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81. 发明申请

US20220073469A1 PROCESS FOR THE PREPARATION OF EXO-TERT-BUTYL N-(3-AZABICYCLO[3.2.1]OCTAN-8-YL)CARBAMATE 有权
公开(公告)号：US20220073469A1
公开(公告)日：2022-03-10
申请号：US17418480
申请日：2019-12-24
申请人： Hoffmann-La Roche Inc.
发明人： Weichun CHEN , Guocai ZHANG
IPC分类号： C07D221/22
摘要： The present invention relates to a process for the preparation of a compound (I) or pharmaceutically acceptable salt thereof, which is useful as the key intermediate for the synthesis of compounds for prophylaxis and treatment of a disease associated with the deposition of β-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.

82. 发明申请

US20220072103A1 Combination therapy of PD-1-targeted IL-2 variant immunocytokines and antibodies against human PD-L1 有权
公开(公告)号：US20220072103A1
公开(公告)日：2022-03-10
申请号：US17464518
申请日：2021-09-01
申请人： Hoffmann-La Roche Inc.
发明人： Laura CODARRI DEAK , Douglas Hanahan , Christian Klein , Valeria Nicolini , Pablo Umana , Stephen Wullschleger
IPC分类号： A61K38/20 , A61K39/395 , A61K35/17 , A61K35/15 , A61K38/17 , A61P35/00
摘要： 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.

83. 发明申请

US20220064178A1 PYRIDINE DERIVATIVES 有权
公开(公告)号：US20220064178A1
公开(公告)日：2022-03-03
申请号：US17400292
申请日：2021-08-12
申请人： Hoffmann-La Roche Inc.
发明人： Beat Frei , Luca Gobbi , Uwe Grether , Fabienne Ricklin , Stephan Roever , Mark Rogers-Evans , Didier Rombach
IPC分类号： C07D491/107 , A61K9/20 , A61K9/28 , A61K9/48 , A61K47/12 , A61K47/34 , C07D213/81 , C07D401/12 , C07D405/12 , C07D413/04 , C07D413/14
摘要： The invention relates to compound of formula (I) wherein R1 to R3 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

84. 发明授权

US11254728B2 Method for producing monomeric and multimeric molecules and uses thereof 有权
公开(公告)号：US11254728B2
公开(公告)日：2022-02-22
申请号：US16777138
申请日：2020-01-30
申请人： Hoffmann-La Roche Inc.
发明人： Johannes Auer , Martin Bader , Stefan Dengl , Stefan Lorenz , Stefan Seeber
IPC分类号： C07K14/525 , C07K14/715 , C07K16/00 , C07K16/32 , A61K49/00 , C07K14/52 , C07K14/54
摘要： Herein is reported a method for the production of a polypeptide that is biologically active as n-mer comprising a nucleic acid encoding a fusion polypeptide according to the following formula (Bn-CSo-Is-CSp-FC-CSq-It-CSr-Bm)u, wherein B denotes a polypeptide that is biologically active as n-mer and forms non-defined aggregates/multimers upon expression in the absence of a fused Fc-region, FC denotes a heavy chain Fc-region polypeptide, CS denotes a cleavage site, and I denotes an intervening amino acid sequence, wherein FC does not substantially bind to an Fc-receptor, recovering the fusion polypeptide from the cell or the cultivation medium, optionally cleaving the fusion polypeptide with a protease, and thereby producing a polypeptide that is biologically active as n-mer and forms non-defined aggregates/multimers upon expression in the absence of a fused Fc-region.

85. 发明授权

US11253826B2 Combination stirrer 有权
公开(公告)号：US11253826B2
公开(公告)日：2022-02-22
申请号：US16103341
申请日：2018-08-14
申请人： HOFFMANN-LA ROCHE INC.
发明人： Marco Jenzsch , Max Lechner , Michael Pohlscheidt , Christoph Reese , Alexander Scholz , Hermann Tebbe
IPC分类号： B01F7/00 , C12M1/06
摘要： The present patent application describes a stirrer comprising a combination of at least one axially-conveying element and at least one radially-conveying element relative to the rotary shaft of the stirrer wherein the largest diameter of the at least one axially-conveying element is equal to or less than the inner diameter di of the radially-conveying element. In one embodiment the stirrer according to the invention is a combination of one anchor stirrer with at least one inclined-blade stirrer. Furthermore the use of the stirrer according to the invention for the culture of cells in a dialysis method is described.

