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：US20240116937A1

公开(公告)日：2024-04-11

申请号：US18004943

申请日：2021-07-08

Applicant: Pfizer Inc.

Inventor： Wesley Dewitt Clark ,  Klimentina Dimitrova Pencheva

IPC: C07D487/04

CPC classification number: C07D487/04 ,  C07B2200/13

Abstract: This invention relates to crystalline free base forms of (1S,2S,3S,5R)-3-((6-(difluoromethyl)-5-fluoro-1,2,3,4-tetrahydroisoquinolin-8-yl)oxy)-5-(4-methyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol, and to compositions and therapeutic uses thereof.

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：US20210388000A1

公开(公告)日：2021-12-16

申请号：US17365270

申请日：2021-07-01

Applicant: Pfizer Inc.

Inventor： Klimentina Dimitrova Pencheva

IPC: C07D498/18

Abstract: This invention relates to new crystalline forms of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile (lorlatinib) maleate. The invention also relates to pharmaceutical compositions comprising lorlatinib maleate, and to methods of using lorlatinib maleate and compositions comprising it in the treatment of abnormal cell growth, such as cancer, in mammals.

公开(公告)号：US20230242539A1

公开(公告)日：2023-08-03

申请号：US18004965

申请日：2021-07-08

Applicant: Pfizer Inc.

Inventor： Michael Heberlein ,  Klimentina Dimitrova Pencheva ,  Michelle Bich Tran-Dubé

IPC: C07D487/04

CPC classification number: C07D487/04 ,  C07B2200/13

Abstract: This invention relates to crystalline mono-HCl salt forms of (1S,2S,3S,5R)-3-((6-(difluoromethyl)-5-fluoro-1,2,3,4-tetrahydroisoquinolin-8-yl)oxy)-5-(4-methyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol, and to compositions and therapeutic uses thereof.

公开(公告)号：US11078215B2

公开(公告)日：2021-08-03

申请号：US16090693

申请日：2017-03-27

Applicant: Pfizer Inc.

Inventor： Klimentina Dimitrova Pencheva

IPC: C07D498/18

Abstract: This invention relates to new crystalline forms of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile(lorlatinib) maleate. The invention also relates to pharmaceutical compositions comprising lorlatinib maleate, and to methods of using lorlatinib maleate and compositions comprising it in the treatment of abnormal cell growth, such as cancer, in mammals.

公开(公告)号：US11020376B2

公开(公告)日：2021-06-01

申请号：US16535747

申请日：2019-08-08

Applicant: Pfizer Inc.

Inventor： Klimentina Dimitrova Pencheva ,  Melissa Jane Birch ,  Stephen Mark McAllister ,  Martin Gregory Rowland ,  Ian Leonard Smales

IPC: A61K31/4162 ,  A61P35/00 ,  C07D498/18 ,  G01N21/65 ,  G01N23/20 ,  G01N24/08

Abstract: This invention relates to acrystalline form of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-5-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h] [2,5,11]benzoxadiazacyclo-tetradecine-3-carbonitrile (lorlatinib) free base (Form 7). This invention also relates to pharmaceutical compositions comprising Form 7, and to methods of using Form 7 and such compositions in the treatment of abnormal cell growth, such as cancer, in a mammal.

公开(公告)号：US11926636B2

公开(公告)日：2024-03-12

申请号：US17365270

申请日：2021-07-01

Applicant: Pfizer Inc.

Inventor： Klimentina Dimitrova Pencheva

IPC: C07D498/18

CPC classification number: C07D498/18 ,  C07B2200/13

Abstract: This invention relates to new crystalline forms of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile(lorlatinib) maleate. The invention also relates to pharmaceutical compositions comprising lorlatinib maleate, and to methods of using lorlatinib maleate and compositions comprising it in the treatment of abnormal cell growth, such as cancer, in mammals.

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：US20200325155A1

公开(公告)日：2020-10-15

申请号：US16090693

申请日：2017-03-27

Applicant: Pfizer Inc.

Inventor： Klimentina Dimitrova Pencheva

IPC: C07D498/18

Abstract: This invention relates to new crystalline forms of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3- h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile(lorlatinib) maleate. The invention also relates to pharmaceutical compositions comprising lorlatinib maleate, and to methods of using lorlatinib maleate and compositions comprising it in the treatment of abnormal cell growth, such as cancer, in mammals.