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1. (WO2018025699) ACTIVE-TARGETING-TYPE POLYMER DERIVATIVE, COMPOSITION CONTAINING SAID POLYMER DERIVATIVE, AND USES OF SAID POLYMER DERIVATIVE AND SAID COMPOSITION
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Pub. No.: WO/2018/025699 International Application No.: PCT/JP2017/026788
Publication Date: 08.02.2018 International Filing Date: 25.07.2017
IPC:
C08G 69/40 (2006.01) ,A61K 9/51 (2006.01) ,A61K 47/34 (2017.01) ,C08L 77/00 (2006.01)
C CHEMISTRY; METALLURGY
08
ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
G
MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
69
Macromolecular compounds obtained by reactions forming a carboxylic amide link in the main chain of the macromolecule
40
Polyamides containing oxygen in the form of ether groups
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
48
Preparations in capsules, e.g. of gelatin, of chocolate
50
Microcapsules
51
Nanocapsules
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
30
Macromolecular compounds
34
Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
C CHEMISTRY; METALLURGY
08
ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
L
COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
77
Compositions of polyamides obtained by reactions forming a carboxylic amide link in the main chain; Compositions of derivatives of such polymers
Applicants:
日本化薬株式会社 NIPPON KAYAKU KABUSHIKI KAISHA [JP/JP]; 東京都千代田区丸の内二丁目1番1号 1-1, Marunouchi 2-chome, Chiyoda-ku, Tokyo 1000005, JP
Inventors:
栗原 大 KURIHARA Dai; JP
福田 剛 FUKUDA Tsuyoshi; JP
川野 裕輝 KAWANO Yuki; JP
山本 啓一朗 YAMAMOTO Keiichirou; JP
Agent:
特許業務法人川口國際特許事務所 KAWAGUTI & PARTNERS; 東京都新宿区北新宿二丁目21番1号新宿フロントタワー20階 Shinjuku Front Tower 20F, 2-21-1 Kita-Shinjuku, Shinjuku-ku, Tokyo 1690074, JP
Priority Data:
2016-15216702.08.2016JP
Title (EN) ACTIVE-TARGETING-TYPE POLYMER DERIVATIVE, COMPOSITION CONTAINING SAID POLYMER DERIVATIVE, AND USES OF SAID POLYMER DERIVATIVE AND SAID COMPOSITION
(FR) DÉRIVÉ DE POLYMÈRE DU TYPE À CIBLAGE ACTIF, COMPOSITION CONTENANT LEDIT DÉRIVÉ DE POLYMÈRE, ET UTILISATIONS DUDIT DÉRIVÉ DE POLYMÈRE ET DE LADITE COMPOSITION
(JA) アクティブターゲティング型高分子誘導体、その高分子誘導体を含む組成物、及びそれらの用途
Abstract:
(EN) The present invention addresses the problem of providing a polymer-micelle-type DDS preparation which makes it possible to improve the transfer, permeability and retention of a pharmacologically active substance to and in an affected target tissue, such as a tumor tissue and an inflammation affected tissue, to improve the activity of the pharmacologically active substance, thereby exerting the pharmacologically active effect of the pharmacologically active substance efficiently. A block copolymer (A) comprising a hydrophilic polymer segment containing a polyethylene glycol chain and a hydrophobic polymer segment containing a polyamic acid chain having a hydrophobic substituent in a side chain thereof, wherein the hydrophilic polymer segment and the hydrophobic polymer segment are linked to each other, a target binding site is bound to the hydrophilic polymer segment, and the molecular weight of a main chain polymer composed of the polyethylene glycol chain and the polyamic acid chain is 2 to 10 kilodaltons inclusive.
(FR) La présente invention vise à proposer une préparation de DDS de type micelle-polymère qui permet d'améliorer le transfert, la perméabilité et la rétention d'une substance pharmacologiquement active dans un tissu cible affecté, par exemple un tissu tumoral ou un tissu inflammé, afin d'améliorer l'activité de la substance pharmacologiquement active, ce qui lui permet d'exercer efficacement son activité pharmacologique. L'invention concerne un copolymère séquencé (A) comprenant un segment polymère hydrophile contenant une chaîne de polyéthylène glycol et un segment polymère hydrophobe contenant une chaîne d'acide polyamique ayant un substituant hydrophobe dans une chaîne latérale de celui-ci, le segment polymère hydrophile et le segment polymère hydrophobe étant liés l'un à l'autre, un site de liaison de cible étant lié au segment de polymère hydrophile, et le poids moléculaire d'un polymère à chaîne principale composé de la chaîne de polyéthylène glycol et de la chaîne d'acide polyamique étant de 2 à 10 kilodaltons inclus.
(JA) 本発明は、腫瘍組織や炎症患部組織といった疾病標的組織に対する移行性、浸透性、滞留性を向上させて薬理活性物質の作用を向上させることにより薬理活性効果を効率的に発揮させることができる高分子ミセル型DDS製剤を提供することを課題とし、ポリエチレングリコール鎖を含有する親水性ポリマーセグメントと、疎水性置換基を側鎖に有するポリアミノ酸鎖を含有する疎水性ポリマーセグメントが連結したブロック共重合体であって、該親水性ポリマーセグメントに標的結合部位が結合しており、該ポリエチレングリコール鎖と該ポリアミノ酸鎖を合せた主鎖ポリマーの分子量が2キロダルトン以上で10キロダルトン以下であるブロック共重合体(A)である。
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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, 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 Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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)