Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides, and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.
Type:
Grant
Filed:
April 19, 2016
Date of Patent:
July 7, 2020
Assignee:
Pfizer Inc.
Inventors:
Atli Thorarensen, Matthew Frank Brown, Agustin Casimiro-Garcia, Ye Che, Mark Edward Flanagan, Adam Matthew Gilbert, Matthew Merrill Hayward, Jean-Baptiste Telliez, Rayomand Jal Unwalla, John I. Trujillo, Sidney Xi Liang
Abstract: The present invention relates to oral sustained release formulations of tofacitinib and pharmaceutical acceptable salts thereof. The formulations described herein have desirable pharmacokinetic characteristics.
Type:
Application
Filed:
March 13, 2020
Publication date:
July 2, 2020
Applicant:
PFIZER INC.
Inventors:
Scott Max Herbig, Sriram Krishnaswami, Joseph Kushner, IV, Manisha Lamba, Thomas C. Stock
Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), and Parkinson's disease.
Type:
Grant
Filed:
August 13, 2019
Date of Patent:
June 30, 2020
Assignee:
Pfizer Inc.
Inventors:
Michael Aaron Brodney, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, David Lawrence Firman Gray, Michael Eric Green, Jaclyn Louise Henderson, Chewah Lee, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Lei Zhang
Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and an Anaplastic Lymphoma Kinase (ALK) inhibitor, and the use of the combination therapies for the treatment of cancer, and in particular for treating cancers that test positive for ALK, PD-L 1, or both ALK and PD-L 1.
Type:
Grant
Filed:
August 24, 2015
Date of Patent:
June 30, 2020
Assignees:
Pfizer Inc., Merck Sharp & Dohme Corp.
Inventors:
Leena Das-Young, Keith David Wilner, Steffan Nicholas Ho
Abstract: The present invention relates to novel crystalline polymorphic and amorphous form of 4-(2-(5-chloro-2-fluorophenyl) -5-isopropylpyridin-4-ylamino)-N-(1,3-dihydroxypropan-2-yl) nicotinamide and to methods for their preparation; and the invention is also directed to pharmaceutical compositions containing at least one polymorphic form and to the therapeutic or prophylactic use of such polymorphic forms and compositions.
Type:
Application
Filed:
December 17, 2019
Publication date:
June 25, 2020
Applicant:
PFIZER INC.
Inventors:
Anand Venkataramana Sistla, Iain David Roy, Andrew Robbins
Abstract: Methods for the detection, enumeration and analysis of circulating tumor cells expressing insulin-like growth factor-1 receptors (IGF-1R) are disclosed. These methods are useful for cancer screening and staging, development of treatment regimens, and for monitoring for treatment responses, cancer recurrence or the like. Test kits that facilitate the detection, enumeration and analysis of such circulating tumor cells are also provided.
Type:
Application
Filed:
July 8, 2019
Publication date:
June 18, 2020
Applicants:
Janssen Diagnostics, LLC, Pfizer Inc.
Inventors:
Antonio GUALBERTO, Maria Luisa PACCAGNELLA, Carrie L. MELVIN, Madeline I. REPOLLET, David CHIANESE, Mark Carle CONNELLY, Leonardus Wendelinus Mathias Marie TERSTAPPEN
Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
Type:
Grant
Filed:
August 8, 2019
Date of Patent:
June 16, 2020
Assignee:
Pfizer Inc.
Inventors:
Gary Erik Aspnes, Scott W. Bagley, John M. Curto, David James Edmonds, Mark E. Flanagan, Kentaro Futatsugi, David A. Griffith, Kim Huard, Yajing Lian, Chris Limberakis, Allyn T. Londregan, Alan M. Mathiowetz, David W. Piotrowski, Roger B. Ruggeri
Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
Type:
Application
Filed:
February 18, 2020
Publication date:
June 11, 2020
Applicant:
Pfizer Inc.
