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71. 发明授权

US5994299A 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：US5994299A
公开(公告)日：1999-11-30
申请号：US997612
申请日：1997-12-23
申请人： Jean-Claude Barriere , Georges Bashiardes , Jean-Christophe Carry , Michel Evers , Bruno Filoche , Serge Mignani
发明人： Jean-Claude Barriere , Georges Bashiardes , Jean-Christophe Carry , Michel Evers , Bruno Filoche , Serge Mignani
IPC分类号： A61K45/00 , A61K38/00 , A61P31/14 , A61P37/02 , A61P43/00 , C07K7/64 , C07K5/12
CPC分类号： C07K7/645 , A61K38/00
摘要： Cyclosporin compounds of formula (I): ##STR1## wherein Alk and R are as defined herein, or a pharmaceutically acceptable salt thereof, which derivatives are 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。

72. 发明授权

US5021420A Derivatives of (AZA)naphthalenesultam, their preparation and compositions containing them 失效
公开(公告)号：US5021420A
公开(公告)日：1991-06-04
申请号：US375934
申请日：1989-07-06
申请人： Marie-Iherese Comte , Claude Gueremy , Jean-Luc Malleron , Serge Mignani , Jean-Francois Peyronel , Alain Truchon
发明人： Marie-Iherese Comte , Claude Gueremy , Jean-Luc Malleron , Serge Mignani , Jean-Francois Peyronel , Alain Truchon
IPC分类号： A61K31/425 , A61K31/428 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61P9/00 , A61P11/00 , A61P25/00 , A61P43/00 , C07D275/06 , C07D417/00 , C07D417/06 , C07D417/14 , C07D513/06
CPC分类号： C07D275/06 , C07D417/06 , C07D417/14 , C07D513/06
摘要： This invention relates to a compound ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or an alkyl, hydroxy or alkoxy radical, (c) a 3-indolyl radical, (d) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (e) a 3-(5-hydroxyindolyl) radical.a 1-piperazinyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by an alkoxy, alkyl, hydroxy, nitro or amino radical or a halogen atom, (c) a 1,2-benzisothiazol-3-yl radical, (d) a 1,2-benzisoxazol-3-yl radical or (e) a 2-pyridyl radical.a piperidino radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or a hydroxy, alkyl or alkoxy radical, (c) two phenyl radicals, (d) a bis(4-fluorophenyl)methylene radical, (e) a 4-fluorobenzoyl radical, (f) a 2-oxo-1-benzimidazolinyl radical, (g) a 2-oxo-1-benzimidazolinyl radical substituted in the 3-position by an alkylcarbonyl or benzoyl radical, (b) a hydroxy radical and a phenyl radical optionally substituted with an alkyl, alkoxy or hydroxy radical or a halogen atom, (i) a 3-indolyl radical, (j) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (k) a 3-(5-hydroxyindolyl) radical.either:R.sub.2 and R.sub.3, which are identical, represent a hydrogen or halogen atom and R.sub.4 represents a hydrogen atom orR.sub.2 and R.sub.4 represent a hydrogen atom and R.sub.3 represents a halogen atom or an acetylamino radical orR.sub.2 and R.sub.3 represent a hydrogen atom and R.sub.4 represents a halogen atom and R.sub.5 represents a --CH.dbd. group.or R.sub.2, R.sub.3 and R.sub.4 represent a hydrogen atom and R.sub.5 represents a nitrogen atom.R.sub.6 represents an alkylene chain containing 2 to 4 carbon atoms or a propylene chain substituted in the 1- or 3-position by an alkyl radical or in the 2-position by an alkyl, alkoxy, hydroxy, dialkylamino, piperidino, morpholino or thiomorpholino radical,with the reservation that when R.sub.6 represents a propylene radical substituted in the 2-position by a dialkylamino, piperidino, morpholino or thiomorpholino radical, R.sub.1 cannot be a radical containing a hydroxy radical, and their salts, are useful in therapy for their ability to block serotonin receptors.

73. 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。

74. 发明申请

US20080032985A1 4-Substituted Quinoline Derivatives, Method and Intermediates for Their Preparation and Pharmaceutical Compositions Containing Them 审中-公开
标题翻译： 4-取代的喹啉衍生物，其制备方法和中间体以及含有它们的药物组合物
公开(公告)号：US20080032985A1
公开(公告)日：2008-02-07
申请号：US11571407
申请日：2005-06-24
申请人： Michel Tabart , Fabrice Viviani , Serge Mignani , Baptiste Ronan
发明人： Michel Tabart , Fabrice Viviani , Serge Mignani , Baptiste Ronan
IPC分类号： A61K31/47 , A61K31/4375 , A61K31/502 , A61K31/517 , A61P31/00 , C07D215/12 , C07D237/28 , C07D239/72 , C07D471/04
CPC分类号： C07D409/12 , C07D215/20
摘要： The present invention relates to 4-substituted quinoline derivatives of general formula I: which are active as antimicrobials. The invention also relates to the method and intermediates for their preparation and the pharmaceutical compositions containing them.
摘要翻译：本发明涉及通式I的4-取代喹啉衍生物：其作为抗微生物剂是有活性的。本发明还涉及其制备方法和中间体以及含有它们的药物组合物。

