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：US20160310483A1

公开(公告)日：2016-10-27

申请号：US15197051

申请日：2016-06-29

Applicant: Takeda Pharmaceutical Company Limited

Inventor： John David Lawson ,  Mark Sabat ,  Nicholas Scorah ,  Christopher Smith ,  Phong H. Vu ,  Haixia Wang

IPC: A61K31/4725 ,  A61K31/4439 ,  A61K31/4375

CPC classification number: A61K31/4725 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/519 ,  A61P35/02 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D471/04

Abstract: Disclosed are compounds of Formula 1, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification. 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 Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.

Abstract translation: 或其药学上可接受的盐，其中R1，R2，R3和R4在说明书中定义。 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I型超敏反应，自身免疫性疾病，炎症性疾病，癌症，非恶性增殖性疾病和其它病症的用途 与BTK相关。

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：US20150225405A1

公开(公告)日：2015-08-13

申请号：US14426369

申请日：2013-09-06

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Zacharia Cheruvallath ,  Mallareddy Komandla ,  John David Lawson ,  Christopher McBride ,  Mingnam Tang

IPC: C07D487/04 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/437 ,  A61K31/496 ,  A61K31/506 ,  A61K31/4162 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  C07D487/14 ,  C07D519/00

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein L, R1, R2, R3, R4, R5, R6, and R7 are defined in the specification. 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 obesity and related diseases, disorders, and conditions associated with MetAP2.

Abstract translation: 公开了式1的化合物及其药学上可接受的盐，其中L，R 1，R 2，R 3，R 4，R 5，R 6和R 7在本说明书中定义。 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MetAP2相关的肥胖症和相关疾病，病症和病症的用途。

公开(公告)号：US20180050051A1

公开(公告)日：2018-02-22

申请号：US15796519

申请日：2017-10-27

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Zacharia Cheruvallath ,  John David Lawson ,  Christopher McBride

IPC: A61K31/665 ,  A61K31/66 ,  C07F9/6558 ,  A61K31/683 ,  A61K45/06

CPC classification number: A61K31/665 ,  A61K31/155 ,  A61K31/192 ,  A61K31/216 ,  A61K31/336 ,  A61K31/397 ,  A61K31/4985 ,  A61K31/64 ,  A61K31/66 ,  A61K31/662 ,  A61K31/683 ,  A61K38/28 ,  A61K45/06 ,  A61P3/10 ,  C07F9/65586 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula 1, stereoisomers thereof and pharmaceutically acceptable salts of the compounds and stereoisomers, wherein R1 and R2 are defined in the specification. 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 obesity and related diseases, disorders, and conditions associated with MetAP2.

公开(公告)号：US20180015083A1

公开(公告)日：2018-01-18

申请号：US15717624

申请日：2017-09-27

Applicant: Takeda Pharmaceutical Company Limited

Inventor： John David Lawson ,  Mark Sabat ,  Nicholas Scorah ,  Christopher Smith ,  Phong H. Vu ,  Haixia Wang

IPC: A61K31/4725 ,  C07D403/14 ,  C07D401/04 ,  A61K31/4375 ,  A61K31/519 ,  A61K31/4439 ,  C07D471/04 ,  C07D401/14

CPC classification number: A61K31/4725 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/519 ,  A61P35/02 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D471/04

Abstract: Disclosed are compounds of Formula 1, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification. 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 Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.

公开(公告)号：US09827255B2

公开(公告)日：2017-11-28

申请号：US14974033

申请日：2015-12-18

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Zacharia Cheruvallath ,  John David Lawson ,  Christopher McBride

IPC: A61K31/665 ,  A61K31/683 ,  C07F9/6558 ,  A61K31/66 ,  A61K45/06

CPC classification number: A61K31/665 ,  A61K31/155 ,  A61K31/192 ,  A61K31/216 ,  A61K31/336 ,  A61K31/397 ,  A61K31/4985 ,  A61K31/64 ,  A61K31/66 ,  A61K31/662 ,  A61K31/683 ,  A61K38/28 ,  A61K45/06 ,  A61P3/10 ,  C07F9/65586 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula 1, stereoisomers thereof and pharmaceutically acceptable salts of the compounds and stereoisomers, wherein R1 and R2 are defined in the specification. 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 obesity and related diseases, disorders, and conditions associated with MetAP2.

公开(公告)号：US09475816B2

公开(公告)日：2016-10-25

申请号：US14426369

申请日：2013-09-06

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Zacharia Cheruvallath ,  Mallareddy Komandla ,  John David Lawson ,  Christopher McBride ,  Mingnam Tang

IPC: C07D487/04 ,  C07D519/00 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/437 ,  A61K31/496 ,  C07D487/14 ,  A61K31/4162 ,  A61K31/506

CPC classification number: C07D487/04 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  C07D487/14 ,  C07D519/00

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein L, R1, R2, R3, R4, R5, R6, and R7 are defined in the specification. 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 obesity and related diseases, disorders, and conditions associated with MetAP2.

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。