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), age-related cognitive decline, dementia, and Parkinson's disease.
Type:
Grant
Filed:
June 23, 2014
Date of Patent:
December 27, 2016
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 disclosure provides isolated binding molecules that bind to human 4-1BB, 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:
September 6, 2016
Publication date:
December 22, 2016
Applicant:
Pfizer Inc.
Inventors:
Bianca Ahrens, Sangita M. Baxi, Timothy Scott Fisher, Richard Michael Jerome, Kathrin Ladetzki-Baehs, Theodore Lawrence Oliphant, Leslie Lynne Sharp, Michael Tesar, Libbey Anne Yates, Moritz Zulley
Abstract: Disclosed are novel pyridine pyrazinones or pharmaceutically acceptable salts thereof. Pharmaceutical compositions and the use of the compounds to treat diseases or disorders that are BET family bromodomain-dependent are also disclosed. Methods for preparing and using these compounds are further described.
Type:
Application
Filed:
June 16, 2016
Publication date:
December 22, 2016
Applicant:
Pfizer Inc.
Inventors:
Agustin Casimiro-Garcia, Bruce Allen Lefker, Nikolaos Papaioannou, Arjun Venkat Narayanan, Jotham Wadsworth Coe
Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
Type:
Application
Filed:
August 26, 2016
Publication date:
December 15, 2016
Applicant:
Pfizer Inc.
Inventors:
Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
Abstract: A compound having the structure: or a pharmaceutically acceptable salt or solvate thereof, wherein A and A? are C or N, where C may be substituted by halo or C1-C6 alkyl; R and R0 are selected from the group consisting of H, C1-C6 alkyl, —(CH2)n—W, etc., where W is 5- or 6-membered heteroaryl or heterocyclic containing N, S and/or O atoms, —NR?SO2—R?, etc., where R? and R? are C1-C6 alkyl, etc.; wherein each alkyl, etc., may be substituted; or, R and R0 and the N atom to which they are bonded together to form a monocyclic or bicyclic heterocyclic ring, etc.; R1 is H, halo or cyano; R2 and R2? are H, C1-C6 alkyl, etc.; X is a bond, etc.; R3 is H, C1-C4 alkyl, etc.; Y is a bond, —(CH2)m—, etc. The invention also relates to compositions and uses in the treatment of various diseases.
Type:
Grant
Filed:
May 13, 2015
Date of Patent:
December 13, 2016
Assignee:
Pfizer Inc.
Inventors:
Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Yogesh Anil Sabnis, Joseph Walter Strohbach, Florian Michel Wakenhut, Gavin Alistair Whitlock
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:
October 3, 2014
Date of Patent:
December 13, 2016
Assignee:
PFIZER INC.
Inventors:
Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
Abstract: The invention provides eTEC linked glycoconjugates comprising a saccharide covalently conjugated to a carrier protein through a (2-((2-oxoethyl)thio)ethyl)carbamate (eTEC) spacer, immunogenic compositions comprising such glycoconjugates, and methods for the preparation and use of such glycoconjugates and immunogenic compositions.
Type:
Grant
Filed:
August 12, 2013
Date of Patent:
December 13, 2016
Assignee:
Pfizer Inc.
Inventors:
Jianxin Gu, Jin-hwan Kim, A. Krishna Prasad, Yu-ying Yang
Abstract: The invention provides a compound of Formula (I) 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:
August 15, 2016
Publication date:
December 1, 2016
Applicant:
PFIZER INC.
Inventors:
Mary Didiuk, Robert Lee Dow, David Andrew Griffith
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:
Application
Filed:
August 10, 2016
Publication date:
December 1, 2016
Applicant:
Pfizer Inc.
Inventors:
John David Trzupek, Katherine Lin Lee, Mark Edward Bunnage, Seungil Han, David Hepworth, Frank Eldridge Lovering, John Paul Mathias, Nikolaos Papaioannou, Betsy Susan Pierce, Joseph Walter Strohbach, Stephen Wayne Wright, Christoph Wolfgang Zapf, Lori Krim Gavrin, Arthur Lee, David Randolph Anderson, Kevin Joseph Curran, Christoph Martin Dehnhardt, Eddine Saiah, Joel Adam Goldberg, Xiaolun Wang, Horng-Chih Huang, Richard Vargas, Michael Dennis Lowe, Akshay Patny
Abstract: The present invention is directed to novel cytotoxic spliceostatin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.
Type:
Grant
Filed:
August 5, 2015
Date of Patent:
November 29, 2016
Assignee:
Pfizer Inc.
Inventors:
Chakrapani Subramanyam, Frank Erich Koehn, Kenneth John Dirico, Alessandra S. Eustaquio, Michael Eric Green, Haiyin He, Min He, Christopher John O'Donnell, Sujiet Puthenveetil, Anokha Ratnayake, Jesse Alexander Teske, Hui Yu Yang
Abstract: The present disclosure generally relates to lyophilized pharmaceutical compositions comprising a sugar, a cyclodextrin, and polymeric nanoparticles comprising a copolymer and a therapeutic agent which, upon reconstitution, have low levels of greater than 10 micron size particles. Other aspects of the invention include methods of making such nanoparticles.
