公开(公告)号：US10662204B2

公开(公告)日：2020-05-26

申请号：US16263185

申请日：2019-01-31

Applicant: PFIZER INC.

Inventor： Simon Planken ,  Hengmiao Cheng ,  Michael Raymond Collins ,  Jillian Elyse Spangler ,  Alexei Brooun ,  Andreas Maderna ,  Cynthia Palmer ,  Maria Angelica Linton ,  Asako Nagata ,  Ping Chen

IPC: C07D403/12 ,  C07D403/14 ,  C07D407/14 ,  C07D487/10 ,  A61P35/00 ,  C07D519/00 ,  C07D471/04 ,  C07D487/04 ,  C07D417/14 ,  C07D413/14 ,  A61P25/00

Abstract: Compounds of the general formula: processes for the preparation of these compounds, compositions containing these compounds, and administration of these compounds to patients to treat pancreatic, lung, colon and other cancers.

公开(公告)号：US10590115B2

公开(公告)日：2020-03-17

申请号：US16265012

申请日：2019-02-01

Applicant: PFIZER INC.

Inventor： Simon Planken ,  Hengmiao Cheng ,  Michael Raymond Collins ,  Jillian Elyse Spangler ,  Alexei Brooun ,  Andreas Maderna ,  Cynthia Palmer ,  Maria Angelica Linton ,  Asako Nagata ,  Ping Chen

IPC: C07D403/14 ,  C07D487/10 ,  A61P35/00 ,  C07D403/04 ,  C07D239/94

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：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。

公开(公告)号：US09249186B2

公开(公告)日：2016-02-02

申请号：US14793942

申请日：2015-07-08

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 ,  C07K7/06

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.

公开(公告)号：US09138486B2

公开(公告)日：2015-09-22

申请号：US14322262

申请日：2014-07-02

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: A61K47/48 ,  A61K38/06 ,  A61K38/08 ,  A61K38/07 ,  C07K7/02 ,  C07K5/083 ,  C07K5/02 ,  C07K16/00

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。