WO1998032443A1 - Ultramicro-emulsions de concentres spontanement dispersibles renfermant des esters de triterpenes pentacycliques a activite antitumorale, antivirale et antiparasitaire - Google Patents

Ultramicro-emulsions de concentres spontanement dispersibles renfermant des esters de triterpenes pentacycliques a activite antitumorale, antivirale et antiparasitaire Download PDF

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Publication number
WO1998032443A1
WO1998032443A1 PCT/CH1997/000023 CH9700023W WO9832443A1 WO 1998032443 A1 WO1998032443 A1 WO 1998032443A1 CH 9700023 W CH9700023 W CH 9700023W WO 9832443 A1 WO9832443 A1 WO 9832443A1
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WO
WIPO (PCT)
Prior art keywords
weight
esters
acid
formulas
surfactant
Prior art date
Application number
PCT/CH1997/000023
Other languages
German (de)
English (en)
Inventor
Carl Eugster
Conrad Hans Eugster
Original Assignee
Marigen S.A.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Marigen S.A. filed Critical Marigen S.A.
Priority to PCT/CH1997/000023 priority Critical patent/WO1998032443A1/fr
Priority to EP97900535A priority patent/EP0902685A1/fr
Publication of WO1998032443A1 publication Critical patent/WO1998032443A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
    • A61K31/231—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
    • A61K31/232—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers

Abstract

L'invention concerne des concentrés spontanément dispersibles renfermant des esters sélectionnés de composés triterpéniques pentacycliques à activité antitumorale, antivirale et antiparasitaire, des ultramicro-émulsions aqueuses de tels concentrés, un procédé de fabrication de ces esters et leur traitement, ainsi que leur utilisation comme agents pour la production d'une préparation systémique pharmaceutique efficace contre les tumeurs, eczémas, psoriasis, infections virales et parasitaires, pour la prophylaxie à long terme des tumeurs et pour l'absorption renforcée des activateurs, modulateurs et régulateurs exogènes.
PCT/CH1997/000023 1997-01-24 1997-01-24 Ultramicro-emulsions de concentres spontanement dispersibles renfermant des esters de triterpenes pentacycliques a activite antitumorale, antivirale et antiparasitaire WO1998032443A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
PCT/CH1997/000023 WO1998032443A1 (fr) 1997-01-24 1997-01-24 Ultramicro-emulsions de concentres spontanement dispersibles renfermant des esters de triterpenes pentacycliques a activite antitumorale, antivirale et antiparasitaire
EP97900535A EP0902685A1 (fr) 1997-01-24 1997-01-24 Ultramicro-emulsions de concentres spontanement dispersibles renfermant des esters de triterpenes pentacycliques a activite antitumorale, antivirale et antiparasitaire

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CH1997/000023 WO1998032443A1 (fr) 1997-01-24 1997-01-24 Ultramicro-emulsions de concentres spontanement dispersibles renfermant des esters de triterpenes pentacycliques a activite antitumorale, antivirale et antiparasitaire

Publications (1)

Publication Number Publication Date
WO1998032443A1 true WO1998032443A1 (fr) 1998-07-30

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CH1997/000023 WO1998032443A1 (fr) 1997-01-24 1997-01-24 Ultramicro-emulsions de concentres spontanement dispersibles renfermant des esters de triterpenes pentacycliques a activite antitumorale, antivirale et antiparasitaire

Country Status (2)

Country Link
EP (1) EP0902685A1 (fr)
WO (1) WO1998032443A1 (fr)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000041676A1 (fr) * 1999-01-12 2000-07-20 Merck Sharp & Dohme Limited Systeme auto-emulsionnant spheronise destine a des agents hydrophobes et sensibles a l'eau
GB2362649A (en) * 2000-05-25 2001-11-28 Univerzita Palackeho V Olomouc Triterpenoid derivatives
WO2001090096A2 (fr) * 2000-05-23 2001-11-29 Univerzita Palackeho V Olomouci Derives triterpenoides
WO2002026762A1 (fr) * 2000-09-29 2002-04-04 Regents Of The University Of Minnesota Triterpènes dotés d'une activité antibactérienne
WO2002026761A1 (fr) * 2000-09-29 2002-04-04 Regents Of The University Of Minnesota Triterpenes ayant une activite fongicide dirigee contre les levures
WO2002055087A1 (fr) * 2001-01-12 2002-07-18 Bsp Pharma Dihydro-triterpenes dans le traitement d'infections virales, de maladies cardiovasculaires, d'inflammations, d'hypersensibilite ou de douleurs
EP1266658A2 (fr) * 1997-05-16 2002-12-18 The Board Of Trustees Of The University Of Illinois Utilisation de dérivés de l'acide bétulinique pour le traitement et la prévention du mélanome
WO2006097337A2 (fr) * 2005-03-18 2006-09-21 Onepharm Gmbh Inhibiteurs de la 11$g(b)-hydroxysteroide deshydrogenases
US7144875B2 (en) 2000-09-29 2006-12-05 Regents Of The University Of Minnesota Methods of treating fungal infections using lupeol
EP1878445A1 (fr) * 2005-04-19 2008-01-16 Shanghai Tianbo Biotechnology Co., Ltd. Procede, formulation et utilisation de medicaments ou de nutriments avec une absorption orale amelioree
WO2009155070A2 (fr) * 2008-05-30 2009-12-23 Novelix Pharmaceuticals, Inc. Compositions et procédés pour le traitement d’inflammation et de lésions hyperkératotiques
US11826374B2 (en) 2018-01-04 2023-11-28 Amryt Research Limited Betulin-containing birch bark extracts and their formulation

