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:
Grant
Filed:
August 9, 2018
Date of Patent:
February 22, 2022
Assignee:
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: The combination of (S)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide or pharmaceutically acceptable salt thereof, and 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4?-piperidine]-1?-carbonyl)-6-methoxypyridin-2-yl)benzoic acid or pharmaceutically acceptable salt thereof, for treatment of diseases, including non-alcoholic steatohepatitis (NASH), in mammals are described herein.
Type:
Grant
Filed:
August 28, 2019
Date of Patent:
February 22, 2022
Assignee:
Pfizer Inc.
Inventors:
William Paul Esler, Trenton Thomas Ross
Abstract: The present invention relates to a manufacturing process and intermediates for preparing a crystalline or non-crystalline form of N-((1S,3S)-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclobutyl)propane-1-sulfonamide. The present invention also relates to salt forms and pharmaceutical compositions comprising the crystalline form, and to methods for use of the compound prepared from a crystalline form in the treatment of various diseases.
Type:
Grant
Filed:
September 29, 2020
Date of Patent:
February 22, 2022
Assignee:
Pfizer Inc.
Inventors:
Kapildev Kashmirilal Arora, Jacob Cole DeForest, Andrew Kevern Hills, Brian Patrick Jones, Kris Nicole Jones, Chad Arthur Lewis, Anil Mahadeo Rane
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:
Grant
Filed:
March 13, 2020
Date of Patent:
February 22, 2022
Assignee:
Pfizer Inc.
Inventors:
Scott Max Herbig, Sriram Krishnaswami, Joseph Kushner, IV, Manisha Lamba, Thomas C. Stock
Abstract: The present disclosure provides human IL-2 variants, recombinant oncolytic viruses comprising the IL-2 variant, compositions comprising the IL-2 variant or recombinant oncolytic virus, and use of the IL-2 variants, recombinant oncolytic virus, or compositions for treating cancer in an individual.
Type:
Application
Filed:
July 9, 2021
Publication date:
February 3, 2022
Applicant:
Pfizer Inc.
Inventors:
Joseph John Binder, Michael Dale Eisenbraun, Clare Lees, Jeremy Shawn Myers, James Travis Patterson
Abstract: This invention relates to a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of abnormal cell growth in mammals, especially humans.
Type:
Application
Filed:
October 6, 2021
Publication date:
January 27, 2022
Applicant:
PFIZER INC.
Inventors:
Eric Christian Hansen, Christopher Scott Seadeek, Anil Mahadeo Rane
Abstract: This invention relates to a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of abnormal cell growth in mammals, especially humans.
Type:
Application
Filed:
October 6, 2021
Publication date:
January 27, 2022
Applicant:
PFIZER INC.
Inventors:
Eric Christian Hansen, Christopher Scott Seadeek
Abstract: The combination of (S)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide or pharmaceutically acceptable salt thereof, and 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4?-piperidine]-1?-carbonyl)-6-methoxypyridin-2-yl)benzoic acid or pharmaceutically acceptable salt thereof, for treatment of diseases, including non-alcoholic steatohepatitis (NASH), in mammals are described herein.
Type:
Application
Filed:
October 11, 2021
Publication date:
January 27, 2022
Applicant:
Pfizer Inc.
Inventors:
William Paul Esler, Trenton Thomas Ross
Abstract: The present invention relates to antibodies that specifically bind to B7-H4 (B7 Homology 4, encoded by gene VTCN1) and bispecific antibodies that specifically bind to both B7-H4 and CD3 (Cluster of Differentiation 3), and polynucleotides, pharmaceutical compositions and methods and uses thereof.
Type:
Application
Filed:
July 16, 2021
Publication date:
January 20, 2022
Applicant:
PFIZER INC.
Inventors:
JAMES REASONER APGAR, ANDREA THERESE HOOPER, MALGORZATA AGNIESZKA NOCULA-LUGOWSKA, LEI WU
Abstract: The invention relates to compounds of formula I wherein R1, R2 and - - - - - are as defined herein, pharmaceutical compositions comprising the compounds and methods of treating COVID-19 in a patient by administering therapeutically effective amounts of the compounds and methods of inhibiting or preventing replication of SARS-CoV-2 with the compounds.
Type:
Application
Filed:
July 1, 2021
Publication date:
January 20, 2022
Applicant:
Pfizer Inc.
