMIDE AS ACTIVE INGREDIENT
(FR) COMPOSITION PHARMACEUTIQUE POUR L'ACTIVATION DU SYSTÈME IMMUNITAIRE ET/OU COMPOSITION PHARMACEUTIQUE POUR L'IMMUNOTHÉRAPIE DU CANCER, CONTENANT COMME PRINCIPE ACTIF UN PYRAZINE CARBOXAMIDE
(JA) ピラジンカルボキサミド化合物を有効成分とするがん免疫治療用医薬組成物、及び/又は、免疫活性化用医薬組成物
Abstract:
(EN) [Problem] To provide a compound that is useful as an active ingredient in a pharmaceutical composition for cancer immunotherapy or a pharmaceutical composition for immunoactivation, for example. [Solution] As a result of having carried out painstaking research with the purpose of creating a pharmaceutical composition for immunoactivation and/or a pharmaceutical composition for cancer immunotherapy, the inventors discovered that 5-{[(3R)-1-acryloyl pyrrolidine-3-yl]oxy}-6-ethyl-3-({4-[4-(4-methyl piperazine-1-yl)piperidine-1-yl]phenyl}amino)pyrazine-2-carboxamide or a pharmacologically acceptable salt thereof has excellent BTK and/or ITK inhibitory action, and suppresses the activation of Th2 cells without suppressing the activation of Th1 cells, therefore leading to the expectation that a pharmaceutical composition containing said compound or a pharmacologically acceptable salt thereof as an active ingredient can be used as a pharmaceutical composition for cancer immunotherapy and/or a composition for immunoactivation, and thereby resulting in the completion of the present invention.
(FR) Le problème que cherche à résoudre l'invention est de fournir un composé qui soit utilisable comme principe actif dans une composition pharmaceutique pour l'immunothérapie du cancer ou une composition pharmaceutique pour l'activation du système immunitaire, par exemple. La solution est basée sur des recherches poussées visant à créer une composition pharmaceutique pour l'activation du système immunitaire et/ou une composition pharmaceutique pour l'immunothérapie du cancer, grâce auxquelles les inventeurs ont découvert que le 5-{[(3R)-1-acryloyl pyrrolidine-3-yl]oxy}-6-éthyl-3-({4-[4-(4-méthyl pipérazine-1-yl)pipéridine-1-yl]phényl}amino)pyrazine-2-carboxamide ou un sel de qualité pharmaceutique de ce dernier présentait une excellente action inhibitrice de la BTK et/ou de l'ITK, et inhibait l'activation des cellules Th2 sans inhiber l'activation des cellules Th1, conduisant à envisager qu'une composition pharmaceutique comprenant comme principe actif ledit composé ou un sel de qualité pharmaceutique de ce dernier puisse être utilisée comme composition pharmaceutique pour l'immunothérapie du cancer et/ou comme composition pharmaceutique pour l'activation du système immunitaire, constituant ainsi l'aboutissement de la présente invention.
(JA) 【課題】医薬組成物、例えば、がん免疫治療用医薬組成物、及び/又は、免疫活性化用医薬組成物の有効成分として有用な化合物を提供する。 【解決手段】本発明者らは、がん免疫治療用医薬組成物、及び/又は、免疫活性化用医薬組成物の創製を目的に鋭意検討した結果、5-{[(3R)-1-アクリロイルピロリジン-3-イル]オキシ}-6-エチル-3-({4-[4-(4-メチルピペラジン-1-イル)ピペリジン-1-イル]フェニル}アミノ)ピラジン-2-カルボキサミド又はその製薬学的に許容される塩に優れたBTK及び/又はITK阻害作用を有し、Th1細胞の活性化を抑制することなく、Th2細胞の活性化を抑制することから、該化合物又はその製薬学的に許容される塩を有効成分として含有する医薬組成物が、がん免疫治療用医薬組成物、及び/又は、免疫活性化用医薬組成物としての使用が期待されることを知見して本発明を完成した。
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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, 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, SA, 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 (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, 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, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)