Abstract: Processes are described for the preparation of estrogen receptor modulating compound, (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid I: and salts thereof, and intermediates useful for the preparation of I.
Type:
Grant
Filed:
October 6, 2016
Date of Patent:
May 22, 2018
Assignee:
Genentech, inc.
Inventors:
Stephan Bachmann, Serena Maria Fantasia, Francis Gosselin, Chong Han, Stefan Hildbrand, Theresa Humphries, Christian Jenny, Ngiap-Kie Lim, Andrew McClory, Christian Moessner, Pankaj Rege, Scott Savage, Haiming Zhang
Abstract: The present invention provides for compounds of Formula I-I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula I-I all have the meaning as defined herein.
Type:
Application
Filed:
January 11, 2018
Publication date:
May 17, 2018
Applicant:
Genentech, Inc.
Inventors:
Anthony Estrada, Liting Dong, Kevin X. Chen, Paul Gibbons, Malcolm Huestis, Terry Kellar, Wen Liu, Changyou Ma, Joseph Lyssikatos, Alan Olivero, Snahel Patel, Daniel Shore, Michael Siu
Abstract: The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid
Type:
Application
Filed:
January 10, 2018
Publication date:
May 17, 2018
Applicant:
Genentech, Inc.
Inventors:
Jinguang Lin, Alexandra Chestakova, Wei Gu, Hans Iding, Jing Li, Xin Linghu, Patrik Meier, Chunbo Sha, Jeffrey Stults, Youchu Wang, Haiming Zhang, Jianqian Zhang, Tao Zhang
Abstract: The present invention is directed to the combination therapy of an afucosylated anti-CD20 antibody with a CD79b antibody-drug conjugate for the treatment of cancer, especially to the combination therapy of CD20 expressing cancers with an afucosylated humanized B-Ly1 antibody and a CD79b antibody-drug conjugate.
Type:
Application
Filed:
November 9, 2017
Publication date:
May 17, 2018
Applicants:
Hoffmann-La Roche Inc., Genentech, Inc.
Inventors:
Christian Klein, Sabine Lang, Pablo Umana, Andrew Polson
Abstract: The present application discloses variants of Pertuzumab. In particular, it discloses: an unpaired cysteine variant comprising Cys23/Cys88 unpaired cysteines in one or both variable light domains of Pertuzumab, an afucosylated variant of Pertuzumab, a low-molecular-weight-species (LMWS) of Pertuzumab, and a high-molecular-weight-species (HMWS) or Pertuzumab. The application further discloses the isolated variants, compositions, pharmaceutical compositions, and articles of manufacture comprising the variants, as well as methods of making and characterizing the variants and compositions thereof.
Type:
Grant
Filed:
October 19, 2017
Date of Patent:
May 15, 2018
Assignee:
Genentech, Inc.
Inventors:
Lynn A. Gennaro, Yung-Hsiang Kao, Yonghua Zhang
Abstract: Processes are described for the preparation of tricyclic lactam compound of Formula (I), having the structure and intermediates useful for the preparation of (I).
Type:
Grant
Filed:
July 18, 2017
Date of Patent:
May 15, 2018
Assignee:
GENENTECH, INC.
Inventors:
Ngiap-Kie Lim, Haiming Zhang, Chong Han
Abstract: Described herein are tetrahydroisoquinoline compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituent 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:
April 7, 2017
Date of Patent:
May 15, 2018
Assignee:
Genentech, Inc.
Inventors:
Sharada Labadie, Jun Liang, Daniel Fred Ortwine, Maia Vinogradova, Xiaojing Wang, Jason Zbieg, Birong Zhang, Tao Wang
Abstract: A process for producing an optically active 2-alkyl-1,1,3-trialkoxycarbonylpropane (2), comprising a step of asymmetric hydrolysis of 2-alkyl-1,1,3-trialokoxycarbonylpropane (1) by using an enzyme capable of selectively hydrolyzing an ester moiety of either one enantiomer of 2-alkyl-1,1,3-trialkoxycarbonylpropane (1), or by using a culture of a microorganism capable of producing the enzyme or a treated object thereof.
