Abstract: The present invention is directed to novel cytotoxic tubulysin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.
Inventors:
Chakrapani SUBRAMANYAM, Lawrence N. TUMEY, Longfei XIE, Carolyn LEVERETT, Beth C. VETELINO, Sai Chetan K. SUKURU, Sarah HUDSON, Venkata Ramana DOPPALAPUDI, Abhijit S. BHAT
Abstract: The present invention provides antibodies that specifically bind to FLT3 (Fms-Like Tyrosine Kinase 3). The invention further provides bispecific antibodies that bind to FLT3 and another antigen (e.g., CD3). The invention further relates to antibody encoding nucleic acids, and methods of obtaining such antibodies (monospecific and bispecific). The invention further relates to therapeutic methods for use of these antibodies for the treatment of FLT3-mediated pathologies, including cancer such as Acute Myeloid Leukemia (AML).
Type:
Application
Filed:
May 31, 2018
Publication date:
December 6, 2018
Applicant:
PFIZER INC.
Inventors:
Danielle Elizabeth DETTLING, Yik Andy YEUNG, Kristian Todd POULSEN, Veena KRISHNAMOORTHY, Cesar Adolfo SOMMER
Abstract: The present invention relates to pyrazolopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-1H-pyrazolo[3,4-c]pyridazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined in the description. The pyrazolopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They may useful in the treatment of a number of conditions, including pain and epilepsy.
Type:
Application
Filed:
November 22, 2016
Publication date:
December 6, 2018
Applicant:
PFIZER LIMITED
Inventors:
KEVIN NEIL DACK, ROBERT MCKENZIE OWEN, DAVID CAMERON PRYDE
Abstract: The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic acid and a therapeutic agent (1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea), or pharmaceutically acceptable salts thereof, and a polymer. Other aspects include methods of making and using such nanoparticles.
Type:
Application
Filed:
August 2, 2018
Publication date:
December 6, 2018
Applicant:
PFIZER INC.
Inventors:
Shubha Bagrodia, Jennifer Lafontaine, Zach Lovatt, Eyoung Shin, Young Ho Song, Greg Troiano, Hong Wang
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:
Application
Filed:
August 7, 2018
Publication date:
December 6, 2018
Applicant:
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
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), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.
Type:
Application
Filed:
August 10, 2018
Publication date:
December 6, 2018
Applicant:
PFIZER INC.
Inventors:
DAVID LAWRENCE FIRMAN GRAY, LEI ZHANG, JENNIFER ELIZABETH DAVOREN, AMY BETH DOUNAY, IVAN VIKTOROVICH EFREMOV, CHEWAH LEE, SCOT RICHARD MENTE, STEVEN VICTOR O'NEIL, BRUCE NELSEN ROGERS, CHAKRAPANI SUBRAMANYAM
Abstract: A compound having the structure: or a pharmaceutically acceptable salt thereof, wherein A, A? and A? are independently O, C?O, etc.; R0 and R are independently H, Br, Cl, F, or C1-C6 alkyl; R1 is H, C1-C6 alkyl, or hydroxy(C1-C6 alkyl); R2 is selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, etc.; R6, R7 and R8 are each independently H, C1-C6 alkyl, C1-C4 alkoxy(C1-C6 alkyl), etc.; and, n is 0, 1, 2 or 3. 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:
Grant
Filed:
February 21, 2017
Date of Patent:
December 4, 2018
Assignee:
Pfizer Inc.
Inventors:
Matthew Frank Brown, Alpay Dermenci, Andrew Fensome, Brian Stephen Gerstenberger, Matthew Merrill Hayward, Dafydd Rhys Owen, Stephen Wayne Wright, Li Huang Xing, Xiaojing Yang
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:
May 31, 2017
Date of Patent:
December 4, 2018
Assignee:
Pfizer Inc.
Inventors:
Shu-Hui Liu, Flavia Mercer Pernasetti, Wei-Hsien Ho
Abstract: The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a antibiotic therapeutic agent; about 0.05 to about 30 weight percent of a hydrophobic acid; and about 35 to about 99.75 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol or diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol. Other aspects include methods of making such nanoparticles.
Abstract: Cytotoxic dimers comprising CBI-based and/or CPI-based sub-units, antibody drug conjugates comprising such dimers, and to methods for using the same to treat cancer and other conditions.
Type:
Application
Filed:
August 2, 2018
Publication date:
November 29, 2018
Applicant:
PFIZER INC.
