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1. 发明授权

US08163768B2 1,4-dihydropyridine-fused heterocycles, process for preparing the same, use and compositions containing them 有权
标题翻译： 1,4-二氢吡啶稠合的杂环，其制备方法，用途和含有它们的组合物
公开(公告)号：US08163768B2
公开(公告)日：2012-04-24
申请号：US12014516
申请日：2008-01-15
申请人： Jacques Mauger , Anil Nair , Nina Ma , Kirsten Bjergarde , Bruno Filoche-Romme , Odile Angouillant-Boniface , Serge Mignani , Jean-Christophe Carry , Francois Clerc , Herve Minoux , Laurent Schio , Cecile Combeau
发明人： Jacques Mauger , Anil Nair , Nina Ma , Kirsten Bjergarde , Bruno Filoche-Romme , Odile Angouillant-Boniface , Serge Mignani , Jean-Christophe Carry , Francois Clerc , Herve Minoux , Laurent Schio , Cecile Combeau
IPC分类号： A61K31/437 , A61K31/4375 , C07D471/14
CPC分类号： C07D471/04 , C07D471/14
摘要： This invention relates to compounds of formula (I) to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment comprising administering of such compounds.
摘要翻译：本发明涉及式（I）化合物，其用于制备这些化合物的方法，包含这些化合物的药物组合物，以及涉及治疗方法，包括施用这些化合物。

2. 发明授权

US07531663B2 3-guanidinocarbonyl-1-heteroaryl-indole derivatives, preparation process, their use as medicaments, and pharmaceutical compositions comprising them 失效
公开(公告)号：US07531663B2
公开(公告)日：2009-05-12
申请号：US10749630
申请日：2003-12-31
申请人： Heinz-Werner Kleemann , Jean-Christophe Carry , Pascal Desmazeau , Serge Mignani , Jean Bouquerel , Arielle Genevois-Borella , Baptiste Ronan
发明人： Heinz-Werner Kleemann , Jean-Christophe Carry , Pascal Desmazeau , Serge Mignani , Jean Bouquerel , Arielle Genevois-Borella , Baptiste Ronan
IPC分类号： C07D215/38
CPC分类号： C07D401/04 , C07D403/04
摘要： The present invention relates to 3-guanidinocarbonyl-1-heteroaryl-indole derivatives, pharmaceutical compositions comprising such derivatives, methods of treatment comprising administering such derivatives, and processes for their preparation.

3. 发明授权

US07348434B2 4-substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them 失效
标题翻译： 4-取代喹啉衍生物，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：US07348434B2
公开(公告)日：2008-03-25
申请号：US10913222
申请日：2004-08-06
申请人： Antony Bigot , Serge Mignani , Baptiste Ronan , Michel Tabart , Fabrice Viviani
发明人： Antony Bigot , Serge Mignani , Baptiste Ronan , Michel Tabart , Fabrice Viviani
IPC分类号： C07D215/38
CPC分类号： C04B35/632 , C07D401/12
摘要： The invention relates to 4-substituted quinoline derivatives of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 and X5 represent >C—R′1 to >C—R′5 respectively, or alternatively at most one represents nitrogen, Y represents CHR, CO, CROH, CRNH2, CRF or CF2, R being a hydrogen or alkyl, m is 0, 1 or 2 and n is 0 or 1, R2 represents a radical R, —CO2R, —CH2CO2R, —CH2—CH2CO2R, —CONH2, —CH2—CONH2, —CH2—CH2—CONH2, —CH2OH, —CH2—CH2OH, —CH2—NH2—CH2—CH2—NH2 or —CH2—CH2—CH2—NH2, R being as defined above, R3 represents phenyl, heteroaryl or alk-Ro3, where alk is alkyl and Ro3 represents various groups, where appropriate containing oxygen, sulfur or amine, in their enantiomeric or diastereoisomeric forms or their mixtures, and/or where appropriate in the syn or anti form or their mixtures, and their salts.
摘要翻译：本发明涉及以下通式的4-取代喹啉衍生物：其作为抗微生物剂是有活性的，其中：X 1，X 2，X 3 ，X 4和X 5分别表示C-R 1至C-R'5 R 2如上所定义，R 3表示苯基，杂芳基或烷基-R（R 2）其中烷基是烷基和R 3表示各种基团，其中适当地含有它们的对映异构体或非对映异构形式或其混合物中的氧，硫或胺，和/或在合适的情况下在顺式或顺式抗体形式或它们的混合物及其盐。

