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1. 发明申请

US20100009980A1 NOVEL 9-SUBSTITUTED-5-CARBOXY-OXADIAZINO-QUINOLONE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION AS ANTI-BACTERIALS 失效
标题翻译：新型9-取代的5-羧氧基 - 喹喔啉酮衍生物，其制备及其作为抗细菌的应用
公开(公告)号：US20100009980A1
公开(公告)日：2010-01-14
申请号：US12489528
申请日：2009-06-23
申请人： Sandrine Ropp , Christophe Morice , Bruno Giethlen , Paola Ciapetti , Florence Chery-Mozziconacci , Camille G. Wermuth , Francoise Leblanc , Marc Schneider
发明人： Sandrine Ropp , Christophe Morice , Bruno Giethlen , Paola Ciapetti , Florence Chery-Mozziconacci , Camille G. Wermuth , Francoise Leblanc , Marc Schneider
IPC分类号： A61K31/5395 , C07D401/04 , C07D498/04 , A61K31/497
CPC分类号： C07D498/06 , C07D519/00
摘要： A subject of the invention is the compounds of formula (I): wherein R1, R2, R3, R′3, R4, R′4, R5, R6 and R7 are as described in the application, in the form of enantiomers or mixtures, as well as their salts with acids and bases, their preparation and their application as anti-bacterials, in both human and veterinary medicine.
摘要翻译：本发明的主题是式（I）的化合物：其中R 1，R 2，R 3，R'3，R 4，R'4，R 5，R 6和R 7如本申请中所述，以对映体或混合物的形式，以及它们与酸和碱的盐，它们的制备及其作为抗菌剂的应用，在人和兽医学中。

2. 发明授权

US08071590B2 9-substituted-5-carboxy-oxadiazino-quinolone derivatives, their preparation and their application as anti-bacterials 失效
标题翻译： 9-取代-5-羧基 - 恶二唑 - 喹诺酮衍生物，其制备及其作为抗菌剂的应用
公开(公告)号：US08071590B2
公开(公告)日：2011-12-06
申请号：US12489528
申请日：2009-06-23
申请人： Sandrine Ropp , Christophe Morice , Bruno Giethlen , Paola Ciapetti , Florence Chery-Mozziconacci , Camille G. Wermuth , Francoise Leblanc , Marc Schneider
发明人： Sandrine Ropp , Christophe Morice , Bruno Giethlen , Paola Ciapetti , Florence Chery-Mozziconacci , Camille G. Wermuth , Francoise Leblanc , Marc Schneider
IPC分类号： C07D498/06 , A61K31/5365
CPC分类号： C07D498/06 , C07D519/00
摘要： A subject of the invention is the compounds of formula (I): wherein R1, R2, R3, R′3, R4, R′4, R5, R6 and R7 are as described in the application, in the form of enantiomers or mixtures, as well as their salts with acids and bases, their preparation and their application as anti-bacterials, in both human and veterinary medicine.
摘要翻译：本发明的主题是式（I）的化合物：其中R 1，R 2，R 3，R'3，R 4，R'4，R 5，R 6和R 7如本申请中所述，以对映体或混合物的形式，以及它们与酸和碱的盐，它们的制备及其作为抗菌剂的应用，在人和兽医学中。

3. 发明申请

US20070129365A1 6-Substituted pyridoindolone derivatives, production and therapeutic use thereof 失效
标题翻译： 6-取代的吡啶并吲哚酮衍生物，其制备和治疗用途
公开(公告)号：US20070129365A1
公开(公告)日：2007-06-07
申请号：US11582769
申请日：2006-10-18
申请人： Bernard Bourrie , Pierre Casellas , Paola Ciapetti , Jean-Marie Deroco , Samir Jegham , Yvette Muneaux , Camille-Georges Wermuth
发明人： Bernard Bourrie , Pierre Casellas , Paola Ciapetti , Jean-Marie Deroco , Samir Jegham , Yvette Muneaux , Camille-Georges Wermuth
IPC分类号： A61K31/5377 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： Compounds of formula: and pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2, R3, R4, and R5, have the meanings given in the description; pharmaceutical compositions comprising said compounds; and processes for preparing said compounds and methods of use thereof.
摘要翻译：其中R 1，R 2，R 3，R 3，R 3， 4 和R 5 5具有在说明书中给出的含义; 包含所述化合物的药物组合物; 以及制备所述化合物的方法及其使用方法。

