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1. WO2006095775 - CONJUGATE OF WATER-SOLUBLE MODIFIED HYALURONIC ACID AND GLP-1 ANALOGUE

Publication Number WO/2006/095775
Publication Date 14.09.2006
International Application No. PCT/JP2006/304480
International Filing Date 08.03.2006
IPC
C08B 37/08 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
BPOLYSACCHARIDES; DERIVATIVES THEREOF
37Preparation of polysaccharides not provided for in groups C08B1/-C08B35/110; Derivatives thereof
08Chitin; Chondroitin sulfate; Hyaluronic acid; Derivatives thereof
A61K 47/48 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C07K 14/605 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
575Hormones
605Glucagons
CPC
A61K 47/61
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
61the organic macromolecular compound being a polysaccharide or a derivative thereof
A61P 3/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 3/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
04Anorexiants; Antiobesity agents
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
C07K 14/605
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
575Hormones
605Glucagons
C08B 37/0072
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
BPOLYSACCHARIDES; DERIVATIVES THEREOF
37Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
006Heteroglycans, i.e. polysaccharides having more than one sugar residue in the main chain in either alternating or less regular sequence; Gellans; Succinoglycans; Arabinogalactans; Tragacanth or gum tragacanth or traganth from Astragalus; Gum Karaya from Sterculia urens; Gum Ghatti from Anogeissus latifolia; Derivatives thereof
0063Glycosaminoglycans or mucopolysaccharides, e.g. keratan sulfate; Derivatives thereof, e.g. fucoidan
0072Hyaluronic acid, i.e. HA or hyaluronan; Derivatives thereof, e.g. crosslinked hyaluronic acid (hylan) or hyaluronates
Applicants
  • 中外製薬株式会社 CHUGAI SEIYAKU KABUSHIKI KAISHA [JP]/[JP] (AllExceptUS)
  • 中村 輝郎 NAKAMURA, Teruo [JP]/[JP] (UsOnly)
  • 加藤 達也 KATO, Tatsuya [JP]/[JP] (UsOnly)
  • 外川 秀幸 TOGAWA, Hideyuki [JP]/[JP] (UsOnly)
  • 八杉 健司 YASUGI, Kenji [JP]/[JP] (UsOnly)
  • 小西 博子 KONISHI, Hiroko [JP]/[JP] (UsOnly)
  • 関森 泰男 SEKIMORI, Yasuo [JP]/[JP] (UsOnly)
  • 下房地 剛 SHIMOBOJI, Tsuyoshi [JP]/[JP] (UsOnly)
Inventors
  • 中村 輝郎 NAKAMURA, Teruo
  • 加藤 達也 KATO, Tatsuya
  • 外川 秀幸 TOGAWA, Hideyuki
  • 八杉 健司 YASUGI, Kenji
  • 小西 博子 KONISHI, Hiroko
  • 関森 泰男 SEKIMORI, Yasuo
  • 下房地 剛 SHIMOBOJI, Tsuyoshi
Agents
  • 社本 一夫 SHAMOTO, Ichio
Priority Data
2005-06412208.03.2005JP
2006-03564513.02.2006JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) CONJUGATE OF WATER-SOLUBLE MODIFIED HYALURONIC ACID AND GLP-1 ANALOGUE
(FR) CONJUGUE D’ACIDE HYALURONIOUE MODIFIE SOLUBLE DANS L’EAU ET ANALOGUE DU GLP-1
(JA) 水溶性ヒアルロン酸修飾物とGLP-1アナログの結合体
Abstract
(EN)
Disclosed is a hyaluronic acid-peptide conjugate wherein one or more glucagon-like peptide-1 (GLP-1) analogues are bonded to a water-soluble modified hyaluronic acid, or a salt thereof. Particularly disclosed is a hyaluronic acid-peptide conjugate wherein not less than 70% of carboxy groups contained in the glucuronic acid unit of hyaluronic acid are converted to N-substituted amide groups in the water-soluble modified hyaluronic acid, or a salt of such a hyaluronic acid-peptide conjugate. In this connection, the N-substituted amide groups in the modified hyaluronic acid may have the same or different substituents, and at least one of the substituents is a divalent linking group to be bonded with the GLP-1 analogue.
(FR)
L’invention concerne un conjugué acide hyaluronique/peptide avec un ou plusieurs analogues du peptide-1 similaire au glucagon (GLP-1) liés à un acide hyaluronique modifié soluble dans l’eau, ou un sel de celui-ci. L’invention présente particulièrement un conjugué acide hyaluronique/peptide où pas moins de 70% des groupes carboxy contenus dans l’unité d’acide glucuronique sont convertis en groupes amide substitués N dans l’acide hyaluronique modifié soluble dans l’eau, ou un sel d'un tel conjugué acide hyaluronique/peptide. Dans cette connexion les groupes amide substitués N dans l’acide hyaluronique modifié peuvent avoir des substituants semblables ou différents, et au moins un des substituant est un groupe de liaison divalent à lier avec l’analogue du GLP-1.
(JA)
 本発明は、水溶性のヒアルロン酸修飾物に1以上のグルカゴン様ペプチド-1(GLP-1)アナログが結合したヒアルロン酸-ペプチド結合体またはその塩、特に、水溶性のヒアルロン酸修飾物において、ヒアルロン酸のグルクロン酸部分に含まれるカルボキシ基の70%以上がN-置換アミド基に変換されており、ここで当該ヒアルロン酸修飾物中の各N-置換アミド基の置換基は同一であっても異なってもよく、当該置換基の少なくとも1つが前記GLP-1アナログと連結する2価の連結基である、前記ヒアルロン酸-ペプチド結合体またはその塩に関する。
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