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1. (WO1998052573) TRITERPENE SAPONIN ANALOGS HAVING ADJUVANT AND IMMUNOSTIMULATORY ACTIVITY
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1998/052573 International Application No.: PCT/US1998/010280
Publication Date: 26.11.1998 International Filing Date: 20.05.1998
Chapter 2 Demand Filed: 18.12.1998
IPC:
A61K 39/39 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39
Medicinal preparations containing antigens or antibodies
39
characterised by the immunostimulating additives, e.g. chemical adjuvants
Applicants:
GALENICA PHARMACEUTICALS, INC. [US/US]; Suite 310 30 West Patrick Street Frederick, MD 21701, US (AllExceptUS)
MARCIANI, Dante, J. [US/US]; US (UsOnly)
Inventors:
MARCIANI, Dante, J.; US
Agent:
FOX, Samuel, L. ; Sterne, Kessler, Goldstein & Fox P.L.L.C. Suite 600 1100 New York Avenue, N.W. Washington, DC 20005-3934, US
Priority Data:
60/047,12920.05.1997US
60/080,38902.04.1998US
Title (EN) TRITERPENE SAPONIN ANALOGS HAVING ADJUVANT AND IMMUNOSTIMULATORY ACTIVITY
(FR) ANALOGUES DE LA SAPONINE TRITERPENIQUE A ACTIVITE D'ADJUVANT ET IMMUNOSTIMULATOIRE
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-$i(O)-glucuronic acid of the triterpene saponin. The attachment of a lipophile moiety to the 3-$i(O)-glucuronic acid of a saponin such as $i(Quillaja) desacylsaponin, lucyoside P, or saponin from $i(Gypsophila), $i(Saponaria) and $i(Acanthophyllum) enhances their adjuvant effects on humoral and cell mediated immunity. Additionally, the attachment of a lipophile moiety to the 3-$i(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.
(FR) L'invention porte sur de nouveaux composés chimiques dans lesquels un fragment lipophile, tel qu'un lipide, un acide gras, du polyéthylène glycol ou du terpène, est lié par covalence à de la saponine triterpénique non acylée ou désacylée par l'intermédiaire d'un groupe carbonyle présent sur l'acide 3-$i(O)-glucuronique de la saponine triterpénique. La fixation d'un fragment lipophile à l'acide 3-$i(O)-glucuronique d'une saponine, telle que la $i(Quillaja) dés-acylsaponine, la lucyoside P, ou la saponine de la $i(Gypsophila), de la $i(Saponaria) et de $i(l'Acanthophyllum), renforce leurs effets d'adjuvants sur l'immunité induite par les humeurs et les cellules. De plus, la fixation d'un fragment lipophile au résidu acide 3-$i(O)-glucuronique de la non ou dés-acylsaponine donne un analogue de la saponine plus facile à purifier, moins toxique, plus stable chimiquement, et possédant des propriétés d'adjuvant égales ou supérieures à celles de la saponine originale.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, GH, GM, GW, HU, ID, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
MXPA/a/1999/010675KR1020010012802SG68878IL132886EP0996451JP2002504099
CA2290646NZ500779AU1998075818DK0996451