Patents Assigned to Genentech
  • Process for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds
    Patent number: 10870626
    Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.
    Type: Grant
    Filed: September 18, 2019
    Date of Patent: December 22, 2020
    Assignees: F. Hoffman-La Roche AG, Genentech, Inc.
    Inventors: Francis Gosselin, Chong Han, Hans Iding, Reinhard Reents, Scott Savage, Beat Wirz
  • INTEGRIN BETA7 ANTAGONISTS AND METHODS OF TREATING CROHN'S DISEASE
    Publication number: 20200392232
    Abstract: Methods of treating gastrointestinal inflammatory disorders such as inflammatory bowel diseases including Crohn's disease are provided. Also provided are methods of administering and dosing integrin beta7 antagonists, such as anti-integrin beta7 antibodies. In addition, methods of administrating and dosing such integrin beta7 antagonists to induce remission or to induce and maintain remission of Crohn's disease are provided.
    Type: Application
    Filed: February 19, 2020
    Publication date: December 17, 2020
    Applicant: GENENTECH, INC.
    Inventors: Azra Hassanali, Romeo Maciuca, Meina Tao Tang, Swati Tole, Xiaohui Wei
  • ANTIBODY FORMULATION
    Publication number: 20200392220
    Abstract: The invention provides a stable aqueous pharmaceutical formulation comprising a therapeutically effective amount of an antibody, optionally, not subjected to prior lyophilization, a buffer maintaining the pH in the range from about 4.0 to about 6.0, and an optional surfactant, methods for making such a formulation, and methods of using such a formulation.
    Type: Application
    Filed: February 21, 2020
    Publication date: December 17, 2020
    Applicant: Genentech, Inc.
    Inventors: Yatin R. GOKARN, Timothy J. KAMERZELL, Megan LI, Mary CROMWELL, Hong LIU
  • SYSTEMS AND METHODS FOR TWO-DIMENSIONAL CHROMATOGRAPHY
    Publication number: 20200393426
    Abstract: Provided are two-dimensional chromatography systems and methods for separating and/or analyzing complex mixtures of organic compounds. In particularly, a two-dimensional reversed-phase liquid chromatography (RPLC)—supercritical fluid chromatography (SFC) system is described including a trapping column at the interface which collects the analytes eluted from the first dimension chromatography while letting the RPLC mobile phase pass through. The peaks of interest from the RPLC dimension column are effectively focused as sharp concentration pulses on the trapping column, which is subsequently injected onto the second dimension SFC column. The system can be used for simultaneous achiral and chiral analysis of pharmaceutical compounds. The first dimension RPLC separation provides the achiral purity result, and the second dimension SFC separation provides the chiral purity result (enantiomeric excess).
    Type: Application
    Filed: August 27, 2020
    Publication date: December 17, 2020
    Applicant: Genentech, Inc.
    Inventors: Cadapakam VENKATRAMANI, Mohammad AL-SAYAH
  • Antigen binding complex having agonistic activity and methods of use
    Patent number: 10865248
    Abstract: Provided herein are antigen binding polypeptides and complexes thereof having agonist activity. Also provided are methods for screening for complexes or polypeptides having agonist activity, enhancing the agonist activity of a polypeptide, and for agonizing a cell surface receptor using the complexes and polypeptide described herein.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: December 15, 2020
    Assignee: Genentech, Inc.
    Inventors: Greg Lazar, Jeong Kim, Jing Zhu, Yanli Yang, Randall Brezski
  • Anti-CD3 antibodies and methods of use
    Patent number: 10865251
    Abstract: The invention provides anti-cluster of differentiation 3 (CD3) antibodies and methods of using the same.
    Type: Grant
    Filed: September 27, 2018
    Date of Patent: December 15, 2020
    Assignee: Genentech, Inc.
