公开(公告)号：EP2955181A1

公开(公告)日：2015-12-16

申请号：EP14748793.8

申请日：2014-02-05

申请人： Nissan Chemical Industries, Ltd.

发明人： TAKAHASHI, Keiji ,  WATANABE, Tsuneo ,  HAYASHI, Keishi ,  KURIHARA, Kazunori ,  NAKAMURA, Takanori ,  YAMAMOTO, Akio ,  NISHIMURA, Takuya ,  KAMIYAMA, Toshihiko ,  HIDAKA, Yuuki

IPC分类号： C07D471/14 ,  A61K31/519 ,  A61P29/00 ,  A61P43/00

摘要： To provide a novel tricyclic pyrrolopyridine compound having a JAK inhibitory activity and useful for prevention, treatment and/or improvement of particularly autoimmune diseases, inflammatory diseases and allergic diseases.
A novel tricyclic pyrrolopyridine compound represented by the formula (I), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof:

wherein the respective substituents are defined in detail in the specification, and R 1 is a C 1-6 alkyl group or the like, R 2 is a hydrogen atom or the like, R 3 is a hydrogen atom or the like, the ring A is C 3-11 cycloalkane or the like, L 1 is a C 1-6 alkylene group or the like, and R 4 is NR a R b or the like.

摘要翻译： 提供具有JAK抑制活性的新型三环吡咯并吡啶化合物，可用于预防，治疗和/或改善特别是自身免疫性疾病，炎性疾病和过敏性疾病。 由式（I）表示的新型三环吡咯并吡啶化合物，该化合物的互变异构体或药学上可接受的盐或其溶剂化物：其中各个取代基在说明书中详细定义，并且R 1是C 1-6烷基或 R 2为氢原子等，R 3为氢原子等，环A为C 3-11环烷烃等，L 1为C 1-6亚烷基等，R 4为NR a R b或 喜欢。

公开(公告)号：EP3144309A1

公开(公告)日：2017-03-22

申请号：EP15791895.4

申请日：2015-05-11

申请人： Nissan Chemical Industries, Ltd.

发明人： WATANABE, Tsuneo ,  TAKAHASHI, Keiji ,  HAYASHI, Keishi ,  NAKAMURA, Takanori ,  MINAMI, Masataka ,  KURIHARA, Kazunori ,  YAMAMOTO, Akio ,  NISHIMURA, Takuya ,  UNI, Miyuki ,  KAMIYAMA, Toshihiko ,  IWAMOTO, Shunsuke

IPC分类号： C07D471/14 ,  A61K31/4375 ,  A61K31/519 ,  A61P29/00 ,  A61P43/00

CPC分类号： C07D471/14 ,  A61K31/4375 ,  A61K31/519 ,  Y02P20/55

摘要： Novel tricyclic compounds which have JAK inhibitory activities are useful for prevention, treatment or improvement of autoimmune diseases, inflammatory diseases and allergic diseases are provided.
Novel tricyclic compound represented by the formula (I), the formula (II) or the formula (III) (wherein : each of A 1 , A 2 and A 3 is a cyclohexane-1,4-diyl group or the like; each of L 1 , L 2 and L 3 is a methylene group or the like; each of X 1 and X 3 is O or NH; each of R 1 and R 3 is a cyano C 1-6 haloalkyl group or the like; and R 2 is an aromatic heterocyclic group), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof.

摘要翻译： 具有JAK抑制活性的新型三环化合物可用于预防，治疗或改善自身免疫疾病，炎性疾病和过敏性疾病。 由式（I），式（II）或式（III）表示的新型三环化合物（其中：A 1，A 2和A 3各自为环己烷-1,4-二基等; 的L 1，L 2和L 3是亚甲基等; X 1和X 3各自为O或NH; R 1和R 3各自为氰基C 1-6卤代烷基等;以及 R 2是芳族杂环基），化合物的互变异构体或药学上可接受的盐或其溶剂合物。