75. 发明申请

US20060148880A1 Isoindolone derivatives, preparation process and intermediates of this process, their use as medicaments, and pharmaceutical compositions comprising them 有权
公开(公告)号：US20060148880A1
公开(公告)日：2006-07-06
申请号：US11365319
申请日：2006-03-01
申请人： Heinz-Werner Kleemann , Armin Hofmeister , Jean-Christophe Carry , Baptiste Ronan , Serge Mignani , Antony Bigot
发明人： Heinz-Werner Kleemann , Armin Hofmeister , Jean-Christophe Carry , Baptiste Ronan , Serge Mignani , Antony Bigot
IPC分类号： A61K31/4035 , C07D403/02 , C07D209/46
CPC分类号： C07D209/46
摘要： The present invention relates to the novel isoindolone derivatives of the formula I in which R1 to R6 have the meanings stated in the claims. The inventive compounds are suitable as antiarrhythmic medicaments with a cardioprotective component for infarction prophylaxis and infarction treatment and for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure.

76. 发明授权

US06815547B2 Quinolylpropylpiperidine derivatives, their preparation, and compositions containing them 失效
标题翻译：醌基丙基哌啶衍生物，它们的制备和含有它们的组合物
公开(公告)号：US06815547B2
公开(公告)日：2004-11-09
申请号：US10387479
申请日：2003-03-14
申请人： Eric Bacque , Serge Mignani , Jean-Luc Malleron , Michel Tabart , Michel Evers , Fabrice Viviani , Youssef El Ahmad , Stéphane Mutti , Christophe Daubié
发明人： Eric Bacque , Serge Mignani , Jean-Luc Malleron , Michel Tabart , Michel Evers , Fabrice Viviani , Youssef El Ahmad , Stéphane Mutti , Christophe Daubié
IPC分类号： C07D21512
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14
摘要： Quinolylpropylpiperidine derivatives of general formula (I) are described, and are useful as antimicrobial agents. Their preparation is also described.
摘要翻译：描述了通式（I）的喹啉基丙基哌啶衍生物，并且可用作抗微生物剂。还描述了它们的制备方法。

77. 发明授权

US06806277B2 Quinolylpropylpiperidine derivatives, preparation process and intermediates, and compositions including them 失效
标题翻译：醌基丙基哌啶衍生物，制备方法和中间体，以及包括它们的组合物
公开(公告)号：US06806277B2
公开(公告)日：2004-10-19
申请号：US10622655
申请日：2003-07-18
申请人： Eric Bacqué , Jean-Luc Malleron , Serge Mignani , Michel Tabart
发明人： Eric Bacqué , Jean-Luc Malleron , Serge Mignani , Michel Tabart
IPC分类号： A61K3147
CPC分类号： C07D401/06 , C07D409/12
摘要： Quinolylpropylpiperidine derivatives of general formula (I) in which: R1 is NH2, alkylamino, dialkylamino, hydroxyamino, alkyl(alkyloxy)amino or alkyloxyamino, R2 is a carboxyl, carboxymethyl or hydroxymethyl radical, R3 is alkyl (1 to 6C) substituted by phenylthio which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2, by cycloalkylthio (3 to 7 members) or by heteroarylthio (5 to 6 members) comprising 1 to 4 heteroatoms selected from N, S and O and optionally itself substituted [by halogen, OH, alkyl, alkyloxy, CF3, OCF3, ═O, COOH, alkyloxycarbonyl, CN or NH2] or R3 is propargyl substituted by phenyl which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2 or substituted by cycloalkyl comprising 3 to 7 members or substituted by 5- to 6-membered heteroaryl comprising 1 to 4 heteroatoms chosen from N, O or S and optionally itself substituted by halogen, OH, alkyl, alkyloxy, CF3, OCF3, ═O, COOH, alkyloxycarbonyl, CN or NH2, and R4 is alkyl (1 to 6C), alkenyl-CH2—, alkynyl-CH2— (3 to 7C), cycloalkyl or (cycloalkyl)alkyl, in their diastereoisomeric forms or their mixtures, and their pharmaceutically acceptable salts. These novel derivatives are particularly advantageous antimicrobial agents.
摘要翻译：通式（I）的喹啉基丙基哌啶衍生物，其中：R1是NH2，烷基氨基，二烷基氨基，羟基氨基，烷基（烷氧基）氨基或烷氧基氨基，R2是羧基，羧甲基或羟甲基，R3是被苯硫基取代的（1-6）其可以自身携带1至3个选自卤素，OH，烷基，烷氧基，CF 3，OCF 3，COOH，烷氧基羰基，CN和NH 2的取代基，被环烷硫基（3至7个成员）或通过杂芳硫基（5至6个成员）包含1至 4个选自N，S和O的杂原子，并且任选地本身被[由卤素，OH，烷基，烷氧基，CF 3，OCF 3，= O，COOH，烷氧基羰基，CN或NH 2]取代的R 3或被苯基取代的苯基，被选自卤素，OH，烷基，烷氧基，CF 3，OCF 3，COOH，烷氧基羰基，CN和NH 2的3个取代基，或被包含3至7个成员的环烷基或被包含1至4个选自 N，O或S，以及任选的其自身取代基 CN，NH 2，R 4是烷基（1-6），链烯基-CH 2 - ，炔基-CH 2 - （3至7C），环烷基（C 1 -C 6）烷基，烷氧基羰基，或（环烷基）烷基，其非对映异构体形式或其混合物及其药学上可接受的盐。这些新型衍生物是特别有利的抗微生物剂。

