Abstract: Pyrazole carboxamide compounds of Formula I are provided, with various substituents, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Application
Filed:
February 28, 2019
Publication date:
June 27, 2019
Applicant:
Genentech, Inc.
Inventors:
Roland J. BILLEDEAU, James J. CRAWFORD, Saul JAIME-FIGUEROA, Wendy LEE, Francisco Javier LOPEZ-TAPIA, Sung-Sau SO
Abstract: Compounds having the formula I wherein R1, X1, X2, X3 and X4 as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
Abstract: Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Application
Filed:
June 27, 2018
Publication date:
June 27, 2019
Applicant:
Genentech, Inc.
Inventors:
James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
Abstract: The invention provides processes of preparation thereof useful in the preparation of compounds that can be used as CHK1 inhibitors.
Type:
Grant
Filed:
August 21, 2014
Date of Patent:
June 25, 2019
Assignees:
Genentech, Inc., Array BioPharma Inc.
Inventors:
Chong Han, Keena Green, Francis Gosselin, Michelangelo Scalone, Paul J. Nichols, Weidong Liu, Keith L. Spencer, Zackary D. Crane, Peter J. Stengel, Sagar Shakya
Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An embodiment of the invention is the provision of a compound of Formula IIIA.
Type:
Grant
Filed:
June 14, 2018
Date of Patent:
June 25, 2019
Assignees:
FORMA TM, LLC, Genentech, Inc.
Inventors:
Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng, Po-Wai Yuen
Abstract: The emergence of mutations in tyrosine kinases following treatment of cancer patients with molecular-targeted therapy represents a major mechanism of acquired drug resistance. Here, mutations in the serpentine receptor, Smoothened (SMO) are described, which result in resistance to a Hedgehog (Hh) pathway inhibitor, such as in medulloblastoma. Amino acid substitutions in conserved residues of SMO maintain Hh signaling, but result in the inability of the Hh pathway inhibitor, GDC-0449, to bind SMO and suppress the pathway. In some embodiments, the disclosure provides for novel mutant SMO proteins and nucleic acids and for screening methods to detect SMO mutations and methods to screen for drugs that specifically modulate mutant SMO exhibiting drug resistance.
Type:
Grant
Filed:
February 4, 2016
Date of Patent:
June 25, 2019
Assignees:
Genentech, Inc., Curis, Inc., Assistance Publique-Hopitaux de Paris, Universite Paris Diderot—Paris 7
Inventors:
Frederic J. De Sauvage, Robert L. Yauch, Gerrit J. P. Dijkgraaf, Hayley Sharpe, Nicole Basset-Seguin
Abstract: This invention concerns in general treatment of diseases and pathological conditions with anti-VEGF antibodies. More specifically, the invention concerns the treatment of human patients susceptible to or diagnosed with cancer using an anti-VEGF antibody, in combination with one or more additional anti-tumor therapeutic agents in previously treated metastatic breast cancer.
Abstract: The present invention relates to anti-FcRH5 antibodies, including anti-FcRH5 antibodies comprising an FcRH5 binding domain and a CD3 binding domain (e.g., FcRH5 T cell-dependent bispecific (TDB) antibodies), and methods of using the same.
Type:
Grant
Filed:
June 16, 2016
Date of Patent:
June 18, 2019
Assignee:
Genentech, Inc.
Inventors:
Isidro Hotzel, Teemu T. Junttila, Ji Li, Justin Scheer, Danielle DiCara, Diego Ellerman, Christoph Spiess, Paul J. Carter
Abstract: The needless vial assemblies described herein allow for the access to the contents of a vial, such as a medication, using a syringe without a needle. In some designs, the vial includes a vial neck, which is itself a syringe interface. The vial assemblies also include a cap with a plug, which can be used to seal the vial assembly. The present disclosure further provides methods of filling a vial assembly and methods of filling a syringe using the vial assemblies described herein.
Abstract: The invention provides PCSK9 inhibitors, compositions comprising the PCSK9 inhibitors, and methods of identifying and using the PCSK9 inhibitors.
Type:
Application
Filed:
December 21, 2018
Publication date:
June 13, 2019
Applicant:
Genentech, Inc.
Inventors:
Maureen Beresini, Daniel Burdick, Charles Eigenbrot, JR., Daniel Kirchhofer, Robert Lazarus, Wei Li, John Quinn, Nicholas Skelton, Mark Ultsch, Yingnan Zhang
Abstract: The presently disclosed subject matter provides antibodies that bind KLB and FGFR1, and methods of using the same. In certain embodiments, an antibody of the present disclosure includes a bispecific antibody that binds to an epitope present on FGFR1 and binds to an epitope present on KLB.
Type:
Application
Filed:
February 25, 2019
Publication date:
June 13, 2019
Applicant:
GENENTECH, INC.
Inventors:
Yongmei Chen, James Ernst, Hok Seon Kim, Junichiro Sonoda, Christoph Spiess, Scott Stawicki, Yan Wu
Abstract: The invention relates generally to pyrrolobenzodiazepine monomer and dimer prodrugs having a glutathione-activated disulfide prodrug moiety, a DT-diaphorase-activated quinone prodrug moiety or a reactive oxygen species-activated aryl boronic acid or aryl boronic ester prodrug moiety. The invention further relates to pyrrolobenzodiazepine prodrug dimer-antibody conjugates.
Type:
Application
Filed:
February 8, 2019
Publication date:
June 13, 2019
Applicant:
GENENTECH, INC.
Inventors:
Peter DRAGOVICH, Zhonghua PEI, Thomas PILLOW, Jack SADOWSKY, Vishal VERMA, Donglu ZHANG
Abstract: The subject matter described herein is directed to compositions comprising a MEK inhibitor, or a pharmaceutically acceptable salt thereof, and a multi-kinase inhibitor that targets PDGFR?, S6 and STAT3 or a pharmaceutically acceptable salt thereof, and their use in treating pancreatic cancer. In another aspect, disclosed herein are methods of treating pancreatic cancer by administering a MEK inhibitor, or a pharmaceutically acceptable salt thereof, and a multi-kinase inhibitor, or a pharmaceutically acceptable salt thereof. In another aspect, the combination of cobimetinib, or a pharmaceutically acceptable salt thereof, and ponatinib or a pharmaceutically acceptable salt thereof is administered in a composition or the combination is administered separately to treat pancreatic cancer.
Abstract: The present invention relates to methods for treating PCAF mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R3-R6, X, and each Re have any of the values defined in the specification. Also included are novel compounds of formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 3, 2017
Date of Patent:
June 11, 2019
Assignees:
GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
Inventors:
Brian K. Albrecht, Alexandre Cote, Terry Crawford, Martin Duplessis, Andrew Charles Good, Yves LeBlanc, Steven Magnuson, Christopher G. Nasveschuk, Richard Pastor, F. Anthony Romero, Alexander M. Taylor