Abstract: Compounds of the general formula (I): or a pharmaceutically acceptable salt thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
Type:
Grant
Filed:
December 4, 2019
Date of Patent:
April 6, 2021
Assignee:
Pfizer Inc.
Inventors:
Martin James Wythes, Indrawan James McAlpine, Ryan Patman, Eugene Yuanjin Rui, Andreas Maderna, Mehran Jalaie, Ketan S. Gajiwala
Abstract: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing them, and therapeutic uses thereof.
Type:
Grant
Filed:
August 10, 2015
Date of Patent:
April 6, 2021
Assignee:
Pfizer Inc.
Inventors:
Michael L. Vazquez, Neelu Kaila, Jamison B. Tuttle, Patrick Robert Verhoest, Matthew R. Reese, Karen J. Coffman, Tarek Samad, James M. Duerr, Simone Sciabola, Mihir D. Parikh
Abstract: The present invention provides stability-modulated antibody-drug conjugates, stability-modulating linker components used to make these stability-modulated antibody-drug conjugates, therapeutic methods using stability-modulated antibody-drug conjugates, and methods of making stability modulating linkers and stability-modulated antibody-drug conjugates.
Type:
Grant
Filed:
August 14, 2015
Date of Patent:
April 6, 2021
Assignees:
PFIZER INC., RINAT NEUROSCIENCE CORP.
Inventors:
Russell George Dushin, Pavel Strop, Magdalena Grazyna Dorywalska, Ludivine Moine
Abstract: The present invention is based on the seminal discovery that BTLA agonist fusion proteins modulate an immune response. Specifically, the present invention provides fusion proteins that bind BTLA enhancing BTLA signaling. The present invention further provides methods of treating cancer and immune and inflammatory diseases and disorders with a BTLA agonist fusion protein as described herein.
Type:
Grant
Filed:
June 29, 2016
Date of Patent:
March 30, 2021
Assignees:
SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE, PFIZER INC.
Inventors:
Carl F. Ware, John Sedy, Tigran Aivazian, Brian Miller, Natasha K. Crellin
Abstract: Compounds of the general formula (I): or a pharmaceutically acceptable salt thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
Type:
Application
Filed:
September 23, 2020
Publication date:
March 25, 2021
Applicant:
PFIZER INC.
Inventors:
Ryan PATMAN, Martin James WYTHES, Eugene Yuanjin RUI, Indrawan James MCALPINE, Andrew FENSOME, Mehran JALAIE, Ketan S. GAJIWALA, Chan Woo HUH, Tuan Phong TRAN, Lei ZHANG, Dahui ZHOU, Ethan Lawrence FISHER
Abstract: Described herein are compounds of Formula I, wherein R1, R2, and R3 are defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetes, NASH and heart failure.
Type:
Application
Filed:
October 23, 2020
Publication date:
March 25, 2021
Applicant:
Pfizer Inc.
Inventors:
Samit Kumar Bhattacharya, Leanne Marie Buzon, Kevin James Filipski, David Andrew Griffith, Bethany Lyn Kormos, Luis Angel Martinez-Alsina, Russell Alan Miller, Matthew Richard Reese, Rachel Jane Roth Flach, Yuan Zhang
Abstract: In one aspect, the invention relates to a composition including a first polypeptide having the sequence set forth in SEQ ID NO: 1 and a second polypeptide having the sequence set forth in SEQ ID NO: 2. In one embodiment, the composition includes about 120 ?g/ml of a first polypeptide including the amino acid sequence set forth in SEQ ID NO: 1, 120 ?g/ml of a second polypeptide including the amino acid sequence set forth in SEQ ID NO: 2, about 2.8 molar ratio polysorbate-80 to the first polypeptide, about 2.8 molar ratio polysorbate-80 to the second polypeptide, about 0.5 mg/ml aluminum, about 10 mM histidine, and about 150 mM sodium chloride. In one embodiment, a dose of the composition is about 0.5 ml in total volume. In one embodiment, two-doses of the composition induce a bactericidal titer against diverse heterologous subfamily A and subfamily B strains in a human.
Type:
Application
Filed:
December 8, 2020
Publication date:
March 25, 2021
Applicant:
Pfizer Inc.
Inventors:
Kathrin Ute Jansen, Annaliesa Sybil Anderson, Rasappa Gounder Arumugham, John Erwin Farley, Leah Diane Fletcher, Shannon Lea Harris, Thomas Richard Jones, Lakshmi Khandke, Bounthon Loun, John Lance Perez, Gary Warren Zlotnick
Abstract: The present disclosure generally relates to nanoparticles comprising an endo-lysosomal escape agent, a nucleic acid, and a polymer. Other aspects include methods of making and using such nanoparticles.