4. 发明授权

US07812165B2 6-substituted pyridoindolone derivatives, production and therapeutic use thereof 失效
标题翻译： 6-取代的吡啶并吲哚酮衍生物，其制备和治疗用途
公开(公告)号：US07812165B2
公开(公告)日：2010-10-12
申请号：US11582769
申请日：2006-10-18
申请人： Bernard Bourrie , Pierre Casellas , Paola Ciapetti , Jean-Marie Deroco , Samir Jegham , Yvette Muneaux , Camille-Georges Wermuth
发明人： Bernard Bourrie , Pierre Casellas , Paola Ciapetti , Jean-Marie Deroco , Samir Jegham , Yvette Muneaux , Camille-Georges Wermuth
IPC分类号： C07D571/02 , A61K31/4745
CPC分类号： C07D471/04
摘要： Compounds of formula: and pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2, R3, R4, and R5, have the meanings given in the description; pharmaceutical compositions comprising said compounds; and processes for preparing said compounds and methods of use thereof.
摘要翻译：式的化合物及其药学上可接受的盐，水合物和溶剂化物，其中R1，R2，R3，R4和R5具有说明书中给出的含义; 包含所述化合物的药物组合物; 以及制备所述化合物的方法及其使用方法。

5. 发明授权

US07713965B2 7-substituted 3-carboxy-oxadiazino-quinolone derivatives, their preparation and their application as anti-bacterials 失效
标题翻译： 7-取代的3-羧基 - 恶二唑 - 喹诺酮衍生物，其制备及其作为抗菌剂的应用
公开(公告)号：US07713965B2
公开(公告)日：2010-05-11
申请号：US12394918
申请日：2009-02-27
申请人： Paola Ciapetti , Florence Chery-Mozziconacci , Camille G. Wermuth , Françoise Leblanc , Marc Schneider , Sandrine Ropp , Christophe Morice , Bruno Giethlen
发明人： Paola Ciapetti , Florence Chery-Mozziconacci , Camille G. Wermuth , Françoise Leblanc , Marc Schneider , Sandrine Ropp , Christophe Morice , Bruno Giethlen
IPC分类号： C07D498/06 , A61K31/5365
CPC分类号： C07D498/06
摘要： A subject of the invention is the compounds of formula (I): in which either R1 represents H, OH, NH2, —(CH2)m—NRaRb(m=0.1 or 2), Ra and Rb represent H, linear, branched or cyclic (C1-C6) alkyl, (C3-C6) cycloalkyl-(C3-C6)— alkyl, Rc, S(O)2Rc, C(O)Rc, S(O)2Rd or C(O)Rd; or Ra and Rb with N form an Rc radical; Rc represents a saturated, unsaturated or 5- or 6-members aromatic ring, containing 1 to 4 heteroatoms chosen from N, O and S, optionally substituted; Rd represents a linear, branched or cyclic (C1-C6) alkyl, optionally substituted by 1 to 4 halogens; or R1 represents Rc or CHReRc or CHReRd; Re represents H, OH, NH2, NH—(C1-C6)-alk or N-(C1-C6)-alk2, or NH—(C1-C7)-acyl or NHRc; R2 represents H, (CH2)m—NRaRb, Rc, CHReRc or CHReRd, and R′2 represents H.
摘要翻译：本发明的主题是式（I）的化合物：其中R 1表示H，OH，NH 2， - （CH 2）m -NR a R b（m = 0.1或2），R a和R b表示H，直链，支链或环（C 1 -C 6）烷基，（C 3 -C 6）环烷基 - （C 3 -C 6） - 烷基，R c，S（O）2 C，C（O）R c，S（O）2 R d或C（O）或R a和R b与N形成R c基团; Rc表示饱和，不饱和或5-或6-元芳环，其含有1至4个选自N，O和S的杂原子，任选地被取代; Rd表示任选被1至4个卤素取代的直链，支链或环状（C 1 -C 6）烷基; 或R1表示Rc或CHRRR或CHRRR; Re表示H，OH，NH2，NH-（C1-C6）-alk或N-（C1-C6）-alk2或NH-（C1-C7） - 酰基或NHRc; R2表示H，（CH2）m-NRaRb，Rc，CHReRc或CHReRd，R'2表示H.

