Abstract: The present invention relates to therapeutic dosing regimens utilizing a dose reduction strategy for treating disorders characterized by marked elevations of low density protein cholesterol (LDL-C) in the plasma of a patient. The subject therapeutic dosing regimens involve delivering as a single administration or plurality of administrations of an anti-proprotein convertase subtilisin kexin type 9 (PCSK9) antagonist antibody as an initial dose of at least about 100 mg, and delivering as a single administration or plurality of administrations at a subsequent dose in an amount that is about the same as the initial dose, or at least half the initial dose after the patient has a LDL-C level at or below about 25, 20, 15 or 10 mg/dL, preferably at or below 10 mg/dL.
Type:
Grant
Filed:
September 9, 2015
Date of Patent:
November 12, 2019
Assignee:
Pfizer Inc.
Inventors:
Anne Barbara Cropp, Albert Kim, David Raymond Plowchalk, Kevin Richard Sweeney, Ellen Qiao Wang
Abstract: A method for the treatment of cancer comprising administration of a therapeutically effective amount of an intralesional chemoablative pharmaceutical composition, or variant of said composition, in combination with a therapeutically effective amount of a systemic immunomodulatory anticancer agent. A further method for the treatment of cancer comprising administration of a therapeutically effective amount of an intralesional chemoablative pharmaceutical composition, or variant of said composition, in combination with a therapeutically effective amount of a systemic targeted anticancer agent. The present invention is further directed to pharmaceutical compositions for treatment of cancer. The intralesional chemoablative pharmaceutical composition can comprise an IL chemoablative agent comprising primarily a halogenated xanthene.
Type:
Grant
Filed:
November 6, 2017
Date of Patent:
November 12, 2019
Assignees:
Provectus Pharmatech, Inc., Pfizer, Inc.
Inventors:
Craig J. Eagle, H. Craig Dees, Eric A. Wachter, Jamie Singer
Abstract: A compound having the structure: or an acceptable salt thereof, wherein X is N or CR, where R is hydrogen, alkyl, etc.; A is selected from the group consisting of a bond, C?O, —SO2—, etc.; A? is selected from the group consisting of a bond, C?O, etc.; Z is —(CH2)h— or a bond, etc.; R1 and R1? are independently selected from the group consisting of hydrogen, alkyl, etc.; R2 is selected from hydrogen, alkyl, etc.; R3 is selected from the group consisting of hydrogen, and amino; R4 is monocyclic or bicyclic, etc.; R5 is independently selected from hydrogen, alkyl, etc.; h, j, k, m, n and q are integers as 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 with other therapeutic agents.
Type:
Grant
Filed:
May 3, 2017
Date of Patent:
November 5, 2019
Assignee:
Pfizer Inc.
Inventors:
Andrew Fensome, Ariamala Gopalsamy, Brian S. Gerstenberger, Ivan Viktorovich Efremov, Zhao-Kui Wan, Betsy Pierce, Jean-Baptiste Telliez, John I. Trujillo, Liying Zhang, Li Xing, Eddine Saiah
Abstract: Disclosed herein are FGF23 c-tail fusion proteins, pharmaceutical compositions comprising the FGF23 c-tail fusion proteins, and methods of treatment using the FGF23 c-tail fusion proteins. This application discloses fusion proteins comprising a FGF-23 c-tail protein fused to a heterologous amino acid sequence, wherein said fusion protein modulates serum phosphate levels but does not substantially modulate serum 1, 25 VitD levels. In some embodiments, the FGF-23 c-tail protein is fused to the heterologous amino acid sequence via a linker. This invention also encompasses vectors comprising the nucleic acids disclosed herein, and a host cell comprising the vector or polynucleotides encoding the proteins of the invention.
Type:
Grant
Filed:
March 30, 2015
Date of Patent:
November 5, 2019
Assignees:
New York University, Pfizer Inc.
Inventors:
Moosa Mohammadi, Regina Goetz, Jeanne Sue Magram, Kristen Leigh Johnson
Abstract: The present invention relates to dosing regimen of avelumab for the treatment of cancer. In particular, the invention relates to improved dosing regimen of avelumab for the treatment of cancer.
Type:
Application
Filed:
October 5, 2017
Publication date:
October 31, 2019
Applicants:
PFIZER INC, MERCK PATENT GmbH
Inventors:
Glen Ian Andrews, Carlo Leonel BELLO, Satjit Singh BRAR, Shaonan WANG, Pascal GIRARD
Abstract: Diagnostic methods for predicting whether a human tumor is sensitive to treatment with axitinib, and methods of treating a human tumor are disclosed. The methods are based on measurement of CD68 polypeptide expression levels in a tissue sample from a tumor. CD68 expression levels can be measured using immunohistochemistry, where the percentage of CD68-positive cells and density of CD68-positive cells within the tumor can be determined.
Type:
Application
Filed:
March 1, 2019
Publication date:
October 31, 2019
Applicant:
PFIZER INC.