78. 发明授权

US06762196B2 Use of 2-amino-4-pyridylmethyl-thiazoline derivatives as inhibitors of inducible no-synthase 失效
标题翻译：使用2-氨基-4-吡啶基甲基 - 噻唑啉衍生物作为诱导型无合成酶的抑制剂
公开(公告)号：US06762196B2
公开(公告)日：2004-07-13
申请号：US10290624
申请日：2002-11-08
申请人： Eric Bacque , Antony Bigot , Jean-Christophe Carry , Serge Mignani , Baptiste Ronan , Michel Tabart
发明人： Eric Bacque , Antony Bigot , Jean-Christophe Carry , Serge Mignani , Baptiste Ronan , Michel Tabart
IPC分类号： A61K314436
CPC分类号： C07D213/40 , C07D213/55 , C07D213/64 , C07D213/89 , C07D417/06 , C07F7/1804
摘要： The present invention relates to the use of 2-amino-4-pyridylmethyl thiazoline derivatives of formula (I) wherein either R1═R2═Cl or (C1-C4)alkyl, or hydroxy; or (C1-C4)alkoxy or at least one of R1 or R2 is a hydrogen and the other is a (C1-C4)alkyl, hydroxy, (C1-C4)alkoxy or chlorine or pharmaceutically acceptable salts thereof as inhibitors of inducible NO-synthase.
摘要翻译：本发明涉及式（I）的2-氨基-4-吡啶基甲基噻唑啉衍生物，其中R 1 = R 2 = Cl或（C 1 -C 4）烷基或羟基; 或（C1-C4）烷氧基，或R1或R2中的至少一个为氢，另一个为（C 1 -C 4）烷基，羟基，（C 1 -C 4）烷氧基或氯或其药学上可接受的盐作为诱导型NO -Synthase。

79. 发明授权

US06362185B1 Polyhydroxyalkylpyrazine derivatives, their preparation and the medicaments comprising them 有权
标题翻译：聚羟基烷基吡嗪衍生物，其制备方法和包含它们的药物
公开(公告)号：US06362185B1
公开(公告)日：2002-03-26
申请号：US09483939
申请日：2000-01-14
申请人： Georges Bashiardes , Jean-Christophe Carry , Michel Evers , Bruno Filoche , Serge Mignani
发明人： Georges Bashiardes , Jean-Christophe Carry , Michel Evers , Bruno Filoche , Serge Mignani
IPC分类号： A61K314965
CPC分类号： A61K31/495 , C07D241/12
摘要： The present invention relates to medicaments comprising at least one compound of formula: wherein either R1 represents a —CH(Ra)—CHOH—CHOH—CH2OH chain and R2 represents a —CH2—CHOH—CHOH—CH2OH chain, or R1 represents a —CHOH—CHF—CHOH—CH2OH chain and R2 represents a —CH2—CHF—CHOH—CH2OH chain, or R1 represents a —CHOH—CHOH—CHOH—Rb chain and R2 represents a —CH2—CHOH—CHOH—Rb chain, or R1 represents a —CH2—CHOH—CHOH—CH2OH chain and R2 represents a —CH2—CHOH—CHOH—CH2OH chain, or R1 and R2 are identical and each represent a —(CHOH)n—CH2OH chain in which n is equal to 1, 2, 3 or 4, Ra represents an alkoxy radical (1-6 C in a straight or branched chain) or a fluorine atom, and Rb represents a carboxyl, —CO—NH2 or —CH2—NH2 radical, or one of their stereoisomers or their salts with an inorganic or organic acid, to novel compounds of formula (I) and to their preparation.
摘要翻译：本发明涉及包含至少一种下式的化合物的药物：其中R1表示-CH（Ra）-CHOH-CHOH-CH2OH链，R2表示-CH2-CHOH-CHOH-CH2OH链，或R1表示-CHOH- CHF-CHOH-CH2OH链，R2表示-CH2-CHF-CHOH-CH2OH链，或R1表示-CHOH-CHOH-CHOH-Rb链，R2表示-CH2-CHOH-CHOH-Rb链，或R1表示 -CH 2 -CHOH-CHOH-CH 2 OH链，R 2表示-CH 2 -CHOH-CHOH-CH 2 OH链，或R 1和R 2相同，各自表示其中n等于1的 - （CHOH）n -CH 2 OH链， 2,3或4中，Ra表示烷氧基（直链或支链中1-6C）或氟原子，Rb表示羧基，-CO-NH2或-CH2-NH2基，或其立体异构体或它们与无机或有机酸的盐，与式（I）的新型化合物及其制备。

80. 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。

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