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11. 发明申请

US20050165005A1 Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them 失效
标题翻译：吡唑基衍生物，该方法的制备方法和中间体作为药物产品和含有它们的药物组合物
公开(公告)号：US20050165005A1
公开(公告)日：2005-07-28
申请号：US10997736
申请日：2004-11-24
申请人： Arielle Genevois-Borella , Jean-Luc Malleron , Jean Bouquerel , Gilles Doerflinger , Andrees Bohme , Gaetan Touyer , Jean-Francois Sabuco , Corrine Terrier , Serge Mignani , Michel Evers , Youssef El-Ahmad
发明人： Arielle Genevois-Borella , Jean-Luc Malleron , Jean Bouquerel , Gilles Doerflinger , Andrees Bohme , Gaetan Touyer , Jean-Francois Sabuco , Corrine Terrier , Serge Mignani , Michel Evers , Youssef El-Ahmad
IPC分类号： A61K31/41 , A61K31/416 , A61K31/435 , A61K31/454 , A61K31/55 , C07D231/12 , C07D231/14 , C07D231/20 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D409/04 , C07D453/02 , C07D453/06 , C07D487/08 , C07D43/02
CPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D401/04 , C07D401/06 , C07D403/06 , C07D409/04 , C07D453/02 , C07D453/06 , C07D487/08
摘要： The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.
摘要翻译：本发明涉及式（I）的新衍生物，其中A是（C 1 -C 6）烷基，（C 3 -C 6）烯基，（C 3 -C 6）炔基，（C 3 （C 5 -C 7）氮杂双环烷基或（C 5 -C 9）氮杂双环链烯基;（C 5 -C 7）氮杂双环烷基或（C 5 -C 9） A-R1使得R 1的氮和吡唑的1位的氮必须分开至少两个碳原子，R 3是H，卤素，OH，SH，NH 2 >，ORc，SRc，SORa，SO 2 Ra，NHCHO，NRaRb，NHC（O）Ra，NHC（S）Ra或NHSO2Ra，R4是芳基或杂芳基; 并且R 5是H，卤素，CF 3，CHF 2，CH 2 F，直链或支链（C 1 -C 6）烷基或（ C3-C7）环烷基与其外消旋体，对映异构体和非对映异构体及其混合物，它们的互变异构体及其药学上可接受的盐。

12. 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。

13. 发明申请

US20080021029A1 Substituted Cyclic Urea Derivatives, Preparation Thereof And Pharmaceutical Use Thereof As Kinase Inhibitors 审中-公开
标题翻译：取代的环状尿素衍生物，其制备方法及其药物用途作为激酶抑制剂
公开(公告)号：US20080021029A1
公开(公告)日：2008-01-24
申请号：US11627515
申请日：2007-01-26
申请人： Hartmut Strobel , Sven Ruf , Dominique Lesuisse , Conception Nemecek , Youssef El-Ahmad , Jacques Mauger , Stefan Guessregen , Kurt Ritter , Jean-Luc Malleron
发明人： Hartmut Strobel , Sven Ruf , Dominique Lesuisse , Conception Nemecek , Youssef El-Ahmad , Jacques Mauger , Stefan Guessregen , Kurt Ritter , Jean-Luc Malleron
IPC分类号： A61K31/506 , A61K31/4709 , A61K31/5377 , A61P11/06 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P3/00 , A61P3/10 , A61P35/00 , A61P37/08 , A61P7/00 , C07D215/58 , C07D401/02 , C07D413/14 , C12N9/99
CPC分类号： C07D401/06 , C07D409/14
摘要： The disclosure relates to the novel compounds of formula (I): wherein R1, R2, R2′, R3, R3′, p, A, B, Y, Y1, and Y2 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and use thereof as protein kinase inhibitors.
摘要翻译：本公开涉及新的式（I）化合物：其中R 1，R 2，R 2，R 3，R 3， p，A，B，Y，Y 1和Y 2具有本说明书中给出的含义及其盐，包含所述化合物的药物组合物及其用途为蛋白激酶抑制剂。

