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1. 发明授权

US07396934B2 Process for preparing 3-fluoroquinolines 失效
标题翻译：制备3-氟喹啉的方法
公开(公告)号：US07396934B2
公开(公告)日：2008-07-08
申请号：US10985533
申请日：2004-11-10
申请人： Youssef El-Ahmad , Jean-Pierre Leconte , Joël Malpart , Serge Mignani , Stéphane Mutti , Michel Tabart
发明人： Youssef El-Ahmad , Jean-Pierre Leconte , Joël Malpart , Serge Mignani , Stéphane Mutti , Michel Tabart
IPC分类号： C07D215/38 , C07D215/18
CPC分类号： C07D215/38 , C07D215/18 , Y02P20/55
摘要： The invention relates to a novel preparation of 3-fluoroquinolines of formula (I) in which R1, R2, R3 and R4 represent: a) a fluorine; b) an alkyl optionally substituted with one to three fluorines, with OR5 in which R5 is an alkyl, a hydrogen or a hydroxyl-protecting group, or with NR′R″ in which R′ and R″ represent an alkyl, a hydrogen or an amino-protecting group; c) OR6 in which R6 represents a hydrogen, a phenol-protecting group or an alkyl, optionally substituted with a fluorine, with OR5 or with NR′R″ as defined above; d) NR′1R″1 in which R′1 and R″1 have the values of R′ et R″ or represent an alkyl substituted with a fluorine, with OR5 or NR′R″ as defined above; e) CO2Ra, in which Ra represents hydrogen, alkyl or a carboxyl-protecting group, and also novel intermediate compounds. The quinolines of formula (I) are intermediates useful in the preparation of compounds having antibacterial activity, described in particular in applications WO 02/40474 or WO 02/72572.
摘要翻译：本发明涉及式（I）的3-氟喹啉的新型制备方法，其中R 1，R 2，R 3和R 3，代表：a）氟; b）任选被一至三个氟取代的烷基，其中R 5是烷基，氢或羟基保护基或NR' 其中R'和R“表示烷基，氢或氨基保护基的”R“ c）OR 6其中R 6表示氢，苯酚保护基或任选被氟取代的烷基，OR 5或N >或如上定义的NR'R“ d）NR'1 R“1其中R'1和R”1 <1的数值为或者代表被氟取代的烷基，其具有如上定义的OR 5或NR'R“; e）其中R aa代表氢，烷基或羧基保护基，以及新的中间体化合物的CO 2 CO 2。式（I）的喹啉是可用于制备具有抗菌活性的化合物的中间体，特别在申请WO 02/40474或WO 02/72572中有所描述。

2. 发明申请

US20050182259A1 Novel process for preparing 3-fluoroquinolines 失效
标题翻译：制备3-氟喹啉的新方法
公开(公告)号：US20050182259A1
公开(公告)日：2005-08-18
申请号：US10985533
申请日：2004-11-10
申请人： Youssef El-Ahmad , Jean-Pierre Leconte , Joel Malpart , Serge Mignani , Stephane Mutti , Michel Tabart
发明人： Youssef El-Ahmad , Jean-Pierre Leconte , Joel Malpart , Serge Mignani , Stephane Mutti , Michel Tabart
IPC分类号： C07D215/18 , C07D215/38 , C07D215/12
CPC分类号： C07D215/38 , C07D215/18 , Y02P20/55
摘要： The invention relates to a novel preparation of 3-fluoroquinolines of formula (I) in which R1, R2, R3 and R4 represent: a) a fluorine; b) an alkyl optionally substituted with one to three fluorines, with OR5 in which R5 is an alkyl, a hydrogen or a hydroxyl-protecting group, or with NR′R″ in which R′ and R″ represent an alkyl, a hydrogen or an amino-protecting group; c) OR6 in which R6 represents a hydrogen, a phenol-protecting group or an alkyl, optionally substituted with a fluorine, with OR5 or with NR′R″ as defined above; d) NR′1R″1 in which R′1 and R″1 have the values of R′ et R″ or represent an alkyl substituted with a fluorine, with OR5 or NR′R″ as defined above; e) CO2Ra, in which Ra represents hydrogen, alkyl or a carboxyl-protecting group, and also novel intermediate compounds. The quinolines of formula (I) are intermediates useful in the preparation of compounds having antibacterial activity, described in particular in applications WO 02/40474 or WO 02/72572.
摘要翻译：本发明涉及式（I）的3-氟喹啉的新型制备方法，其中R 1，R 2，R 3和R 3，代表：a）氟; b）任选被一至三个氟取代的烷基，其中R 5是烷基，氢或羟基保护基或NR' 其中R'和R“表示烷基，氢或氨基保护基的”R“ c）OR 6其中R 6表示氢，苯酚保护基或任选被氟取代的烷基，OR 5或N >或如上定义的NR'R“ d）NR'1 R“1其中R'1和R”1 <1的数值为或者代表被氟取代的烷基，其具有如上定义的OR 5或NR'R“; e）其中R aa代表氢，烷基或羧基保护基，以及新的中间体化合物的CO 2 CO 2。式（I）的喹啉是可用于制备具有抗菌活性的化合物的中间体，特别在申请WO 02/40474或WO 02/72572中有所描述。