4. 发明授权

US07232834B2 Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor 失效
标题翻译：醌基丙基哌啶衍生物，含有它们的中间体和组合物及其制备方法
公开(公告)号：US07232834B2
公开(公告)日：2007-06-19
申请号：US10659164
申请日：2003-09-10
申请人： Eric Bacque , Antony Bigot , Youssef El Ahmad , Jean-Luc Malleron , Serge Mignani , Baptiste Ronan , Michel Tabart , Fabrice Viviani
发明人： Eric Bacque , Antony Bigot , Youssef El Ahmad , Jean-Luc Malleron , Serge Mignani , Baptiste Ronan , Michel Tabart , Fabrice Viviani
IPC分类号： A61K31/4545 , C07D401/06
CPC分类号： C07D401/06 , C07D211/34 , C07D409/14 , Y02P20/55
摘要： Quinolylpropylpiperidine derivatives of general formula (I) in which R1 is hydrogen or fluorine, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl substituted either with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino or R3 is propargyl substituted by phenyl or heteroaryl as defined above and R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them. These novel derivatives are potent antibacterial agents
摘要翻译： R 1是氢或氟的通式（I）的喹啉基丙基哌啶衍生物，R 2是羧基，羧甲基或羟甲基，R 3是被任选被卤素，羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基取代的苯硫基取代或被任选被卤素或三氟甲基取代的环烷硫基（3至7成员）或与杂芳硫基 6个成员和1至4个选自N，O和S的杂原子），任选被卤素，羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基取代的杂原子，或者R 3是炔丙基被如上定义的苯基或杂芳基取代，并且R 4是烷基，链烯基-CH 2 - 或炔基-CH 2 - ，环烷基或环烷基烷基以其各种异构体形式，分别或作为混合物，以及它们的盐，其制备方法和含量 ermediates和含有它们的组合物。这些新型衍生物是有效的抗菌剂

5. 发明授权

US07227022B2 Use of 2-amino-thiazoline derivatives as inhibitors of inducible no-synthase 失效
标题翻译：使用2-氨基 - 噻唑啉衍生物作为诱导型无合成酶的抑制剂
公开(公告)号：US07227022B2
公开(公告)日：2007-06-05
申请号：US11200713
申请日：2005-08-10
申请人： Antony Bigot , Jean-Christophe Carry , Serge Mignani
发明人： Antony Bigot , Jean-Christophe Carry , Serge Mignani
IPC分类号： C07D241/04
CPC分类号： C07D295/13 , C07D241/04 , C07D277/18 , C07D295/15 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention relates to a process for preparing 2-amino-thiazoline derivatives of formula (II): in which either Y is a methylene (CH2) and X is chosen from the following groups: O, NH, (C1–C4) N-Alkyl, N-Bn, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO2, CH2 or CHPh; or Y is a carbonyl (C═O) and X is chosen from the following groups: NH, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl or N-5-pyrimidyl.
摘要翻译：本发明涉及制备式（II）的2-氨基 - 噻唑啉衍生物的方法：其中Y是亚甲基（CH 2 CH 2），X选自下列基团：O， NH，（C 1 -C 4）N-烷基，N-Bn，N-Ph，N-（2-Py），N-（3-Py），N-（4-Py），N-2-嘧啶基，N -5-嘧啶基，S，SO，SO 2，CH 2或CHPh; 或者Y是羰基（CO），X选自下列基团：NH，N-Ph，N-（2-Py），N-（3-Py），N-（4-Py），N-2 - 嘧啶基或N-5-嘧啶基。

6. 发明申请

US20050288501A1 Use of 2-amino-thiazoline derivatives as inhibitors of inducible no-synthase 失效
标题翻译：使用2-氨基 - 噻唑啉衍生物作为诱导型无合成酶的抑制剂
公开(公告)号：US20050288501A1
公开(公告)日：2005-12-29
申请号：US11200713
申请日：2005-08-10
申请人： Antony Bigot , Jean-Christophe Carry , Serge Mignani
发明人： Antony Bigot , Jean-Christophe Carry , Serge Mignani
IPC分类号： C07D295/12 , A61K31/497 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P35/00 , A61P43/00 , C07D277/18 , C07D295/13 , C07D295/15 , C07D413/02 , C07D417/06 , C07D417/12 , C07D417/14 , C07D43/02
CPC分类号： C07D295/13 , C07D241/04 , C07D277/18 , C07D295/15 , C07D417/06 , C07D417/12 , C07D417/14
摘要： The present invention relates to a process for preparing 2-amino-thiazoline derivatives of formula (II): in which either Y is a methylene (CH2) and X is chosen from the following groups: O, NH, (C1-C4) N-Alkyl, N—Bn, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO2, CH2 or CHPh; or Y is a carbonyl (C═O) and X is chosen from the following groups: NH, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl or N-5-pyrimidyl.
摘要翻译：本发明涉及制备式（II）的2-氨基 - 噻唑啉衍生物的方法：其中Y是亚甲基（CH 2 CH 2），X选自下列基团：O， NH，（C 1 -C 4）N-烷基，N-Bn，N-Ph，N-（2-Py），N-（3-Py），N-（4-Py），N-2-嘧啶基，N -5-嘧啶基，S，SO，SO 2，CH 2或CHPh; 或者Y是羰基（CO），X选自下列基团：NH，N-Ph，N-（2-Py），N-（3-Py），N-（4-Py），N-2 - 嘧啶基或N-5-嘧啶基。