6. 发明授权

US07354918B2 Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol and applications thereof 失效
标题翻译： 14.15-二氢20.21-二烧烤蛋白-14-醇的衍生物及其应用
公开(公告)号：US07354918B2
公开(公告)日：2008-04-08
申请号：US11581950
申请日：2006-10-13
申请人： Paola Ciapetti , Laurence Deyon , Camille-Georges Wermuth , Jean-François Pujol , Dinah Weissmann
发明人： Paola Ciapetti , Laurence Deyon , Camille-Georges Wermuth , Jean-François Pujol , Dinah Weissmann
IPC分类号： A61K31/5377 , A61K31/4375 , C07D413/14 , C07D471/22
CPC分类号： C07D461/00
摘要： The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I) in which R represents a radical —AR′ wherein A represents a heteroatom and R′ represents a group selected from the group comprising linear or branched C1-C6 alkyl radicals, C2-C6 alkenyls, C2-C6 alkynyls, arylalkyls; esters comprising the formula —R1— CO—O—R2; amides comprising the formula —R3—CO—NZY, wherein Y and Z together can form a cycloalkyl radical or a heterocyclic radical, optionally substituted by one or more alkyl radicals; a radical selected from the group comprising alkyl radicals, alkenyls or alkynyls, substituted by at least one amine with formula —NZY; or one of the pharmaceutically-acceptable salts thereof, including the isomers, enantiomers and diastereoisomers thereof and mixtures thereof. The invention also relates to the use of the novel derivatives for the preparation of a pharmaceutical composition which is intended, in particular, for the treatment and/or prevention of depression, sleep-wake cycle disorders and symptomatic frontal disorders in cognitive components among humans.
摘要翻译：本发明涉及具有式（I）的式14所示的衍生物，其中R表示自由基-AR'，其中A表示杂原子，R'表示选自包括直链或支链C 1 -C 6烷基，C 2 -C 6亚烷基，C 2 -C 6亚烷基， C 2 -C 6炔基，芳基烷基; 包含式-R 1 -CO-O-R 2的酯; 酰胺，其包含式-NR 3 -CO-NZY，其中Y和Z一起可以形成任选被一个或多个烷基取代的环烷基或杂环基; 选自由至少一个具有式-NZY的胺取代的烷基，烯基或炔基的基团; 或其药学上可接受的盐之一，包括其异构体，对映体和非对映异构体及其混合物。本发明还涉及新型衍生物用于制备药物组合物的用途，其特别用于治疗和/或预防人类中认知成分中的抑郁症，睡眠 - 苏醒循环障碍和症状性前额症。

7. 发明授权

US07390818B2 Pyridoindolone derivatives substituted in the 3-position by a phenyl, their preparation and their application in therapeutics 有权
标题翻译：吡啶并吲哚酮衍生物在3-位被苯基取代，其制备及其在治疗中的应用
公开(公告)号：US07390818B2
公开(公告)日：2008-06-24
申请号：US11109068
申请日：2005-04-19
申请人： Bernard Bourrie , Pierre Casellas , Paola Ciapetti , Jean-Marie Derocq , Samir Jegham , Yvette Muneaux , Camille-Georges Wermuth
发明人： Bernard Bourrie , Pierre Casellas , Paola Ciapetti , Jean-Marie Derocq , Samir Jegham , Yvette Muneaux , Camille-Georges Wermuth
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to pyridoindolone derivatives substituted in the 3-position by a phenyl of general formula (I): to processes for preparing the same and to their use in therapeutics.
摘要翻译：本发明涉及通过通式（I）的苯基在3-位上取代的吡啶并吲哚酮衍生物：其制备方法及其在治疗中的用途。

8. 发明授权

US08063061B2 6-heteroarylpyridoindolone derivatives, their preparation and therapeutic use thereof 失效
标题翻译： 6-杂芳基吡啶并吲哚酮衍生物，其制备和治疗用途
公开(公告)号：US08063061B2
公开(公告)日：2011-11-22
申请号：US12100079
申请日：2008-04-09
申请人： Yvette Muneaux , Samir Jegham , Bernard Bourrie , Pierre Casellas , Paola Ciapetti , Jean-Marie Deroco , Camille-Georges Wermuth
发明人： Yvette Muneaux , Samir Jegham , Bernard Bourrie , Pierre Casellas , Paola Ciapetti , Jean-Marie Deroco , Camille-Georges Wermuth
IPC分类号： A61K31/44 , C07D471/04
CPC分类号： C07D471/04
摘要： The disclosure relates to compounds of formula (I): wherein R1, R2, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and therapeutic use thereof.
摘要翻译：本公开涉及式（I）的化合物：其中R1，R2，R3，R4是R5如本公开中所定义; 它们的制备方法，含有其的组合物和治疗用途。