Type:
Grant
Filed:
May 24, 2018
Date of Patent:
March 23, 2021
Assignee:
Pfizer Inc.
Inventors:
Allen Thomas Horhota, Young-Ho Song, Ujjwal Chaitanya Joshi, Nicholas Jon Boylan, Matthew John Simmons
Abstract: The present invention relates to media and fermentation methods for producing polysaccharides in bacterial cell culture. In one aspect, the invention relates to a complex culture medium comprising a vegetable hydrolysate, a yeast extract, and a carbon source. In another aspect, the invention relates to a defined media having a total amino acid concentration greater than about 50 mM. A further aspect of the invention relates to the use of fed batch and perfusion fermentation methods for cultivating polysaccharide-producing bacteria.
Type:
Grant
Filed:
November 10, 2016
Date of Patent:
March 16, 2021
Assignee:
Pfizer Inc.
Inventors:
Sunil Gururao Desai, Michael Allen Hanson, Jonathan Patrick Kinross, Daniel R. Lasko, Scott Ellis Lomberk, Jason Arnold Lotvin, Sujata Kaushikbhai Patel-Brown, Weiqiang Sun, Peter Anthony Tomasello
Abstract: The invention relates to immunogenic polysaccharide-protein conjugates comprising a capsular polysaccharide (CP) from Streptococcus agalactiae, commonly referred to as group B streptococcus (GBS), and a carrier protein, wherein the CP is selected from the group consisting of serotypes Ia, Ib, II, III, IV, V, VI, VII, VIII, and IX, and wherein the CP has a sialic acid level of greater than about 60%. The invention also relates to methods of making the conjugates and immunogenic compositions comprising the conjugates. The invention also relates to immunogenic compositions comprising polysaccharide-protein conjugates, wherein the conjugates comprise a CP from GBS serotype IV and at least one additional serotype. The invention further relates to methods for inducing an immune response in subjects against GBS and/or for reducing or preventing invasive GBS disease in subjects using the compositions disclosed herein. The resulting antibodies can be used to treat or prevent GBS infection via passive immunotherapy.
Type:
Grant
Filed:
January 11, 2019
Date of Patent:
March 16, 2021
Assignee:
Pfizer Inc.
Inventors:
Annaliesa Sybil Anderson, Amardeep Singh Bhupender Bhalla, Robert G. K. Donald, Jianxin Gu, Kathrin Ute Jansen, Rajesh Kumar Kainthan, Lakshmi Khandke, Jin-Hwan Kim, Paul Liberator, Avvari Krishna Prasad, Mark Edward Ruppen, Ingrid Lea Scully, Suddham Singh, Cindy Xudong Yang
Abstract: The present invention relates to PDE4 inhibitor (R)-4-(5-(4-methoxy-3-propoxyphenyl)pyridin-3-yl)-1,2-oxaborolan-2-ol including the crystalline monohydrate thereof.
Type:
Grant
Filed:
October 4, 2019
Date of Patent:
March 16, 2021
Assignee:
Pfizer Inc.
Inventors:
Joseph Walter Strohbach, David Clive Blakemore, Peter Jones, Matthew Alexander Perry
Abstract: Combinations of an IDO1 inhibitor (e.g., a 3-(5-fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione compound), with an anti-PD1 antibody or anti-PD-L1 antibody, and an anti-4-1BB antibody, as selected anti-cancer or anti-viral agents are provided. Also provided are use of these combinations for the treatment and/or prevention of cancer and endometriosis.
Abstract: The present invention relates to boron containing compounds of Formula (I) X—Y—Z?? Formula (I) that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.
Type:
Application
Filed:
October 28, 2020
Publication date:
March 11, 2021
Applicant:
Pfizer Inc.
Inventors:
Joseph Walter Strohbach, Tsutomu Akama, David Clive Blakemore, Robert Toms Jacobs, Peter Jones, David Christopher Limburg, Martins Sunday Oderinde, Matthew Alexander Perry, Jacob John Plattner, Rubben Federico Torella, Yasheen Zhou, Thean Yeow Yeoh
Abstract: The present disclosure relates to: a) solid state forms of hydrobromide salts of Compound 1; b) pharmaceutical compositions comprising one or more solid state forms of hydrobromide salts of Compound 1, and, optionally, a pharmaceutically acceptable carrier; c) methods of treating tumors or cancers by administering one or more solid state forms of hydrobromide salts of Compound 1 to a subject in need thereof; and d) methods for the preparation of solid state forms of Compound 1.
Type:
Grant
Filed:
May 28, 2020
Date of Patent:
March 9, 2021
Assignee:
Pfizer Inc.
