公开(公告)号：US09365566B2

公开(公告)日：2016-06-14

申请号：US14381187

申请日：2013-03-25

Applicant: Takeda Pharmaceutical Company Limited

Inventor： John David Lawson ,  Mark Sabat ,  Christopher Smith ,  Haixia Wang ,  Young K. Chen ,  Toufike Kanouni

IPC: C07D471/04 ,  C07D413/14 ,  C07D401/04 ,  C07D403/04 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  A61K31/502 ,  A61K31/5377 ,  A61K45/06 ,  C07D403/14 ,  C07D405/14

CPC classification number: C07D471/04 ,  A61K31/502 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  Y02A50/401

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined in the specification. The compounds are inhibitors of Bruton's tyrosine kinase (BTK). This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders or conditions associated with BTK.

Abstract translation: 公开了式1的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5在本说明书中定义。 这些化合物是Bruton酪氨酸激酶（BTK）的抑制剂。 本公开还涉及用于制备式1化合物的材料和方法，含有它们的药物组合物及其用于治疗与BTK相关的疾病，病症或病症的用途。

公开(公告)号：US20150038510A1

公开(公告)日：2015-02-05

申请号：US14381187

申请日：2013-03-25

Applicant: Takeda Pharmaceutical Company Limited

Inventor： John David Lawson ,  Mark Sabat ,  Christopher Smith ,  Haixia Wang ,  Young K. Chen ,  Toufike Kanouni

IPC: C07D471/04 ,  A61K31/502 ,  C07D403/04 ,  C07D409/14 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  A61K31/5377 ,  A61K45/06

CPC classification number: C07D471/04 ,  A61K31/502 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  Y02A50/401

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined in the specification. The compounds are inhibitors of Bruton's tyrosine kinase (BTK). This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders or conditions associated with BTK.

Abstract translation: 公开了式1的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5在本说明书中定义。 这些化合物是Bruton酪氨酸激酶（BTK）的抑制剂。 本公开还涉及用于制备式1化合物的材料和方法，含有它们的药物组合物及其用于治疗与BTK相关的疾病，病症或病症的用途。

公开(公告)号：US20130184252A1

公开(公告)日：2013-07-18

申请号：US13787514

申请日：2013-03-06

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： John David Lawson ,  Toufike Kanouni ,  Michael B. Wallace ,  Qing Dong

IPC: A61K31/541 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  C07D471/16 ,  A61K31/4375

CPC classification number: A61K31/541 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  C07D471/16

Abstract: Disclosed are JAK inhibitors of formula I where G1, R1, R2, R3, R4, R5, R6, and R7 are defined in the specification. Also disclosed are pharmaceutical compositions, kits and articles of manufacture which contain the compounds, methods and materials for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other diseases, disorders or conditions associated with JAK.

Abstract translation: 公开了式I中的JAK抑制剂，其中在说明书中定义了G1，R1，R2，R3，R4，R5，R6和R7。 还公开了含有化合物的化合物，制备该化合物的方法和材料的药物组合物，试剂盒和制品，以及使用该化合物治疗涉及免疫系统和炎症的疾病，病症和病症的方法，包括类风湿性关节炎，血液学 恶性肿瘤，上皮癌（即癌）以及与JAK有关的其他疾病，病症或病症。

公开(公告)号：US08785429B2

公开(公告)日：2014-07-22

申请号：US13787514

申请日：2013-03-06

Applicant: Takeda Pharmaceutical Company Limited

Inventor： John David Lawson ,  Toufike Kanouni ,  Michael B. Wallace ,  Qing Dong

IPC: A61K31/4375 ,  A61K31/407 ,  A61K31/5025 ,  C07D471/16

CPC classification number: A61K31/541 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  C07D471/16

Abstract: Disclosed are JAK inhibitors of formula I where G1, R1, R2, R3, R4, R5, R6, and R7 are defined in the specification. Also disclosed are pharmaceutical compositions, kits and articles of manufacture which contain the compounds, methods and materials for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other diseases, disorders or conditions associated with JAK.

Abstract translation: 公开了式I中的JAK抑制剂，其中在说明书中定义了G1，R1，R2，R3，R4，R5，R6和R7。 还公开了含有化合物的化合物，制备该化合物的方法和材料的药物组合物，试剂盒和制品，以及使用该化合物治疗涉及免疫系统和炎症的疾病，病症和病症的方法，包括类风湿性关节炎，血液学 恶性肿瘤，上皮癌（即癌）以及与JAK有关的其他疾病，病症或病症。