Abstract: Disclosed herein are compounds of formula Ar—N(SO2F)2, wherein Ar is selected from an optionally substituted aryl, an optionally substituted five-membered heteroaryl, or an optionally substituted six-membered heteroaryl. Also disclosed are methods of synthesizing the above compounds by reacting a compound of formula Ar—NH—R9 with MN(SO2F)2.
Type:
Application
Filed:
August 14, 2018
Publication date:
February 14, 2019
Applicants:
BIODURO, LLC, PFIZER INC.
Inventors:
Hua ZHOU, Paramita MUKHERJEE, Rongqiang LIU, Christopher W. AM ENDE, Tianjing DENG
Abstract: The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, R4, R5, a and A are as defined herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D3-mediated (or D3-associated) disorders including, e.g., substance addiction, substance abuse, schizophrenia (e.g., its cognitive symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD or PD), Parkinson's disease, mania, anxiety, impulse control disorders, sexual disorders and depression.
Type:
Application
Filed:
January 9, 2017
Publication date:
February 14, 2019
Applicant:
Pfizer Inc.
Inventors:
Thomas Allen Chappie, Jaclyn Louise Henderson, Joseph Michael Young, Travis T. Wager, Bethany Lyn Kormos, Nandini Chaturbhai Patel, Simone Sciabola, Jamison Bryce Tuttle, Patrick Robert Verhoest, Joseph Walter Tucker
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.
Type:
Application
Filed:
October 10, 2018
Publication date:
February 7, 2019
Applicant:
Pfizer Inc.
Inventors:
Michael Raymond Collins, Robert Steven Kania, Robert Arnold Kumpf, Pei-Pei Kung, Daniel Tyler Richter, Scott Channing Sutton, Martin James Wythes
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:
Application
Filed:
October 11, 2018
Publication date:
February 7, 2019
Applicant:
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: The present disclosure provides isolated binding molecules that bind to the human OX40R, nucleic acid molecules encoding an amino acid sequence of the binding molecules, vectors comprising the nucleic acid molecules, host cells containing the vectors, methods of making the binding molecules, pharmaceutical compositions containing the binding molecules, and methods of using the binding molecules or compositions.
Type:
Grant
Filed:
November 8, 2017
Date of Patent:
February 5, 2019
Assignees:
Pfizer Inc., Bristol-Myers Squibb Company
Inventors:
Jing Min, Yanli Wu, Rory F. Finn, Barrett R. Thiele, Wei Liao, Ronald P. Gladue, Arvind Rajpal, Timothy J. Paradis, Peter Brams, Brigitte Devaux, Yi Wu, Kristopher Toy, Heidi N. Leblanc, Haichun Huang
Abstract: In one aspect, the invention relates to a non-lipidated and non-pyruvylated Neisseria meningitidis serogroup B subfamily A A12 polypeptide. In another aspect, the invention relates to an immunogenic composition including an isolated non-lipidated, non-pyruvylated ORF2086 polypeptide from Neisseria meningitidis serogroup B, and at least one conjugated capsular saccharide from a meningococcal serogroup.
Type:
Grant
Filed:
June 22, 2017
Date of Patent:
February 5, 2019
Assignee:
Pfizer Inc.
Inventors:
Annaliesa Sybil Anderson, Susan Kay Hoiseth, Kathrin Ute Jansen, Justin Keith Moran, Mark E. Ruppen
Abstract: The present disclosure describes combination therapies comprising an agonist of OX40 and an agonist of 4-1BB, and the use of the combination therapies for the treatment of cancer.
Abstract: An antibody production process in mammalian cells in which engineered unpaired cysteine residues are post-translationally modified and capped with particular chemical entities, which capped antibodies are well suited to further site-specific conjugation steps to form antibody-drug conjugates (ADCs) or protein drug conjugates; ADCs produced using these capped antibodies including in particular ADCs formed by the selective reduction of the capped antibodies' cysteine residues, and ADCs formed using chemical handles such as aldehyde/azide/alkyne biorthogonal groups, which permit additional drug conjugation chemistry; and uncapped antibodies produced by cells in low cysteine, cysteine and glutathione media, and ADCs produced via direct conjugation to these uncapped antibodies.
Type:
Application
Filed:
August 9, 2016
Publication date:
January 31, 2019
Applicant:
PFIZER INC.
Inventors:
Xiaotian Zhong, Amarnauth Shastrie Prashad, Ronald William Kriz, Tao He, Will Somers, Wenge Wang, Leo Joseph Letendre
Abstract: Provided herein in part is a therapeutic nanoparticle that includes a biocompatible polymer; a polymer-EGFR ligand conjugate, wherein the EGFR ligand is covalently bound directly or through a chemical linker to the polymer, and a therapeutic agent.
Type:
Application
Filed:
October 12, 2018
Publication date:
January 31, 2019
Applicant:
Pfizer Inc.
Inventors:
Stephen E. Zale, Kevin Andrew McDonnell, Allen Thomas Horhota
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.
