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1.发明公开DERIVES DE STREPTOGRAMINES, LEUR PREPARATION ET LES COMPOSITIONS QUI LES CONTIENNENT 失效STREPTOGRAMINDERIVATE，生产和含筹备工作
公开(公告)号：EP0989994A1
公开(公告)日：2000-04-05
申请号：EP98940328.2
申请日：1998-07-24
发明人： COMMERCON, Alain , BOUCHARD, Hervé , RIBEILL, Yves , BACQUES, Eric , RONAN, Baptiste , BARRIERE, Jean-Claude , PUCHAULT, Gérard , TERRIER, Corinne
CPC分类号： C07K5/06182 , A61K38/00
摘要： The invention concerns derivatives of group A of streptogramines of general formula (I) in which R1 is a -NR'R'' radical in which R' is a hydrogen atom or a methyl radical, and R'' is a hydrogen atom, an alkyl, cycloalkyl, allyl, propynyl, benzyl radical or -OR''', R''' being a hydrogen atom, an alkyl, cycloalkyl, allyl, propynyl or benzyl radical, or -NR3R4, R3 and R4 representing a methyl radical, or forming together with the nitrogen atom to which they are bound a saturated or unsaturated heterocyclic compound with 5 or 6 chains, further capable of containing another heteroatom selected among nitrogen, oxygen or sulphur; R2 is a hydrogen atom or a methyl or ethyl radical, and the bond --- represents a single or double bond, and in which, except if it is specified, the alkyl radicals are linear or branched and contain 1 to 6 carbon atoms, the cycloalkyl radicals contain 3 to 4 carbon atoms, and the chain $(1,3)$ in position 16 means: when R'' is other than -OR''' or -NR3R4, the epimer R or the mixture of epimers R and S in which the epimer R constitutes the major part, and when R'' is -OR''' or -NR3R4, the epimers R and S and their mixtures and their salts. Said novel derivatives are particularly useful as antimicrobial agents, optionally combined with components of group B of streptogramines.
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2.发明授权
公开(公告)号：EP0788492B1
公开(公告)日：1999-03-31
申请号：EP95935998.5
申请日：1995-10-23
发明人： BOUCHARD, Hervé , BOURZAT, Jean-Dominique , COMMER ON, Alain , TERRIER, Corinne , ZUCCO, Martine
IPC分类号： C07D305/14 , A61K31/335
CPC分类号： C07D305/14
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3.发明公开
公开(公告)号：EP0788492A1
公开(公告)日：1997-08-13
申请号：EP95935998.0
申请日：1995-10-23
发明人： BOUCHARD, Hervé , BOURZAT, Jean-Dominique , COMMER ON, Alain , TERRIER, Corinne , ZUCCO, Martine
CPC分类号： C07D305/14
摘要： Novel taxoids of general formulas (I) and (II), preparation thereof, and pharmaceutical compositions containing same. In general formula (I), Ra is hydrogen, hydroxy, alkoxy, acyloxy or alkoxyacetoxy and Rb is hydrogen, or Ra and Rb, taken together with the carbon atom to which they are attached, form a ketone function; Z is a hydrogen atom or a radical of general formula (II), wherein R1 is an optionally substituted benzoyl, thenoyl or furoyl radical or a radical R2-O-CO- where R2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical; R3 is an aromatic heterocyclic, alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or naphthyl radical; R4 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, aryl or heterocyclyl radical; and R5 is an optionally substituted cycloalkenyl, alkyl, alkenyl, alkynyl or cycloalkyl radical. The novel products of general formula (I), wherein Z is a radical of general formula (II), have remarkable antitumoral and antineoplastic properties.
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4.发明公开
公开(公告)号：EP0764156A1
公开(公告)日：1997-03-26
申请号：EP95922572.0
申请日：1995-06-07
发明人： BOUCHARD, Hervé , BOURZAT, Jean-Dominique , COMMER ON, Alain , TERRIER, Corinne , ZUCCO, Martine
CPC分类号： C07D407/12 , C07D305/14 , C07D409/12 , C07D417/12
摘要： New taxoids having general formula (I), (II), preparation thereof and pharmaceutical compositions containing them. In general formula (I), Ra is hydrogen, hydroxy, alkoxy, acyloxy, alkoxyacetoxy and Rb is hydrogen or Ra and Rb form together with the carbon atom to which they are linked a ketone function; Z is a hydrogen atom or a radical having general formula (II) wherein R1 is an optionally substituted benzoyl radical, thenoyl or furoyl or a radical R2-O-CO- wherein R2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical; R3 is an alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, naphtyl or heterocyclic aromatic radical, and R4 and R5, which are the same or different, represent an alkyl, alkenyl, alkynyl, cycoalkyl, cycloalkenyl, bicycloalkyl, aryl, or heterocyclyl radical, R5 not representing a methyl radical. The new products having general formula (I) wherein Z is a radical of general formula (II) have remarkable antitumoral and antileukaemic properties.
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5.发明公开
公开(公告)号：EP0764154A1
公开(公告)日：1997-03-26
申请号：EP95922569.0
申请日：1995-06-07
发明人： BOUCHARD, Hervé , BOURZAT, Jean-Dominique , COMMERCON, Alain , TERRIER, Corinne , ZUCCO, Martine
CPC分类号： C07D305/14
摘要： New taxoids having general formula (I), (II) preparation thereof and pharmaceutical compositions containing them. In general formula (I): Ra is hydrogen, hydroxy, alkoxy, acyloxy, alkoxyacetoxy, and Rb is hydrogen or Ra and Rb form together with the carbon atom to which they are linked a ketone function, Z is a hydrogen atom or a radical having general formula (II) wherein R1 is an optionally substituted benzoyl radical, a thenyl or furoyl radical or a radical R2-O-CO- wherein R2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical; R3 is an alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, naphtyl or heterocyclic aromatic radical, and R4 and R5, similar or different, represent an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, aryl or heterocyclyl radical, with the condition that R5 does not represent a methyl radical. The new products having general formula (I) wherein Z is a radical having general formula (II) have remarkable antitumoral and antileukaemic properties.
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