Type:
Grant
Filed:
November 7, 2014
Date of Patent:
November 22, 2016
Assignee:
Pfizer Inc.
Inventors:
Greg Troiano, Young-Ho Song, Stephen E. Zale, James Wright, Christina Van Geen Hoven
Abstract: The present invention provides a process for preparing a compound of formula: (Formula XI and XII) (XI) (XII) wherein X, Y, Z, A, B and E are as defined herein, by reacting a compound of formula: (Formula XIII) (XIII) with a compound of formula: (Formula XIV and XV) (XIV) (XV) respectively, in the presence of a transition metal catalyst, a ligand suitable for use with 15 the catalyst and a reducing agent. The invention also provides novel intermediates.
Type:
Grant
Filed:
April 20, 2016
Date of Patent:
November 22, 2016
Assignee:
Pfizer Ireland Pharmaceuticals
Inventors:
Adam James Musgrave Burrell, Padraig Mary O'Neill, Alan John Pettman
Abstract: The present invention relates to new immunogenic compositions comprising conjugated Streptococcus pneumoniae capsular saccharide antigens (glycoconjugates) 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 pneumoccocal infections using said novel immunogenic compositions.
Type:
Grant
Filed:
January 15, 2015
Date of Patent:
November 15, 2016
Assignee:
Pfizer Inc.
Inventors:
Emilio Anthony Emini, Wendy Jo Watson, Avvari Krishna Prasad, Mingming Han, Jin-Hwan Kim, Jianxin Gu, Yu-ying Yang, Rajesh Kumar Kainthan, David Cooper, Michael William Pride, Kathrin Ute Jansen
Abstract: The present invention provides for novel compositions of anti-CTLA-4 antibodies comprising a chelating agent. Also provided are method of treating diseases and conditions with novel compositions of CTLA-4 antibodies, including various neoplasia conditions.
Type:
Grant
Filed:
March 2, 2006
Date of Patent:
November 8, 2016
Assignee:
Pfizer Inc.
Inventors:
Justin Abate, Kevin Muthurania, Sandeep Nema, Satish Singh, Carrie Elliott, Tapan Das
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:
Grant
Filed:
June 16, 2015
Date of Patent:
November 1, 2016
Assignee:
PFIZER INC.
Inventors:
Robert Steven Kania, Robert Arnold Kumpf, Pei-Pei Kung, Scott Channing Sutton, Martin James Wythes
Abstract: The present invention relates to the provision of immunogens comprising an antigenic PCSK9 peptide linked to an immunogenic carrier for the prevention, treatment or alleviation of PCSK9-mediated disorders. The invention further relates to methods for production of these medicaments, immunogenic compositions and pharmaceutical compositing thereof and their use in medicine.
Type:
Grant
Filed:
October 7, 2014
Date of Patent:
November 1, 2016
Assignee:
Pfizer Vaccines LLC
Inventors:
Brian Robert Champion, Leonard Gabriel Contillo, Jr., Michael Dale Eisenbraun, James Downey Fraser, Julie Jia Li Hawkins, James Richard Merson, Brian Gregory Pierce, Xiayang Qiu, Jakir Hussain Ullah, David Michael Wyatt
Abstract: The present disclosure provides a compound of Formula I: or a pharmaceutically acceptable salt wherein X, R1-R8, Y1-Y5, m, n, p, and q are defined herein. The novel 2H-chromene compounds are useful for the modulation of disorders mediated by estrogen, and other disorders, as described herein. The present invention also relates to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions.
Type:
Application
Filed:
April 22, 2016
Publication date:
October 27, 2016
Applicant:
PFIZER INC.
Inventors:
Peter J. KUSHNER, David C. MYLES, Cyrus L. HARMON, Leslie Carol HODGES GALLAGHER
Abstract: The present invention relates in part to chemical compounds, and methods for producing these compounds. The compounds may also be incorporated into compositions to enhance quit rates or reduce relapse in smoking cessation and further in treating nicotine-related dependence.
Type:
Grant
Filed:
March 1, 2016
Date of Patent:
October 25, 2016
Assignee:
Pfizer Inc.
Inventors:
Janice Ethel Sieser, Robert Alan Singer
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.
Type:
Application
Filed:
June 27, 2016
Publication date:
October 20, 2016
Applicant:
PFIZER INC.
Inventors:
SHAWN CABRAL, KENTARO FUTATSUGI, DAVID HEPWORTH, KIM HUARD, DANIEL WEI-SHUNG KUNG, SUVI TUULA MARJUKKA ORR, KUN SONG
Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
Type:
Application
Filed:
June 24, 2016
Publication date:
October 20, 2016
Applicant:
Pfizer Inc.
Inventors:
Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang