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1. (WO2019009434) DRUG DELIVERY POLYMER MICELLES
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Pub. No.: WO/2019/009434 International Application No.: PCT/JP2018/026250
Publication Date: 10.01.2019 International Filing Date: 06.07.2018
IPC:
C08G 81/00 (2006.01) ,A61K 9/107 (2006.01) ,A61K 45/00 (2006.01) ,A61K 47/28 (2006.01) ,A61K 47/34 (2017.01) ,A61K 47/62 (2017.01) ,A61K 48/00 (2006.01) ,A61K 49/00 (2006.01) ,A61K 51/00 (2006.01) ,A61P 19/10 (2006.01) ,A61P 29/00 (2006.01) ,A61P 35/00 (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
81
Macromolecular compounds obtained by interreacting polymers in the absence of monomers, e.g. block polymers
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
10
Dispersions; Emulsions
107
Emulsions
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45
Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
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
06
Organic compounds
28
Steroids
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
[IPC code unknown for A61K 47/62]
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
48
Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49
Preparations for testing in vivo
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51
Preparations containing radioactive substances for use in therapy or testing in vivo
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19
Drugs for skeletal disorders
08
for bone diseases, e.g. rachitism, Paget's disease
10
for osteoporosis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
学校法人京都薬科大学 KYOTO PHARMACEUTICAL UNIVERSITY [JP/JP]; 京都府京都市山科区御陵中内町5 5, Misasagi-Nakauchi-cho, Yamashina-ku, Kyoto-shi, Kyoto 6078414, JP
Inventors:
勝見 英正 KATSUMI, Hidemasa; JP
山本 昌 YAMAMOTO, Akira; JP
Agent:
高島 一 TAKASHIMA, Hajime; 大阪府大阪市中央区伏見町四丁目1番1号 明治安田生命大阪御堂筋ビル Meiji Yasuda Seimei Osaka Midosuji Bldg., 1-1, Fushimimachi 4-chome, Chuo-ku, Osaka-shi, Osaka 5410044, JP
Priority Data:
2017-13280506.07.2017JP
Title (EN) DRUG DELIVERY POLYMER MICELLES
(FR) MICELLES POLYMÈRES POUR L'ADMINISTRATION DE MÉDICAMENTS
(JA) 薬物送達用高分子ミセル
Abstract:
(EN) The present invention relates to: a compound that is formed by linking the α carbonyl group of aspartic acid directly or via a linker to at least 50% of all of the terminal groups of a dendritic polymer that has a plurality of terminal groups by means of a peptide bond or an ester linkage, by linking a hydrophilic polymer segment directly or via a linker to at least 3% of the total of the terminal amino groups from the aspartic acid and the terminal groups of the dendritic polymer not modified with aspartic acid, and linking a hydrophobic segment directly or via a linker to at least 1% of the total of the terminal amino groups from the aspartic acid and the terminal groups of the dendritic polymer not modified with aspartic acid; and a drug delivery carrier that comprises polymer micelles that self-assemble from the compound. The drug delivery carrier forms micelles when mixed with a drug and thereby makes it possible for the drug to be selectively delivered to bones, which makes it possible to provide useful medicine for the treatment of various bone diseases.
(FR) La présente invention concerne : un composé qui est formé par liaison du groupe alpha-carbonyle de l'acide aspartique directement ou par l'intermédiaire d'un lieur à au moins 50 % de tous les groupes terminaux d'un polymère dendritique qui a une pluralité de groupes terminaux au moyen d'une liaison peptidique ou d'une liaison ester, par liaison d'un segment polymère hydrophile directement ou par l'intermédiaire d'un lieur à au moins 3 % de tous les groupes amino terminaux de l'acide aspartique et des groupes terminaux du polymère dendritique non modifié avec l'acide aspartique, et par liaison d'un segment hydrophobe directement ou par l'intermédiaire d'un lieur à au moins 1 % de tous les groupes amino terminaux de l'acide aspartique et des groupes terminaux du polymère dendritique non modifié avec l'acide aspartique ; et un vecteur d'administration de médicaments qui comprend des micelles polymères qui s'auto-assemblent à partir du composé. Le vecteur d'administration de médicaments forme des micelles lorsqu'il est mélangé avec un médicament et permet ainsi au médicament d'être administré sélectivement aux os, ce qui permet de fournir un médicament utile pour le traitement de diverses maladies osseuses.
(JA) 本発明は、複数の末端基を有する樹状高分子の全末端基数の少なくとも50%に直接又はリンカーを介して、アスパラギン酸のα位カルボニル基がぺプチド結合又はエステル結合により連結し、該アスパラギン酸由来の末端アミノ基及びアスパラギン酸修飾されていない樹状高分子上の末端基の総数の少なくとも3%に、直接又はリンカーを介して親水性重合体セグメントが結合し、且つ前記アスパラギン酸由来の末端アミノ基及びアスパラギン酸修飾されていない樹状高分子上の末端基の総数の少なくとも1%に、直接又はリンカーを介して疎水性セグメントが結合してなる化合物、及び該化合物の自己集合により形成される高分子ミセルからなる薬物送達用担体に関する。本発明の薬物送達用担体によれば、薬物との混合によるミセル形成により、骨へ選択的に薬物が送達されるので、各種骨疾患等の治療において有用な医薬を提供することができる。
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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)