公开(公告)号：US20230279090A1

公开(公告)日：2023-09-07

申请号：US18301187

申请日：2023-04-14

申请人： Genentech, Inc. ,  HOFFMANN-LA ROCHE INC.

发明人： Stefan Dengl ,  Rami Hannoush ,  Simon Theodor Hansen ,  Peter Michael Huelsmann ,  Robert Franklin Kelley ,  Hubert Kettenberger ,  Shrenik Chetan Mehta ,  Devin Brent Tesar

IPC分类号： C07K16/22 ,  C07K14/705 ,  A61P27/02

CPC分类号： C07K16/22 ,  A61P27/02 ,  C07K14/70578 ,  C07K14/70585

摘要： A conjugate may comprise a first component capable of binding to a therapeutic target in the eye, one or more second component(s) capable of binding to hyaluronan, and one or more third component(s) comprising hyaluronan, wherein each second component is covalently bound to the first component and non-covalently bound to a third component, a composition comprising the conjugate for use as a medicament or for use in the treatment of an eye disease and a method of treating an eye disease in a subject. Additionally, a therapeutic molecule targeted to a tissue in a patient may comprises a hyaluronic acid binding moiety and a therapeutically active agent, wherein the hyaluronic acid binding moiety comprises at least two link domains of Versican.

公开(公告)号：US20230278997A1

公开(公告)日：2023-09-07

申请号：US18318144

申请日：2023-05-16

申请人： Hoffmann-La Roche Inc.

发明人： Jianping WANG ,  Hongying YUN ,  Bo ZHANG ,  Xiufang ZHENG

IPC分类号： C07D417/12 ,  C07D417/14 ,  C07D413/12 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07D417/12 ,  C07D417/14 ,  C07D413/12 ,  C07D405/12 ,  C07D409/12

摘要： The present invention provides novel compounds having the general formula (I):




wherein A, L, and B are as described herein, compositions including the compounds and methods of using the compounds.

公开(公告)号：US11738003B2

公开(公告)日：2023-08-29

申请号：US16951153

申请日：2020-11-18

申请人： Hoffmann-La Roche Inc.

发明人： Kellie Glenn ,  Brian Higgins ,  Gwen Nichols ,  Kathryn Packman

IPC分类号： A61K31/401 ,  A61K31/40 ,  A61K9/14

CPC分类号： A61K31/401 ,  A61K9/146 ,  A61K31/40

摘要： There is provided a new dosage regimen for Compound A which maximizes anti-tumor activity while maintaining acceptable toxicity levels.

公开(公告)号：US20230265177A1

公开(公告)日：2023-08-24

申请号：US18091056

申请日：2022-12-29

申请人： Hoffmann-La Roche Inc.

发明人： Stefan Dengl ,  Thomas Emrich ,  Guy Georges ,  Ulrich Goepfert ,  Fiona Grueninger ,  Adrian Hugenmatter ,  Anton Jochner ,  Hubert Kettenberger ,  Joerg Moelleken ,  Ekkehard Moessner ,  Olaf Mundigl ,  Jens Niewoehner ,  Tilman Schlothauer ,  Michael Molhoj ,  Kevin Brady

IPC分类号： C07K16/18

CPC分类号： C07K16/18 ,  C07K2317/24 ,  C07K2317/34 ,  C07K2317/92 ,  A61K2039/505

摘要： The invention provides humanized anti-human Tau(pS422) antibodies and methods of using the same.

公开(公告)号：US20230250074A1

公开(公告)日：2023-08-10

申请号：US18164302

申请日：2023-02-03

申请人： Genentech, Inc. ,  Hoffmann-La Roche Inc.

发明人： 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分类号： C07D401/04 ,  B01J23/44 ,  B01J23/755

CPC分类号： C07D401/04 ,  B01J23/44 ,  B01J23/755

摘要： 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：US20230248723A1

公开(公告)日：2023-08-10

申请号：US16769284

申请日：2018-12-04

申请人： Hoffmann-La Roche Inc.

