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1. WO1996004016 - CONJUGATES OF VITAMIN B12 AND PROTEINS

Publication Number WO/1996/004016
Publication Date 15.02.1996
International Application No. PCT/US1995/009477
International Filing Date 28.07.1995
Chapter 2 Demand Filed 26.02.1996
IPC
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
CPC
A61K 47/551
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
54the modifying agent being an organic compound
55the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
551one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
Applicants
  • AMGEN INC. [US/US]; Amgen Center 1840 Dehavilland Drive Thousand Oaks, CA 91320-1789, US
Inventors
  • HABBERFIELD, Alan, David; US
  • KINSTLER, Olaf, Boris; US
  • PITT, Colin, Geoffrey; US
Agents
  • ODRE, Steven, M. ; Amgen Inc. Amgen Center 1840 Dehavilland Drive Thousand Oaks, CA 91320-1789, US
Priority Data
08/282,38429.07.1994US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CONJUGATES OF VITAMIN B12 AND PROTEINS
(FR) CONJUGUES DE VITAMINES B12 ET DE PROTEINES
Abstract
(EN)
Therapeutically useful proteins are conjugated to vitamin B12 by covalent binding at the primary hydroxyl site of the ribose moiety. The resulting conjugates are biologically active and can be formulated into pharmaceutical compositions suitable for delivery by various routes of administration, preferably oral. Uptake in the gut following oral delivery is further enhanced by the co-administration of purified intrinsic factor.
(FR)
La présente invention consiste à conjuguer des protéines d'utilité thérapeutique à la vitamine B12 par liaison covalente au niveau du site hydroxyle primaire d'un segment ribose. Les conjugués résultants sont biologiquement actifs et peuvent se formuler en compositions pharmaceutiques convenant à l'administration par voies diverses, de préférence par voie orale. La co-administration de facteur intrinsèque purifié améliore la fixation dans l'intestin suivant l'administration par voie orale.
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