86. 发明授权

US11242390B2 Protease-activated T cell bispecific molecules 有权
公开(公告)号：US11242390B2
公开(公告)日：2022-02-08
申请号：US16138417
申请日：2018-09-21
申请人： Hoffmann-La Roche Inc.
发明人： Peter Bruenker , Rebecca Croasdale-Wood , Christian Klein , Juergen Michael Schanzer , Kay-Gunnar Stubenrauch , Pablo Umana , Martina Geiger , Eric Sullivan , Jigar Patel
IPC分类号： C07K16/28 , A61P35/00 , C07K16/42 , A61K39/00
摘要： The present invention generally relates to novel protease-activatable T cell activating bispecific molecules and idiotype-specific polypeptides. The present invention also relates to polynucleotides encoding such protease-activatable T cell activating bispecific molecules and idiotype-specific polypeptides, and vectors and host cells comprising such polynucleotides. The invention further relates to methods for producing the protease-activatable T cell activating bispecific molecules and idiotype-specific polypeptides of the invention, and to methods of using these protease-activatable T cell activating bispecific molecules and idiotype-specific polypeptides in the treatment of disease.

87. 发明申请

US20220025069A1 BISPECIFIC ANTIGEN BINDING MOLECULES COMPRISING LIPOCALIN MUTEINS 有权
公开(公告)号：US20220025069A1
公开(公告)日：2022-01-27
申请号：US17498515
申请日：2021-10-11
申请人： Hoffmann-La Roche Inc.
发明人： Christina CLAUS , Claudia FERRARA KOLLER , Christian KLEIN , Pablo UMAÑA
IPC分类号： C07K16/40 , C07K14/475 , C07K16/46 , C07K16/32
摘要： The invention relates to bispecific antigen binding molecule capable of bivalent binding to 4-1BB and monovalent binding to a target cell antigen comprising two lipocalin muteins capable of specific binding to 4-1BB and their use in the treatment of cancer or infectious diseases.

88. 发明申请

US20220024616A1 MANUFACTURING A FLEXIBLE CONTAINER 有权
公开(公告)号：US20220024616A1
公开(公告)日：2022-01-27
申请号：US17296770
申请日：2019-11-25
申请人： HOFFMANN-LA ROCHE INC.
发明人： Carmen LEMA MARTINEZ , Joerg LUEMKEMANN , Tobias WERK , Thomas ZUMSTEIN , Daniel KULLMANN
IPC分类号： B65B3/00 , B29D22/00 , B65B5/04 , B65B3/02 , A61J1/10 , A61J1/14 , A61J1/20
摘要： A method of manufacturing a flexible container (1) housing a drug substance, comprises: forming a first compartment (11) of the container (1) out of a flexible sheet-like material, filling a liquid (2) into the first compartment (11) of the container (1), sealing the first compartment (11), forming a second compartment (12) of the container (1) out of the flexible sheet-like material, filling a dry drug formulation (3) into the second compartment (12), and sealing the second compartment (12). The method further involves lyophilizing the drug formulation inside a tubular cartridge such that the dry drug formulation (3) is generated and held in the tubular cartridge, wherein filling the dry drug formulation (3) into the second compartment (12) comprises: introducing the tubular cartridge holding the dry drug formulation (3) through an opening of the second compartment (12) of the container (1) such that an open end of the tubular cartridge is positioned distant from the opening of the second compartment (12), providing the dry drug formulation (3) out of the open end of the tubular cartridge into the second compartment (12), and withdrawing the tubular cartridge out of the opening of the second compartment (12) of the container (1). The first compartment (11) is separated from the second compartment (12) by a frangible seal (14) which opens when the first compartment (11) is compressed.

89. 发明申请

US20220017640A1 ACTIVATABLE BISPECIFIC ANTIBODIES 有权
公开(公告)号：US20220017640A1
公开(公告)日：2022-01-20
申请号：US17091883
申请日：2020-11-06
申请人： HOFFMANN-LA ROCHE INC.
发明人： Ulrich BRINKMANN , Rebecca CROASDALE , Silke METZ , Juergen Michael SCHANZER , Claudio SUSTMANN , Pablo UMANA
IPC分类号： C07K16/46 , C07K16/28 , C07K16/32
摘要： The current invention relates to bispecific antibodies wherein the binding affinity to one of the two antigens is reduced and which can be activated by tumor- or inflammation-specific proteases, and the preparation and use of such bispecific antibodies.

90. 发明申请

US20220017637A1 AGONISTIC CD28 ANTIGEN BINDING MOLECULES TARGETING HER2 有权
公开(公告)号：US20220017637A1
公开(公告)日：2022-01-20
申请号：US17354409
申请日：2021-06-22
申请人： Hoffmann-La Roche Inc.
发明人： Stephan GASSER , Thomas HOFER , Teemu Tapani JUNTTILA , Christian KLEIN , Christine KUETTEL , Jenny Tosca THOM , Pablo UMAÑA
IPC分类号： C07K16/32 , C07K16/28 , A61P35/00 , A61K45/06 , A61K39/395
摘要： The present invention relates to Her2-targeted bispecific agonistic CD28 antigen binding molecules characterized by monovalent binding to CD28, methods for their production, pharmaceutical compositions containing these antibodies, and methods of using the same.

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