Inventors:
Andreas MADERNA, Matthew David DOROSKI, Zecheng CHEN, Hud Lawrence RISLEY, Jeffrey Michael CASAVANT, Christopher John O'DONNELL, Alexander M. PORTE, Chakrapani SUBRAMANYAM
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:
Grant
Filed:
August 19, 2016
Date of Patent:
November 27, 2018
Assignee:
Pfizer Inc.
Inventors:
Stephen E. Zale, Kevin Andrew McDonnell, Allen Thomas Horhota
Abstract: The present invention provides antibodies, or antigen-binding portions thereof, which specifically bind to IL-2 and reduce the affinity of IL-2 binding to IL-2R? and IL-2R?. 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 autoimmune diseases, disorders or conditions and for immunosuppression, including, but not limited to, administering a complex comprising the antibody and IL-2.
Type:
Grant
Filed:
October 21, 2016
Date of Patent:
November 27, 2018
Assignees:
The Regents of the University of California, The Board of Trustees of the Leland Stanford Junior University, Pfizer Inc.
Inventors:
Isaac J. Rondon, Natasha Crellin, Paul Bessette, Eleonora Trotta, Jeffrey A. Bluestone, Lauren K. Ely, Kenan C. Garcia
Abstract: The present invention is directed to pyrazolopyrimine compounds or pharmaceutically acceptable salts which are inhibitors of PDE4 isozymes, especially with a binding affinity for PDE4B isoform, and compositions thereof.
Type:
Grant
Filed:
July 10, 2015
Date of Patent:
November 20, 2018
Assignee:
Pfizer Inc.
Inventors:
Thomas Allen Chappie, Patrick Robert Verhoest, Nandini Chaturbhai Patel, Matthew Merrill Hayward, Christopher John Helal, Simone Sciabola, Travis T. Wager, Erik Alphie LaChapelle, Joseph Michael Young
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:
November 29, 2017
Date of Patent:
November 13, 2018
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: The present invention relates to new immunogenic compositions comprising conjugated Streptococcus pneumoniae capsular saccharide antigens (glycoconjugates), kits comprising said immunogenic compositions and uses thereof. Immunogenic compositions of the present invention will typically comprise at least one glycoconjugate from a S. pneumoniae serotype not found in PREVNAR®, SYNFLORIX® and/or PREVNAR 13®. The invention also relates to vaccination of human subjects, in particular infants and elderly, against pneumococcal infections using said novel immunogenic compositions.
Type:
Grant
Filed:
July 20, 2016
Date of Patent:
November 13, 2018
Assignee:
Pfizer Inc.
Inventors:
Wendy Jo Watson, Luis Pascual Jodar Martin-Montalvo, Raul Enrique Isturiz, Ralf Rene Reinert
Abstract: A device for dispensing individual doses of powder from respective pockets of a disc-shaped carrier by outwardly rupturing a lidding foil by means of pressure on an opposite side surface, the device providing individual respective deaggregation flow paths for each pocket, split airstreams allowing improved entrainment of powder, a cam mechanism for outwardly rupturing the pockets, an indexing mechanism linked to the cam mechanism and a dose counter.
Type:
Grant
Filed:
June 13, 2016
Date of Patent:
November 13, 2018
Assignee:
Pfizer Limited
Inventors:
Peter J. Houzego, John Kelshaw Conway, Martin Douglas Pearl, Andrew Mark Bryant
Abstract: The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic base, an acidic therapeutic agent, and a polymer. Other aspects include methods of making and using such nanoparticles.
Type:
Application
Filed:
October 28, 2016
Publication date:
November 1, 2018
Applicant:
Pfizer Inc.
Inventors:
Young-Ho Song, Maria Conceicao Figueiredo, David Michael DeWitt
Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1, R2 and R3 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Type:
Grant
Filed:
July 11, 2017
Date of Patent:
October 30, 2018
Assignee:
Pfizer Inc.
Inventors:
Michael Aaron Brodney, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill, Patrick Robert Verhoest, Peter Justin Mikochik, John Charles Murray, Xinjun Hou
Abstract: The invention relates to activated Streptococcus pneumoniae serotype 10A, 22F or 33F polysaccharides and processes for their preparation. The invention also relates to immunogenic conjugates comprising Streptococcus pneumoniae serotype 10A, 22F or 33F polysaccharides covalently linked to a carrier protein, processes for their preparation and immunogenic compositions and vaccines comprising them.
Type:
Grant
Filed:
January 15, 2015
Date of Patent:
October 23, 2018
Assignee:
Pfizer Inc.
Inventors:
Jianxin Gu, Rajesh Kumar Kainthan, Jin-Hwan Kim, Avvari Krishna Prasad, Yu-Ying Yang
Abstract: Compositions, methods, and kits that deliver a compound, such as 5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, through a keratin substrate are presented.