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11. 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。

12. 发明授权

US06451821B1 Use of 2-aminothiazoline 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：US06451821B1
公开(公告)日：2002-09-17
申请号：US09878814
申请日：2001-06-08
申请人： Jean-Christophe Carry , Dominique Damour , Claude Guyon , Serge Mignani , Antony Bigot , Eric Bacque , Michel Tabart
发明人： Jean-Christophe Carry , Dominique Damour , Claude Guyon , Serge Mignani , Antony Bigot , Eric Bacque , Michel Tabart
IPC分类号： A61K3144
CPC分类号： C07D417/06 , A61K31/426 , A61K31/4439 , C07D277/18
摘要： The present invention relates to the use of 2-aminothiazoline derivatives of formula: in which either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk—NH2, —CH2—R3, —CH2—S—R4 or phenyl radical substituted with a nitro or —NH— C (═NH) CH3 radical, or R1 is an alkyl radical and R2 is a hydrogen atom, R3 is a (3-6C) cycloalkyl, pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl or phenyl radical or a phenyl radical substituted with a nitro, hydroxy or carboxyl radical, R4 represents a pyridyl or pyridyl N-oxide radical, alk represents an alkylene radical, or pharmaceutically acceptable salts thereof, as inhibitors of inducible NO-synthase.
摘要翻译：本发明涉及下式的2-氨基噻唑啉衍生物的用途：其中R1是氢原子或烷基，R2是烷基，-alk-NH2，-CH2-R3，-CH2-S-R4或被硝基或-NH- C（= NH）CH 3基取代的苯基，或R 1是烷基，R 2是氢原子，R 3是（3-6C）环烷基，吡啶基，吡啶基N-氧化物，噻吩基，噻唑基，咪唑基，吡嗪基，三唑基或苯基或被硝基，羟基或羧基取代的苯基，R4表示吡啶基或吡啶基N-氧化物基，alk表示亚烷基或其药学上可接受的盐，作为诱导型NO合成酶。

13. 发明授权

US06699895B2 2-aminothiazoline derivatives and process for preparing the same 失效
标题翻译： 2-氨基噻唑啉衍生物及其制备方法
公开(公告)号：US06699895B2
公开(公告)日：2004-03-02
申请号：US10159498
申请日：2002-05-31
申请人： Jean-Christophe Carry , Dominique Damour , Claude Guyon , Serge Mignani , Antony Bigot , Eric Bacque , Michel Tabart
发明人： Jean-Christophe Carry , Dominique Damour , Claude Guyon , Serge Mignani , Antony Bigot , Eric Bacque , Michel Tabart
IPC分类号： C07D41706
CPC分类号： C07D417/06 , A61K31/426 , A61K31/4439 , C07D277/18
摘要： The present invention relates to a class of 2-aminothiazoline derivatives of formula I: in which either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, —CH2—R3, —CH2—S—R4 or phenyl radical substituted with a nitro or —NH—C(═NH)CH3 radical, or R1 is an alkyl radical and R2 is a hydrogen atom, R3 is a (3-6C) cycloalkyl, pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl or phenyl radical or a phenyl radical substituted with a nitro, hydroxy or carboxyl radical, R4 represents a pyridyl or pyridyl N-oxide radical, alk represents an alkylene radical, or pharmaceutically acceptable salts thereof, which are useful as inhibitors of inducible NO-synthase.
摘要翻译：本发明涉及一类式I的2-氨基噻唑啉衍生物：其中R1是氢原子或烷基，R2是烷基，-alk-NH2，-CH2-R3，-CH2-S-R4 或被硝基或-NH-C（= NH）CH 3基团取代的苯基，或R 1是烷基，R 2是氢原子，R 3是（3-6C）环烷基，吡啶基，吡啶基N-氧化物，噻吩基，噻唑基，咪唑基，吡嗪基，三唑基或苯基或被硝基，羟基或羧基取代的苯基，R4表示吡啶基或吡啶基N-氧化物基，alk表示亚烷基或其药学上可接受的盐，它们是可用作诱导型NO合成酶的抑制剂。

14. 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。

15. 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。

16. 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。

17. 发明申请

US20050032800A1 4-Substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them 失效
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：US20050032800A1
公开(公告)日：2005-02-10
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： C07D401/12 , C07D487/02 , C07D41/02
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-R°3, where alk is alkyl and R°3 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：其作为抗微生物剂具有活性，其中：X 1，X 2，X 3，X 4和X 5分别表示> C-R'1至> C-R'5，或者替代地大多数代表氮，Y代表CHR，CO，CROH，CRNH2，CRF或CF2，R是氢或烷基，m是0,1或2，n是0或1，R2代表基团R，-CO 2 R， CH2CO2R，-CH2-CH2CO2R，-CONH2，-CH2-CONH2，-CH2-CH2-CONH2，-CH2OH，-CH2-CH2OH，-CH2-NH2-CH2-CH2-NH2或-CH2-CH2-CH2-NH2， R如上定义，R 3表示苯基，杂芳基或烷基-R 3，其中alk是烷基，R 3表示各种基团，其中适当地含有其对映体或非对映异构体形式的氧，硫或胺，或其混合物，以及 /或适当时以合成或反式形式或其混合物及其盐。

18. 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。

19. 发明授权

US5484804A Perhydroisoindole derivatives as antagonists of substance P 失效
标题翻译：全氟异吲哚衍生物作为P物质的拮抗剂
公开(公告)号：US5484804A
公开(公告)日：1996-01-16
申请号：US313121
申请日：1994-10-11
申请人： Daniel Achard , Serge Grisoni , Jean-Luc Malleron , Jean-Francois Peyronel , Michel Tabart
发明人： Daniel Achard , Serge Grisoni , Jean-Luc Malleron , Jean-Francois Peyronel , Michel Tabart
IPC分类号： C07D405/06 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61P9/02 , A61P9/12 , A61P11/00 , A61P11/06 , A61P25/04 , A61P29/00 , A61P43/00 , C07D209/44 , C07D403/06 , C07D409/06 , C07D401/06
CPC分类号： C07D403/06 , C07D209/44 , C07D409/06
摘要： This invention relates to novel perhydroisoindole derivatives of general formula (I), ##STR1## wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; R.sub.3 is optionally 2-substituted phenyl; R.sub.4 is OH or fluorine when R.sub.5 is H, or R.sub.4 and R.sub.5 are OH or R.sub.4 and R.sub.5 together form a bond; isomeric forms and mixtures thereof; optionally salts thereof where applicable; and preparation thereof. The novel derivatives are particularly useful as P substance antagonists.
摘要翻译： PCT No。PTC / FR93 / 00352 Sec。 371日期：1994年10月11日 102（e）日期1994年10月11日PCT提交1993年4月8日PCT公布。公开号WO93 / 21155 本发明涉及通式（I）的新型全氢异吲哚衍生物，其中基团R是任选被卤素原子或甲基取代的2-或3-取代的苯基; R1是任选取代的苯基，环己二烯基，萘基，茚基或任选取代的杂环基; R2是H，卤素，OH，烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，烷氧基，烷硫基，酰氧基，羧基，任选取代的烷氧基羰基，苄氧羰基，氨基或酰氨基; R3是任选的2-取代的苯基; 当R 5为H或R 4和R 5为OH或R 4和R 5一起形成键时，R 4为OH或氟; 异构形式及其混合物; 任选的盐; 及其制备。新型衍生物作为P物质拮抗剂是特别有用的。

20. 发明授权

US06566362B2 Benzo[f]naphthyridine derivatives, their preparation and compositions containing them 失效
标题翻译：苯并[f]萘啶衍生物，其制备方法和含有它们的组合物
公开(公告)号：US06566362B2
公开(公告)日：2003-05-20
申请号：US10029950
申请日：2001-12-31
申请人： Jean-François Desconclois , Arielle Genevois-Borella , Philippe Girard , Michel Kryvenko , Marc Pierre Lavergne , Jean-Luc Malleron , Guy Picaut , Michel Tabart , Sylvie Wentzler
发明人： Jean-François Desconclois , Arielle Genevois-Borella , Philippe Girard , Michel Kryvenko , Marc Pierre Lavergne , Jean-Luc Malleron , Guy Picaut , Michel Tabart , Sylvie Wentzler
IPC分类号： A61K314375
CPC分类号： C07D215/38 , C07D471/04
摘要： Benzo[f]naphthyridine derivatives of formula (I): benzo[f]naphthyridine derivatives and benzo[f]naphthyridine esters of formula (IVa): aminoquinoline derivatives of formula (X): processes for preparing such compounds; and compositions comprising them.
摘要翻译：式（I）的苯并[f]萘啶衍生物：苯并[f]萘啶衍生物和式（IVa）的苯并[f]萘啶酯：式（X）的氨基喹啉衍生物：制备此类化合物的方法; 和包含它们的组合物。

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