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1. (WO2018159604) HEPARIN CONJUGATE
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Pub. No.: WO/2018/159604 International Application No.: PCT/JP2018/007240
Publication Date: 07.09.2018 International Filing Date: 27.02.2018
IPC:
C08B 37/10 (2006.01) ,A61K 31/727 (2006.01) ,A61K 47/18 (2006.01) ,A61P 7/02 (2006.01)
C CHEMISTRY; METALLURGY
08
ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
B
POLYSACCHARIDES; DERIVATIVES THEREOF
37
Preparation of polysaccharides not provided for in groups C08B1/-C08B35/110; Derivatives thereof
10
Heparin; Derivatives thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
715
Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
726
Glycosaminoglycans, i.e. mucopolysaccharides
727
Heparin; Heparan
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
16
containing nitrogen
18
Amines; Quaternary ammonium compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
02
Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
Applicants:
国立大学法人 千葉大学 NATIONAL UNIVERSITY CORPORATION CHIBA UNIVERSITY [JP/JP]; 千葉県千葉市稲毛区弥生町1番33号 1-33, Yayoi-cho, Inage-ku, Chiba-shi, Chiba 2638522, JP
Inventors:
東 恭平 HIGASHI, Kyohei; JP
Agent:
平澤 賢一 HIRASAWA, Kenichi; JP
山下 耕一郎 YAMASHITA, Kouichiro; JP
Priority Data:
2017-03956002.03.2017JP
Title (EN) HEPARIN CONJUGATE
(FR) CONJUGUÉ D'HÉPARINE
(JA) ヘパリンの会合体
Abstract:
(EN) The present invention relates to a novel conjugate of heparin and polyamine, an anticoagulant comprising the conjugate, a pharmaceutical composition containing the conjugate, a kit for producing the conjugate, a sustained release agent, a method for producing the conjugate, etc. (1) A conjugate of heparin and a linear or branched polyamine that has at least 3 amino groups; (2) an anticoagulant comprising the conjugate described in (1); (3) a pharmaceutical composition containing the conjugate described in (1); (4) a kit for producing the conjugate, which contains heparin or a salt thereof and a linear or branched polyamine having at least 3 amino groups or a salt thereof; (5) a sustained release agent for providing a sustained release behavior for heparin, comprising a linear or branched polyamine having at least 3 amino groups or a salt thereof; and (6) a method for producing the conjugate, the method comprising mixing an aqueous solution of heparin or a salt thereof with an aqueous solution of a linear or branched polyamine having at least 3 amino groups or a salt thereof.
(FR) La présente invention concerne un nouveau conjugué d'héparine et de polyamine, un anticoagulant et une composition pharmaceutique le contenant, un kit pour produire le conjugué, un agent à libération prolongée, un procédé de production du conjugué, etc. Plus spécifiquement, la présente invention concerne (1) un conjugué d'héparine et d'une polyamine linéaire ou ramifiée ayant au moins 3 groupes amino; (2) un anticoagulant contenant le conjugué décrit en (1); (3) une composition pharmaceutique contenant le conjugué décrit en (1); (4) un kit pour produire le conjugué, qui contient de l'héparine ou un sel de celle-ci et une polyamine linéaire ou ramifiée ayant au moins 3 groupes amino ou un sel de celle-ci; (5) un agent à libération prolongée pour conférer un comportement à libération prolongée à l'héparine, comprenant une polyamine linéaire ou ramifiée ayant au moins 3 groupes amino ou un sel de celle-ci; et (6) un procédé de production du conjugué, où le procédé comprend le mélange d'une solution aqueuse d'héparine ou d'un sel de celle-ci avec une solution aqueuse d'une polyamine linéaire ou ramifiée ayant au moins 3 groupes amino ou un sel de celle-ci.
(JA) 本発明は、ヘパリンとポリアミンとの新規会合体、会合体からなる抗血液凝固剤、会合体を含む薬剤組成物、会合体の製造のためのキット、徐放性付与剤、及び会合体の製造方法等に関する。 〔1〕ヘパリンと、3以上のアミノ基を有する直鎖状又は分岐状のポリアミンとの会合体、〔2〕〔1〕に記載の会合体からなる抗血液凝固剤、〔3〕〔1〕に記載の会合体を含む薬剤組成物、〔4〕ヘパリン又はその塩と、3以上のアミノ基を有する直鎖状若しくは分岐状のポリアミン、又はその塩とを含む、会合体の製造のためのキット、〔5〕3以上のアミノ基を有する直鎖状若しくは分岐状のポリアミン、又はその塩を含むからなる、ヘパリンの徐放性を付与するための徐放性付与剤、及び〔6〕ヘパリン又はその塩の水溶液と、3以上のアミノ基を有する直鎖状若しくは分岐状のポリアミン又はその塩の水溶液とを混合すること含む、会合体の製造方法。
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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)