Abstract: The present invention relates to a process for the preparation of a compound (I), and its solid form, which is a modulator of ?-secretase and may be useful for prophylaxis and treatment of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
Abstract: The invention comprises a process for the preparation of a chiral triol of formula I wherein, R1 is hydrogen or halogen by way of an asymmetric hydrogenation of a ketone compound of formula IIa wherein, R1 is hydrogen or halogen and R2 is C1-6-alkyl; with hydrogen in the presence of an iridium spiro-pyridylamidophosphine catalyst (Ir-SpiroPAP catalyst). The chiral triols of formula I are versatile building blocks for the preparation of various pharmaceutically active drug substances such as for instance for statins.
Type:
Application
Filed:
July 12, 2023
Publication date:
January 18, 2024
Applicants:
Hoffmann-La Roche Inc., Genentech, Inc.
Inventors:
Anna-Lena GLASS, Allen Yu HONG, Kurt PUENTENER
Abstract: The present invention relates to novel solid forms of compound (I), 3-[(8aS)-7-[[(4S)-5-ethoxycarbonyl-4-(3-fluoro-2-methyl-phenyl)-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[1,5-a]pyrazin-2-yl]-2,2-dimethyl-propanoic acid and pharmaceutical compositions comprising solid forms thereof disclosed herein, which can be used as a HBV capsid inhibitor (or HBV Core Protein Allosteric Modifier), or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.
Abstract: Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
Type:
Grant
Filed:
June 28, 2021
Date of Patent:
January 16, 2024
Assignees:
Genentech, Inc., Hoffmann-La Roche Inc.
Inventors:
Haiming Zhang, Jie Xu, Georg Wuitschik, Remy Angelaud, Sebastian Herold, Alfred Stutz, Tobias Bruetsch, Johannes Burkhard
Abstract: Herein are reported modified mammalian cells wherein the expression of the MYC gene and one or more of the BAK, BAX, SIRT-1 and ICAM-1 genes has been reduced or eliminated as well as methods for the recombinant production of a heterologous polypeptide using a modified mammalian cell according to the current invention. Further reported are use of the reduction of the expression of the genes for increasing volumetric productivity, increasing cell volume, increasing viability and increasing the possible cultivation time without cell split.
Type:
Application
Filed:
April 19, 2023
Publication date:
January 11, 2024
Applicants:
Genentech, Inc., Hoffmann-La Roche Inc.
Inventors:
Shahram Misaghi, Amy Shen, Inn Huam Yuk, Gavin Christian Barnard, Simon Auslaender, Niels Bauer, Benedikt Oswald
Abstract: The invention relates to a compound of formula (I) wherein R1-R4 and A1 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
Type:
Application
Filed:
September 15, 2023
Publication date:
January 11, 2024
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Cosimo DOLENTE, Nadine GRETHER, Fionn Susannah O'HARA, Matilde PIRAS, Hasane RATNI, Michael REUTLINGER, Walter VIFIAN, Claudio ZAMBALDO
Abstract: The present invention relates to anti-VEGF/anti-IL-1beta antibodies and methods of using the same.
Type:
Grant
Filed:
September 8, 2021
Date of Patent:
January 9, 2024
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Roland Beckmann, Joerg Benz, Stefan Dengl, Christian Gassner, Guido Hartmann, Peter Michael Huelsmann, Sabine Imhof-Jung, Kristian Hobolt Jensen, Hubert Kettenberger, Stefan Lorenz, Joerg Moelleken, Olaf Mundigl
Abstract: The invention relates to a comparison unit (130) configured for determining if a first pH measuring device of a first tank (104; 106) is affected by a pH-measuring problem, the comparison unit being configured for: receiving a first CO2 concentration and a first pH value, the first CO2 concentration being a CO2 concentration of a first gas volume above a medium in a first tank, the first CO2 concentration and the first pH value being measured at a first time when the medium in the first tank is in pH-CO2 equilibrium state with the first gas volume and before said equilibrium state is modified by the metabolism of a cell culture in the first tank, the first pH value being a measured value provided by a first pH measuring device operatively coupled to the first tank (102); receiving a second CO2 concentration and a second pH value, the second CO2 concentration being a CO2 concentration of a second gas volume above a medium in a second tank, the second CO2 concentration and the second pH value being measured
Type:
Grant
Filed:
January 13, 2022
Date of Patent:
January 9, 2024
Assignee:
Hoffmann-La Roche, Inc.
Inventors:
Detlef Eisenkraetzer, Christian Klinger, Katrin Greppmair
Abstract: The present invention relates to the combination therapy of specific PD-1-targeted IL-2 variant immunocytokines with specific antibodies which bind human PD-L1.