Inventors:
Markus Boehm, Shawn Cabral, Matthew S. Dowling, Kentaro Futatsugi, Kim Huard, Esther Cheng Yin Lee, Allyn T. Londregan, Jana Polivkova, David A. Price, Qifang Li
Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
Type:
Grant
Filed:
August 8, 2019
Date of Patent:
June 9, 2020
Assignee:
Pfizer Inc.
Inventors:
Gary Erik Aspnes, Scott W. Bagley, John M. Curto, David James Edmonds, Mark E. Flanagan, Kentaro Futatsugi, David A. Griffith, Kim Huard, Yajing Lian, Chris Limberakis, Allyn T. Londregan, Alan M. Mathiowetz, David W. Piotrowski, Roger B. Ruggeri
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.
Type:
Grant
Filed:
May 20, 2019
Date of Patent:
June 9, 2020
Assignee:
Pfizer Inc.
Inventors:
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
Abstract: This invention relates to compounds of general Formula (I) and pharmaceutically acceptable salts thereof, in which R1, R1a, R2, R3, R4, and (R5)a are as defined herein, to pharmaceutical compositions comprising such compounds and pharmaceutically acceptable salts thereof, and to methods of using such compounds, pharmaceutically acceptable salts and compositions for the treatment of abnormal cell growth, including cancer.
Type:
Application
Filed:
November 11, 2019
Publication date:
June 4, 2020
Applicant:
Pfizer Inc.
Inventors:
Rebecca Anne Gallego, Sajiv Krishnan Nair, Robert Steven Kania, Omar Khaled Ahmad, Ted William Johnson, Jamison Bryce Tuttle, Mehran Jalaie, Michele Ann McTigue, Dahui Zhou, Matthew L. Del Bel, Ru Zhou, Mingying He
Abstract: The invention relates to pyrazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to HbS modulators of formula (I) or tautomers thereof, or pharmaceutically acceptable salts of said modulators or tautomers thereof, wherein X, Y, R2 and R3 are as defined in the description. HbS modulators are potentially useful in the treatment of a wide range of disorders, including sickle cell disease (SCD).
Type:
Application
Filed:
November 26, 2019
Publication date:
June 4, 2020
Applicant:
Pfizer Inc.
Inventors:
Ariamala Gopalsamy, Arjun Venkat Narayanan, Agustin Casimiro-Garcia, Chulho Choi, David Hepworth, David Walter Piotrowski, Hatice Gizem Yayla, Jayasankar Jasti, Lee Richard Roberts, Lyn Howard Jones, Mihir Dineshkumar Parikh, Ming Zhu Chen, Olugbeminiyi Omezia Fadeyi, Ralph Pelton Robinson, JR., Robert Lee Dow, Shawn Cabral
Abstract: A compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein variables are defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.
Type:
Application
Filed:
August 9, 2018
Publication date:
June 4, 2020
Applicant:
Pfizer Inc.
Inventors:
Brian Stephen Gerstenberger, Andrew Fensome, Dafydd Rhys Owen, Matthew Frank Brown, Matthew Merrill Hayward, Felix Vajdos, Li Huang Xing, Stephen Wayne Wright
Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, 7-aza- and 4,7-diaza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
Type:
Grant
Filed:
December 14, 2018
Date of Patent:
June 2, 2020
Assignee:
Pfizer Inc.
Inventors:
Gary Erik Aspnes, Scott W. Bagley, John M. Curto, Matthew S. Dowling, David Edmonds, Mark E. Flanagan, Kentaro Futatsugi, David A. Griffith, Kim Huard, Gajendra Ingle, Wenhua Jiao, Chris Limberakis, Alan M. Mathiowetz, David W. Piotrowski, Roger B. Ruggeri
Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents R1, R3, R6, R7, and b are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.
Type:
Grant
Filed:
June 27, 2019
Date of Patent:
June 2, 2020
Assignee:
Pfizer Inc.
Inventors:
Thomas Allen Chappie, Nandini Chaturbhai Patel, Matthew Merrill Hayward, Christopher John Helal, Simone Sciabola, Erik Alphie LaChapelle, Joseph Michael Young, Patrick Robert Verhoest