COMPOSES EN SERIE TRITERPENES TETRACYCLIQUES, LEURS PROCEDES DE PREPARATION, LEURS APPLICATIONS COMME MEDICAMENTS ET LES COMPOSES PHARMACEUTIQUES LES RENFERMANT

COMPOSES EN SERIE TRITERPENES TETRACYCLIQUES, LEURS PROCEDES DE PREPARATION, LEURS APPLICATIONS COMME MEDICAMENTS ET LES COMPOSES PHARMACEUTIQUES LES RENFERMANT

Triterpenic alkaloids (I) and their addition salts, isomers, enantiomers and/or diastereomers are new. Triterpenic alkaloids of formula (I) and their addition salts, isomers, enantiomers and/or diastereomers are new. R 1-CH 2X 1R 7, -CH=NR 5or -CH=O; X 1-X 3O, NH or S; R 7, R 8H, 1-10C alkyl, 1-10C...

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Hauptverfasser: HERLEM DENYSE, SAUVAITRE THIBAULT, LALLEMAND JEAN YVES, GUENARD DANIEL, GUILLOU CATHERINE, MOLGO JORDI, KHUONG HUU FRANCOISE
Format: Patent
Sprache:fre
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CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
STEROIDS
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Zusammenfassung:Triterpenic alkaloids (I) and their addition salts, isomers, enantiomers and/or diastereomers are new. Triterpenic alkaloids of formula (I) and their addition salts, isomers, enantiomers and/or diastereomers are new. R 1-CH 2X 1R 7, -CH=NR 5or -CH=O; X 1-X 3O, NH or S; R 7, R 8H, 1-10C alkyl, 1-10C alkyl-phenyl, 1-10C alkyl-carbonyl or SO 2R 9; R 91-10C alkyl or 1-10C alkyl-phenyl; either R ,R 3H or -C(=X)-R 10; or R 10H, 1-10C alkyl, (1-10C alkyl)phenyl, 3-10C cycloalkyl; R 4H, 10C alkyl or -X 3-R 12; R 12H (preferred), 1-10C alkylcarbonyl, 1-10C alkyl-phenyl or 1-10C alkyl-sulfonyl; R 5N-oxide-N +>OCH 3R 13or NCH 3R 13; R 13H, 3-10C cycloalkyl, 1-10C alkyl, phenyl or phthalimide (preferably CH 3); R 6=O or -OR 14; and R 14H, 1-10C alkyl, 1-10C alkylcarbonyl, 1-10C alkyl-phenyl or 1-10C alkyl-sulfonyl. Provided that: when X 1is S, R 7is not SO 2R 9; at least one of R 2and R 3is H. Provided that: when R 2is absent, then R 1is -CH 2X 1R 7, and NR 7and X 1R 7together forms -N=C(R 11)-X 1- (where R 11is H, 1= 1-C alkyl, (1-C alkyl)phenyl) or 3-10C cycloalkyl); when R 2= H, then R 1is -CH 2X 1R 7, and NR 7and X 1R 7together forms -N-CH(R 11)-X 1-. Provided that (I) is not: N-(16-Hydroxy-4-hydroxymethyl-17-isopropyl-4,13,14-trimethyl-11-oxo-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-3-yl)-isobutyramide; N-[3-(1-dimethylamino-ethyl)-2-hydroxy-10-hydroxymethyl-3a,10,12b-trimethyl-5-oxo-1,2,3,3a,4,5,5a,6,8,9,10,10a,11,12,12a,12b-hexadecahydro-benzo[4,5]cyclohepta[1,2-e]inden-9-yl]-isobutyramide; N-[17-(1-dimethylamino-ethyl)-16-hydroxy-4-hydroxymethyl-4,13,14-trimethyl-11-oxo-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-3-yl]-benzamide; acetic acid 4-acetoxymethyl-17-(1-dimethylamino-ethyl)-3-isobutyrylamino-4,13,14-trimethyl-11-oxo-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-16-yl ester; 3-(1-dimethylamino-ethyl)-2-hydroxy-10-isopropyl-3a,12a,14b-trimethyl-2,3,3a,5a,6,8,8a,12,12a,12b,13,14,14a,14b-tetradecahydro-1H,4H-11-oxa-9-aza-indeno[5',4':4,5]cyclohepta[1,2-a]naphthalen-5-one; acetic acid 3-(1-dimethylamino-ethyl)-10-isopropyl-3a,12a,14b-trimethyl-5-oxo-2,3,3a,4,5,5a,6,8,8a,12,12a,12b,13,14,14a,14b-hexadecahydro-1H-11-oxa-9-aza-indeno[5',4':4,5]cyclohepta[1,2-a]naphthalen-2-yl ester, 3-(1-dimethylamino-ethyl)-2-hydroxy-10-isopropyl-3a,12a,14b-trimethyl-2,3,3a,5a,6,8,8a,9,10,12,12a,12b,13,14,14a,14b-hexadecahydro-1H,4H-11-oxa-9-aza-indeno[5',4':4,5]cyclohepta[1,2-a]naphthalen-5-one; N-[3-(1-dimethylamino-ethyl)-2-hydroxy-10