    Inventors: Xiaocheng Chen, Mark S. Dennis, Allen J. Ebens, Jr., Robert F. Kelley, Mary A. Mathieu, Liping L. Sun
  • IL-17A/F HETEROLOGOUS POLYPEPTIDES AND THERAPEUTIC USES THEREOF
    Publication number: 20200385452
    Abstract: The present invention is directed to a novel naturally occurring human cytokine that is comprised of a heterodimer of interleukin-17 and interleukin-17F designated herein as interleukin 17A/F (IL-17A/F). Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, specific antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention. Further provided herein are methods for treating degenerative cartilaginous disorders and other inflammatory diseases.
    Type: Application
    Filed: December 2, 2019
    Publication date: December 10, 2020
    Applicant: Genentech, Inc.
    Inventors: David P. ARNOTT, Austin L. GURNEY, Philip E. HASS, James M. LEE, Yan WU
  • Anti-Jagged1 antibodies and methods of use
    Patent number: 10858440
    Abstract: The invention provides anti-Jagged1 antibodies and methods of using the same.
    Type: Grant
    Filed: June 4, 2018
    Date of Patent: December 8, 2020
    Assignee: Genentech, Inc.
    Inventors: Yvonne Chinn, Julie Q. Hang, Christian W. Siebel, Yan Wu, Daniel Lafkas
  • Processes for the preparation of pyrimidinylcyclopentane compounds
    Patent number: 10858324
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.
    Type: Grant
    Filed: August 29, 2019
    Date of Patent: December 8, 2020
    Assignee: GENENTECH, INC.
    Inventors: Hans Iding, Reinhard Reents, Michelangelo Scalone, Francis Gosselin
  • Antibody selection apparatus and methods
    Patent number: 10861584
    Abstract: Apparatus, systems, computer-readable media, articles of manufacture and methods for selecting an antibody. Apparatus, systems, computer-readable media, articles of manufacture and methods for producing the selected antibody. The selecting may include determining one or more physiochemical characteristics of the antibody. The determining may be based on antibody structural parameters.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: December 8, 2020
    Assignee: GENENTECH, INC.
    Inventors: Vikas K. Sharma, Trevor E. Swartz, Thomas W. Patapoff
  • DECREASING LACTATE LEVEL AND INCREASING POLYPEPTIDE PRODUCTION BY DOWNREGULATING THE EXPRESSION OF LACTATE DEHYDROGENASE AND PYRUVATE DEHYDROGENASE KINASE
    Publication number: 20200377919
    Abstract: The present invention provides ethods 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: Application
    Filed: May 29, 2020
    Publication date: December 3, 2020
    Applicant: Genentech, Inc.
    Inventors: Meixia ZHOU, Bradley Richard SNEDECOR, Chi Kin Domingos NG, Amy SHEN
  • IL-17A/F HETEROLOGOUS POLYPEPTIDES AND THERAPEUTIC USES THEREOF
    Publication number: 20200377585
    Abstract: The present invention is directed to a novel naturally occurring human cytokine that is comprised of a heterodimer of interleukin-17 and interleukin-17F designated herein as interleukin 17A/F (IL-17A/F). Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, specific antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention. Further provided herein are methods for treating degenerative cartilaginous disorders and other inflammatory diseases.
    Type: Application
    Filed: February 6, 2020
    Publication date: December 3, 2020
    Applicant: Genentech, Inc.
    Inventors: David P. ARNOTT, Mercedesz BALAZS, Nico GHILARDI, Austin L. GURNEY, Philip E. HASS, Sarah HYMOWITZ, James M. LEE, Wenjun OUYANG, Melissa A. STAROVASNIK, Yan WU
  • USES FOR AND ARTICLE OF MANUFACTURE INCLUDING HER2 DIMERIZATION INHIBITOR PERTUZUMAB
    Publication number: 20200376120
    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: August 17, 2020
    Publication date: December 3, 2020
    Applicant: Genentech, Inc.
