公开(公告)号：EP1382603A1

公开(公告)日：2004-01-21

申请号：EP02722791.7

申请日：2002-04-25

申请人： Eisai Co., Ltd.

发明人： YOSHIDA, Ichiro ,  YONEDA, Naoki ,  OHASHI, Yoshiaki ,  SUZUKI, Shuichi ,  MIYAMOTO, Mitsuaki ,  MIYAZAKI, Futoshi ,  SESHIMO, Hidenori ,  KAMATA, Junichi ,  TAKASE, Yasutaka ,  SHIRATO, Manabu ,  SHIMOKUBO, Daiya ,  SAKUMA, Yoshinori ,  YOKOHAMA, Hiromitsu

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D413/04 ,  C07D471/04 ,  C07F5/02 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5415 ,  A61K31/551 ,  A61P1/04 ,  A61P3/04 ,  A61P11/00

CPC分类号： C07D401/04 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5415 ,  A61K31/551 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04 ,  C07F5/025 ,  Y02P20/55

摘要： The present invention provides a compound having an excellent inhibitory action on activation of STAT6 and a pharmaceutical composition thereof. Inparticular, it provides a compound represented by the following formula (I), a salt thereof or a hydrate of them.
In the formula, X represents a nitrogen-containing condensed aromatic heterocyclic group such as imidazo[1,2-a]pyridine, benzimidazole, quinazoline, quinoline, or 2,1-benzisoxazole and has (R 4 ) n as substituent groups; Y represents a C 3-8 cycloalkyl group, C 4-8 cycloalkenyl group, 5- to 14-membered non-aromatic heterocyclic group, C 6-14 aromatic hydrocarbon cyclic group or 5- to 14-membered aromatic heterocyclic group; n in (R 4 ) n is 0, 1, 2 or 3, and Z groups independently represent (1) hydrogen atom, (2) amino group, (3) halogen atom, (4) hydroxyl group, (5) nitro group, (6) cyano group, (7) azido group, (8) formyl group, (9) hydroxyamino group, (10) sulfamoyl group, (11) guanodino group, (12) oxo group, (13) C 2-6 alkenyl group, (14) C 1-6 alkoxy group, (15) C 1-6 alkylhydroxyamino group, (16) halogenated C 1-6 alkyl group, (17) halogenated C 2-6 alkenyl group, (18) (i) C 3-7 cycloalkyl group, (ii) C 3-7 cycloalkenyl group, (iii) 5- to 14-membered non-aromatic heterocyclic group, each of which may have one or more substituent groups Q, or (19) formula -M 1 -M 2 -M 3 , R 1 represents (1) hydrogen atom, (2) halogen atom, (3) hydroxyl group, (4) nitro group, (5) cyano group, (6) halogenated C 1-6 alkyl group, (7) C 2-6 alkyl group substituted with a hydroxyl or cyano group, (8) C 2-6 alkenyl group, or (9) formula -L 1 -L 2 -L 3 , and R 2 represents a hydrogen atom or a protecting group; and R 3 represents a hydrogen atom, halogen atom, cyano group, amino group, C 1-4 alkyl group or halogenated C 1-4 alkyl group.

摘要翻译： 本发明提供具有上STAT6活化优异的抑制作用和它们的药物组合物的化合物。 Inparticular，它提供了由下式（I）表示的化合物，其盐或它们的水合物。 在该式中，X darstellt含氮稠环芳香杂环基团：如imidazoÄ1,2-aÜpyridine，苯并咪唑，喹唑啉，喹啉，或2,1-苯并异恶唑和具有（R <4>）n的取代基; Y表示C 3-8环烷基，C 4-8环烯基，5至14元非芳香族杂环基，C 6-14的芳香族烃环基团或5-至14-元芳族杂环基团; n的（R <4>）n为0，1，2或3，和Z基团独立地代表（1）氢原子，（2）氨基，（3）卤素原子，（4）羟基，（5） 硝基，（6）氰基，（7）叠氮基，（8）甲酰基，（9）羟基，（10）氨磺酰基，（11）鸟粪恐龙基，（12）氧代基团，（13）C 2 -C 6烯基，（14）C1-6烷氧基，（15）C 1-6烷基羟氨基基团，（16）卤代C 1-6烷基，（17）卤代C2-6链烯基，（18）（ⅰ）C3 3-7环基，（ⅱ）C3-7cycloalkenyl基，（ⅲ）5-至14-元非芳族杂环基团，其中的每一个可以具有一个或多个取代基Q，或（19）式-M <1> -M <2> -M <3>，R <1>表示（1）氢原子，（2）卤素原子，（3）羟基，（4）硝基，（5）氰基，（6）卤代的C1 6烷基，（7）C2-6烷基substituiertem用羟基或氰基，（8）C2-6链烯基，或（9）式-L <1> -L <2> -L <3>， 且R <2> darstellt一个氢原子或一个保护基团; 且R <3> darstellt一个氢原子，卤素原子，氰基，氨基，C 1-4烷基或卤代C 1-4烷基。