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1. (MXPA/a/1999/010675) TRITERPENE SAPONIN ANALOGS HAVING ADJUVANT AND IMMUNOSTIMULATORY ACTIVITY

Office : Mexico
Application Number: PA/a/1999/010675 Application Date: 19.11.1999
Publication Number: PA/a/1999/010675 Publication Date: 01.08.2000
Publication Kind : A
Prior PCT appl.: Application Number:US1998010280 ; Publication Number:98052573 Click to see the data
IPC:
A61K 31/56
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
56
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
Applicants: GALENICA PHARMACEUTICALS, INC.
Inventors: DANTE J. MARCIANI
Agents: BERNARDO GOMEZ VEGA
Priority Data: 60/047,129 20.05.1997 US
60/080,389 02.04.1998 US
Title: (EN) TRITERPENE SAPONIN ANALOGS HAVING ADJUVANT AND IMMUNOSTIMULATORY ACTIVITY
(ES) ANALOGOS DE SAPONINA DE TRITERPENO QUE TIENEN ACTIVIDAD ADYUVANTE E INMUNOESTIMULADORA
Abstract:
(EN) The present invention is directed to novel chemical compounds in which a lipophilic moiety such as a lipid, fatty acid, polyethylene glycol or terpene is covalently attached to a non-acylated or desacylated triterpene saponin via a carboxyl group present on the 3-O-glucuronic acid of the triterpene saponin. The attachment of a lipophile moiety to the 3-O-glucuronic acid of a saponin such as Quillaja desacylsaponin, lucyoside P, or saponin from Gypsophila, Saponaria and Acanthophyllum enhances their adjuvant effects on humoral and cell mediated immunity. Additionally, the attachment of a lipophile moiety to the 3-O-glucuronic acid residue of non- or des-acylsaponin yields a saponin analog that is easier to purify, less toxic, chemically more stable, and possesses equal or better adjuvant properties than the original saponin.
(ES) La presente invención se dirige a nuevos compuestos químicos en los cuales, la porción lipofílica tal como un lípido,ácido graso, polietilenglicol o terpeno estácovalentemente unida a una saponina triterpeno no acilada o desacilada vía un grupo carboxilo presente en elácido 3-0-glucurónico de la saponina triterpeno. La unión de la porción lipófila alácido 3-0-glucurónico de una saponina tal como desacilsaponina Quillaja, luciosido P, o una saponina a partir de Gypsophi1a, Sponaria y Acanthophyllum incremento sus efectos adyuvantes en la inmunidad mediada por la célula y el humoral. De manera adicional, la unión de una porción lipofila al residuo delácido 3-0-glucurónico de una no o desacilsaponina, proporcionando un análogo que es más fácil de purificar, menos tóxico, químicamente más estable, y posee igual o mejores propiedades adyuvantes que la saponina original.
Also published as:
KR1020010012802SG68878IL132886EP0996451JP2002504099 CA2290646
NZ500779AU1998075818DK0996451WO/1998/052573