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1. (WO2015115091) ANTI-HER2 ANTIBODY-DRUG CONJUGATE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2015/115091    International Application No.:    PCT/JP2015/000355
Publication Date: 06.08.2015 International Filing Date: 28.01.2015
IPC:
C07K 16/28 (2006.01), A61K 31/4745 (2006.01), A61K 39/395 (2006.01), A61P 35/00 (2006.01), C07D 491/052 (2006.01)
Applicants: DAIICHI SANKYO COMPANY, LIMITED [JP/JP]; 3-5-1, Nihonbashi Honcho, Chuo-ku, Tokyo 1038426 (JP)
Inventors: NAITO, Hiroyuki; (JP).
OGITANI, Yusuke; (JP).
MASUDA, Takeshi; (JP).
NAKADA, Takashi; (JP).
YOSHIDA, Masao; (JP).
ASHIDA, Shinji; (JP).
MORITA, Koji; (JP).
MIYAZAKI, Hideki; (JP).
KASUYA, Yuji; (JP).
HAYAKAWA, Ichiro; (JP).
ABE, Yuki; (JP)
Agent: OHNO, Seiji; (JP)
Priority Data:
2014-017777 31.01.2014 JP
2014-168944 22.08.2014 JP
2014-227886 10.11.2014 JP
Title (EN) ANTI-HER2 ANTIBODY-DRUG CONJUGATE
(FR) CONJUGUÉ ANTICORPS ANTI-HER2-MÉDICAMENT
(JA) 抗HER2抗体-薬物コンジュゲート
Abstract: front page image
(EN)As an anti-tumor drug having an excellent anti-tumor effect and safety and also having an excellent therapeutic effect, an antibody-drug conjugate is provided, which is characterized in that an anti-tumor compound represented by formula (1) is linked to an anti-HER2 antibody through a linker having a structure represented by the formula: -L1-L2-LP-NH-(CH2)n1-La-(CH2)n2-C(=O)- (wherein the anti-HER2 antibody is linked at the terminal of L1, and the anti-tumor compound is linked to a carbonyl group in a -(CH2)n2-C(=O)- moiety wherein a nitrogen atom in an amino group located at position-1 in the anti-tumor compound serves as a linking part).
(FR)L'invention concerne, en tant que médicament antitumoral possédant un excellent effet antitumoral et une excellente innocuité et présentant également un excellent effet thérapeutique, un conjugué anticorps-médicament, qui est caractérisé en ce que le composé antitumoral représenté par la formule (1) est lié à un anticorps anti-HER2 par l'intermédiaire d'une séquence de liaison possédant une structure représentée par la formule : -L1-L2-LP-NH-(CH2)n1-La-(CH2)n2-C(=O)- (l'anticorps anti-HER2 étant lié au niveau de la terminaison de L1 et le composé antitumoral étant lié à un groupe carbonyle dans un fragment -(CH2)n2-C(=O)-, un atome d'azote dans un groupe amino situé en position 1 du composé antitumoral servant de partie de liaison).
(JA) 抗腫瘍効果と安全性面に優れる、優れた治療効果を有する抗腫瘍薬として、次式 (1)で示される抗腫瘍性化合物と抗HER2抗体とを、次式: -L-L-L-NH-(CH2)n-L-(CH2)n-C(=O)- で示される構造のリンカーを介して結合させたことを特徴とする抗体-薬物コンジュゲート(抗HER2抗体はLの末端において結合し、抗腫瘍性化合物は、1位のアミノ基の窒素原子を結合部位として、-(CH2)n-C(=O)-部分のカルボニル基に結合する)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, IR, IS, JP, KE, KG, KN, KP, KR, 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 (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)