9. 发明授权

US08012991B2 Pyridoindolone derivatives substituted in the 3-position by a phenyl, their preparation and their application in therapeutics 有权
标题翻译：吡啶并吲哚酮衍生物在3-位被苯基取代，其制备及其在治疗中的应用
公开(公告)号：US08012991B2
公开(公告)日：2011-09-06
申请号：US12118920
申请日：2008-05-12
申请人： Bernard Bourrie , Pierre Casellas , Paola Ciapetti , Jean-Marie Derocq , Samir Jegham , Yvette Muneaux , Camille-Georges Wermuth
发明人： Bernard Bourrie , Pierre Casellas , Paola Ciapetti , Jean-Marie Derocq , Samir Jegham , Yvette Muneaux , Camille-Georges Wermuth
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04
摘要： The present disclosure relates to pyridoindolone derivatives of general formula (I): to processes for preparing the same and to their use in therapeutics.
摘要翻译：本公开涉及通式（I）的吡啶并吲哚酮衍生物：其制备方法及其在治疗中的用途。

10. 发明申请

US20090221565A1 NOVEL 7-SUBSTITUTED 3-CARBOXY-OXADIAZINO-QUINOLONE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION AS ANTI-BACTERIALS 失效
公开(公告)号：US20090221565A1
公开(公告)日：2009-09-03
申请号：US12394918
申请日：2009-02-27
申请人： Sandrine Ropp , Christophe Morice , Bruno Giethlen , Paola Ciapetti , Florence Chery-Mozziconacci , Camille G. Wermuth , Francoise Leblanc , Marc Schneider
发明人： Sandrine Ropp , Christophe Morice , Bruno Giethlen , Paola Ciapetti , Florence Chery-Mozziconacci , Camille G. Wermuth , Francoise Leblanc , Marc Schneider
IPC分类号： C07D498/04 , A61K31/5383 , A61P31/04
CPC分类号： C07D498/06
摘要： A subject of the invention is the compounds of formula (I): in which either R1 represents H, OH, NH2, —(CH2)m—NRaRb(m=0.1 or 2), Ra and Rb represent H, linear, branched or cyclic (C1 -C6) alkyl, (C3-C6) cycloalkyl-(C3-C6)— alkyl, Rc, S(O)2Rc, C(O)Rc, S(O)2Rd or C(O)Rd; or Ra and Rb with N form an Rc radical; Rc represents a saturated, unsaturated or 5- or 6-members aromatic ring, containing 1 to 4 heteroatoms chosen from N, O and S, optionally substituted; Rd represents a linear, branched or cyclic (C1-C6) alkyl, optionally substituted by 1 to 4 halogens; or R1 represents Rc or CHReRc or CHReRd; Re represents H, OH, NH2, NH—(C1-C6)-alk or N-(C1-C6)-alk2, or NH—(C1-C7)-acyl or NHRc; R2 represents H, (CH2)m—NRaRb, Rc, CHReRc or CHReRd, and R′2 represents H; it being understood that R1 and R2 cannot at the same time be H or that R1 and R2 or R2 and R1 cannot be one (CH2)m—NRaRb or Rc or H and the other one OH, or one H and the other one NH2, or one H and the other one (CH2)m—NRaRb in which Ra and Rb represent H or alkyl or C(O)Rd, in which Rd represents an unsubstituted alkyl or cycloalkyl; or R1 has the above definition except H and R2 and R′2 together represent gem dialkyl or alkyl-oxime, or R2 and R′2 represent respectively Rc or Rd and OH, NH2, NHRc or NHRf, Rf being a (C1-C7) acyl radical; or R1 represents H and R2 and R′2 together represent alkyl-oxime or one represents Rc and the other one represents OH, NH2, NHRc or NHRf; n is 0 or 1; R3 and R′3 represent H or (C1-C6) alkyl optionally substituted by 1 to 3 halogens or R3 represents (C1-C6) alkoxy carbonyl and R′3 represents H; R4 represents methyl optionally substituted by halogen; R5 represents H, (C1-C6) alkyl or (C7-C12) arylalkyl; R6 represents H, fluorine, NO2, CF3 or CN; in the form of enantiomers or mixtures, as well as their salts with acids and bases; their preparation and their application as anti-bacterials, in both human and veterinary medicine.

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