公开(公告)号：US20080045561A1

公开(公告)日：2008-02-21

申请号：US11692321

申请日：2007-03-28

Applicant: Conception NEMECEK ,  William METZ ,  Sylvie WENTZLER ,  Dominique LESUISSE ,  Youssef EL-AHMAD

Inventor： Conception NEMECEK ,  William METZ ,  Sylvie WENTZLER ,  Dominique LESUISSE ,  Youssef EL-AHMAD

IPC: A61K31/5375 ,  A61K31/435 ,  A61P35/00 ,  C07D413/14 ,  C07D471/02

CPC classification number: C07D519/00

Abstract: Disclosed are compounds of formula (I): wherein R1, R2, R3, R4, and R5 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and the use thereof as protein kinase inhibitors.

Abstract translation: 公开了式（I）化合物：其中R1，R2，R3，R4和R5具有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作为蛋白激酶抑制剂的用途。

公开(公告)号：US20080004300A1

公开(公告)日：2008-01-03

申请号：US11627518

申请日：2007-01-26

Applicant: Hartmut Strobel ,  Sven Ruf ,  Dominique Lesuisse ,  Conception Nemecek ,  Youssef El-Ahmad ,  Stefan Guessregen ,  Anne Lebrun ,  Kurt Ritter ,  Didier Benard ,  Augustin Hittinger ,  Herve Bouchard

Inventor： Hartmut Strobel ,  Sven Ruf ,  Dominique Lesuisse ,  Conception Nemecek ,  Youssef El-Ahmad ,  Stefan Guessregen ,  Anne Lebrun ,  Kurt Ritter ,  Didier Benard ,  Augustin Hittinger ,  Herve Bouchard

IPC: A61K31/505 ,  A61P43/00 ,  C07D239/02

CPC classification number: C07D403/04

Abstract: The invention relates to compounds of formula (I): in which R1, R2, L1, X, R3, A, R4, R4′, R4″, R4″′, R5, Y and L2 are as herein defined, salts and prodrugs thereof, to their use as protein kinase inhibitors, and to methods of treating diseases comprising adminstration thereof.

Abstract translation: 本发明涉及式（I）化合物：其中R 1，R 2，L 1，X，R 3，A，R 4，R 4， R 4，R 4，R 5，Y和L 2如本文所定义，其盐和前药，用作蛋白激酶 抑制剂，以及治疗疾病的方法，包括给药。

公开(公告)号：US20070238734A1

公开(公告)日：2007-10-11

申请号：US11608977

申请日：2006-12-11

Applicant: Conception Nemecek ,  Sylvie Wentzler ,  Corinne Venot

Inventor： Conception Nemecek ,  Sylvie Wentzler ,  Corinne Venot

IPC: A61K31/495 ,  A61P35/00

CPC classification number: A61K31/495

Abstract: The present invention concerns compounds of general formula (I): in which the substituents are as described herein.

Abstract translation: 本发明涉及通式（I）的化合物：其中取代基如本文所述。

公开(公告)号：US07119115B2

公开(公告)日：2006-10-10

申请号：US10761982

申请日：2004-01-21

Applicant: Michel Tabart ,  Eric Bacqué ,  Sylvie Wentzler ,  Cécile Combeau ,  Conception Nemecek ,  Patrick Mailliet ,  Fabienne Thompson

Inventor： Michel Tabart ,  Eric Bacqué ,  Sylvie Wentzler ,  Cécile Combeau ,  Conception Nemecek ,  Patrick Mailliet ,  Fabienne Thompson

IPC: A61K31/416 ,  C07D231/56

CPC classification number: C07D231/56 ,  C07D209/36 ,  C07D209/44 ,  C07D413/04

Abstract: The present invention relates to novel compounds derived from indazoles or indoles of formula (1) or formula (2), to methods for treating tumors or cancerous cells with compounds of formula (1) or formula (2) and to pharmacaetutical compositions comprising a pharmaceutically acceptable carrier and a compound of formula (1) or formula (2)

Abstract translation: 本发明涉及衍生自式（1）或式（2）的吲唑或吲哚的新化合物，涉及用式（1）或式（2）化合物治疗肿瘤或癌细胞的方法和药物组合物， 可接受的载体和式（1）或式（2）的化合物