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0243248A1 (fr) * 1986-04-18 1987-10-28 Laboratoires Pharmaceutiques Roche-Posay Compositions pour le traitement de la calvitie et des alopécies
WO1991001139A1 (fr) * 1989-07-21 1991-02-07 Marigen S.A. Sterols, leurs esters d'acides gras et leur glucosides; procede pour leur fabrication; agents spontanement dispersibles avec ces composes, ainsi que leur utilisation pour le traitement des tumeurs
JPH0426650A (ja) * 1990-05-17 1992-01-29 Kuraray Co Ltd オレアノール酸の製造法
WO1992012989A1 (fr) * 1991-01-28 1992-08-06 Marigen S.A. Nouveaux esters de sterol et composes de phosphore de sterol
WO1992021670A1 (fr) * 1991-06-04 1992-12-10 Marigen S.A., Riehen Nouveaux esters et phospholipides biotensioactifs avec des composes de vitamines d et de vitamine e; leur preparation et leur traitement pour la formation de concentres susceptibles de se disperser spontanement, ainsi que leur utilisation dans la therapie de tumeurs
WO1995004526A1 (fr) * 1993-08-09 1995-02-16 Glycomed Incorporated Derives triterpenoides de lupane
JPH0748260A (ja) * 1993-08-04 1995-02-21 Japan Energy Corp 血球増加剤
WO1995035103A1 (fr) * 1994-06-20 1995-12-28 Kurt Berg Composition pharmaceutique pour prevenir et/ou traiter des infections virales, ainsi qu'eventuellement des inflammations, et utilisation de cette composition
CN1129573A (zh) * 1995-02-22 1996-08-28 胡幼圃 抗病毒药阿昔洛韦经皮吸收制剂
WO1996039033A1 (fr) * 1995-06-05 1996-12-12 The University Of North Carolina At Chapel Hill Derives d'acide betulinique et leurs utilisations

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0243248A1 (fr) * 1986-04-18 1987-10-28 Laboratoires Pharmaceutiques Roche-Posay Compositions pour le traitement de la calvitie et des alopécies
WO1991001139A1 (fr) * 1989-07-21 1991-02-07 Marigen S.A. Sterols, leurs esters d'acides gras et leur glucosides; procede pour leur fabrication; agents spontanement dispersibles avec ces composes, ainsi que leur utilisation pour le traitement des tumeurs
JPH0426650A (ja) * 1990-05-17 1992-01-29 Kuraray Co Ltd オレアノール酸の製造法
WO1992012989A1 (fr) * 1991-01-28 1992-08-06 Marigen S.A. Nouveaux esters de sterol et composes de phosphore de sterol
WO1992021670A1 (fr) * 1991-06-04 1992-12-10 Marigen S.A., Riehen Nouveaux esters et phospholipides biotensioactifs avec des composes de vitamines d et de vitamine e; leur preparation et leur traitement pour la formation de concentres susceptibles de se disperser spontanement, ainsi que leur utilisation dans la therapie de tumeurs
JPH0748260A (ja) * 1993-08-04 1995-02-21 Japan Energy Corp 血球増加剤
WO1995004526A1 (fr) * 1993-08-09 1995-02-16 Glycomed Incorporated Derives triterpenoides de lupane
WO1995035103A1 (fr) * 1994-06-20 1995-12-28 Kurt Berg Composition pharmaceutique pour prevenir et/ou traiter des infections virales, ainsi qu'eventuellement des inflammations, et utilisation de cette composition
CN1129573A (zh) * 1995-02-22 1996-08-28 胡幼圃 抗病毒药阿昔洛韦经皮吸收制剂
WO1996039033A1 (fr) * 1995-06-05 1996-12-12 The University Of North Carolina At Chapel Hill Derives d'acide betulinique et leurs utilisations

