公开(公告)号：US10246433B2

公开(公告)日：2019-04-02

申请号：US15585880

申请日：2017-05-03

Applicant: Pfizer Inc.

Inventor： Martin Paul Edwards ,  Robert Arnold Kumpf ,  Pei-Pei Kung ,  Indrawan James McAlpine ,  Sacha Ninkovic ,  Eugene Yuanjin Rui ,  Scott Channing Sutton ,  John Howard Tatlock ,  Martin James Wythes ,  Luke Raymond Zehnder

IPC: C07D401/06 ,  C07D401/14 ,  C07D403/14 ,  C07D407/14 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

Abstract: This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, 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：US10968242B2

公开(公告)日：2021-04-06

申请号：US16702738

申请日：2019-12-04

Applicant: PFIZER INC.

Inventor： Martin James Wythes ,  Indrawan James McAlpine ,  Ryan Patman ,  Eugene Yuanjin Rui ,  Andreas Maderna ,  Mehran Jalaie ,  Ketan S. Gajiwala

IPC: A61K31/7084 ,  A61K47/68 ,  A61P35/00 ,  C07H21/02 ,  C07H21/04 ,  C07F9/6574 ,  C07H19/213

Abstract: Compounds of the general formula (I): or a pharmaceutically acceptable salt thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.

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：US10220037B2

公开(公告)日：2019-03-05

申请号：US15612030

申请日：2017-06-02

Applicant: Pfizer Inc.

Inventor： John Howard Tatlock ,  Indrawan James McAlpine ,  Michelle Bich Tran-Dube ,  Eugene Yuanjin Rui ,  Martin James Wythes ,  Robert Arnold Kumpf ,  Michele Ann McTigue ,  Ryan Patman

IPC: C07D487/04 ,  A61K31/519 ,  C07D519/00 ,  A61K31/137 ,  A61K31/53 ,  C07D237/22 ,  C07D251/16 ,  C07D471/06 ,  C07D239/42 ,  C07D239/84 ,  C07D251/18 ,  C07D491/048 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61K31/02 ,  C07C255/34

Abstract: Compounds of the general formula): processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.

公开(公告)号：US20180222862A1

公开(公告)日：2018-08-09

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: C07D209/18 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D413/12 ,  C07D405/12 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  A61P3/04 ,  A61P31/18 ,  A61P35/02

CPC classification number: C07D209/18 ,  A61P3/04 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  A61P31/18 ,  A61P35/02 ,  C07D209/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12

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：US09873690B2

公开(公告)日：2018-01-23

申请号：US15072534

申请日：2016-03-17

Applicant: Pfizer Inc. ,  iTeos Therapeutics

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

IPC: C07D417/04 ,  C07D417/14 ,  A61K31/404 ,  C07D417/12

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.

公开(公告)号：US20170348313A1

公开(公告)日：2017-12-07

申请号：US15612030

申请日：2017-06-02

Applicant: Pfizer Inc.

Inventor： John Howard Tatlock ,  Indrawan James McAlpine ,  Michelle Bich Tran-Dube ,  Eugene Yuanjin Rui ,  Martin James Wythes ,  Robert Arnold Kumpf ,  Michele Ann McTigue ,  Ryan Patman

IPC: A61K31/519 ,  C07D471/06 ,  C07D251/16 ,  A61K31/137 ,  A61K31/53 ,  C07D519/00 ,  C07D237/22 ,  A61K31/02 ,  C07C255/34

CPC classification number: A61K31/519 ,  A61K31/02 ,  A61K31/137 ,  A61K31/53 ,  C07C255/34 ,  C07D237/22 ,  C07D239/42 ,  C07D239/84 ,  C07D251/16 ,  C07D251/18 ,  C07D471/06 ,  C07D487/04 ,  C07D491/048 ,  C07D519/00

Abstract: Compounds of the general formula): processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.

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：US20210230196A1

公开(公告)日：2021-07-29

申请号：US17190924

申请日：2021-03-03

Applicant: PFIZER INC.

Inventor： Martin James Wythes ,  Indrawan James McAlpine ,  Ryan Patman ,  Eugene Yuanjin Rui ,  Andrew Fensome ,  Andreas Maderna ,  Mehran Jalaie ,  Ketan S. Gajiwala

IPC: C07F9/6574 ,  A61K47/68 ,  A61P35/00 ,  C07H19/213

Abstract: Compounds of the general formula (I): or a pharmaceutically acceptable salt thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.

公开(公告)号：US10538542B2

公开(公告)日：2020-01-21

申请号：US16297910

申请日：2019-03-11

Applicant: PFIZER INC.

Inventor： Martin James Wythes ,  Indrawan James McAlpine ,  Ryan Patman ,  Eugene Yuanjin Rui ,  Andrew Fensome ,  Andreas Maderna ,  Mehran Jalaie ,  Ketan S. Gajiwala

IPC: A61K31/7084 ,  C07H21/02 ,  C07H21/04 ,  C07F9/6574 ,  A61K47/68 ,  A61P35/00

Abstract: Compounds of the general formula (I): or a pharmaceutically acceptable salt thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.