Abstract: The disclosure provides novel molecules related to growth and differentiation factor-8 (GDF8), in particular epitopes specific to GDF8 and other specific antagonists of GDF8 in particular anti-GDF8 antibodies or antigen binding protein or fragment thereof which may inhibit GDF8 activity and signal in vitro and/or in vivo. The disclosure also provides for an immunoassay used to detect and quantitate GDF8. The disclosure also provides methods for diagnosing, preventing, ameliorating, and treating GDF8-associated disorders, e.g., degenerative orders of muscle, bone, and insulin metabolism. Finally, the disclosure provides pharmaceuticals for the treatment of such disorders by using the antibodies, polypeptides, polynucleotides, and vectors of the invention.
Type:
Grant
Filed:
December 16, 2017
Date of Patent:
January 29, 2019
Assignee:
PFIZER INC.
Inventors:
Edward Roland LaVallie, Lisa Anne Collins-Racie, Christopher John Corcoran, Lioudmila Gennadievna Tchistiakova, John Adam Nowak, Riyez Karim, Xiang-Yang Tan, Kimberly Ann Marquette, Geertruida Machteld Veldman
Abstract: The present invention relates generally to the field of pharmaceutical formulations of antibodies. Specifically, the present invention relates to a stable liquid antibody formulation and its pharmaceutical preparation and use. This invention is exemplified by a liquid formulation of a humanized anti-NGF antibody.
Type:
Grant
Filed:
September 18, 2009
Date of Patent:
January 29, 2019
Assignee:
Pfizer Inc.
Inventors:
Advait Vijay Badkar, Leigh Kristen Bohack, Kevin Roger King, Alanta Lea Lary
Abstract: In one aspect, the invention relates to a composition including a factor H binding protein (fHBP) and a Neisseria meningitidis non-serogroup B capsular polysaccharide. The invention further relates to uses of a composition that includes fHBP, such as, for example, uses to elicit an immune response against N. meningitidis serogroup B strains and non-serogroup B strains. The compositions and methods described herein are directed to administration in humans, including adults, adolescents, toddlers, and infants.
Type:
Grant
Filed:
January 30, 2018
Date of Patent:
January 22, 2019
Assignee:
Pfizer Inc.
Inventors:
Kathrin Ute Jansen, Annaliesa Sybil Anderson, Judith Absalon, Jose Miguel Aste-Amezaga, Johannes Frederik Beeslaar, David Cooper, John Erwin Farley, Leah Diane Fletcher, Shannon Lea Harris, Thomas Richard Jones, Isis Kanevsky, Lakshmi Khandke, Paul Liberator, John Lance Perez, Lynn Marie Phelan, Gary Warren Zlotnick
Abstract: Described herein are polymeric nanoparticles that include a therapeutic agent, and methods of making and using such therapeutic nanoparticles. In some embodiments, the contemplated nanoparticles may include an excipient.
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.
Type:
Grant
Filed:
December 10, 2015
Date of Patent:
January 8, 2019
Assignee:
Pfizer Inc.
Inventors:
Kevin Richard Back, Michael Cram, Aidan James Harper, W. James Huang, Jonathan Richard Lillis, Timothy Michael Lukas, Sumit Luthra
Abstract: Provided herein are substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
Type:
Grant
Filed:
October 11, 2017
Date of Patent:
January 8, 2019
Assignee:
Pfizer Inc.
Inventors:
Matthew Dowling, Dilinie Fernando, Kentaro Futatsugi, Kim Huard, Thomas Victor Magee, Brian Raymer, Andre Shavnya, Aaron Smith, Benjamin Thuma, Andy Tsai, Meihua Tu
Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Type:
Grant
Filed:
August 16, 2016
Date of Patent:
January 8, 2019
Assignee:
Pfizer Inc.
Inventors:
Katherine Lin Lee, Christophe Philippe Allais, Christoph Martin Dehnhardt, Lori Krim Gavrin, Seungil Han, David Hepworth, Arthur Lee, Frank Eldridge Lovering, John Paul Mathias, Dafydd Rhys Owen, Nikolaos Papaioannou, Eddine Saiah, Joseph Walter Strohbach, John David Trzupek, Stephen Wayne Wright, Christoph Wolfgang Zapf
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:
Application
Filed:
April 19, 2016
Publication date:
January 3, 2019
Applicant:
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 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:
Application
Filed:
September 6, 2018
Publication date:
January 3, 2019
Applicant:
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 invention relates to a novel anti-PD-L1 antibody formulation. In particular, the invention relates to an aqueous pharmaceutical formulation of the anti-PD-L1 antibody Avelumab.
Type:
Application
Filed:
December 5, 2016
Publication date:
December 27, 2018
Applicants:
MERCK PATENT GmbH, PFIZER INC.
Inventors:
Gianluca RINALDI, Alessandra DEL RIO, Silvia FRATAR-CANGELI, Senta VOSS, Markus WEIGANDT