Abstract: The present invention relates to a highly concentrated, stable pharmaceutical formulation of a pharmaceutically active anti-HER2 antibody, such as e.g. Trastuzumab (HERCEPTIN™), Pertuzumab or T-DM1, or a mixture of such antibody molecules for subcutaneous injection. In particular, the present invention relates to formulations comprising, in addition to a suitable amount of the anti-HER2 antibody, an effective amount of at least one hyaluronidase enzyme as a combined formulation or for use in form of a co-formulation. The formulations comprise additionally at least one buffering agent, such as e.g. a histidine buffer, a stabilizer or a mixture of two or more stabilizers (e.g. a saccharide, such as e.g. ?,?-trehalose dihydrate or sucrose, and optionally methionine as a second stabilizer), a nonionic surfactant and an effective amount of at least one hyaluronidase enzyme. Methods for preparing such formulations and their uses thereof are also provided.
Type:
Grant
Filed:
February 25, 2016
Date of Patent:
May 15, 2018
Assignee:
Genentech, Inc.
Inventors:
Michael Adler, Ulla Grauschopf, Hanns-Christian Mahler, Oliver Boris Stauch
Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
Type:
Application
Filed:
June 16, 2017
Publication date:
May 10, 2018
Applicants:
Array BioPharma Inc., Genentech, Inc.
Inventors:
James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
Abstract: The invention relates to pyridopyrimidinone compounds of formula I or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5 and R6 are as defined herein, as well as pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
Type:
Application
Filed:
October 13, 2017
Publication date:
May 10, 2018
Applicant:
Genentech, Inc.
Inventors:
Matthew Volgraf, Yu Jiang, Elisia Villemure, Benjamin Sellers, Guosheng Wu, Aijun Lu
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. Also described are methods of making the benzoxazepin oxazolidinone compounds having the Formula I structure.
Type:
Application
Filed:
October 10, 2017
Publication date:
May 10, 2018
Applicant:
Genentech, Inc.
Inventors:
Marie-Gabrielle Braun, Emily Hanan, Steven T. Staben, Robert Andrew Heald, Calum MacLeod, Richard Elliott
Abstract: The invention provides rF1 antibody antibiotic conjugates and methods of using same.
Type:
Application
Filed:
June 2, 2017
Publication date:
May 10, 2018
Applicant:
Genentech, Inc.
Inventors:
Eric Brown, Wouter Hazenbos, Isidro Hotzel, Kimberly Kajihara, Sophie M. Lehar, Sanjeev Mariathasan, Thomas Pillow, Leanna Staben, Vishal Verma, Binqing Wei, Yi Xia, Min Xu
Abstract: Oxepan-2-yl pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
September 15, 2016
Date of Patent:
May 8, 2018
Assignee:
Genentech, Inc.
Inventors:
Jason Burch, Huifen Chen, Xiaojing Wang
Abstract: The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II 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:
Application
Filed:
December 21, 2017
Publication date:
May 3, 2018
Applicant:
Genentech, Inc.
Inventors:
Huifen Chen, Yanyan Chu, Steven Do, Anthony Estrada, Baihua Hu, Aleksandr Kolesnikov, Xingyu Lin, Joseph P. Lyssikatos, Daniel Shore, Vishal Verma, Lan Wang, Guosheng Wu, Po-wai Yuen
Abstract: The present disclosure relates generally to rapid-release pharmaceutical dosage unit tablets containing a drug that is an inhibitor of the mitogen-activated protein kinase enzyme, a filler and a disintegrant, and to processes for forming the tablets. More specifically, the present disclosure relates to pharmaceutical dosage unit tablets containing cobimetinib, a least one filler, at least one lubricant and at least one disintegrant, and to methods for preparing the tablets from granules formed by dry granulation.
Type:
Application
Filed:
December 22, 2017
Publication date:
May 3, 2018
Applicant:
Genentech, Inc.
Inventors:
Sanjeev Kothari, Priscilla Mantik, Alexander Mauerer, Hamid Rezaei