7. 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。

8. 发明授权

US06713468B2 Methods of using thiazolobenzoheterocycles 失效
标题翻译：使用噻唑并苯杂环的方法
公开(公告)号：US06713468B2
公开(公告)日：2004-03-30
申请号：US10201902
申请日：2002-07-25
申请人： Jean-Claude Hardy , Jean Bouquerel , Patrick Nemecek , Jean-Claude Aloup , Serge Mignani , Jean-François Peyronel
发明人： Jean-Claude Hardy , Jean Bouquerel , Patrick Nemecek , Jean-Claude Aloup , Serge Mignani , Jean-François Peyronel
IPC分类号： A61K3133
CPC分类号： C07D513/06 , C07D517/06 , C07D517/08
摘要： Methods of using compounds of formula (I): their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof.
摘要翻译：使用式（I）化合物的方法：其外消旋物，对映异构体，非对映异构体和无机酸盐及其有机酸盐。

9. 发明授权

US06603005B2 Heterocyclylalkylpiperidine derivatives, their preparation and compositions containing them 失效
标题翻译：杂环基烷基哌啶衍生物，它们的制备方法和含有它们的组合物
公开(公告)号：US06603005B2
公开(公告)日：2003-08-05
申请号：US09987386
申请日：2001-11-14
申请人： Eric Baque , Jean-Christophe Carry , Youssef El-Ahmad , Michel Evers , Philippe Hubert , Jean-Luc Malleron , Serge Mignani , Guy Pantel , Michel Tabart , Fabrice Viviani
发明人： Eric Baque , Jean-Christophe Carry , Youssef El-Ahmad , Michel Evers , Philippe Hubert , Jean-Luc Malleron , Serge Mignani , Guy Pantel , Michel Tabart , Fabrice Viviani
IPC分类号： C07D47102
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14
摘要： Heterocyclylalkylpiperidine derivatives of general formula (I) in their enantiomeric or diastereoisomeric forms or mixtures of these forms, and/or, where appropriate, in their syn or anti form or a mixture thereof, as well as any salt thereof.
摘要翻译：通式（I）的杂环基烷基哌啶衍生物在它们的对映异构体或非对映异构体形式或这些形式的混合物中，和/或在适当时以其顺式或反式或其混合物以及其任何盐。

10. 发明授权

US5677306A Derivatives of 5H, 10H-imidazo�1, 2-a!indeno�1,2-e!pyrazin-4-one, preparation thereof and medicaments containing them 失效
标题翻译： 5H，10H-咪唑并[1,2-a]茚并[1,2-e]吡嗪-4-酮的衍生物，其制备方法和含有它们的药物
公开(公告)号：US5677306A
公开(公告)日：1997-10-14
申请号：US406982
申请日：1995-03-31
申请人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Dominique Damour , Arielle Genevois-Borella , Patrick Jimonet , Serge Mignani
发明人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Dominique Damour , Arielle Genevois-Borella , Patrick Jimonet , Serge Mignani
IPC分类号： A61K31/495 , A61P9/00 , A61P9/02 , A61P25/00 , A61P25/28 , C07D487/04
CPC分类号： C07D487/04
摘要： Compounds having the formula (I) wherein R and R.sub.1, similar or different, represent a hydrogen or halogen atom or a radical alkyl, alkoxy, amino, acylamino, phenylureido, --N.dbd.CH--N(R.sub.2)R.sub.3, nitro, imidazolyl, phenyl, SO.sub.3 H or cyano; R.sub.2 and R.sub.3 which may be similar or different, represent each an alkyl radical; the invention also relates to the salts of such compounds, their preparation, intermediates for preparing them and drugs containing them. ##STR1##
摘要翻译： PCT No.PCT / FR93 / 00946 Sec。 371日期1995年3月31日 102（e）1995年3月31日PCT PCT 1993年9月28日PCT公布。公开号WO94 / 07893 日期：1994年04月14日具有式（I）的化合物其中R和R 1相同或不同，表示氢或卤素原子或烷基，烷氧基，氨基，酰氨基，苯基脲基，-N = CH-N（R2）R3 ，硝基，咪唑基，苯基，SO 3 H或氰基; 可以相似或不同的R 2和R 3各自表示烷基; 本发明还涉及这些化合物的盐，它们的制备，制备它们的中间体和含有它们的药物。

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