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:
Application
Filed:
February 25, 2021
Publication date:
February 9, 2023
Applicant:
Genentech, Inc.
Inventors:
Sharada Labadie, Jun Liang, Daniel Fred Ortwine, Xiaojing Wang, Jason Zbieg, Birong Zhang, Simon Charles Goodacre, Nicholas Charles Ray, Jun Li, Tommy Lai, Jiangpeng Liao, Zhiguo Liu, John Wai, Tao Wang
Abstract: The invention provides liquid pharmaceutical formulations comprising an anti-PD-L1 antibody, such as liquid pharmaceutical formulations for subcutaneous administration. The invention also provides methods for making such formulations and methods of using such formulations.
Abstract: Apparatus and methods for delivering medicament to a patient. The apparatus may include elements with different capacities to attenuate or absorb sterilizing radiation. The apparatus may include a medicament delivery assembly with interactive elements for dose-setting, priming and medicament ejection. The assembly may include a chamber housing a radiation-sensitive medicament present in the apparatus during sterilization by electron beam. The assembly may include an actuator chassis, a drive mechanism, a needle-priming mechanism and a fluid-displacement mechanism including a fluid-displacement member. The chassis may be fixed, relative to an outlet, to the chamber. The member may be slidingly and/or threadingly engaged with the chassis, and may be configured to move relative to the outlet to deliver the medicament through the outlet. Assembly elements may be nested coaxially and/or stacked axially. The assembly may include at least one hollow region.
Type:
Grant
Filed:
April 15, 2019
Date of Patent:
February 7, 2023
Assignee:
Genentech, Inc.
Inventors:
Joshua Horvath, Lionel Vedrine, Nathan A. Goltz, Mukund R. Patel, Aaron D. Chesterman, Mayumi Naito Bowen
Abstract: The presently disclosed subject matter relates to compositions, systems and methods of screening one or more species of polypeptide in a complex mixture of polypeptides, e.g., multi-subunit proteins. For example, the subject matter relates to ligands used in connection with affinity capillary electrophoresis, as well as methods and systems for detecting polypeptides in a mixture of multimers that include multispecific antibodies, e.g., bispecific antibodies.
Type:
Grant
Filed:
September 11, 2019
Date of Patent:
February 7, 2023
Assignee:
Genentech, Inc.
Inventors:
Kelsey Catherine Dent, David John Fischer, David A. Michels
Abstract: Drug delivery systems and methods of use thereof for recording administration of a drug dose to a subject are provided. Aspects of the invention include a syringe stopper rod comprising a sensor component that is configured to detect a delivery signature, and to transmit a report comprising a drug dose completion signal to a data management component, e.g., a mobile computing device.
Abstract: Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquinoline compounds.
Type:
Grant
Filed:
July 6, 2020
Date of Patent:
January 31, 2023
Assignee:
Genentech, Inc.
Inventors:
Bryan Chan, Joy Drobnick, Lewis Gazzard, Timothy Heffron, Jun Liang, Sushant Malhotra, Rohan Mendonca, Naomi Rajapaksa, Craig Stivala, John Tellis, Weiru Wang, BinQing Wei, Aihe Zhou, Matthew W. Cartwright, Michael Lainchbury, Emanuela Gancia, Eileen Seward, Andrew Madin, David Favor, Kin Chiu Fong, Yonghan Hu, Andrew Good
Abstract: Provided herein are methods for treating acute myeloid leukemia (AML) in a patient with cytopenia when on a combination therapy of venetoclax and azacitidine. Also provided herein are methods of managing a cytopenia in such patient.
Type:
Application
Filed:
September 15, 2022
Publication date:
January 26, 2023
Applicants:
GENENTECH, INC., ABBVIE INC.
Inventors:
Ahmed Hamed SALEM, Jalaja POTLURI, Jiuhong ZHA, Mehrdad MOBASHER, Wan-Jen HONG
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 2 and a highly chemoselective PtN/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:
June 28, 2022
Publication date:
January 26, 2023
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: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of lipoprotein signal peptidase II (LspA), a key protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
Type:
Application
Filed:
September 10, 2021
Publication date:
January 26, 2023
Applicant:
Genentech, Inc.