Inventors:
Elaine Greer, Stephen Anderson, Mark Maloney, Shu Yu, Ekaterina Albert, Emily Rigsbee
Abstract: The present invention provides engineered polypeptide conjugates (e.g., antibody-drug-conjugates, toxin-(biocompatible polymer) conjugates, antibody-(biocompatible polymer) conjugates, and bispecific antibodies) comprising acyl donor glutamine-containing tags and amine donor agents. In one aspect, the invention provides an engineered Fc-containing polypeptide conjugate comprising the formula (Fc-containing polypeptide)-T-A, wherein T is an acyl donor glutamine-containing tag engineered at a specific site or comprises an endogenous glutamine made reactive by the Fc-containing polypeptide engineering, wherein A is an amine donor agent, and wherein the amine donor agent is site-specifically conjugated to the acyl donor glutamine-containing tag or the endogenous glutamine. The invention also provides methods of making engineered polypeptide conjugates using transglutaminase.
Type:
Grant
Filed:
May 11, 2017
Date of Patent:
March 9, 2021
Assignee:
Pfizer Inc.
Inventors:
Pavel Strop, Magdalena Grazyna Dorywalska, Arvind Rajpal, David Shelton, Shu-Hui Liu, Jaume Pons, Russell Dushin
Abstract: The present invention is directed to novel bifunctional CTI-CTI and CBI-CTI dimers of the formula: F1-L1-T-L2-F2 where F1, L1, T, L2 and F2 are as defined herein, useful for the treatment for proliferative diseases, where the inventive dimers can function as stand-alone drugs, payloads in antibody-drug-conjugates (ADCs), and linker-payload compounds useful in connection with the production or administration of such ADCs; and to compositions including the aforementioned dimers, linker-payloads and ADCs, and methods for using these dimers, linker-payloads and ADCs, to treat pathological conditions including cancer.
Type:
Application
Filed:
November 6, 2020
Publication date:
March 4, 2021
Applicant:
PFIZER INC.
Inventors:
Andreas MADERNA, Chakrapani SUBRAMANYAM, Lawrence N. TUMEY, Zecheng CHEN, Jeffrey M. CASAVANT
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:
June 10, 2019
Date of Patent:
March 2, 2021
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 antibodies, e.g., full length antibodies or antigen binding fragments thereof, that specifically bind to BCMA (B-Cell Maturation Antigen) and/or CD3 (Cluster of Differentiation 3). The invention also relates to antibody conjugates (e.g., antibody-drug-conjugates) comprising the BCMA antibodies, compositions comprising the BCMA antibodies, and methods of using the BCMA antibodies and their conjugates for treating conditions associated with cells expressing BCMA (e.g., cancer or autoimmune disease). The invention further relates to heteromultimeric antibodies that specifically bind to CD3 and a tumor cell antigen, (e.g., bispecific antibodies that specifically bind to CD3 and BCMA). Compositions comprising such heteromultimeric antibodies, methods for producing and purifying such heterodimeric antibodies, and their use in diagnostics and therapeutics are also provided.
Type:
Application
Filed:
August 27, 2020
Publication date:
February 25, 2021
Applicant:
PFIZER INC.
Inventors:
Tracy Chia-Chien KUO, Javier Fernando CHAPARRO RIGGERS, Wei CHEN, Amy Shaw-Ru CHEN, Edward Derrick PASCUA, Thomas John VAN BLARCOM, Leila Marie BOUSTANY, Weihsien HO, Yik Andy YEUNG, Pavel STROP, Arvind RAJPAL
Abstract: The present invention provides antibodies and related molecules that bind to chemokine receptor 4 (CXCR4). The invention further provides antibody-drug conjugates comprising such antibodies, antibody encoding nucleic acids, and methods of obtaining such antibodies. The invention further relates to therapeutic methods for use of these antibodies and anti-CXCR4 antibody-drug conjugates for the treatment of a disorder associated with CXCR4 function or expression (e.g., cancer), such as colon, RCC, esophageal, gastric, head and neck, lung, ovarian, pancreatic cancer or hematological cancers.
Type:
Grant
Filed:
August 8, 2019
Date of Patent:
February 23, 2021
Assignee:
PFIZER INC.
Inventors:
Shu-Hui Liu, Flavia Mercer Pernasetti, Wei-Hsien Ho
Abstract: The invention provides a compound of Formula (1) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
Type:
Application
Filed:
September 28, 2020
Publication date:
February 18, 2021
Applicant:
Pfizer Inc.
Inventors:
Mary Theresa Didiuk, Robert Lee Dow, David Andrew Griffith