公开(公告)号：US20050267304A1

公开(公告)日：2005-12-01

申请号：US10995103

申请日：2004-11-23

Applicant: Paul Cox ,  Tahir Majid ,  Justine Lai ,  Andrew Morley ,  Shelley Amendola ,  Stephanie Deprets ,  Christopher Edlin ,  Charles Gardner ,  Dorothea Kominos ,  Brian Pedgrift ,  Frank Halley ,  Timothy Gillespy ,  Michael Edwards ,  Francois Clerc ,  Conception Nemecek ,  Olivier Houille ,  Dominique Damour ,  Herve Bouchard ,  Daniel Bezard ,  Chantal Carrez

Inventor： Paul Cox ,  Tahir Majid ,  Justine Lai ,  Andrew Morley ,  Shelley Amendola ,  Stephanie Deprets ,  Christopher Edlin ,  Charles Gardner ,  Dorothea Kominos ,  Brian Pedgrift ,  Frank Halley ,  Timothy Gillespy ,  Michael Edwards ,  Francois Clerc ,  Conception Nemecek ,  Olivier Houille ,  Dominique Damour ,  Herve Bouchard ,  Daniel Bezard ,  Chantal Carrez

IPC: A61K20060101 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/541 ,  A61P20060101 ,  A61P9/00 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P13/08 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P27/14 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07D20060101 ,  C07D209/00 ,  C07D221/00 ,  C07D241/00 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  C07D487/02 ,  A61K31/4745 ,  A61K31/498 ,  C07D471/02

CPC classification number: C07D519/00 ,  C07D471/04 ,  C07D487/04

Abstract: The invention is directed to physiologically active compounds of general formula (I):— and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Abstract translation: 本发明涉及通式（I）的生理活性化合物： - 和含有这些化合物的组合物; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物，以及式（I）范围内的新化合物。 这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

公开(公告)号：US20140005189A1

公开(公告)日：2014-01-02

申请号：US14011110

申请日：2013-08-27

Applicant: Eva Albert ,  Eric Bacque ,  Conception Nemecek ,  Antonio Ugolini ,  Sylvie Wentzler

Inventor： Eva Albert ,  Eric Bacque ,  Conception Nemecek ,  Antonio Ugolini ,  Sylvie Wentzler

IPC: C07D487/04

CPC classification number: C07D487/04 ,  A61K31/5025 ,  C07D277/82 ,  C07D417/12

Abstract: The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.

Abstract translation: 本公开涉及式（I）的化合物：其中，A，W，X和Ra如本公开内容所定义，及其盐，以及包含所述化合物的药物组合物，其制备方法及其用途 作为药物，特别是作为MET抑制剂。

公开(公告)号：US08546393B2

公开(公告)日：2013-10-01

申请号：US12693736

申请日：2010-01-26

Applicant: Eva Albert ,  Eric Bacque ,  Conception Nemecek ,  Antonio Ugolini ,  Sylvie Wentzler

Inventor： Eva Albert ,  Eric Bacque ,  Conception Nemecek ,  Antonio Ugolini ,  Sylvie Wentzler

IPC: A61K31/50 ,  A61K31/495 ,  C07D487/04 ,  C07D403/12

CPC classification number: C07D487/04 ,  A61K31/5025 ,  C07D277/82 ,  C07D417/12

Abstract: The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.

公开(公告)号：US20120165326A1

公开(公告)日：2012-06-28

申请号：US13147644

申请日：2010-02-04

Applicant: Conception Nemecek ,  Antonio Ugolini ,  Eric Bacque ,  Dominique Damour ,  Gilles Barbalat ,  Sylvie Wentzler

Inventor： Conception Nemecek ,  Antonio Ugolini ,  Eric Bacque ,  Dominique Damour ,  Gilles Barbalat ,  Sylvie Wentzler

IPC: A61K31/5025 ,  A61K31/5377 ,  C07D277/82 ,  A61P35/00 ,  A61P9/00 ,  A61P3/00 ,  A61P37/08 ,  A61P11/06 ,  A61P7/02 ,  A61P25/00 ,  A61P9/10 ,  A61P3/10 ,  A61P21/00 ,  A61P17/06 ,  A61P19/02 ,  A61P35/04 ,  C07D417/12 ,  A61P29/00 ,  C07D487/04