14. 发明授权

US07825115B2 Cyclic urea compounds, preparation thereof and pharmaceutical use thereof as kinase inhibitors 失效
标题翻译：环状尿素化合物，其制备及其作为激酶抑制剂的药物用途
公开(公告)号：US07825115B2
公开(公告)日：2010-11-02
申请号：US11972314
申请日：2008-01-10
申请人： Marcel Patek , Anil Nair , Augustin Hittinger , Conception Nemecek , Daniel Bond , Greg Harlow , Herve Bouchard , Jacques Mauger , Jean-Luc Malleron , Mark Palermo , Fahad Al-Obeidi , Thomas Faitg , Hartmut Strobel , Sven Ruf , Kurt Ritter , Youssef El-Ahmad , Dominique Lesuisse , Didier Bénard
发明人： Marcel Patek , Anil Nair , Augustin Hittinger , Conception Nemecek , Daniel Bond , Greg Harlow , Herve Bouchard , Jacques Mauger , Jean-Luc Malleron , Mark Palermo , Fahad Al-Obeidi , Thomas Faitg , Hartmut Strobel , Sven Ruf , Kurt Ritter , Youssef El-Ahmad , Dominique Lesuisse , Didier Bénard
IPC分类号： C07D401/06 , C07D403/06 , A61K31/41
CPC分类号： C07D401/06 , C07D401/14
摘要： The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
摘要翻译：本公开涉及式I的环脲化合物：如本文所定义，其制备方法，包含其的药物组合物及其作为蛋白激酶上的抑制剂的药物用途。因此，式I化合物可用于预防或治疗能够通过抑制蛋白激酶如实体瘤的活性而被调节的生理障碍。

15. 发明授权

US07354933B2 Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors 失效
标题翻译：环状尿素衍生物，其制备方法及其作为激酶抑制剂的药物用途
公开(公告)号：US07354933B2
公开(公告)日：2008-04-08
申请号：US10770382
申请日：2004-02-02
申请人： Marcel Patek , Anil Nair , Augustin Hittinger , Conception Nemecek , Daniel Bond , Greg Harlow , Herve Bouchard , Jacques Mauger , Jean-Luc Malleron , Mark Palermo , Fahad Al-Obeidi , Thomas Faitg , Hartmut Strobel , Sven Ruf , Kurt Ritter , Youssef El-Ahmad , Dominique Lesuisse , Didier Bénard
发明人： Marcel Patek , Anil Nair , Augustin Hittinger , Conception Nemecek , Daniel Bond , Greg Harlow , Herve Bouchard , Jacques Mauger , Jean-Luc Malleron , Mark Palermo , Fahad Al-Obeidi , Thomas Faitg , Hartmut Strobel , Sven Ruf , Kurt Ritter , Youssef El-Ahmad , Dominique Lesuisse , Didier Bénard
IPC分类号： C07D401/06 , C07D403/06 , A61K31/41
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
摘要翻译：本发明涉及式I的环脲化合物：如本文所定义。本发明还涉及其制备方法，包含其的药物组合物及其药物用途，作为蛋白激酶上的抑制剂。因此，通过抑制蛋白激酶（例如实体瘤）的活性来预防或治疗能够调节的生理障碍是有用的。

16. 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。

17. 发明申请

US20060270649A1 AZETIDINE DERIVATIVES, THEIR PREPARATION AND MEDICAMENTS CONTAINING THEM 审中-公开
标题翻译： AZETIDINE DERIVATIVES，他们的准备和药物包含他们
公开(公告)号：US20060270649A1
公开(公告)日：2006-11-30
申请号：US11420238
申请日：2006-05-25
申请人： Daniel Achard , Herve Bouchard , Jean Bouquerel , Marc Capet , Serg Grisoni , Jean-Luc Malleron , Serge Mignani , Augustin Hittinger
发明人： Daniel Achard , Herve Bouchard , Jean Bouquerel , Marc Capet , Serg Grisoni , Jean-Luc Malleron , Serge Mignani , Augustin Hittinger
IPC分类号： A61K31/397
CPC分类号： C07D401/06 , C07D205/06 , C07D409/06 , C07D409/14 , C07D417/06
摘要： Disclosed are azetidine derivatives of formula: their optical isomers, their salts, their preparation and medicaments containing them.
摘要翻译：公开的是下式的氮杂环丁烷衍生物：它们的光学异构体，它们的盐，它们的制备物和含有它们的药物。

