Abstract: The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.
Type:
Grant
Filed:
October 14, 2016
Date of Patent:
August 4, 2020
Assignee:
Genentech, Inc.
Inventors:
Peter Dragovich, Zhonghua Pei, Thomas Pillow, Jack Sadowsky, Jinhua Chen, John Wai
Abstract: Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
Type:
Grant
Filed:
March 26, 2018
Date of Patent:
August 4, 2020
Assignees:
FORMA TM, LLC, Genentech, Inc.
Inventors:
Kenneth W. Bair, Timm R. Baumeister, Peter Dragovich, Xiongcai Liu, Snahel Patel, Po-Wai Yuen, Mark Zak, Guiling Zhao, Yamin Zhang, Xiaozhang Zheng
Abstract: Apparatus and methods for lyophilizing and sealing a medicament within a medical delivery device having an opening. The apparatus may include a stopper for sealing the opening. The stopper may have one or more elongated members extending from a base, in a direction that is parallel to a central axis of the base. One or more of the members may be set radially away from the axis and define a coaxial central well. The member or members may define a void. The elongated member or members may engage a device inner wall and support the base away from the opening. The void may provide gas exchange between a device interior and a device exterior. The gas may be a lyophilization byproduct that escapes from the device interior between the inner wall, the base and the member or members. The stopper may be advanced into the device to seal the opening.
Abstract: Methods for the treatment of patients with HER2-positive, HER2-amplified and/or HER2-mutated advanced cancer by administration of pertuzumab plus trastuzumab are disclosed. In one aspect, the cancer is advanced HER2-positive, HER2-amplified and/or HER2-mutated colorectal, biliary, bladder, urothelial, salivary, lung, pancreatic, ovarian, prostate, or skin cancer. In another aspect, the cancer is HER2-positive, HER2-amplified and/or HER2-mutated colorectal, biliary, bladder, urothelial, salivary, lung, pancreatic, ovarian, prostate, or skin cancer that is refractory to one or more other treatment regimens.
Abstract: The invention provides interleukin-33 (IL-33) antibodies and methods of using the same.
Type:
Grant
Filed:
August 31, 2018
Date of Patent:
July 28, 2020
Assignee:
Genentech, Inc.
Inventors:
Philip E. Hass, Meredith Hazen, Yi-Chun Hsiao, Rajita Khosla, Gerald R. Nakamura, Dhaya Seshasayee, Menno Van Lookeren Campagne, Hongkang Xi, Wenwu Zhai, Jack Bevers, III, Nancy Chiang
Abstract: The present invention relates to hydrogel prodrug compositions comprising cross-linked hyaluronic acid (HA), or a derivative or a salt thereof, wherein the cross-linker system comprises a biodegradable spacer, wherein the cross-linked HA comprises a conjugated drug-linker, and wherein the linker is capable of releasing the drug under physiological conditions. The present invention further relates to methods for preparing the hydrogel prodrug compositions. The present invention further relates to methods for treating an ocular condition using the hydrogel compositions.
Type:
Application
Filed:
September 19, 2019
Publication date:
July 16, 2020
Applicant:
Genentech, Inc.
Inventors:
Sebastian STARK, Thomas KNAPPE, Harald RAU, Nicola BISEK, Burkhardt LAUFER, Samuel WEISBROD, Tobias VOIGT, Germaine FUH, Patrick KOENIG, Chingwei Vivian LEE, Daniela BUMBACA YADAV
Abstract: The invention relates generally to a silvestrol molecule activated with a leaving group. The invention further relates generally to an antibody-drug conjugate comprising an antibody conjugated by a linker to one or more silvestrol drug moieties and methods of treatment.
Type:
Application
Filed:
March 23, 2020
Publication date:
July 16, 2020
Applicant:
Genentech, Inc.
Inventors:
Thomas Pillow, Andrew G. Polson, Bing Zheng
Abstract: The present invention provides methods for analyzing compositions of polypeptides such as antibodies by ionic strength-mediated pH gradient ion exchange chromatography. In some aspects, the methods use a combination of pH gradients and ionic strength gradients to separate the polypeptide from charge variants of the polypeptide. In some aspects, the methods use a stable ionic strength to optimize the pH gradient separation window to separate the polypeptide from charge variants. Such methods are useful for analyzing polypeptide, e.g. antibodies, with a pI greater than 9 or a pI less than 7. In some aspects, the invention provides a multiproduct method for the analysis of polypeptides of varying pI's.
Type:
Grant
Filed:
September 29, 2017
Date of Patent:
July 14, 2020
Assignee:
Genentech, Inc.
