公开(公告)号：US10086085B2

公开(公告)日：2018-10-02

申请号：US14605697

申请日：2015-01-26

Applicant: Pfizer Inc.

Inventor： Andreas Maderna ,  Matthew David Doroski ,  Zecheng Chen ,  Hud Lawrence Risley ,  Jeffrey Michael Casavant ,  Christopher John O'Donnell ,  Alexander M. Porte ,  Chakrapani Subramanyam

IPC: C07D487/04 ,  C07D487/06 ,  C07D209/30 ,  A61K31/404 ,  A61K31/407 ,  A61K47/48 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/675 ,  A61K31/7056 ,  A61K38/05 ,  A61K38/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07F9/6561 ,  C07H17/02 ,  C07K5/06 ,  C07K5/08 ,  C07K9/00 ,  A61K47/68

Abstract: Cytotoxic dimers comprising CBI-based and/or CPI-based sub-units, antibody drug conjugates comprising such dimers, and to methods for using the same to treat cancer and other conditions.

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.

公开(公告)号：US08828401B2

公开(公告)日：2014-09-09

申请号：US13670612

申请日：2012-11-07

Applicant: Pfizer Inc.

Inventor： Matthew David Doroski ,  Andreas Maderna ,  Christopher John O'Donnell ,  Chakrapani Subramanyam ,  Beth Vetelino ,  Russell George Dushin ,  Pavel Strop ,  Edmund Idris Graziani

IPC: C07K7/02 ,  C07K5/02 ,  C07K16/00 ,  A61K47/48

CPC classification number: C07K7/06 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K47/6803 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6863 ,  A61K47/6889 ,  C07K5/0205 ,  C07K5/0808 ,  C07K7/02 ,  C07K16/00 ,  C07K2319/30

Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.

Abstract translation: 本发明涉及细胞毒性五肽，其抗体药物偶联物及其用于治疗癌症的方法。

公开(公告)号：US20190284216A1

公开(公告)日：2019-09-19

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: C07F9/6574 ,  A61P35/00 ,  A61K47/68

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：US10391182B2

公开(公告)日：2019-08-27

申请号：US16053344

申请日：2018-08-02

Applicant: PFIZER INC.

Inventor： Andreas Maderna ,  Matthew David Doroski ,  Zecheng Chen ,  Hud Lawrence Risley ,  Jeffrey Michael Casavant ,  Christopher John O'Donnell ,  Alexander M. Porte ,  Chakrapani Subramanyam

IPC: C07D487/04 ,  C07D487/06 ,  A61K47/68 ,  A61K31/404 ,  A61K31/407 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/675 ,  A61K31/7056 ,  A61K38/05 ,  A61K38/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07F9/6561 ,  C07H17/02 ,  C07K5/06 ,  C07K5/08 ,  C07K9/00

Abstract: Cytotoxic dimers comprising CBI-based and/or CPI-based sub-units, antibody drug conjugates comprising such dimers, and to methods for using the same to treat cancer and other conditions.

公开(公告)号：US11365263B2

公开(公告)日：2022-06-21

申请号：US17091097

申请日：2020-11-06

Applicant: PFIZER INC.

Inventor： Andreas Maderna ,  Chakrapani Subramanyam ,  Lawrence N. Tumey ,  Zecheng Chen ,  Jeffrey M. Casavant

IPC: C07K16/32 ,  C07D519/00 ,  C07F9/6561 ,  C07K5/062 ,  C07K5/09 ,  C07B59/00 ,  C07K16/28 ,  C07D495/04 ,  A61K47/68 ,  A61K47/65

Abstract: The present invention is directed to novel bifunctional CTI-CTI and CBI-CTI dimers of the formula: F1-L1-T-L2-F2 where F1, L1, T, L2 and F2 are as defined herein, useful for the treatment for proliferative diseases, where the inventive dimers can function as stand-alone drugs, payloads in antibody-drug-conjugates (ADCs), and linker-payload compounds useful in connection with the production or administration of such ADCs; and to compositions including the aforementioned dimers, linker-payloads and ADCs, and methods for using these dimers, linker-payloads and ADCs, to treat pathological conditions including cancer.

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：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.