Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined herein, and salts thereof, that are useful as JAK kinase inhibitors are described herein. Also provided are pharmaceutical compositions that include such a JAK inhibitor and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.
Type:
Grant
Filed:
December 8, 2022
Date of Patent:
March 11, 2025
Assignee:
Genentech, Inc.
Inventors:
Mark Edward Zak, Naomi S. Rajapaksa, Yun-Xing Cheng, Jessica Grandner, Daniel G. M. Shore, F. Anthony Romero, Marian C. Bryan
Abstract: The subject matter described herein is directed to molecules referred to herein as chemical inducers of degradation (CIDEs) and antibody-conjugated CIDEs (Ab-CIDEs), wherein the Ab-CIDEs comprise an antibody covalently bound to the CIDE through a linker, wherein the CIDE can be further covalently bound to a phosphate moiety, and to the uses of the molecules in treating diseases and conditions where targeted protein degradation is beneficial.
Type:
Application
Filed:
July 25, 2024
Publication date:
March 6, 2025
Applicant:
Genentech, Inc.
Inventors:
Daniel P. SUTHERLIN, Donglu ZHANG, Summer A. BAKER DOCKERY, Peter Scott DRAGOVICH
Abstract: Provided herein are methods of synthesizing quinazoline compounds comprising at least one atropisomeric center.
Type:
Application
Filed:
November 13, 2024
Publication date:
March 6, 2025
Applicants:
Genentech, Inc., Hoffmann-La Roche Inc.
Inventors:
NGIAP-KIE LIM, JEFF SHEN, LAUREN ELIZABETH SIROIS, JACOB C. TIMMERMAN, ETIENNE TRACHSEL, NICHOLAS ANDREW WHITE, JIE XU, HAIMING ZHANG, STEPHAN BACHMANN, RAPHAEL BIGLER, KYLE BRADLEY PASCUAL CLAGG, ANTONIO GIOVANNI DIPASQUALE, FRANCIS GOSSELIN, UGO JONATHAN ORCEL, ROLAND CHRISTOPH MEIER
Abstract: This disclosure relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.
Type:
Application
Filed:
September 3, 2024
Publication date:
March 6, 2025
Applicant:
Genentech, Inc.
Inventors:
Jason Robert ZBIEG, Russell Tyler SMITH, Paul Powell BEROZA, Vishal Anil VERMA, Bing-Yan ZHU, Ramsay BEVERIDGE, Lisa Marie BARTON, Bryan Ka Ip CHAN, Curtis COLWELL, Samir BOUAYAD-GERVAIS, Anwesha DEY, Marie Anne EVANGELISTA
Abstract: Provided herein are methods of treating B-cell proliferative disorders in particular Follicular Lymphoma and/or Diffuse Large B-Cell Lymphoma using immunoconjugates comprising anti-CD79b antibodies in combination with additional therapeutic agents.
Type:
Application
Filed:
May 10, 2024
Publication date:
March 6, 2025
Applicant:
Genentech, Inc.
Inventors:
Andrew POLSON, Shang-Fan YU, Yu-Waye CHU, Michael WENGER, Jamie Harue HIRATA, Dan LU
Abstract: The present disclosure relates to engineered T cells and methods of making and using the same, as well as reagents for making the engineered T cells.
Type:
Grant
Filed:
March 24, 2022
Date of Patent:
March 4, 2025
Assignee:
GENENTECH, INC.
Inventors:
Sascha Rutz, Benjamin Joseph Haley, Shravan Madireddi, Soyoung Oh, David Shaw, Kate Halliwell Senger
Abstract: An apparatus and method for direct drug infusion from a vial to a patient are provided. A movable hanger label is provided to adhere to and support the vial to facilitate direct infusion of a drug, such as one or more pharmaceuticals, biopharmaceuticals, and/or biologics, from the vial to the patient. Additionally, a process is provided in which the drug, contained in the vial with the movable hanger label, may be directly infused through a primed infusion line with a rapid infusion rate. A saline flush is incorporated at the end of the administration to flush the infusion line, resulting in a reduced amount of the drug remaining in the line.