    Inventors: Mark C. Benyunes, Emma L. Clark, Graham A. Ross
  • CELL-BASED ASSAY FOR DETECTING ANTl-CD3 HOMODIMERS
    Publication number: 20200378987
    Abstract: The present invention provides a cell-based assay for identifying and/or quantifying anti-CD3 homodimers in a composition comprising a T cell-dependent Bispecific antibody (TDB). In some aspects, the invention T cells comprising a T cell activation responsive reporter are contacted with the TDB to detect the presence of anti-CD3 homodimers. Compositions of reporter T cells and kits are also contemplated.
    Type: Application
    Filed: May 14, 2020
    Publication date: December 3, 2020
    Applicant: Genentech, Inc.
    Inventor: Kendall CAREY
  • Anti-Jagged Antibodies and Methods of Use
    Publication number: 20200377610
    Abstract: The invention provides anti-Jagged antibodies and methods of using the same.
    Type: Application
    Filed: May 12, 2020
    Publication date: December 3, 2020
    Applicant: Genentech, Inc.
    Inventors: Christian W. Siebel, Yan Wu
  • HIGH DOSE TREATMENTS FOR ALZHEIMER'S DISEASE
    Publication number: 20200377582
    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.
    Type: Application
    Filed: December 20, 2019
    Publication date: December 3, 2020
    Applicant: GENENTECH, INC.
    Inventors: Jillian Smith, Janice Smith, Geoff Kerchner
  • Fc Variants and Methods for their Production
    Publication number: 20200377604
    Abstract: Described herein are Fc variants and methods for the efficient production of antibodies and other multimeric protein complexes (collectively referred to herein as heteromultimeric proteins). Heteromultimeric proteins may be capable of specifically binding to more than one target. The targets may be, for example, different epitopes on a single molecule or located on different molecules. The methods combine efficient, high gene expression level, appropriate assembly, and ease of purification for the heteromultimeric proteins. The invention also provides methods of using these heteromultimeric proteins, and compositions, kits and articles of manufacture comprising these antibodies.
    Type: Application
    Filed: May 12, 2020
    Publication date: December 3, 2020
    Applicant: Genentech, Inc.
    Inventors: J. Michael Elliott, Justin Scheer
  • Subcutaneous HER2 antibody formulations
    Patent number: 10849849
    Abstract: Fixed dose HER2 antibody formulations for subcutaneous administration are provided along with their use in the treatment of cancer. The formulations include fixed dose subcutaneous formulations of pertuzumab and subcutaneous co-formulations of pertuzumab and trastuzumab, and their use in the treatment of cancer.
    Type: Grant
    Filed: January 16, 2018
    Date of Patent: December 1, 2020
    Assignees: GENENTECH INC., HOFFMANN-LA ROCHE INC
    Inventors: Jennifer Eng-Wong, Whitney Kirschbrown, Tarik Khan, Jasper Lin, Sreedhara Alavattam, Amit Garg, Sarah Heeson, Tanja Badovinac-Crnjevic, Christine Wurth
  • Benzoxazepin oxazolidinone compounds and methods of use
    Patent number: 10851091
    Abstract: Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or 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 PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
    Type: Grant
    Filed: September 24, 2018
    Date of Patent: December 1, 2020
    Assignee: Genentech, Inc.
    Inventors: Marie-Gabrielle Braun, Emily Hanan, Steven T. Staben, Robert Andrew Heald, Calum Macleod, Richard Elliott
  • REGIO-SELECTIVE SYNTHESIS OF IMIDAZO[1,2-a]PYRIMIDINES
    Publication number: 20200369670
    Abstract: A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb) comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2 This annulation reaction between ?-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines.
    Type: Application
    Filed: May 7, 2020
    Publication date: November 26, 2020
    Applicant: Genentech, Inc.
    Inventors: Kyle Bradley Pascual Clagg, Nicholas Andrew White, Haiming Zhang, Francis Gosselin, William Nack, Paul D. O'Shea