公开(公告)号：US20160221989A1

公开(公告)日：2016-08-04

申请号：US14817416

申请日：2015-08-04

Applicant: Pfizer Inc.

Inventor： Sharanjeet Kaur Bagal ,  Kiyoyuki Omoto ,  Sarah Elizabeth Skerratt ,  Jingrong Jean Cui ,  Samantha Elizabeth Greasley ,  Indrawan James McAlpine ,  Asako Nagata ,  Sacha Ninkovic ,  Michelle Bich Tran-Dubé

IPC: C07D401/12 ,  A61K31/4439

CPC classification number: C07D401/12 ,  A61K31/4439

Abstract: The present invention relates to compounds of Formula I described herein and their pharmaceutically acceptable salts, and their use in medicine, in particular as Trk antagonists.

Abstract translation: 本发明涉及本文所述的式I化合物及其药学上可接受的盐，以及它们在医药中的用途，特别是作为Trk拮抗剂。

公开(公告)号：US20210261530A1

公开(公告)日：2021-08-26

申请号：US17235836

申请日：2021-04-20

Applicant: Pfizer Inc.

Inventor： Douglas Carl Behenna ,  Kevin Daniel Freeman-Cook ,  Robert Louis Hoffman ,  Asako Nagata ,  Sacha Ninkovic ,  Scott Channing Sutton

IPC: C07D403/12 ,  A61P35/00 ,  C07D413/12

Abstract: This invention relates to compounds of Formula (I) and enantiomers thereof, and to pharmaceutically acceptable salts of Formula (I) and said enantiomers, wherein R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions comprising such compounds and salts, and to methods and uses of such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject in need thereof.

公开(公告)号：US10800783B2

公开(公告)日：2020-10-13

申请号：US16251032

申请日：2019-01-17

Applicant: Pfizer Inc.

Inventor： Douglas Carl Behenna ,  Ping Chen ,  Kevin Daniel Freeman-Cook ,  Robert Louis Hoffman ,  Mehran Jalaie ,  Asako Nagata ,  Sajiv Krishnan Nair ,  Sacha Ninkovic ,  Martha Alicia Ornelas ,  Cynthia Louise Palmer ,  Eugene Yuanjin Rui

IPC: A61K31/519 ,  A61K31/4375 ,  A61K31/4545 ,  C07D487/04 ,  C07D401/12 ,  C07D471/04 ,  C07D401/14

Abstract: This invention relates to compounds of general Formula (I) and pharmaceutically acceptable salts thereof, in which R1, R2, R2A, R2B, R3, R4, R5A, R5B, R6, R7, R8, R9, p, q and r are as defined herein, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.

公开(公告)号：US20200247784A1

公开(公告)日：2020-08-06

申请号：US16774786

申请日：2020-01-28

Applicant: Pfizer Inc.

Inventor： Douglas Carl Behenna ,  Kevin Daniel Freeman-Cook ,  Robert Louis Hoffman ,  Asako Nagata ,  Sacha Ninkovic ,  Scott Channing Sutton

IPC: C07D403/12 ,  C07D413/12 ,  A61P35/00

Abstract: This invention relates to compounds of Formula (I) and enantiomers thereof, and to pharmaceutically acceptable salts of Formula (I) and said enantiomers, wherein R1, R2 and R3 are as defined herein. The invention further relates to pharmaceutical compositions comprising such compounds and salts, and to methods and uses of such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject in need thereof.

公开(公告)号：US10544095B2

公开(公告)日：2020-01-28

申请号：US15749963

申请日：2016-08-04

Applicant: Pfizer Inc. ,  iTeos Therapeutics

Inventor： Sacha Ninkovic ,  Michael Raymond Collins ,  Stefano Crosignani ,  Andreas Maderna ,  Indrawan James McAlpine ,  Stephanie Anne Scales ,  Martin Wythes

IPC: A61K31/404 ,  C07D209/10 ,  C07D209/18 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D413/12 ,  A61P25/28 ,  A61P35/02 ,  A61P25/24 ,  A61P25/16 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D405/12

Abstract: A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula I.

公开(公告)号：US20160272628A1

公开(公告)日：2016-09-22

申请号：US15072534

申请日：2016-03-17

Applicant: Pfizer Inc. ,  iTeos Therapeutics

Inventor： Sacha Ninkovic ,  Stefano Crosignani ,  lndrawan James McAlpine ,  Michael Raymond Collins ,  Stephanie Anne Scales ,  Andreas Maderna ,  Martin Wythes

IPC: C07D417/04 ,  C07D417/14

CPC classification number: C07D417/04 ,  A61K31/404 ,  C07D417/12 ,  C07D417/14

Abstract: A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula I.

Abstract translation: 或其药学上可接受的对映体，盐或溶剂化物。 本发明还涉及式I化合物作为TDO 2抑制剂的用途。 本发明还涉及式I化合物用于治疗和/或预防癌症，神经变性疾病如帕金森病，阿尔茨海默病和亨廷顿病，慢性病毒感染如HCV和HIV，抑郁症和肥胖症的用途。 本发明还涉及制备式I化合物的方法。