Type:
Grant
Filed:
September 1, 2021
Date of Patent:
January 9, 2024
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Laura Codarri Deak, Douglas Hanahan, Christian Klein, Valeria Nicolini, Pablo Umana, Stephan Wullschleger
Abstract: Compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and X are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Application
Filed:
July 20, 2023
Publication date:
January 4, 2024
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Giuseppe CECERE, Luca GOBBI, Maria-Clemencia HERNANDEZ, Frédéric KNOFLACH, Andreas KOBLET, Eoin Cornelius O'CONNOR, Andres Miguel OLIVARES MORALES, Michael REUTLINGER, Valerie RUNTZ-SCHMITT, Jaclyn Ivy WAMSTEEKER CUSULIN, Nicolas ZORN
Abstract: The invention provides novel compounds having the general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R2?, R3, R4 and R5 are as described herein. The compound of formula (I) can be used as a medicament.
Type:
Application
Filed:
November 29, 2021
Publication date:
January 4, 2024
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Cosimo DOLENTE, Annick GOERGLER, David Stephen HEWINGS, Georg JAESCHKE, Ulrike OBST SANDER, Antonio RICCI
Abstract: Disclosed are techniques for using artificial intelligence (AI) to facilitate the selection of lines of therapy for subjects diagnosed with cancer. Methods and systems disclosed herein relate to techniques for using AI to predict therapeutic outcomes and cancer evolution in subjects based on mutation profiles of subjects across cancer types, to predict treatment survival prospects for subjects using enriched subject-specific data sets, and to automatically validate whether the reasons (e.g., represented by features in a subject record) that contributed to the selection of a particular line of therapy comply with oncological treatment guidelines.
Type:
Application
Filed:
October 6, 2021
Publication date:
January 4, 2024
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Silvia Elena MOLERO LEON, Turap Tasoglu
Abstract: The invention relates in particular to a process for the preparation of a compound of formula (I) wherein R1 and R2 are as defined in the description and in the claims.
Type:
Application
Filed:
May 22, 2023
Publication date:
January 4, 2024
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Dainis KALDRE, Christian Oliver KAPPE, Christian Steffen MOESSNER, Peter SAGMEISTER, Joerg Mathias SEDELMEIER, Jason Douglas WILLIAMS
Abstract: The invention relates to a compound of formula (I) wherein X, R1-R4 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
Type:
Application
Filed:
September 15, 2023
Publication date:
January 4, 2024
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Cosimo DOLENTE, Nadine GRETHER, Fionn Susannah O'HARA, Matilde PIRAS, Hasane RATNI, Michael REUTLINGER, Walter VIFIAN, Claudio ZAMBALDO
Abstract: Methods and systems for determining a location of an individual in a home, business, structure, or other finite amount of space using one or more beacons.
Type:
Application
Filed:
June 29, 2023
Publication date:
January 4, 2024
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Christopher Hughes CHATHAM, Joerg Felix HIPP, Lito KRIARA, Michael LINDEMANN, Florian LIPSMEIER, David NOBBS, David Alexander SLATER
Abstract: The invention relates to combination therapies employing anti-PD1/anti-LAG3 bispecific antibody and a CD20 T cell-activating bispecific antibody, the use of these combination therapies for the treatment of cancer and methods of using the combination therapies.
Type:
Application
Filed:
July 5, 2023
Publication date:
January 4, 2024
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Laura Codarri Deak, Christian Klein, Mario Perro, Patrick Alexander Aaron Weber
Abstract: Herein is reported a method for co-cultivating one or more B-cells comprising the step of incubating the one or more B-cells with EL4-B5 cells, whereby the EL4-B5 cells have been obtained/are from a cultivation of EL4-B5 cells that has a cell density of from 600,000 cells/ml up to 1,500,000 cells/ml.
Abstract: The present invention is directed to a combination therapy involving a type II anti-CD20 antibody and a selective Bcl-2 inhibitor for the treatment of a patient suffering from cancer, particularly, a CD20-expressing cancer.
Type:
Application
Filed:
September 7, 2023
Publication date:
January 4, 2024
Applicants:
GENENTECH, INC., HOFFMANN-LA ROCHE INC., ABBVIE INC.
Inventors:
Deepak Sampath, Christian Klein, Wayne John Fairbrother, Sari L. Heitner Enschede, Rod A. Humerickhouse, Andrew W. Roberts, John F. Seymour
Abstract: The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein X, D, R1 to R4, and R6 to R10 are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
Type:
Grant
Filed:
July 14, 2022
Date of Patent:
January 2, 2024
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Mathis Braendlin, Sandra Marie Joseph Grall-Ulsemer, Xingchun Han, Christian Lerner, Mingming Li, Yongqiang Liu, Sébastien Schmitt, Jianhua Wang, Yongguang Wang, Min Wang, Song Yang, Chengang Zhou