公开(公告)号：US20220251075A1

公开(公告)日：2022-08-11

申请号：US17620188

申请日：2020-06-17

Applicant: Pfizer Inc. ,  CTXT PTY LTD

Inventor： Oleg Brodsky ,  Samantha Elizabeth Greasley ,  Robert Louis Hoffman ,  Pei-Pei Kung ,  Paul Francis Richardson ,  Paul Anthony Stupple

IPC: C07D413/14 ,  C07D413/06

Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Ring A, Y, R1-R8, m, n and p are defined herein. The novel cycloalkyl and heterocycloalkyl benzisoxazole sulfonamide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in patients. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in patients.

公开(公告)号：US20180044344A1

公开(公告)日：2018-02-15

申请号：US15664265

申请日：2017-07-31

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: C07D487/04 ,  C07D401/14

CPC classification number: C07D487/04 ,  C07D401/14 ,  C07D471/04

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：US20170050958A1

公开(公告)日：2017-02-23

申请号：US15306979

申请日：2015-04-17

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 ,  A61K45/06 ,  A61K31/501 ,  C07D401/14 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/444 ,  C07D277/46

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.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中A，L，D，R 1 -R 15，w，x，y和z在本文中定义。 在哺乳动物中可用于治疗异常细胞生长例如癌症的新型环烷基连接的二杂环衍生物。 本发明还涉及含有该化合物的药物组合物以及使用该化合物和组合物治疗哺乳动物异常细胞生长的方法。

公开(公告)号：US11926642B2

公开(公告)日：2024-03-12

申请号：US17365213

申请日：2021-07-01

Applicant: Pfizer Inc.

Inventor： Robert Steven Kania ,  Padmavani Bezawada ,  Emma Louise Hawking ,  Rohit Jaini ,  Samir Kulkarni ,  Matthew Nathan O'Brien Laramy ,  Jonathan Richard Lillis ,  Suman Luthra ,  Dafydd Rhys Owen ,  Klimentina Dimitrova Pencheva ,  Anil Mahadeo Rane ,  Matthew Forrest Sammons ,  Bradley Paul Sullivan ,  Andrew John Thiel ,  Martyn David Ticehurst ,  Jamison Bryce Tuttle ,  Robert Louis Hoffman

IPC: C07F9/572 ,  A61P31/14

CPC classification number: C07F9/5728 ,  A61P31/14 ,  C07B2200/13

Abstract: The invention relates to compounds of formula I




wherein R1, R2 and - - - - - are as defined herein, pharmaceutical compositions comprising the compounds and methods of treating COVID-19 in a patient by administering therapeutically effective amounts of the compounds and methods of inhibiting or preventing replication of SARS-CoV-2 with the compounds.

公开(公告)号：US11014911B2

公开(公告)日：2021-05-25

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 ,  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：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：US11773082B2

公开(公告)日：2023-10-03

申请号：US17235846

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

CPC classification number: C07D403/12 ,  A61P35/00 ,  C07D413/12 ,  C07B2200/07

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：US20230157998A1

公开(公告)日：2023-05-25

申请号：US17905686

申请日：2021-03-03

Applicant: Pfizer Inc.

Inventor： Padmavani Bezawada ,  Benjamin Joseph Burke ,  Emma Louise Hawking ,  Robert Louis Hoffman ,  Robert Steven Kania ,  Jonathan Richard Lillis ,  Matthew Nathan O'Brien Laramy ,  Klimentina Dimitrova Pencheva ,  Bradley Paul Sullivan ,  Andrew John Thiel ,  Martyn David Ticehurst

IPC: A61K31/405 ,  A61K31/706 ,  A61K31/7052 ,  A61K9/00

CPC classification number: A61K31/405 ,  A61K31/706 ,  A61K31/7052 ,  A61K9/0019

Abstract: The invention relates to methods of treating COVID-19 in a patient by administering therapeutically effective amounts of certain SARS-CoV-2 inhibitor compounds or pharmaceutical compositions containing them to a patient in need thereof. The invention also relates to inhibiting SARS-CoV-2 coronavirus viral replication activity comprising contacting SARS-CoV-2-related coronavirus protease with a therapeutically effective amount of a SARS-Cov-2 protease inhibitor, such as a SARS-Cov-2 3CL protease inhibitor and compositions comprising the same

公开(公告)号：US20190040055A1

公开(公告)日：2019-02-07

申请号：US16157618

申请日：2018-10-11

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 ,  C07D277/46 ,  A61K45/06 ,  A61K31/427 ,  A61K31/501 ,  A61K31/444 ,  A61K31/4439 ,  C07D401/14 ,  A61K31/506

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：US20180148441A1

公开(公告)日：2018-05-31

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 ,  C07D277/46 ,  A61K45/06 ,  A61K31/427 ,  A61K31/501 ,  A61K31/444 ,  A61K31/4439 ,  C07D401/14 ,  A61K31/506

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

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.