公开(公告)号：US10676465B2

公开(公告)日：2020-06-09

申请号：US16535616

申请日：2019-08-08

申请人： Pfizer Inc.

发明人： Gary Erik Aspnes ,  Scott W. Bagley ,  John M. Curto ,  David James Edmonds ,  Mark E. Flanagan ,  Kentaro Futatsugi ,  David A. Griffith ,  Kim Huard ,  Yajing Lian ,  Chris Limberakis ,  Allyn T. Londregan ,  Alan M. Mathiowetz ,  David W. Piotrowski ,  Roger B. Ruggeri

IPC分类号： C07D405/12 ,  C07D405/14 ,  C07D471/04 ,  C07C53/06 ,  C07C53/10 ,  C07C215/40 ,  C07D413/14

摘要： Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.

公开(公告)号：US10669279B2

公开(公告)日：2020-06-02

申请号：US16455020

申请日：2019-06-27

申请人： Pfizer Inc.

发明人： Thomas Allen Chappie ,  Nandini Chaturbhai Patel ,  Matthew Merrill Hayward ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Joseph Michael Young ,  Patrick Robert Verhoest

IPC分类号： C07D487/04 ,  C07D519/00

摘要： 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.

公开(公告)号：US10669259B2

公开(公告)日：2020-06-02

申请号：US16220184

申请日：2018-12-14

申请人： Pfizer Inc.

发明人： Gary Erik Aspnes ,  Scott W. Bagley ,  John M. Curto ,  Matthew S. Dowling ,  David Edmonds ,  Mark E. Flanagan ,  Kentaro Futatsugi ,  David A. Griffith ,  Kim Huard ,  Gajendra Ingle ,  Wenhua Jiao ,  Chris Limberakis ,  Alan M. Mathiowetz ,  David W. Piotrowski ,  Roger B. Ruggeri

IPC分类号： A61K31/496 ,  A61K31/4545 ,  C07D401/14 ,  C07D487/04 ,  A61P3/00 ,  A61P15/10 ,  A61P17/06 ,  A61P9/10 ,  A61P19/06 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  A61P1/16 ,  A61P25/02 ,  A61P3/04 ,  A61P19/02 ,  A61P3/10 ,  A61P13/12 ,  A61P25/18 ,  A61P1/00 ,  A61P15/00 ,  A61P25/16 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

摘要： Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, 7-aza- and 4,7-diaza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.

公开(公告)号：US20200165582A1

公开(公告)日：2020-05-28

申请号：US16704744

申请日：2019-12-05

申请人： Pfizer Inc.

发明人： 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

IPC分类号： C12N9/10 ,  C12N1/20 ,  C07K14/33

摘要： 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.

公开(公告)号：US20200164056A1

公开(公告)日：2020-05-28

申请号：US16704701

申请日：2019-12-05

申请人： PFIZER INC.

发明人： 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

IPC分类号： A61K39/095 ,  A61P31/00 ,  A61K47/64 ,  A61K31/7028 ,  A61K47/26 ,  A61K47/10 ,  A61K47/18 ,  C07K16/12 ,  C07K14/22 ,  A61K39/12

摘要： 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.

公开(公告)号：US10662204B2

公开(公告)日：2020-05-26

申请号：US16263185

申请日：2019-01-31

申请人： PFIZER INC.

发明人： Simon Planken ,  Hengmiao Cheng ,  Michael Raymond Collins ,  Jillian Elyse Spangler ,  Alexei Brooun ,  Andreas Maderna ,  Cynthia Palmer ,  Maria Angelica Linton ,  Asako Nagata ,  Ping Chen

IPC分类号： C07D403/12 ,  C07D403/14 ,  C07D407/14 ,  C07D487/10 ,  A61P35/00 ,  C07D519/00 ,  C07D471/04 ,  C07D487/04 ,  C07D417/14 ,  C07D413/14 ,  A61P25/00

摘要： Compounds of the general formula: processes for the preparation of these compounds, compositions containing these compounds, and administration of these compounds to patients to treat pancreatic, lung, colon and other cancers.

公开(公告)号：US10660959B2

公开(公告)日：2020-05-26

申请号：US16189009

申请日：2018-11-13

申请人： Pfizer Inc.

发明人： Kevin Richard Back ,  Michael Cram ,  Aidan James Harper ,  W. James Huang ,  Jonathan Richard Lillis ,  Timothy Michael Lukas ,  Sumit Luthra

IPC分类号： A61K47/12 ,  C07D401/12 ,  A61K9/00 ,  A61K47/26 ,  A61K9/08 ,  A61K9/19 ,  A61K31/5377 ,  A61K47/02

摘要： The present invention relates to a pharmaceutical aqueous formulation comprising 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 a pharmaceutically acceptable salt thereof, that is a clear solution. Such a formulation is particularly suitable for intravenous or parenteral administration to a patient.

公开(公告)号：US10653794B2

公开(公告)日：2020-05-19

申请号：US15748268

申请日：2016-08-09

申请人： PFIZER INC.

发明人： Xiaotian Zhong ,  Amarnauth Shastrie Prashad ,  Ronald William Kriz ,  Tao He ,  Will Somers ,  Wenge Wang ,  Leo Joseph Letendre

IPC分类号： A61K47/68 ,  C07K16/00 ,  C07K16/30 ,  A61K38/05

摘要： 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.

公开(公告)号：US10590115B2

公开(公告)日：2020-03-17

申请号：US16265012

申请日：2019-02-01

申请人： PFIZER INC.

发明人： Simon Planken ,  Hengmiao Cheng ,  Michael Raymond Collins ,  Jillian Elyse Spangler ,  Alexei Brooun ,  Andreas Maderna ,  Cynthia Palmer ,  Maria Angelica Linton ,  Asako Nagata ,  Ping Chen

IPC分类号： C07D403/14 ,  C07D487/10 ,  A61P35/00 ,  C07D403/04 ,  C07D239/94

摘要： Compounds of the general formula: processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.

公开(公告)号：US10583092B2

公开(公告)日：2020-03-10

申请号：US16124605

申请日：2018-09-07

申请人： Pfizer Inc.

发明人： Maria Figueiredo ,  Erick Peeke ,  David Dewitt ,  Christina Van Geen Hoven ,  Greg Troiano ,  James Wright ,  Yong-ho Song ,  Hong Wang

IPC分类号： A61K9/51 ,  A61K9/00 ,  A61K31/404 ,  A61K31/506 ,  B82Y5/00 ,  B82Y40/00

摘要： The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic acid, a basic therapeutic agent having a protonatable nitrogen, and a polymer. Other aspects include methods of making and using such nanoparticles.