Type:
Grant
Filed:
January 26, 2021
Date of Patent:
March 4, 2025
Assignees:
Genentech, Inc., Hoffmann-La Roche Inc.
Inventors:
Kai Zheng, Edward Porock, Mahesh Khurana, Geoffrey Colin Wise, Lorenzo Myles Paredes Pesino, Michelle Hatch, Stefan Yohe, Raffaella Claudia Bondi
Abstract: The present invention relates generally to glutamine-free cell culture media supplemented with arginine. The invention further concerns the production of recombinant proteins, such as antibodies, in arginine-supplemented glutamine-free mammalian cell culture.
Type:
Application
Filed:
November 8, 2024
Publication date:
February 27, 2025
Applicant:
Genentech, Inc.
Inventors:
Martin GAWLITZEK, Shun LUO, Christina Teresa BEVILACQUA
Abstract: Provided herein are methods of treating B-cell proliferative disorders (such as diffuse large B-cell lymphoma (DLBCL)) using immunoconjugates comprising anti-CD79b antibodies in combination with an anti-CD20 antibody (such as rituximab) and one or more chemotherapeutic agents (such as gemcitabine and oxaliplatin).
Type:
Application
Filed:
May 21, 2024
Publication date:
February 27, 2025
Applicants:
Genentech, Inc., Hoffmann-La Roche Inc.
Inventors:
Juana Elva HERNANDEZ MONTALVO, Naseer Ul Din QAYUM, Jamie Harue HIRATA
Abstract: The subject matter described herein relates generally to hydrolysable maleimide-containing molecules that are useful as linkers to covalently bind chemical inducers of degradation to antibodies and to the conjugates produced therefrom and their uses to treat conditions, and to the uses of the conjugates in treating diseases and conditions where targeted protein degradation is beneficial.
Type:
Application
Filed:
July 25, 2024
Publication date:
February 27, 2025
Applicant:
Genentech, Inc.
Inventors:
Daniel P. SUTHERLIN, Donglu ZHANG, Summer A. BAKER DOCKERY, Peter Scott DRAGOVICH
Abstract: Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
Type:
Grant
Filed:
February 25, 2021
Date of Patent:
February 25, 2025
Assignee:
Genentech, Inc.
Inventors:
Sharada Labadie, Jun Liang, Daniel Fred Ortwine, Xiaojing Wang, Jason Zbieg, Birong Zhang, Simon Charles Goodacre, Nicholas Charles Ray, Jun Li
Abstract: The present disclosure relates to novel sulfonimidamide compounds and related compounds and their use in treating a disorder responsive to modulation of cytokines such as IL-1? and IL-18, modulation of NLRP3 or inhibition of the activation of NLRP3 or related components of the inflammatory process.
Type:
Grant
Filed:
January 15, 2021
Date of Patent:
February 25, 2025
Assignee:
Genentech, Inc.
Inventors:
Christopher McBride, Lynnie Lin Trzoss, Amogh Boloor, Nadezda V. Sokolova, Richard M. Pastor, Steven Thomas Staben, Craig Stivala, Matthew Volgraf, Sarah M. Bronner
Abstract: Provided herein are methods to synthesize compounds useful in the treatment of cancer where such compounds comprise a quinazolinyl core moiety and at least one stereoisomeric or atropisomeric moiety.
Type:
Application
Filed:
July 18, 2024
Publication date:
February 20, 2025
Applicants:
Genentech, Inc., Hoffmann-La Roche Inc.
Inventors:
Rene LEBL, Ngiap Kie LIM, Roland Christoph MEIER, Ugo Jonathan ORCEL, Joerg SEDELMEIER, Jeff SHEN, Lauren Elizabeth SIROIS, Jacob C. TIMMERMAN, Etienne TRACHSEL, Nicholas Andrew WHITE, Jie XU, Haiming ZHANG, Stephan BACHMANN, Thomas Michael BASS, Raphael BIGLER, Johannes Adrian BURKHARD, Kyle Bradley Pascual CLAGG, Francis GOSSELIN, Chong HAN, Dainis KALDRE, Sean M. KELLY, Sebastian HEROLD, Christian LEITNER
Abstract: Provided are phenyltetrahydrofuran compounds that are useful as intermediates in the preparation of pharmaceutical compounds and further provided are processes for the preparation of phenyltetrahydrofuran compounds.
