公开(公告)号：US07354933B2

公开(公告)日：2008-04-08

申请号：US10770382

申请日：2004-02-02

Applicant: 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

Inventor： 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: C07D401/06 ,  C07D403/06 ,  A61K31/41

CPC classification number: C07D401/06 ,  C07D401/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07232833B2

公开(公告)日：2007-06-19

申请号：US10810711

申请日：2004-03-26

Applicant: Antony Bigot ,  Youssef El-Ahmad ,  Jean-Luc Malleron ,  Jean-Paul Martin ,  Serge Mignani ,  Guy Pantel ,  Baptiste Ronan ,  Michel Tabart ,  Michel Cheve ,  Fabrice Viviani

Inventor： Antony Bigot ,  Youssef El-Ahmad ,  Jean-Luc Malleron ,  Jean-Paul Martin ,  Serge Mignani ,  Guy Pantel ,  Baptiste Ronan ,  Michel Tabart ,  Michel Cheve ,  Fabrice Viviani

IPC: A61K31/47 ,  A61K31/517 ,  A61K31/44 ,  A61K31/50 ,  A61K31/54

CPC classification number: C07D401/06 ,  C07D409/14 ,  C07D413/06

Abstract: The invention relates to 4-substituted quinoline compounds of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 and X5 is C—R′1, to C—R′5 respectively, or alternatively at most one represents N, Y represents CHR, CO, CROH, CRNH2, CRF or CF2, R being a hydrogen or alkyl, m is 1, 2 or 3 and n is 0, 1 or 2, Z is CH2 or Z is O, S, SO, SO2 and, in this case, n is equal to 2, R2 is —CO2R, —CH2CO2R, —CH2—CH2CO2R, —CH2OH or —CH2—CH2OH, wherein R is 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.

Abstract translation: 本发明涉及以下通式的4-取代喹啉化合物：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分别为C-R'1，C-R'5， 或者至多一个表示N，Y表示CHR，CO，CROH，CRNH 2，CRF或CF 2，R为氢或烷基，m为1,2 或3，n为0,1或2，Z为CH 2或Z为O，S，SO，SO 2，在这种情况下，n等于 2，R 2是-CO 2 R，-CH 2 CO 2 R，-CH 2， 2个-CH 2 CO 2 R 2，-CH 2 OH或-CH 2 -CH（CH 2） R 2 OH，其中R如上所定义，R 3表示苯基，杂芳基或烷基-SO 3 - ， - 其中烷基是烷基，R 3 O 3表示各种基团，其中适当地含有它们的对映体或非对映异构形式或其混合物中的氧，硫或胺， d /或适当时以合成或反式形式或其混合物及其盐。

公开(公告)号：US20050165005A1

公开(公告)日：2005-07-28

申请号：US10997736

申请日：2004-11-24

Applicant: 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

Inventor： 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: 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 classification number: C07D231/12 ,  C07D231/14 ,  C07D231/20 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D409/04 ,  C07D453/02 ,  C07D453/06 ,  C07D487/08

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US06403610B1

公开(公告)日：2002-06-11

申请号：US09664959

申请日：2000-09-18

Applicant: Jean-Luc Malleron ,  Michel Tabart ,  Jean-Christophe Carry ,  Michel Evers ,  Youssef El Ahmad ,  Serge Mignani ,  Fabrice Viviani ,  Michel Cheve

Inventor： Jean-Luc Malleron ,  Michel Tabart ,  Jean-Christophe Carry ,  Michel Evers ,  Youssef El Ahmad ,  Serge Mignani ,  Fabrice Viviani ,  Michel Cheve

IPC: A61K3147

CPC classification number: C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D417/14

Abstract: Quinolylpropylpiperidine derivatives of formula (I) which are particularly advantageous antimicrobial agents, their compositions, and their use.

Abstract translation: 式（I）的喹啉基丙基哌啶衍生物，其是特别有利的抗微生物剂，它们的组成及其用途。