Inventors:
Jean-François André MARTINI, Jamal Christo TARAZI, James Andrew WILLIAMS
Abstract: The present invention provides antibodies, or antigen-binding fragment thereof, which specifically bind to TL1A. The invention further provides a method of obtaining such antibodies and nucleic acids encoding the same. The invention further relates to compositions and therapeutic methods for use of these antibodies for the treatment and/or prevention of TL1A mediated diseases, disorders or conditions.
Type:
Application
Filed:
May 24, 2019
Publication date:
October 31, 2019
Applicants:
Pfizer Inc., Bristol-Myers Squibb Company
Inventors:
Robert Arch, Jun Zhang, Michelle Mader, Tetsuya Ishino, Joel Bard, William Finlay, Orla Cunningham, Ciara Reilly, Peter Brams, Brigitte Devaux, Haichun Huang, Karla Henning
Abstract: This invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof, in which R-groups R1 to R23, A, Q, U, V, W, X, Y, Z, n, p and q are as defined herein, 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, in a subject.
Type:
Application
Filed:
April 23, 2019
Publication date:
October 31, 2019
Applicant:
Pfizer Inc.
Inventors:
Ping Chen, Sujin Cho-Schultz, Judith Gail Deal, Gary Michael Gallego, Mehran Jalaie, Robert Steven Kania, Sajiv Krishnan Nair, Sacha Ninkovic, Suvi Tuula Marjukka Orr, Cynthia Louise Palmer
Abstract: Compounds of Formula (A) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by pharmaceutical compositions and the uses thereof as asialoglycoprotein receptor (ASGPR) targeting agents.
Type:
Application
Filed:
June 24, 2019
Publication date:
October 24, 2019
Applicant:
Pfizer Inc.
Inventors:
Spiros Liras, Vincent Mascitti, Benjamin Thuma
Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
Type:
Grant
Filed:
April 5, 2018
Date of Patent:
October 22, 2019
Assignee:
Pfizer, Inc.
Inventors:
Michael J. Luzzio, Kevin D. Freeman-Cook, Samit K. Bhattacharya, Matthew M. Hayward, Catherine A. Hulford, Christopher L. Autry, Xumiao Zhao, Jun Xiao, Kendra L. Nelson
Abstract: Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Type:
Application
Filed:
July 7, 2017
Publication date:
October 17, 2019
Applicant:
Pfizer Inc.
Inventors:
Agustin Casimiro-Garcia, Joseph Walter Strohbach, David Hepworth, Frank Eldridge Lovering, Chulho Choi, Christophe Philippe Allais, Stephen Wayne Wright
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 MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, traumatic brain injury, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.
Type:
Grant
Filed:
November 9, 2017
Date of Patent:
October 1, 2019
Assignee:
Pfizer Inc.
Inventors:
Christopher Ryan Butler, Laura Ann McAllister, Elizabeth Mary Beck, Michael Aaron Brodney, Adam Matthew Gilbert, Christopher John Helal, Douglas Scott Johnson, Justin Ian Montgomery, Steven Victor O'Neil, Bruce Nelsen Rogers, Patrick Robert Verhoest, Damien Webb
Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating ROR? activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.
Type:
Grant
Filed:
February 6, 2019
Date of Patent:
October 1, 2019
Assignee:
Pfizer Inc.
Inventors:
Mark Edward Schnute, Andrew Christopher Flick, Peter Jones, Neelu Kaila, Scot Richard Mente, John David Trzupek, Michael L. Vazquez, Goran Mattias Wennerstal, Li Xing, Edouard Zamaratski, Liying Zhang, Rayomand Jal Unwalla
Abstract: Compounds such as: processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds to treat neoplasms have been disclosed.
Type:
Grant
Filed:
February 17, 2016
Date of Patent:
October 1, 2019
Assignee:
Pfizer Inc.
Inventors:
John Howard Tatlock, Indrawan James McAlpine, Michelle Bich Tran-Dube, Eugene Yuanjin Rui, Martin James Wythes, Robert Arnold Kumpf, Michele Ann McTigue
Abstract: The present invention provides, in part, heterocyclic spiro 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 MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.
Type:
Application
Filed:
June 3, 2019
Publication date:
September 26, 2019
Applicant:
Pfizer Inc.
Inventors:
Michael Aaron Brodney, Christopher Ryan Butler, Laura Ann McAllister, Chistopher John Helal, Steven Victor O'Neil, Patrick Robert Verhoest
Abstract: Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Type:
Application
Filed:
April 10, 2019
Publication date:
September 26, 2019
Applicant:
Pfizer Inc.
Inventors:
Agustin Casimiro-Garcia, Jeffrey Scott Condon, Andrew Christopher Flick, Ariamala Gopalsamy, Steven J. Kirincich, John Paul Mathias, Joseph Walter Strohbach, Jason Shaoyun Xiang, Li Huang Xing, Xiaolun Wang
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:
September 6, 2018
Date of Patent:
September 24, 2019
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 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:
October 22, 2018
Date of Patent:
September 24, 2019
Assignee:
Pfizer Inc.
Inventors:
Shu-Hui Liu, Flavia Mercer Pernasetti, Wei-Hsien Ho