Inventors:
Guosheng WU, Emily J. HANAN, Marie-Gabrielle BRAUN, Sharada S. LABADIE, Keira GARLAND, Richard M. PASTOR, Paul Anthony GIBBONS, Yuhong FU, Yun-Xing CHENG
Abstract: The present disclosure relates to novel sulfonylurea compounds and related compounds useful 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:
January 24, 2023
Assignee:
Genentech, Inc.
Inventors:
Jeffrey A. Stafford, James M. Veal, Lynnie Lin Trzoss, Christopher McBride, Richard M. Pastor, Steven Thomas Staben, Craig Stivala, Matthew Volgraf
Abstract: wherein R1, R2, R3, R4, R5 and R6 are as defined herein, and salts thereof that are useful as JAK kinse 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:
Application
Filed:
August 24, 2022
Publication date:
January 19, 2023
Applicant:
Genentech, Inc.
Inventors:
Mark Edward Zak, Naomi S. Rajapaksa, Yun-Xing Cheng, Jessica Marie Grandner, Daniel G.M. Shore, Marian C. Bryan
Abstract: The invention provides anti-MIC antibodies and methods of using the same.
Type:
Grant
Filed:
October 27, 2017
Date of Patent:
January 17, 2023
Assignee:
Genentech, Inc.
Inventors:
Twyla Noelle Lombana, Christoph Spiess, Jeong Kim, Evangeline Toy, Jill Schartner, Zhengmao Ye, Jack Bevers, III, Ryan Cook, Marissa Matsumoto, Amy Berkley
Abstract: Techniques are disclosed for using a genetic algorithm to identify a processing pipeline that transforms spectra into a form usable to generate predicted characteristics of corresponding samples. The genetic algorithm is used to generate and evaluate multiple candidate solutions specifying various pre-processing and machine-learning-processing configurations. The processing pipeline is defined based on the candidate solutions.
Type:
Application
Filed:
September 19, 2022
Publication date:
January 12, 2023
Applicant:
GENENTECH, INC.
Inventors:
Dana Lauren McDaniel, Elvira Kadaub, Bingchuan Wei, Andrew James Maier, Gordon Edward Magill
Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
Type:
Grant
Filed:
September 11, 2020
Date of Patent:
January 10, 2023
Assignees:
Valo Health, Inc., Genentech, Inc.
Inventors:
Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Bingsong Han, Jian Lin, Dominic J. Reynolds, Bruce Roth, Chase C. Smith, Zhongguo Wang, Po-Wai Yuen, Xiaozhang Zheng
Abstract: The subject matter described herein is directed to methods of preparing certain antibody-drug conjugates (ADCs) wherein the antibody is linked to the drug through a linker, wherein the drug contains a heteroaryl group having a secondary nitrogen, and the linker is attached to the drug via the secondary nitrogen. The resulting conjugates are useful in treating various diseases and conditions.
Abstract: Methods and systems disclosed herein relate generally to processing images to estimate whether at least part of a tumor is represented in the images. A computer-implemented method includes accessing an image of at least part of a biological structure of a particular subject, processing the image using a segmentation algorithm to extract a plurality of image objects depicted in the image, determining one or more structural characteristics associated with an image object of the plurality of image objects, processing the one or more structural characteristics using a trained machine-learning model to generate estimation data corresponding to an estimation of whether the image object corresponds to a lesion or tumor associated with the biological structure, and outputting the estimation data for the particular subject.
Type:
Application
Filed:
August 30, 2022
Publication date:
January 5, 2023
Applicant:
Genentech, Inc.
Inventors:
Gregory Zelinsky FERL, Richard Alan Duray CARANO, Kai Henrik BARCK, Jasmine PATIL
Abstract: Methods are provided for the adjuvant treatment of operable HER2-positive primary breast cancer in human patients by administration of pertuzumab in addition to chemotherapy and trastuzumab. The methods reduce the risk of recurrence of invasive breast cancer or death for a patient diagnosed with HER2-positive early breast cancer (eBC) compared to administration of trastuzumab and chemotherapy, without pertuzumab.
Type:
Application
Filed:
August 22, 2022
Publication date:
January 5, 2023
Applicants:
Genentech, Inc., Hoffmann-La Roche Inc.
Inventors:
Mark C. BENYUNES, Graham Alexander ROSS