Novel disaccharide derivative

C - Chemistry – Metallurgy – 07 – H

Patent

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C07H 11/04 (2006.01) A61K 31/70 (2006.01) C07H 3/04 (2006.01) C07H 13/04 (2006.01) C07H 13/06 (2006.01) C12P 19/26 (2006.01)

Patent

CA 2148824

ABSTRACT A novel disaccharide derivative represented by the following formula, which is the compound of the present invention, its stereoisomers and salts and a medicinal composition comprising the same as an active ingredient. Image The compound of the present invention has various biological activities, for example, potent mitogenic activity, adjuvant activity, polyclonal B cell activating (nonspecific protective) activity, natural killer activity, antitumor activity, antiviral activity, etc. but little harmful effects, for example, function of inducing the production of so-called inflammatory cytokines such as tumor necrosis factor (TNF) and IL-1 from macrophages. Therefore it is highly useful as an immunopotentiator, an antitumor agent, an antiviral agent as well as an agent for preventing - 27 - and treating sepsis, chronic rheumatoid arthritis, etc. without showing any harmful effects such as lethal toxicity or pyrogenicity as observed in the conventional lipid A and derivatives thereof. - 28 -

Nouveau dérivé de disaccharide représenté par la formule chimique (I), isomètres stéréochimiques et sels de celui-ci, et composition pharmaceutique le renfermant comme principe actif. Ce composé présente diverses activités biologiques telles qu'une puissante activité mitogène, une activité d'ajuvant, une activité (protectrice non spécifique) d'activation des lymphocytes B polyclonaux, une activité de cellule tueuse naturelle, une activité antitumorale, et une activité antivirale, mais est pratiquement dépourvu de l'activité d'induction de la production de cytokines dites inflammatoires, telles que le facteur de nécrose tumorale (TNF) et l'IL-1, à partir de macrophages différents du lipide A et de ses dérivés. Il est par conséquent dépourvu d'effets nocifs pour lesquels le lipide A et ses dérivés ont posés problème, tels que la toxicité létale et la pyrogénicité, et il est par conséquent utile non seulement comme immunopotentiateur, agent antitumoral et agent antiviral, mais également comme agent thérapeutique ou préventif pour la septicémie, la polyarthrite rhumatoïde, etc.

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