Inventors:
Robert Steven Kania, Padmavani Bezawada, Emma Louise Hawking, Rohit Jaini, Samir Kulkarni, Matthew Nathan O'Brien Laramy, Jonathan Richard Lillis, Suman Luthra, Dafydd Rhys Owen, Klimentina Dimitrova Pencheva, Martin Youngjin Pettersson, Anil Mahadeo Rane, Matthew Forrest Sammons, Bradley Paul Sullivan, Andrew John Thiel, Martyn David Ticehurst, Jamison Bryce Tuttle, Robert Louis Hoffman
Abstract: The present invention relates to new glycoconjugates comprising Streptococcus pneumoniae capsular saccharide antigens and uses thereof. Glycoconjugates of the present invention will typically comprise 2 or more saccharides antigens conjugated to the same molecule of the protein carrier. The invention also relates to vaccination of human subjects, in particular infants and elderly, against pneumoccocal infections using immunogenic compositions comprising said novel glycoconjugates.
Type:
Application
Filed:
December 9, 2019
Publication date:
January 20, 2022
Applicant:
Pfizer Inc.
Inventors:
Avvari Krishna Prasad, Jianxin Gu, Jin-Hwan Kim, Suddham Singh
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:
Grant
Filed:
July 29, 2020
Date of Patent:
January 11, 2022
Assignee:
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: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
Type:
Grant
Filed:
April 17, 2019
Date of Patent:
January 11, 2022
Assignee:
PFIZER INC.
Inventors:
Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
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:
Application
Filed:
July 13, 2021
Publication date:
January 6, 2022
Applicants:
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: A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently hydrogen or hydroxy; wherein R1 and R2 are not both hydroxy. 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:
June 30, 2021
Publication date:
January 6, 2022
Applicant:
Pfizer Inc.
Inventors:
Brian Stephen GERSTENBERGER, Wenhua JIAO, Manjinder Singh LALL, Ricardo LIRA, Mark Edward SCHNUTE
Abstract: In one aspect, the invention relates to an immunogenic composition that includes a mutant Clostridium difficile toxin A and/or a mutant Clostridium difficile toxin B. The mutant toxin may include a glucosyltransferase domain having at least one mutation and a cysteine protease domain having at least one mutation, relative to the corresponding wild-type C. difficile toxin. The mutant toxins may include at least one amino acid that is chemically crosslinked. In another aspect, the invention relates to methods and compositions for use in culturing Clostridium difficile and in producing C. difficile toxins.
Type:
Grant
Filed:
December 5, 2019
Date of Patent:
December 28, 2021
Assignee:
Pfizer Inc.
Inventors:
Jason Arnold Lotvin, Annaliesa Sybil Anderson, Robert G. K. Donald, Michael James Flint, Narender Kumar Kalyan, Kathrin Ute Jansen, Maninder K. Sidhu, Justin Keith Moran, Mark Edward Ruppen, Weiqiang Sun
Abstract: This invention relates to compounds of general Formula I in which A, R1, R2, R3 and R4 are as defined herein, and the pharmaceutically acceptable salts thereof; to pharmaceutical compositions comprising such compounds and salts; to methods of using such compounds, salts and compositions for treating pulmonary hypertension and related diseases, like pulmonary arterial hypertension; to methods of using such compounds, salts and compositions for treating abnormal cell growth, such as cancer; and to processes to make such compounds, salts and compositions.
Type:
Grant
Filed:
April 15, 2020
Date of Patent:
December 21, 2021
Assignee:
Pfizer Inc.
Inventors:
Samit Kumar Bhattacharya, Douglas Carl Behenna, Kimberly O. Cameron, Ping Chen, John M. Curto, Kevin Daniel Freeman-Cook, Mehran Jalaie, Robert Steven Kania, Yajing Lian, Sajiv Krishnan Nair, Cynthia Louise Palmer, Martin Youngjin Pettersson, Eugene Yuanjin Rui, Matthew Sammons, Qingyi Yang, Liying Zhang
Abstract: The present invention discloses a novel p-toluenesulfonic acid salt and a crystalline polymorphic Form 1 of said salt of 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one, pharmaceutical composition containing the same, as well as preparations and uses thereof. The present invention also discloses a novel phosphoric acid salt of 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one, pharmaceutical composition containing the same, as well as preparations and uses thereof.
Type:
Application
Filed:
October 21, 2019
Publication date:
December 16, 2021
Applicant:
Pfizer Inc.
Inventors:
Brian Matthew SAMAS, Yong TAO, Douglas James Critcher, David Sydney Bernard Daniels, Kevin Paul Girard, Gregory Scott Goeken, Peter Robert Rose
Abstract: This invention relates to crystalline (1S,2S,3S,5R)-3-((6-(difluoromethyl)-5-fluoro-1,2,3,4-tetrahydroisoquinolin-8-yl)oxy)-5-(4-methyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol monophosphate hydrate, and to compositions and therapeutic uses thereof.
Abstract: Provided herein are methods and combinations for treating a subject having cancer by administering to the subject a PD-1/PD-L1 axis inhibitor, a CD-122-biased cytokine agonist, and an anti-androgen or a pharmaceutically acceptable salt thereof.