发明人： Jitao David ZHANG ,  Xingchun HAN ,  Song YANG ,  Miriam TRIYATNI ,  Brian LEONARD ,  Angelina WALLIER ,  Josephine SCHMALER ,  Daniel TURLEY ,  Philipp TROPBERGER ,  Samuel CROSET

IPC分类号： A61K31/4985 ,  A61P31/20 ,  G01N33/50

CPC分类号： A61K31/4985 ,  A61P31/20 ,  G01N33/5067 ,  G01N33/5023

摘要： The present invention relates to novel therapeutic agents against hepatitis B virus (HBV) infection, particularly inhibitors of viral covalently closed circular DNA (cccDNA) which is the key barrier for HBV cure. Accordingly, the invention provides the pyrrolo[2,3-b]pyrazine compounds of formula (I), as described and defined herein, for use in the treatment of HBV infection. The compounds provided herein are highly potent against HBV infection and enable an improved therapy, particularly of chronic HBV infection and HBV rebound. The present invention further relates to a novel screening assay for the identification of therapeutic agents against HBV infection, particularly cccDNA inhibitors, which is performed in hepatocyte-like cells that recapitulate the complete HBV life cycle following infection with patient-derived HBV.

公开(公告)号：US20230242553A1

公开(公告)日：2023-08-03

申请号：US18299299

申请日：2023-04-12

申请人： Hoffmann-La Roche Inc.

发明人： Weichun CHEN ,  Xing LIANG ,  Guocai ZHANG

IPC分类号： C07D519/00

CPC分类号： C07D519/00

摘要： The present invention relates to a process for synthesizing a compound of formula (I),




wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen or cyano; n is 0-7, particularly n is 2-3, more particularly n is 2; or diastereomer, pharmaceutically acceptable salts thereof, which is useful for prophylaxis and treatment of a disease caused by bacteria infection.

公开(公告)号：US20230242520A1

公开(公告)日：2023-08-03

申请号：US17999196

申请日：2021-05-18

申请人： Hoffmann-La Roche Inc.

发明人： Guillaume DÉCORET ,  Guido GALLEY ,  Katrin GROEBKE ZBINDEN ,  Wolfgang GUBA ,  Daniel HUNZIKER

IPC分类号： C07D413/12 ,  C07D233/64 ,  C07D261/08 ,  C07D249/04 ,  C07D263/32 ,  C07D275/02 ,  C07D495/04

CPC分类号： C07D413/12 ,  C07D233/64 ,  C07D261/08 ,  C07D249/04 ,  C07D263/32 ,  C07D275/02 ,  C07D495/04

摘要： The invention relates to a compound of formula (I) wherein R1-R2 are as defined in the description and in the claims The compound of formula (I) can be used as a medicament.

公开(公告)号：US11708354B2

公开(公告)日：2023-07-25

申请号：US17103648

申请日：2020-11-24

申请人： Hoffmann-La Roche Inc.

发明人： Martin Duplessis ,  Georg Jaeschke ,  Bernd Kuhn ,  Kiel Lazarski ,  Yanke Liang ,  Yvonne Alice Nagel ,  Antonio Ricci ,  Daniel Rueher ,  Sandra Steiner

IPC分类号： C07D403/12 ,  C07D403/14 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14 ,  A61P35/00 ,  A61K9/48 ,  A61K9/20 ,  A61K9/02 ,  A61K9/00

CPC分类号： C07D403/12 ,  A61K9/009 ,  A61K9/0019 ,  A61K9/02 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/485 ,  A61K9/4825 ,  A61K9/4858 ,  A61K9/4866 ,  A61K9/4875 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D417/12 ,  C07D417/14

摘要： The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.

公开(公告)号：US20230227564A1

公开(公告)日：2023-07-20

申请号：US18125691

申请日：2023-03-23

申请人： Hoffmann-La Roche Inc.

发明人： Silke Hansen ,  Klaus-Peter Kuenkele ,  Dietmar Reusch ,  Ralf Schumacher

IPC分类号： C07K16/28 ,  C07K16/00

CPC分类号： C07K16/2863 ,  C07K16/00 ,  C07K2317/52 ,  C07K2317/41

摘要： The invention provides an antibody comprising human IgG1 or IgG3 heavy chain constant domains that are glycosylated with a sugar chain at Asn297, said antibody being characterized in that the amount of fucose within said sugar chain is at least 99%, and in addition the amount of NGNA is 1% or less and/or the amount of N-terminal alpha 1,3 galactose is 1% or less, and uses thereof.