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：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：US20170360935A1

公开(公告)日：2017-12-21

申请号：US15534999

申请日：2015-12-10

Applicant: Pfizer Inc.

Inventor： Kevin Richard Back ,  Michael Cram ,  Aidan James Harper ,  W. James Huang ,  Jonathan Richard Lillis ,  Timothy Michael Lukas ,  Sumit Luthra

IPC: A61K47/12 ,  A61K9/19 ,  A61K9/08 ,  A61K47/02 ,  C07D401/12 ,  A61K47/26

CPC classification number: A61K47/12 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/19 ,  A61K31/5377 ,  A61K47/02 ,  A61K47/26 ,  C07B2200/13 ,  C07D401/12

Abstract: The present invention relates to a pharmaceutical aqueous formulation comprising -(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-,3,5-triazin-2-yl)phenyl]urea, or a pharmaceutically acceptable salt thereof, that is a clear solution. Such a formulation is particularly suitable for intravenous or parenteral administration to a patient.

公开(公告)号：US20220017548A1

公开(公告)日：2022-01-20

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 ,  Martin Youngjin Pettersson ,  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

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：US10660959B2

公开(公告)日：2020-05-26

申请号：US16189009

申请日：2018-11-13

Applicant: Pfizer Inc.

Inventor： Kevin Richard Back ,  Michael Cram ,  Aidan James Harper ,  W. James Huang ,  Jonathan Richard Lillis ,  Timothy Michael Lukas ,  Sumit Luthra

IPC: A61K47/12 ,  C07D401/12 ,  A61K9/00 ,  A61K47/26 ,  A61K9/08 ,  A61K9/19 ,  A61K31/5377 ,  A61K47/02

Abstract: The present invention relates to a pharmaceutical aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea, or a pharmaceutically acceptable salt thereof, that is a clear solution. Such a formulation is particularly suitable for intravenous or parenteral administration to a patient.

公开(公告)号：US20190105390A1

公开(公告)日：2019-04-11

申请号：US16189009

申请日：2018-11-13

Applicant: Pfizer Inc.

Inventor： Kevin Richard Back ,  Michael Cram ,  Aidan James Harper ,  W. James Huang ,  Jonathan Richard Lillis ,  Timothy Michael Lukas ,  Sumit Luthra

IPC: A61K47/12 ,  A61K31/5377 ,  C07D401/12 ,  A61K47/26 ,  A61K9/00 ,  A61K47/02 ,  A61K9/19 ,  A61K9/08

Abstract: The present invention relates to a pharmaceutical aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea, or a pharmaceutically acceptable salt thereof, that is a clear solution. Such a formulation is particularly suitable for intravenous or parenteral administration to a patient.

公开(公告)号：US10172942B2

公开(公告)日：2019-01-08

申请号：US15534999

申请日：2015-12-10

Applicant: Pfizer Inc.

Inventor： Kevin Richard Back ,  Michael Cram ,  Aidan James Harper ,  W. James Huang ,  Jonathan Richard Lillis ,  Timothy Michael Lukas ,  Sumit Luthra

IPC: A61K47/12 ,  A61K47/26 ,  A61K47/02 ,  A61K9/00 ,  A61K9/08 ,  A61K9/19 ,  A61K31/5377 ,  C07D401/12

Abstract: The present invention relates to a pharmaceutical aqueous formulation comprising -(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-,3,5-triazin-2-yl)phenyl]urea, or a pharmaceutically acceptable salt thereof, that is a clear solution. Such a formulation is particularly suitable for intravenous or parenteral administration to a patient.