CPC classification number: C07D277/82 ,  C07D487/04

Abstract: The invention relates to novel products of the formula (I) where: (II) is a single or double bond; F is a fluorine atom, Ra is H, HaI, alkoxy, O-cycloalkyl, —O— heterocycloalkyl; —NH-heterocycloalkyl, heteroaryl, phenyl, NHCOalk NHCOcycloalk or NR1 R2; X is S, SO or SO2, A is NH or S; W is H, alkyl, or COR with R being cycloalkyl; alkyl optionally substituted by NR3R4, alkoxy, hydroxy, phenyl, heteroaryl or heterocycloalkyl; alkoxy optionally substituted by NR3R4, i.e. a O—(CH2)n-NR3R4 radical, an O-phenyl or an O—(CH2)n-phenyl radical, with phenyl optionally substituted and n=1 to 4; or the NR1 R2 radical; R1 is H or alk and R2 is H, cycloalkyl or alkyl; R3 and R4 are H, alk, cycloalkyl, heteroaryl or phenyl; R1, R2 and/or R3, R4 form a cycle together with N optionally containing O, S, N and/or NH; heterocycloalkyl, heteroaryl and phenyl and cycles all being optionally substituted; wherein said products can be in any isomer or salt form, and can be used as drugs, in particular as MET inhibitors.

Abstract translation: 本发明涉及式（I）的新产物，其中：（II）是单键或双键; F是氟原子，R a是H，H I，烷氧基，O-环烷基，-O-杂环烷基; -NH-杂环烷基，杂芳基，苯基，NHCOalk NHCO环或NR1R2; X是S，SO或SO 2，A是NH或S; W是H，烷基或COR，其中R是环烷基; 任选被NR 3 R 4，烷氧基，羟基，苯基，杂芳基或杂环烷基取代的烷基; 任选被NR 3 R 4取代的烷氧基，即O-（CH 2）n -NR 3 R 4基团，O-苯基或O-（CH 2）n - 苯基，任选被取代且n = 1-4的苯基; 或NR1R2基团; R1是H或烷基，R2是H，环烷基或烷基; R3和R4是H，烷基，环烷基，杂芳基或苯基; R1，R2和/或R3，R4与任选含有O，S，N和/或NH的N一起形成一个循环; 杂环烷基，杂芳基和苯基，并且全部被任选取代; 其中所述产物可以是任何异构体或盐形式，并且可以用作药物，特别是作为MET抑制剂。

公开(公告)号：US20110263593A1

公开(公告)日：2011-10-27

申请号：US13007830

申请日：2011-01-17

Applicant: Eric Bacque ,  Dominique Damour ,  Conception Nemecek ,  Patrick Nemecek ,  Laurent Schio ,  Sylvie Wentzler

Inventor： Eric Bacque ,  Dominique Damour ,  Conception Nemecek ,  Patrick Nemecek ,  Laurent Schio ,  Sylvie Wentzler

IPC: A61K31/519 ,  C07D417/10 ,  A61K31/5377 ,  A61P9/00 ,  A61P7/04 ,  A61P3/00 ,  A61P37/08 ,  A61P11/06 ,  A61P7/02 ,  A61P25/00 ,  A61P9/10 ,  A61P17/06 ,  A61P29/00 ,  A61P3/10 ,  A61P21/00 ,  A61P35/00 ,  C07D471/04

CPC classification number: C07D277/82 ,  C07D487/04

Abstract: The disclosure concerns imidazo[1,2-a]pyrimidine derivatives of formula (I) and isomers and pharmaceutically acceptable salts thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed.

Abstract translation: 本公开涉及式（I）的咪唑并[1,2-a]嘧啶衍生物及其异构体及其药学上可接受的盐。 还公开了制备化合物的方法，药物组合物和治疗方法。

公开(公告)号：US20100298315A1

公开(公告)日：2010-11-25

申请号：US12693736

申请日：2010-01-26

Applicant: Eva ALBERT ,  Eric BACQUE ,  Conception NEMECEK ,  Antonio UGOLINI ,  Sylvie WENTZLER

Inventor： Eva ALBERT ,  Eric BACQUE ,  Conception NEMECEK ,  Antonio UGOLINI ,  Sylvie WENTZLER

IPC: A61K31/5377 ,  C07D487/04 ,  A61K31/5025 ,  C07D413/14 ,  A61P35/00 ,  A61P3/00 ,  A61P7/02 ,  A61P11/06 ,  A61P19/02 ,  A61P25/00 ,  A61P17/06 ,  C12N5/02

CPC classification number: C07D487/04 ,  A61K31/5025 ,  C07D277/82 ,  C07D417/12

Abstract: The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.

Abstract translation: 本公开涉及式（I）的化合物：其中，A，W，X和Ra如本公开内容所定义，及其盐，以及包含所述化合物的药物组合物，其制备方法及其用途 作为药物，特别是作为MET抑制剂。