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
CHEMICAL ABSTRACTS, vol. 115, no. 23, 9 December 1991, Columbus, Ohio, US; abstract no. 256427s, page 894; column l; XP002053424 *
CHEMICAL ABSTRACTS, vol. 67, no. 11, 11 September 1967, Columbus, Ohio, US; abstract no. 54279z, page 5113; column r; XP002053423 *
DATABASE EPODOC EPO; 28 August 1996 (1996-08-28), HU YOUPU: "CN-A-1129573", XP002041152 *
G.A. TOLSTKOV ET AL, ZH. PRIKL. KHIM, vol. 40, no. 4, 1967, RUSSIA, pages 920 - 921 *
MAURYA S K ET AL: "CONTENT OF BETULIN AND BETULINIC ACID, ANTITUMOR AGENTS OF ZIZYPHUS SPECIES", FITOTERAPIA, vol. 60, no. 5, 1989, pages 468/469, XP000612857 *
SEJBAL ET AL, COLLECT. CZECH. CHEM. COMMUN., vol. 56, no. 8, 1991, TCHECKIEN, pages 1732 - 1743 *

Cited By (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1266658A3 (fr) * 1997-05-16 2004-05-26 The Board Of Trustees Of The University Of Illinois Utilisation de dérivés de l'acide bétulinique pour le traitement et la prévention du mélanome
EP1266658A2 (fr) * 1997-05-16 2002-12-18 The Board Of Trustees Of The University Of Illinois Utilisation de dérivés de l'acide bétulinique pour le traitement et la prévention du mélanome
US6630150B1 (en) 1999-01-12 2003-10-07 Merck Sharp & Dohme Limited Spheronized self-emulsifying system for hydrophobic and water-sensitive agents
WO2000041676A1 (fr) * 1999-01-12 2000-07-20 Merck Sharp & Dohme Limited Systeme auto-emulsionnant spheronise destine a des agents hydrophobes et sensibles a l'eau
AU769541B2 (en) * 1999-01-12 2004-01-29 Merck Sharp & Dohme Limited Spheronised self-emulsifying system for hydrophobic and water-sensitive agents
WO2001090096A2 (fr) * 2000-05-23 2001-11-29 Univerzita Palackeho V Olomouci Derives triterpenoides
WO2001090096A3 (fr) * 2000-05-23 2002-03-07 Univerzita Palackeho V Olomouc Derives triterpenoides
GB2362649A (en) * 2000-05-25 2001-11-28 Univerzita Palackeho V Olomouc Triterpenoid derivatives
WO2002026761A1 (fr) * 2000-09-29 2002-04-04 Regents Of The University Of Minnesota Triterpenes ayant une activite fongicide dirigee contre les levures
US7144875B2 (en) 2000-09-29 2006-12-05 Regents Of The University Of Minnesota Methods of treating fungal infections using lupeol
US6689767B2 (en) 2000-09-29 2004-02-10 Regents Of The University Of Minnesota Triterpenes having antibacterial activity
WO2002026762A1 (fr) * 2000-09-29 2002-04-04 Regents Of The University Of Minnesota Triterpènes dotés d'une activité antibactérienne
US6642217B2 (en) 2000-09-29 2003-11-04 Naturtek, Llc Triterpenes having human antifungal and antiyeast activity
WO2002055087A1 (fr) * 2001-01-12 2002-07-18 Bsp Pharma Dihydro-triterpenes dans le traitement d'infections virales, de maladies cardiovasculaires, d'inflammations, d'hypersensibilite ou de douleurs
WO2006097337A3 (fr) * 2005-03-18 2007-08-23 Bionetworks Gmbh Inhibiteurs de la 11$g(b)-hydroxysteroide deshydrogenases
WO2006097337A2 (fr) * 2005-03-18 2006-09-21 Onepharm Gmbh Inhibiteurs de la 11$g(b)-hydroxysteroide deshydrogenases
EP1878445A1 (fr) * 2005-04-19 2008-01-16 Shanghai Tianbo Biotechnology Co., Ltd. Procede, formulation et utilisation de medicaments ou de nutriments avec une absorption orale amelioree
EP1878445A4 (fr) * 2005-04-19 2008-06-25 Shanghai Tianbo Biotechnology Procede, formulation et utilisation de medicaments ou de nutriments avec une absorption orale amelioree
WO2009155070A2 (fr) * 2008-05-30 2009-12-23 Novelix Pharmaceuticals, Inc. Compositions et procédés pour le traitement d’inflammation et de lésions hyperkératotiques
WO2009155070A3 (fr) * 2008-05-30 2010-02-11 Novelix Pharmaceuticals, Inc. Compositions et procédés pour le traitement d’inflammation et de lésions hyperkératotiques
AU2009260485B2 (en) * 2008-05-30 2015-01-29 Novelix Pharmaceuticals, Inc. Compositions and methods for treatment of inflammation and hyperkeratotic lesions
US11826374B2 (en) 2018-01-04 2023-11-28 Amryt Research Limited Betulin-containing birch bark extracts and their formulation

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Publication number Publication date
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