公开(公告)号：US09045496B2

公开(公告)日：2015-06-02

申请号：US14313259

申请日：2014-06-24

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Edcon Chang ,  Tony Gibson ,  Bohan Jin ,  Nicholas Scorah ,  Qing Dong

IPC: A61K31/5383 ,  C07D498/14 ,  A61K45/06

CPC classification number: C07D498/14 ,  A61K31/5383 ,  A61K45/06

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3, G1, G2, and m 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 inflammatory disorders, cardiovascular disease, cancer, and other conditions associated with PI3Kδ.

Abstract translation: 公开了式1的化合物及其药学上可接受的盐，其中Ar，R1，R2，R3，G1，G2和m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与PI3Kδ相关的炎性疾病，心血管疾病，癌症和其它病症的用途。

公开(公告)号：US20140309219A1

公开(公告)日：2014-10-16

申请号：US14313259

申请日：2014-06-24

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Edcon Chang ,  Tony Gibson ,  Bohan Jin ,  Nicholas Scorah ,  Qing Dong

IPC: C07D498/14 ,  A61K45/06 ,  A61K31/5383

CPC classification number: C07D498/14 ,  A61K31/5383 ,  A61K45/06

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3, G1, G2, and m 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 inflammatory disorders, cardiovascular disease, cancer, and other conditions associated with PI3Kδ.

Abstract translation: 公开了式1的化合物及其药学上可接受的盐，其中Ar，R1，R2，R3，G1，G2和m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与PI3Kδ相关的炎性疾病，心血管疾病，癌症和其它病症的用途。

公开(公告)号：US09108970B2

公开(公告)日：2015-08-18

申请号：US13886032

申请日：2013-05-02

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Yasuyoshi Arikawa ,  Benjamin Jones ,  Betty Lam ,  Christopher Smith ,  Masashi Takahashi ,  Qing Dong ,  Victoria Feher ,  Zhe Nie

IPC: C07D471/04 ,  A61K31/437 ,  A61P11/06 ,  A61P35/00 ,  A61P17/06 ,  A61P29/00 ,  A61P11/08 ,  A61P37/02 ,  A61K31/527 ,  A61K45/06 ,  C07D487/10 ,  C07D519/00 ,  C07D487/04 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  A61K31/527 ,  A61K45/06 ,  C07D471/04 ,  C07D487/10 ,  C07D519/00

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

Abstract translation: 公开了式1的化合物及其药学上可接受的盐，其中G，L1，L2，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涉及免疫系统和炎症的疾病，疾病和病症的用途，包括类风湿性关节炎，血液恶性肿瘤，上皮癌（即， 癌症）以及其它疾病，疾病和表示SYK抑制的病症。

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。

公开(公告)号：US20150336964A1

公开(公告)日：2015-11-26

申请号：US14814878

申请日：2015-07-31

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Yasuyoshi Arikawa ,  Benjamin Jones ,  Betty Lam ,  Christopher Smith ,  Masashi Takahashi ,  Qing Dong ,  Victoria Feher ,  Zhe Nie

IPC: C07D487/04 ,  A61K45/06 ,  A61K31/527 ,  A61K31/437 ,  C07D487/10 ,  A61K31/519 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  A61K31/527 ,  A61K45/06 ,  C07D471/04 ,  C07D487/10 ,  C07D519/00

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

Abstract translation: 公开了式1的化合物及其药学上可接受的盐，其中G，L1，L2，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涉及免疫系统和炎症的疾病，疾病和病症的用途，包括类风湿性关节炎，血液恶性肿瘤，上皮癌（即， 癌症）以及其它疾病，疾病和表示SYK抑制的病症。

公开(公告)号：US20180141951A1

公开(公告)日：2018-05-24

申请号：US15681953

申请日：2017-08-21

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Yasuyoshi Arikawa ,  Benjamin Jones ,  Betty Lam ,  Masashi Takahashi ,  Christopher Smith ,  Qing Dong ,  Victoria Feher ,  Zhe Nie

IPC: C07D487/04 ,  C07D519/00 ,  C07D487/10 ,  C07D471/04 ,  A61K31/437 ,  A61K31/527 ,  A61K31/519 ,  A61K45/06

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  A61K31/527 ,  A61K45/06 ,  C07D471/04 ,  C07D487/10 ,  C07D519/00

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

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。