Inventors:
Yajun Wang, George Tony Moreno, Boyan Zhang, Liangyi Zhang, Dell Farnan, Thomas Patapoff
Abstract: The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
Type:
Grant
Filed:
March 15, 2019
Date of Patent:
July 14, 2020
Assignee:
Genentech, Inc.
Inventors:
Jack Alexander Terrett, Huifen Chen, Lea Constantineau-Forget, Robin Larouche-Gauthier, Luce Lépissier, Francis Beaumier, Martin Déry, Chantal Grand-Maître, Claudio Sturino, Matthew Volgraf, Elisia Villemure
Abstract: The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
Type:
Grant
Filed:
September 3, 2019
Date of Patent:
July 14, 2020
Assignee:
Genentech, Inc.
Inventors:
Huifen Chen, Brian Safina, Daniel Shore, Jack Terrett, Elisia Villemure, Matthew Volgraf, Stuart Ward, Aijun Lu, Robin Larouche-Gauthier, Francis Beaumier, Martin Dery, Lea Constantineau-Forget, Chantal Grand-Maitre, Luce Lepissier
Abstract: The invention provides for methods of viral inactivation using high temperature short time (HTST) treatment and adjustment of various parameters such that generation of precipitate and depositions of precipitate are reduced and/or minimized.
Type:
Application
Filed:
July 18, 2019
Publication date:
July 9, 2020
Applicant:
Genentech, Inc.
Inventors:
Masaru Ken SHIRATORI, Robert David KISS, Hardayal PRASHAD, Raquel IVERSON, Justin BOURRET, Michael KIM, Salim CHARANIYA
Abstract: The invention provides methods for making such formulations and methods of using such formulations. The invention further provides methods of reducing polysorbate degradation, methods of reducing the amount of visible and sub-visible particles in an aqueous formulation, and methods of disaggregating polysorbate degradation products comprising adding a cyclodextrin to a formula comprising polysorbate and a polypeptide. The invention also provides aqueous formulations comprising a polypeptide, a polysorbate, and a cyclodextrin with reduced polysorbate degradation.
Type:
Application
Filed:
November 21, 2019
Publication date:
July 9, 2020
Applicant:
Genentech, Inc.
Inventors:
Brian CONNOLLY, Lydia HAMBURG, Emily HOLZ
Abstract: The present invention provides methods and compositions for reducing lactate production and increasing polypeptide production in cultured cells. In one aspect, the invention provides a method comprising culturing cells expressing a) a small interfering RNA (siRNA) specific for a lactate dehydrogenase (LDH) and b) an siRNA specific for a pyruvate dehydrogenase kinase (PDHK). In another aspect, the invention provides cultured cells or vectors comprising an siRNA specific for a LDH and an siRNA specific for a PDHK.
Type:
Grant
Filed:
May 31, 2018
Date of Patent:
July 7, 2020
Assignee:
Genentech, Inc.
Inventors:
Meixia Zhou, Bradley Richard Snedecor, Chi Kin Domingos Ng, Amy Shen
Abstract: The present application describes uses for Pertuzumab, a first-in-class HER2 dimerization inhibitor. In particular, the application describes methods for extending progression free survival in a HER2-positive breast cancer patient population; and combining two HER2 antibodies to treat HER2-positive cancer without increasing cardiac toxicity.
Type:
Application
Filed:
February 20, 2020
Publication date:
July 2, 2020
Applicant:
Genentech, Inc.
Inventors:
Mark C. Benyunes, Emma L. Clark, Jayantha Ratnayake, Graham A. Ross
Abstract: The present invention relates to compounds of formula (I) and formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R5-R6 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II), or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
Type:
Grant
Filed:
November 21, 2018
Date of Patent:
June 30, 2020
Assignees:
GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
Inventors:
Patrick Cyr, Sarah Bronner, F. Anthony Romero, Steven Magnuson, Vickie Hsiao-Wei Tsui, John Wai, Kwong Wah Lai, Fei Wang
Abstract: The invention provides compounds of formula I: and pharmaceutically acceptable salts thereof where R1 is a substituted or unsubstituted phenyl or a fused bicyclic comprising a substituted or unsubstituted phenyl. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
Type:
Grant
Filed:
February 7, 2019
Date of Patent:
June 30, 2020
Assignee:
Genentech, Inc.
Inventors:
Vishal Verma, Matthew Volgraf, Baihua Hu
Abstract: Provided are non-naturally occurring cystine knot peptides (CKPs) that bind to VEGF-A. Additionally, provided are methods of using non-naturally occurring CKPs that bind to VEGF-A, including diagnostic and therapeutic compositions and methods. Non-naturally CKPs that bind low density lipoprotein receptor-related protein 6 (LRP6) are also provided.