公开(公告)号：US20150274723A1

公开(公告)日：2015-10-01

申请号：US14706876

申请日：2015-05-07

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Mark E. Adams ,  Rongliang Chen ,  Betty Lam ,  Matthew Lardy ,  Srinivasa Reddy Natala ,  Steven James Wilkens ,  Mitsunori Kono ,  Zhe Nie

IPC: C07D471/04 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/4985 ,  A61K31/437 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/5383 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, p, R1, R2, R3a, R4, and R5 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 disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, cancer, 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，p，R1，R2，R3a，R4和R5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，癌症和其它疾病 ，疾病和表示SYK抑制的病症。

公开(公告)号：US11786608B2

公开(公告)日：2023-10-17

申请号：US17145006

申请日：2021-01-08

Applicant: Takeda Pharmaceutical Company Limited ,  Rongliang Chen ,  Padma Manam ,  Lu Zeng

Inventor： Rongliang Chen ,  Padma Manam ,  Lu Zeng

IPC: A61K47/69 ,  C07D401/14 ,  A61K31/4725 ,  A61K31/519 ,  C08B37/16

CPC classification number: A61K47/6951 ,  A61K31/4725 ,  A61K31/519 ,  C07D401/14 ,  C08B37/0015

Abstract: Disclosed is a complex of a compound of Formula 1,




a stereoisomer thereof, or a tautomer of the compound of Formula 1 or stereoisomer thereof, and a cyclodextrin, in which the complex is an amorphous solid. This disclosure also relates to materials and methods for preparing the complex, to pharmaceutical compositions which contain the complex, and to the use of the complex to treat Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.

公开(公告)号：US20200339573A1

公开(公告)日：2020-10-29

申请号：US16870653

申请日：2020-05-08

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Rongliang Chen ,  Tomonori Ichibakase ,  Chunrong Ma ,  Christopher F. Matthews ,  Hajime Motoyoshi ,  Colin O'Bryan ,  Kentaro Yaji ,  Naoki Yoshikawa

IPC: C07D471/04 ,  A61K9/20 ,  A61K9/48

Abstract: Disclosed are chemical entities which are inhibitors of spleen tyrosine kinase (SYK), namely, chemical entities comprising 6-((1R,2S)-2-aminocyclohexylamino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]pyridine-3(2H)-one and certain solid state forms thereof. Also disclosed are methods of using the chemical entities to treat disorders such as a cancer.

公开(公告)号：US10676473B2

公开(公告)日：2020-06-09

申请号：US14973180

申请日：2015-12-17

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Rongliang Chen ,  Tomonori Ichibakase ,  Chunrong Ma ,  Christopher F. Matthews ,  Hajime Motoyoshi ,  Colin O'Bryan ,  Kentaro Yaji ,  Naoki Yoshikawa

IPC: C07D471/04 ,  A61K9/20 ,  A61K9/48

Abstract: Disclosed are chemical entities which are inhibitors of spleen tyrosine kinase (SYK), namely, chemical entities comprising 6-((1R,2S)-2-aminocyclohexylamino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]pyridine-3(2H)-one and certain solid state forms thereof. Also disclosed are methods of using the chemical entities to treat disorders such as a cancer.

公开(公告)号：US20170327497A1

公开(公告)日：2017-11-16

申请号：US15599337

申请日：2017-05-18

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Mark E. Adams ,  Rongliang Chen ,  Betty Lam ,  Matthew Lardy ,  Srinivasa Reddy Natala ,  Steven James Wilkens ,  Mitsunori Kono ,  Zhe Nie

IPC: C07D471/04 ,  C07D498/04 ,  C07D495/04 ,  C07D487/04 ,  A61K31/5383 ,  A61K31/5365 ,  A61K31/519 ,  A61K31/4985 ,  A61K31/437 ,  C07D519/00 ,  A61K31/4365

CPC classification number: C07D471/04 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/5383 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, p, R1, R2, R3a, R4, and R5 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 disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, cancer, and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

公开(公告)号：US20210138086A1

公开(公告)日：2021-05-13

申请号：US17145006

申请日：2021-01-08

Applicant: Rongliang Chen ,  Padma Manam ,  Lu Zeng ,  Takeda Pharmaceutical Company Limited

Inventor： Rongliang Chen ,  Padma Manam ,  Lu Zeng

IPC: A61K47/69 ,  C08B37/16 ,  C07D401/14 ,  A61K31/4725 ,  A61K31/519

Abstract: Disclosed is a complex of a compound of Formula 1, a stereoisomer thereof, or a tautomer of the compound of Formula 1 or stereoisomer thereof, and a cyclodextrin, in which the complex is an amorphous solid. This disclosure also relates to materials and methods for preparing the complex, to pharmaceutical compositions which contain the complex, and to the use of the complex to treat Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.

公开(公告)号：US20160176869A1

公开(公告)日：2016-06-23

申请号：US14973180

申请日：2015-12-17

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Rongliang Chen ,  Tomonori ICHIBAKASE ,  Chunrong MA ,  Christopher MATTHEWS ,  Hajime MOTOYOSHI ,  Colin O'BRYAN ,  Kentaro YAJI ,  Naoki YOSHIKAWA

IPC: C07D471/04 ,  A61K9/20 ,  A61K9/48

Abstract: Disclosed are chemical entities which are inhibitors of spleen tyrosine kinase (SYK), namely, chemical entities comprising 6-((1R,2S)-2-aminocyclohexylamino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]pyridine-3(2H)-one and certain solid state forms thereof. Also disclosed are methods of using the chemical entities to treat disorders such as a cancer.

Abstract translation: 公开了作为脾脏酪氨酸激酶（SYK）抑制剂的化学实体，即包含6 - （（1R，2S）-2-氨基环己基氨基）-7-氟-4-（1-甲基-1H-吡唑-4-基） - 基）-1H-吡咯并[3,4-c]吡啶-3（2H） - 酮及其某些固体形式。 还公开了使用化学实体来治疗诸如癌症的疾病的方法。