公开(公告)号：US08349857B2

公开(公告)日：2013-01-08

申请号：US13359326

申请日：2012-01-26

申请人： Masaharu Kume ,  Kenji Matsuo ,  Naoki Omori ,  Masami Takayama ,  Aiko Omori ,  Takeshi Endo

发明人： Masaharu Kume ,  Kenji Matsuo ,  Naoki Omori ,  Masami Takayama ,  Aiko Omori ,  Takeshi Endo

IPC分类号： A01N43/54 ,  A61K31/517 ,  C07D239/72

CPC分类号： C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D407/12 ,  C07D417/12

摘要： A compound which inhibits both of EGF receptor tyrosine kinase and HER2 tyrosine kinase is provided.A compound represented by the general formula (I): wherein RX is a group represented by the formula: wherein R1 is a hydrogen atom, optionally substituted alkyl, etc.; Z is —O—, —N(R10)—, etc.; R10 is a hydrogen atom, alkyl, etc.; R2 is a hydrogen atom, optionally substituted alkyl, etc.; R18 is a hydrogen atom, optionally substituted alkyl, etc.; R19 is optionally substituted alkyl, etc.; W1 is an optionally substituted non-aromatic nitrogen-containing group; R17 is a hydrogen atom, optionally substituted alkyl, etc.; R3 and R4 are independently a hydrogen atom, optionally substituted alkyl, etc.; X is —O—, —S—, or —N(R12)—, etc.; R12 is a hydrogen atom, alkyl, etc.; and A is phenyl optionally having a substituent, etc., its pharmaceutically acceptable salt, or a solvate thereof.

摘要翻译： 提供抑制EGF受体酪氨酸激酶和HER2酪氨酸激酶两者的化合物。 由通式（I）表示的化合物：其中RX是由下式表示的基团：其中R1是氢原子，任选取代的烷基等; Z是-O - ， - N（R 10） - 等; R10是氢原子，烷基等; R2是氢原子，任选取代的烷基等; R18是氢原子，任意取代的烷基等; R19是任选取代的烷基等; W1是任选取代的非芳族含氮基团; R 17是氢原子，任选取代的烷基等; R3和R4独立地是氢原子，任选取代的烷基等; X是-O-，-S-或-N（R 12） - 等; R12是氢原子，烷基等; 和A是任选具有取代基的苯基等，其药学上可接受的盐或其溶剂合物。

公开(公告)号：US20120123114A1

公开(公告)日：2012-05-17

申请号：US13359326

申请日：2012-01-26

申请人： Masaharu KUME ,  Kenji MATSUO ,  Naoki OMORI ,  Masami TAKAYAMA ,  Aiko OMORI ,  Takeshi ENDO

发明人： Masaharu KUME ,  Kenji MATSUO ,  Naoki OMORI ,  Masami TAKAYAMA ,  Aiko OMORI ,  Takeshi ENDO

IPC分类号： C07D417/12 ,  C07D239/94 ,  C07D403/12 ,  C07D413/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/14 ,  C07D413/14 ,  C07D403/14 ,  C07D401/12 ,  C07D401/14

CPC分类号： C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D407/12 ,  C07D417/12

摘要： A compound which inhibits both of EGF receptor tyrosine kinase and HER2 tyrosine kinase is provided.A compound represented by the general formula (I): wherein RX is a group represented by the formula: wherein R1 is a hydrogen atom, optionally substituted alkyl, etc.; Z is —O—, —N(R10)—, etc.; R10 is a hydrogen atom, alkyl, etc.; R2 is a hydrogen atom, optionally substituted alkyl, etc.; R18 is a hydrogen atom, optionally substituted alkyl, etc.; R19 is optionally substituted alkyl, etc.; W1 is an optionally substituted non-aromatic nitrogen-containing group; R17 is a hydrogen atom, optionally substituted alkyl, etc.; R3 and R4 are independently a hydrogen atom, optionally substituted alkyl, etc.; X is —O—, —S—, or —N(R12)—, etc.; R12 is a hydrogen atom, alkyl, etc.; and A is phenyl optionally having a substituent, etc., its pharmaceutically acceptable salt, or a solvate thereof.

摘要翻译： 提供抑制EGF受体酪氨酸激酶和HER2酪氨酸激酶两者的化合物。 由通式（I）表示的化合物：其中RX是由下式表示的基团：其中R1是氢原子，任选取代的烷基等; Z是-O - ， - N（R 10） - 等; R10是氢原子，烷基等; R2是氢原子，任选取代的烷基等; R18是氢原子，任意取代的烷基等; R19是任选取代的烷基等; W1是任选取代的非芳族含氮基团; R 17是氢原子，任选取代的烷基等; R3和R4独立地是氢原子，任选取代的烷基等; X是-O-，-S-或-N（R 12） - 等; R12是氢原子，烷基等; 和A是任选具有取代基的苯基等，其药学上可接受的盐或其溶剂合物。