3. 发明授权

US5965527A Cyclosporin compounds, their preparation and the pharmaceutical compositions which contain them 失效
标题翻译：环孢菌素化合物，它们的制备和含有它们的药物组合物
公开(公告)号：US5965527A
公开(公告)日：1999-10-12
申请号：US996699
申请日：1997-12-23
申请人： Jean-Claude Barriere , Georges Bashiardes , Jean-Christophe Carry , Michel Evers , Bruno Filoche , Jean-Pierre Leconte , Serge Mignani
发明人： Jean-Claude Barriere , Georges Bashiardes , Jean-Christophe Carry , Michel Evers , Bruno Filoche , Jean-Pierre Leconte , Serge Mignani
IPC分类号： A61K38/00 , A61P31/14 , C07K7/64 , A61K37/02 , C07K5/12
CPC分类号： C07K7/645 , A61K38/00
摘要： A cyclosporin compound of the formula (I): ##STR1## wherein Alk and R are as defined herein, or a pharmaceutically acceptable salt thereof, which derivatives are is useful in the treatment and/or prophylaxis of retrovirus infections.
摘要翻译：式（I）的环孢菌素化合物：其中Alk和R如本文所定义，或其药学上可接受的盐，该衍生物可用于治疗和/或预防逆转录病毒感染。

4. 发明授权

US5670658A Process for preparing 7-trialkylsilyl baccatin III 失效
标题翻译：制备7-三烷基甲硅烷基浆果赤霉素III的方法
公开(公告)号：US5670658A
公开(公告)日：1997-09-23
申请号：US722103
申请日：1996-10-03
申请人： Jean-Pierre Bastart , Jean-Pierre Leconte
发明人： Jean-Pierre Bastart , Jean-Pierre Leconte
IPC分类号： C07D305/14 , C07F7/18
CPC分类号： C07F7/1892 , C07F7/1856 , C07F7/188
摘要： The present invention relates to a novel process for the preparation of 7-trialkylsilylbaccatin III of general formula: ##STR1## in which the symbols R, which may be identical or different, represent alkyl radicals containing 1 to 4 carbon atoms which are optionally substituted with a phenyl radical, starting with 10-deacetylbaccatin III of formula: ##STR2## In the general formula (I), each of the symbols R preferably represents a straight or branched alkyl radical containing 1 to 4 carbon atoms. Even more particularly, each of the symbols R represents an ethyl radical.
摘要翻译： PCT No.PCT / FR95 / 00419 Sec。 371日期：1996年10月3日 102（e）日期1996年10月3日PCT提交1995年4月3日PCT公布。 WO95 / 26967 PCT公开号日期1995年10月12日本发明涉及一种制备通式如下的7-三烷基甲硅烷基浆果赤霉素Ⅲ的新方法：其中符号R可以相同或不同，代表含有1至（II）的10-脱乙酰基浆果赤霉素III起始于通式（I）中，每个符号R优选表示含有1个直链或支链烷基的直链或支链烷基，至4个碳原子。更具体地，每个符号R表示乙基。

5. 发明授权

US07166594B2 Streptogramin derivatives, their preparation and compositions containing them 有权
标题翻译：链球菌素衍生物，它们的制备和含有它们的组合物
公开(公告)号：US07166594B2
公开(公告)日：2007-01-23
申请号：US10310773
申请日：2002-12-06
申请人： Daniel Achard , Eric Bacque , Jean-Claude Barriere , Jean Bouquerel , Pascal Desmazeau , Serge Grisoni , Jean-Pierre Leconte , Yves Ribeill , Baptiste Ronan
发明人： Daniel Achard , Eric Bacque , Jean-Claude Barriere , Jean Bouquerel , Pascal Desmazeau , Serge Grisoni , Jean-Pierre Leconte , Yves Ribeill , Baptiste Ronan
IPC分类号： A61K31/535 , A61K31/655 , A61K31/42
CPC分类号： A61K38/12 , A61K38/15 , C07K5/06182 , A61K38/08 , A61K2300/00
摘要： Group A streptogramin derivatives of general formula (I) in which: R1 represents a halogen atom or an azido or thiocyanato radical, R2 represents a hydrogen atom or a methyl or ethyl radical, R3 represents a hydrogen atom, or the residue of an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclylaliphatic ester which may be substituted, and the bond --- represents a single bond (stereochemistry 27R) or a double bond, as well as its salts when they exist
摘要翻译： A组通式（I）的链霉素衍生物，其中：R 1表示卤素原子或叠氮基或硫氰酸根基团，R 2表示氢原子或甲基或乙基，R 3表示氢原子，或可以被取代的脂族，脂环族，芳族，芳脂族，杂环或杂环脂族酯的残基，并且键 ---表示单键（立体化学27R）或双键，以及其存在时的盐