Type:
Application
Filed:
August 27, 2024
Publication date:
February 20, 2025
Applicants:
Genentech, Inc., Hoffmann-La Roche Inc.
Inventors:
Allen Yu HONG, Jacob C. TIMMERMAN, Francis GOSSELIN, Katarzyna Aleksandra PIECHOWICZ, Filip PETRONIJEVIC, Kurt PUENTENER, Anna-Lena GLASS, Etienne TRACHSEL
Abstract: A manufacturing process to a bis-mesylate salt 1b of the pan-RAF inhibitor 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl) thieno[3,2-d]pyrimidine-7-carboxamide. The process features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2and a highly chemoselective Pt/V/C-catalyzed nitro group reduction to access penultimate intermediate 7. The final amide coupling of 7 and 2 was accomplished by a mild and safe protocol employing N,N,N?,N?-tetramethylchloroformamidinium hexafluorophosphate (TCFH) as the coupling reagent, to produce a 1:1 adduct of the freebase and THF. The adduct afforded compound 1b with excellent yield, purity, and form stability on a multikilogram production scale after reaction with MsOH and recrystallization. The methods are able to produce a compound having upwards of 95% purity.
Type:
Application
Filed:
May 31, 2024
Publication date:
February 13, 2025
Applicants:
Genentech, Inc., Hoffmann-La Roche Inc.
Inventors:
Francis GOSSELIN, Stefan G. KOENIG, Eduardo V. MERCADO-MARIN, Andreas STUMPF, Daniel ZELL, Haiming ZHANG, Stephan BACHMANN, Diane E. CARRERA, Michael E. DALZIEL, Yonghui GE, Jie ZHANG, Raphael BIGLER, Laure Elizabeth Simone FINET, Regis Jean Georges MONDIERE, Yuki NAKAGAWA
Abstract: A method of preparing a prefilled syringe is disclosed that includes obtaining a syringe barrel and a needle adaptor cap assembled on the tip of the syringe barrel, wherein the needle adaptor cap has a rubber element tightly sealing the orifice of the tip of the syringe barrel and the syringe barrel together with the needle adaptor cap assembled on the tip of the syringe barrel is sterilized by a first sterilizing. Filling a drug substance into an interior of the syringe barrel and sealing the interior of the syringe barrel. Packaging the syringe barrel with a rubber stopper sealing the interior thereof and the needle adaptor cap assembled on the tip of the syringe barrel. Providing a second external surface sterilizing of the packaged syringe barrel with the rubber stopper sealing the interior thereof and the needle adaptor cap assembled on the tip of the syringe barrel.
Type:
Grant
Filed:
June 6, 2023
Date of Patent:
February 11, 2025
Assignees:
F. HOFFMANN-LA ROCHE AG, GENENTECH, INC.
Inventors:
Markus Hemminger, Ulla Grauschopf, Frank Bamberg, Mayumi Bowen, Robert Müller, Flora Felsovalyi, Denny Christensen
Abstract: The invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof; wherein, A, B, ring C, R3, R4, R5, R6, and R7 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Type:
Application
Filed:
October 10, 2024
Publication date:
February 6, 2025
Applicant:
Genentech, Inc.
Inventors:
Steven MCKERRALL, Brian Salvatore SAFINA, Aleksandr KOLESNIKOV, Birong ZHANG, Wenfeng LIU, Kwong Wah LAI
Abstract: Provided herein are tetracyclic oxazepinyl compounds useful in the treatment on cancers.
Type:
Application
Filed:
September 11, 2024
Publication date:
February 6, 2025
Applicant:
Genentech, Inc.
Inventors:
Lewis J. Gazzard, Samantha Alyson Green, Matthew Leo Landry, Sushant Malhotra, Michael Siu, Steven Do, Yun-Xing Cheng, Limin Cheng, Jianfeng Xin, Mingtao He
Abstract: Methods of treating Alzheimer's Disease (AD) in patients suffering from early AD, including amyloid positive patients, ApoE4 positive patients, and patients suffering from prodromal or mild AD are provided.