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：US20150361067A1

公开(公告)日：2015-12-17

申请号：US14740439

申请日：2015-06-16

Applicant: PFIZER INC.

Inventor： Michael Raymond Collins ,  Robert Steven Kania ,  Robert Arnold Kumpf ,  Pei-Pei Kung ,  Daniel Tyler Richter ,  Scott Channing Sutton ,  Martin James Wythes

IPC: C07D401/06 ,  C07D409/14 ,  C07D413/14 ,  C07D405/14 ,  C07D401/14

CPC classification number: C07D405/14 ,  C07B59/002 ,  C07B2200/05 ,  C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14

Abstract: This invention relates to compounds of general formula (I) in which R1, R2, R3, R4, L, X 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.

Abstract translation: 本发明涉及其中R1，R2，R3，R4，L，X和Z如本文所定义的通式（I）化合物及其药学上可接受的盐，涉及包含这些化合物和盐的药物组合物，以及方法 使用这些化合物，盐和组合物来治疗异常细胞生长，包括癌症。

公开(公告)号：US20140135339A1

公开(公告)日：2014-05-15

申请号：US14156144

申请日：2014-01-15

Applicant: PFIZER INC.

Inventor： Simon Bailey ,  Benjamin Joseph Burke ,  Michael Raymond Collins ,  Jingrong Jean Cui ,  Judith Gail Deal ,  Robert Louis Hoffman ,  Qinhua Huang ,  Ted William Johnson ,  Robert Steven Kania ,  John Charles Kath ,  Phuong Thi Quy Le ,  Michele Ann McTigue ,  Cynthia Louise Palmer ,  Paul Francis Richardson ,  Neal William Sach

IPC: C07D498/18 ,  C07D498/22

CPC classification number: C07D498/08 ,  C07D273/02 ,  C07D413/04 ,  C07D413/14 ,  C07D491/08 ,  C07D491/18 ,  C07D498/18 ,  C07D498/22 ,  C07D513/18

Abstract: The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.

Abstract translation: 本发明涉及本文进一步定义的式（Φ）化合物及其药学上可接受的盐，涉及包含这些化合物和盐的药物组合物及其用途。 本发明的化合物和盐抑制间变性淋巴瘤激酶（ALK）和/或EML4-ALK，并且可用于治疗或改善异常细胞增殖性疾病如癌症。

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：US10125130B2

公开(公告)日：2018-11-13

申请号：US15826027

申请日：2017-11-29

Applicant: PFIZER INC.

Inventor： Aaron Craig Burns ,  Michael Raymond Collins ,  Samantha Elizabeth Greasley ,  Robert Louis Hoffman ,  Peter Qinhua Huang ,  Robert Steven Kania ,  Pei-Pei Kung ,  Maria Angelica Linton ,  Lakshmi Sourirajan Narasimhan ,  Paul Francis Richardson ,  Daniel Tyler Richter ,  Graham Smith

IPC: C07D417/14 ,  C07D417/08 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  C07D277/46 ,  C07D401/14

Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein A, L, D, R1-R15, w, x, y, and z are defined herein. The novel cycloalkyl-linked diheterocycle derivatives that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. The present invention also relates to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

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：US08680111B2

公开(公告)日：2014-03-25

申请号：US13786106

申请日：2013-03-05

Applicant: Pfizer Inc.

Inventor： Simon Bailey ,  Benjamin Joseph Burke ,  Michael Raymond Collins ,  Jingrong Jean Cui ,  Judith Gail Deal ,  Robert Louis Hoffman ,  Qinhua Huang ,  Ted William Johnson ,  Robert Steven Kania ,  John Charles Kath ,  Phuong Thi Quy Le ,  Michele Ann McTigue ,  Cynthia Louise Palmer ,  Paul Francis Richardson ,  Neal William Sach

IPC: A01N43/42 ,  A61K31/44 ,  A01N43/02 ,  A61K31/335 ,  C07D471/00 ,  C07D491/00 ,  C07D498/00 ,  C07D513/00 ,  C07D515/00 ,  C07D313/00

CPC classification number: C07D498/08 ,  C07D273/02 ,  C07D413/04 ,  C07D413/14 ,  C07D491/08 ,  C07D491/18 ,  C07D498/18 ,  C07D498/22 ,  C07D513/18

Abstract: The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.

Abstract translation: 本发明涉及本文进一步定义的式（Φ）化合物及其药学上可接受的盐，涉及包含这些化合物和盐的药物组合物及其用途。 本发明的化合物和盐抑制间变性淋巴瘤激酶（ALK）和/或EML4-ALK，并且可用于治疗或改善异常细胞增殖性疾病如癌症。