公开(公告)号：US20120165326A1

公开(公告)日：2012-06-28

申请号：US13147644

申请日：2010-02-04

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

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

IPC分类号： 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分类号： C07D277/82 ,  C07D487/04

摘要： 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.

摘要翻译： 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。