公开(公告)号：US12252533B2

公开(公告)日：2025-03-18

申请号：US18069838

申请日：2022-12-21

Applicant: Hoffmann-La Roche Inc.

Inventor： Stefan Dengl ,  Guy Georges ,  Ulrich Goepfert ,  Jens Niewoehner ,  Tilman Schlothauer

IPC: C07K16/28 ,  A61K39/395 ,  A61P25/00 ,  C07K14/79

Abstract: Herein is reported an anti-transferrin receptor antibody that specifically binds to human transferrin receptor and cynomolgus transferrin receptor, which comprises i) a humanized heavy chain variable domain derived from the heavy chain variable domain of SEQ ID NO: 01, and ii) a humanized light chain variable domain derived from the light chain variable domain of SEQ ID NO: 26, wherein the antibody has an off-rate for the human transferrin receptor that is equal to or less than (i.e. at most) the off-rate of the anti-transferrin receptor antibody 128.1 for the cynomolgus transferrin receptor, whereby the off-rates are determined by surface plasmon resonance, and whereby the anti-transferrin receptor antibody 128.1 has a heavy chain variable domain of SEQ ID NO: 64 and a light chain variable domain of SEQ ID NO: 65.

公开(公告)号：US20250074901A1

公开(公告)日：2025-03-06

申请号：US18710702

申请日：2022-11-17

Applicant: ICAGEN, LLC ,  HOFFMANN-LA ROCHE INC.

Inventor： Mark CHAPMAN ,  James DAVIDSON ,  Nicholas Gareth Morse DAVIES ,  Aaron GERLACH ,  Christopher John GRAHAM ,  Sylvain LEBRETON ,  Ronghua LI ,  Nina MA ,  Ingrid MECHIN ,  David MOWREY ,  Karthigeyan NAGARAJAN ,  Anil NAIR ,  Roger David NORCROSS ,  Roger Lluis REDONDO PENA ,  Alena SAFAROVA ,  Martin SMRCINA

IPC: C07D405/14 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/50 ,  A61K31/505 ,  A61K31/506 ,  A61K31/55 ,  A61K31/695 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/84 ,  C07D237/14 ,  C07D239/34 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/04 ,  C07D493/08 ,  C07F7/08

Abstract: The invention provides new heteroaromatic compounds having the general formula (I′), or a solvate or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, Y1, Y2, Y3, and n are as defined herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

公开(公告)号：US20250074893A1

公开(公告)日：2025-03-06

申请号：US18946050

申请日：2024-11-13

Applicant: Genentech, Inc. ,  Hoffmann-La Roche Inc.

Inventor： NGIAP-KIE LIM ,  JEFF SHEN ,  LAUREN ELIZABETH SIROIS ,  JACOB C. TIMMERMAN ,  ETIENNE TRACHSEL ,  NICHOLAS ANDREW WHITE ,  JIE XU ,  HAIMING ZHANG ,  STEPHAN BACHMANN ,  RAPHAEL BIGLER ,  KYLE BRADLEY PASCUAL CLAGG ,  ANTONIO GIOVANNI DIPASQUALE ,  FRANCIS GOSSELIN ,  UGO JONATHAN ORCEL ,  ROLAND CHRISTOPH MEIER

IPC: C07D401/14

Abstract: Provided herein are methods of synthesizing quinazoline compounds comprising at least one atropisomeric center.

公开(公告)号：US20250073308A1

公开(公告)日：2025-03-06

申请号：US18746802

申请日：2024-06-18

Applicant: Hoffmann-La Roche Inc.

Inventor： Laura Codarri Deak ,  Christian Klein ,  Laura Lauener ,  Valeria G. Nicolini ,  Stefan Seeber ,  Pablo Umaña ,  Inja Waldhauer

IPC: A61K38/20 ,  A61K38/00 ,  A61K39/00 ,  A61K39/395 ,  A61K47/68 ,  A61P35/00 ,  C07K14/55 ,  C07K16/28

Abstract: The present invention generally relates to immunoconjugates, particularly immunoconjugates comprising a mutant interleukin-2 polypeptide and an antibody that binds to PD-1. In addition, the invention relates to polynucleotide molecules encoding the immunoconjugates, and vectors and host cells comprising such polynucleotide molecules. The invention further relates to methods for producing the mutant immunoconjugates, pharmaceutical compositions comprising the same, and uses thereof.

公开(公告)号：US20250059185A1

公开(公告)日：2025-02-20

申请号：US18720022

申请日：2022-12-14

Applicant: Hoffmann-La Roche Inc.

Inventor： Joerg BENZ ,  Maude GIROUD ,  Uwe GRETHER ,  Bernd KUHN ,  Fionn Susannah O'HARA ,  Matthias Beat WITTWER

IPC: C07D471/04 ,  A61K9/20 ,  A61K9/48 ,  A61K31/437 ,  A61K31/444 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/675 ,  C07D487/04 ,  C07D519/00 ,  C07F9/6561

Abstract: The invention provides new MAGL inhibitors having the general formula (II)AB(II) wherein the variables are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

公开(公告)号：US20250059155A1

公开(公告)日：2025-02-20

申请号：US18776585

申请日：2024-07-18

Applicant: Genentech, Inc. ,  Hoffmann-La Roche Inc.

