公开(公告)号：US20220401424A1

公开(公告)日：2022-12-22

申请号：US17246551

申请日：2021-04-30

Applicant: PFIZER INC.

Inventor： Joyann Barber ,  Sujin Cho-Schultz ,  Matthew L. Del Bel ,  Rebecca Anne Gallego ,  Mingying He ,  Mehran Jalaie ,  Robert Steven Kania ,  Michele Ann McTigue ,  Sajiv Krishnan Nair ,  Anne-Marie Dechert Schmitt ,  Jamison Bryce Tuttle ,  Dahui Zhou ,  Ru Zhou

IPC: A61K31/444 ,  A61K45/06 ,  C07D519/00 ,  C07D471/04

Abstract: This invention relates to compounds of general Formula I and pharmaceutically acceptable salts thereof, in which R1, R2, R3a, R3b, and R4 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：US20220089580A1

公开(公告)日：2022-03-24

申请号：US17544303

申请日：2021-12-07

Applicant: Pfizer Inc.

Inventor： Ping Chen ,  Sujin Cho-Schultz ,  Judith Gail Deal ,  Gary Michael Gallego ,  Mehran Jalaie ,  Robert Steven Kania ,  Sajiv Krishnan Nair ,  Sacha Ninkovic ,  Suvi Tuula Marjukka Orr ,  Cynthia Louise Palmer

IPC: C07D407/14 ,  C07D401/14 ,  C07D487/04 ,  C07D498/04

Abstract: This invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof, in which R-groups R1 to R23, A, Q, U, V, W, X, Y, Z, n, p and q 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, in a subject.

公开(公告)号：US20200331909A1

公开(公告)日：2020-10-22

申请号：US16849329

申请日：2020-04-15

Applicant: Pfizer Inc.

Inventor： Samit Kumar Bhattacharya ,  Douglas Carl Behenna ,  Kimberly O. Cameron ,  Ping Chen ,  John M. Curto ,  Kevin Daniel Freeman-Cook ,  Mehran Jalaie ,  Robert Steven Kania ,  Yajing Lian ,  Sajiv Krishnan Nair ,  Cynthia Louise Palmer ,  Martin Youngjin Pettersson ,  Eugene Yuanjin Rui ,  Matthew Sammons ,  Qingyi Yang ,  Liying Zhang

IPC: C07D471/04 ,  A61P9/12

Abstract: This invention relates to compounds of general Formula I in which A, R1, R2, R3 and R4 are as defined herein, and the pharmaceutically acceptable salts thereof; to pharmaceutical compositions comprising such compounds and salts; to methods of using such compounds, salts and compositions for treating pulmonary hypertension and related diseases, like pulmonary arterial hypertension; to methods of using such compounds, salts and compositions for treating abnormal cell growth, such as cancer; and to processes to make such compounds, salts and compositions.

公开(公告)号：US20170298048A1

公开(公告)日：2017-10-19

申请号：US15635648

申请日：2017-06-28

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

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.

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：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.

公开(公告)号：US20160376254A1

公开(公告)日：2016-12-29

申请号：US15262230

申请日：2016-09-12

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 ,  C07B59/00 ,  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: 其中R 1，R 2，R 3，R 4，L，X和Z如本文所定义，及其药学上可接受的盐，包含这些化合物和盐的药物组合物，以及使用这些化合物，盐和组合物进行治疗的方法 的细胞生长异常，包括癌症。

公开(公告)号：US09481666B2

公开(公告)日：2016-11-01

申请号：US14740439

申请日：2015-06-16

Applicant: PFIZER INC.

Inventor： Robert Steven Kania ,  Robert Arnold Kumpf ,  Pei-Pei Kung ,  Scott Channing Sutton ,  Martin James Wythes

IPC: C07D401/06 ,  C07D401/14 ,  A61K31/44 ,  A61K31/47 ,  C07D405/14 ,  C07D413/14 ,  C07D409/14

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。