18. 发明授权

US06518264B2 Azetidine derivatives, their preparation and medicaments containing them 失效
标题翻译：氮杂环丁烷衍生物，其制备方法和含有它们的药物
公开(公告)号：US06518264B2
公开(公告)日：2003-02-11
申请号：US09803723
申请日：2001-03-09
申请人： Daniel Achard , Hervé Bouchard , Jean Bouquerel , Marc Capet , Serg Grisoni , Jean-Luc Malleron , Serge Mignani , Augustin Hittinger
发明人： Daniel Achard , Hervé Bouchard , Jean Bouquerel , Marc Capet , Serg Grisoni , Jean-Luc Malleron , Serge Mignani , Augustin Hittinger
IPC分类号： C07D20506
CPC分类号： C07D401/06 , C07D205/06 , C07D409/06 , C07D409/14 , C07D417/06
摘要： Disclosed are azetidine derivatives of formula: their optical isomers, their salts, their preparation and medicaments containing them.
摘要翻译：公开的是下式的氮杂环丁烷衍生物：它们的光学异构体，它们的盐，它们的制备物和含有它们的药物。

19. 发明授权

US5114949A Heterocyclic derivatives, their preparation and medicinal products containing them 失效
标题翻译：杂环衍生物，其制备和含有它们的药物
公开(公告)号：US5114949A
公开(公告)日：1992-05-19
申请号：US615670
申请日：1990-11-19
申请人： Claude Gueremy , Jean-Luc Malleron , Serge Mignani
发明人： Claude Gueremy , Jean-Luc Malleron , Serge Mignani
IPC分类号： C07D209/46 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/428 , A61K31/47 , A61K31/495 , A61K31/496 , A61P3/04 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D209/92 , C07D235/26 , C07D275/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D513/04 , C07D513/06
CPC分类号： C07D403/06 , C07D403/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D513/04
摘要： Compounds are disclosed of formula:R.sub.1 --(CH.sub.2).sub.n --Hetin which R.sub.1 represents a residue of formula ##STR1## X represents a hydrogen atom or an alkyl radical, Y represents a hydrogen atom or an alkyl or alkoxy radical,Z represents an alkyl radical,n is equal to 2 or 3,Het represents a substituted piperidino (substituted at the 4-position with a 1-indenylidene, 1-indenyl or 1-indanyl radical or with a chain --(CH.sub.2).sub.m --R.sub.2 or .dbd.CH--R.sub.2), substituted 1,2,3,6-tetrahydro-1-pyridyl (substituted at the 4-position with a chain --(CH.sub.2).sub.m --R.sub.2),m is equal to 1 or 2, andR.sub.2 represents an optionally substituted 2- or 3-indolyl radical, a 1- or 2-indanyl, 1- or 2-indenyl, an optionally substituted 1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-2-yl radical, a 1,2,3,4-tetrahydro-3-quinolyl radical, an optionally substituted 1,2,3,4-tetrahydro-2-naphthyl radical or a 1-indolyl radical, their preparation and medicinal products containing them.
摘要翻译：（C）＆gt;（C）＆lt; IMAGE＆gt;（D）＆lt; IMAGE＆gt;（D）＆lt; IMAGE＆gt; J）X表示氢原子或烷基，Y表示氢原子或烷基或烷氧基，Z表示烷基，n表示2或3，Het表示取代的哌啶子基（在4-位取代具有1-茚基，1-茚基或1-茚满基或与链 - （CH 2）m -R 2或= CH-R 2）取代的1,2,3,6-四氢-1-吡啶基（在具有链 - （CH 2）m -R 2）的4-位，m等于1或2，并且R 2表示任选取代的2-或3-吲哚基，1-或2-二氢茚基，1-或2- 茚基，任选取代的1,2,3,4-四氢-5H-吡啶并[4,3-b]吲哚-2-基，1,2,3,4-四氢-3-喹啉基，任选地取代的1,2,3,4-四氢-2-萘基或1-吲哚基，它们的制备方法和含有它们的药用产品。

20. 发明授权

US5036075A Derivatives of (AZA) naphthalensultam, their preparation and compositions containing them 失效
标题翻译：（AZA）萘磺酸的衍生物，它们的制备和含有它们的组合物
公开(公告)号：US5036075A
公开(公告)日：1991-07-30
申请号：US609506
申请日：1990-11-06
申请人： Marie-Therese Comte , Claude Gueremy , Jean-Luc Malleron , Serge Mignani , Jean-Francois Peyronel , Alain Truchon
发明人： Marie-Therese 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 of the formula: ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position.a 1-piperazinyl radical substituted in the 4-position.a piperidino radical substituted in the 4-positioneither: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, and their salts, are useful in therapy for their ability to block serotonin receptors.

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