6. 发明授权

US5750738A Process for the preparation of 7-hydroxytaxanes 失效
标题翻译：制备7-羟基塔沙的方法
公开(公告)号：US5750738A
公开(公告)日：1998-05-12
申请号：US722106
申请日：1996-10-03
申请人： Jean-Pierre Bastart , Jean-Dominique Boursat , Alain Commercon , Jean-Pierre Leconte
发明人： Jean-Pierre Bastart , Jean-Dominique Boursat , Alain Commercon , Jean-Pierre Leconte
IPC分类号： C07D305/14 , C07D413/12 , C07F7/18
CPC分类号： C07D413/12 , C07D305/14 , Y02P20/55
摘要： This invention relates to a process for the preparation of 7-hydroxy taxanes of general formula (I) from 7-trialkylsilyl taxanes of general formula (II), wherein R.sub.1 is hydrogen, alkoxy, acyloxy, or alkoxyacetoxy, and Z is a hydrogen atom or a radical of general formula (III), wherein R.sub.2 is an optionally substituted benzyl radical or an R'.sub.2 --O--CO-- radical wherein R'.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical, R.sub.3 is an aromatic alkyl, alkenyl, alkynyl, cycloalyl, phenyl, naphthyl or heterocyclyl radical and either R.sub.4 is a hydrogen atom and R.sub.5 is a hydroxyl function protecting group, or R.sub.4 and R.sub.5 together form a saturated 5- or 6-membered heterocylic ring. In general formula (II), each R, which are the same or different, is an alkyl radical optionally substituted by a phenyl radical. ##STR1##
摘要翻译： PCT No.PCT / FR95 / 00420 Sec。 371日期：1996年10月3日 102（e）日期1996年10月3日PCT提交1995年4月3日PCT公布。 WO95 / 26961 PCT公开号日期：1995年10月12日本发明涉及由通式（II）的7-三烷基甲硅烷基紫杉烷类制备通式（I）的7-羟基紫杉烷的方法，其中R1为氢，烷氧基，酰氧基或烷氧基乙酰氧基， Z是氢原子或通式（III）的基团，其中R2是任选取代的苄基或R'2-O-CO-基，其中R'2是烷基，烯基，炔基，环烷基，环烯基，二环烷基，任选取代的苯基或杂环基，R 3是芳族烷基，烯基，炔基，环烷基，苯基，萘基或杂环基，并且R 4是氢原子，R 5是羟基官能保护基，或者R 4和R 5一起形成饱和的5-或6-元杂环。在通式（II）中，相同或不同的每个R是任选被苯基取代的烷基。（一）图像（二）<图像>（三）

7. 发明授权

US06569854B1 Streptogramin derivatives, their preparation and compositions containing them 有权
标题翻译：链球菌素衍生物，它们的制备和含有它们的组合物
公开(公告)号：US06569854B1
公开(公告)日：2003-05-27
申请号：US09609717
申请日：2000-06-30
申请人： Daniel Achard , Eric Bacque , Jean-Claude Barriere , Jean Bouquerel , Pascal Desmazeau , Serge Grisoni , Jean-Pierre Leconte , Yves Ribeill , Baptiste Ronan
发明人： Daniel Achard , Eric Bacque , Jean-Claude Barriere , Jean Bouquerel , Pascal Desmazeau , Serge Grisoni , Jean-Pierre Leconte , Yves Ribeill , Baptiste Ronan
IPC分类号： A61K3805
CPC分类号： A61K38/12 , A61K38/15 , C07K5/06182 , A61K38/08 , A61K2300/00
摘要： Group A streptogramin derivatives of general formula (I) in which: R1 represents a halogen atom or an azido or thiocyanato radical, R2 represents a hydrogen atom or a methyl or ethyl radical, R3 represents a hydrogen atom, or the residue of an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclylaliphatic ester which may be substituted, and the bond - - - represents a single bond (stereochemistry 27R) or a double bond, as well as its salts when they exist.
摘要翻译： A组通式（I）的链霉素衍生物，其中：R1表示卤素原子或叠氮基或硫氰酸根基，R2表示氢原子或甲基或乙基，R3表示氢原子，或脂族，脂环族，芳香族，芳脂族，杂环或杂环脂族酯，并且键 - - 表示单键（立体化学27R）或双键，以及它们存在时的盐。

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