Inventor： Rene LEBL ,  Ngiap Kie LIM ,  Roland Christoph MEIER ,  Ugo Jonathan ORCEL ,  Joerg SEDELMEIER ,  Jeff SHEN ,  Lauren Elizabeth SIROIS ,  Jacob C. TIMMERMAN ,  Etienne TRACHSEL ,  Nicholas Andrew WHITE ,  Jie XU ,  Haiming ZHANG ,  Stephan BACHMANN ,  Thomas Michael BASS ,  Raphael BIGLER ,  Johannes Adrian BURKHARD ,  Kyle Bradley Pascual CLAGG ,  Francis GOSSELIN ,  Chong HAN ,  Dainis KALDRE ,  Sean M. KELLY ,  Sebastian HEROLD ,  Christian LEITNER

IPC: C07D401/04 ,  B01J23/44 ,  B01J23/755

Abstract: Provided herein are methods to synthesize compounds useful in the treatment of cancer where such compounds comprise a quinazolinyl core moiety and at least one stereoisomeric or atropisomeric moiety.

公开(公告)号：US12221420B2

公开(公告)日：2025-02-11

申请号：US17571182

申请日：2022-01-07

Applicant: Hoffmann-La Roche Inc.

Inventor： Paul Spurr ,  Rene Trussardi

IPC: C07D231/14

Abstract: The invention provides a process for manufacturing 5-ethyl-4-methyl-N-[4-[(2S) morpholin-2-yl]phenyl]-1H-pyrazole-3-carboxamide (Formula I), or a pharmaceutically acceptable salt thereof, on an industrial scale, comprising a one-pot process for manufacturing 5-ethyl-4-methyl-1H-pyrazole-3-carboxylic acid (1).

公开(公告)号：US12220496B2

公开(公告)日：2025-02-11

申请号：US18330083

申请日：2023-06-06

Applicant: F. HOFFMANN-LA ROCHE AG ,  GENENTECH, INC.

Inventor： Markus Hemminger ,  Ulla Grauschopf ,  Frank Bamberg ,  Mayumi Bowen ,  Robert Müller ,  Flora Felsovalyi ,  Denny Christensen

IPC: A61L11/00 ,  A61L2/00 ,  A61L2/20 ,  A61L9/00 ,  A61M5/00 ,  A61M5/31 ,  A61M5/315 ,  A61M5/32 ,  B65B3/00 ,  B65B7/28 ,  B65B55/10 ,  B65B55/02

Abstract: A method of preparing a prefilled syringe is disclosed that includes obtaining a syringe barrel and a needle adaptor cap assembled on the tip of the syringe barrel, wherein the needle adaptor cap has a rubber element tightly sealing the orifice of the tip of the syringe barrel and the syringe barrel together with the needle adaptor cap assembled on the tip of the syringe barrel is sterilized by a first sterilizing. Filling a drug substance into an interior of the syringe barrel and sealing the interior of the syringe barrel. Packaging the syringe barrel with a rubber stopper sealing the interior thereof and the needle adaptor cap assembled on the tip of the syringe barrel. Providing a second external surface sterilizing of the packaged syringe barrel with the rubber stopper sealing the interior thereof and the needle adaptor cap assembled on the tip of the syringe barrel.

公开(公告)号：US20250034576A1

公开(公告)日：2025-01-30

申请号：US18743170

申请日：2024-06-14

Applicant: Hoffmann-La Roche Inc.

Inventor： Philipp Friedrich BERNINGER ,  Konrad BLEICHER ,  Erik FUNDER ,  Helle JACOBSEN ,  Dennis Jul HANSEN ,  Michael KELLER ,  Inna Appeldorff LARSEN ,  Meiling LI ,  Disa Elisabet TEHLER ,  Lotte WINTHER ,  Jesper WORM ,  Lena WYSS ,  Tiago Francisco SANTOS FERREIRA

IPC: C12N15/113

Abstract: The present invention relates to double stranded oligonucleotides that are complementary to JAK1, leading to modulation of the expression of JAK1. Modulation of JAK1 expression is beneficial for a range of medical disorders including inflammatory bowel disease, organ transplant rejection, graft-versus-host disease, multiple sclerosis, rheumatoid arthritis (RA), juvenile idiopathic arthritis, psoriasis, dermatitis, diabetic nephropathy, systemic lupus erythematosus (SLE), dry eye disease, cancer, myelofibrosis, and asthma. Also included are compositions comprising the double stranded oligonucleotide and methods of treatment using the double stranded oligonucleotide.

公开(公告)号：US20250034269A1

公开(公告)日：2025-01-30

申请号：US18747055

申请日：2024-06-18

Applicant: Hoffmann-La Roche Inc.

Inventor： Roberta Bianchi ,  Felix Bormann ,  Michelle Victoria Brydon ,  Stefan Dengl ,  Harald Duerr ,  Guy Georges ,  Lydia Jasmin Hanisch ,  Monika Heidrich ,  Ralf Hosse ,  Leo Frederik Kunz ,  Stephane Leclair ,  Desirée Leisibach ,  Fanny Mende ,  Olaf Mundigl ,  Miroslav Nikolov ,  Pablo Umaña ,  Cornelia Wagner

IPC: C07K16/28 ,  A61P35/00 ,  C07K16/40

Abstract: The invention relates to novel antibodies that bind to lymphotoxin beta receptor (LTBR) and to bispecific antigen binding molecules comprising these novel LTBR antibodies and an antigen binding domain that binds a tumor associated antigen, in particular to Fibroblast Activation Protein (FAP), to methods of producing these molecules and to methods of using the same.