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公开(公告)号：US20230047100A1
公开(公告)日：2023-02-16
申请号：US17797293
申请日：2021-01-29
发明人： Fillippo ARCADU , Benjamin GUTIERREZ-BECKER , Andreas THALHAMMER , Marco PRUNOTTO , Young Suk OH
摘要： The application relates to devices and methods for analysing a colonoscopy video or a portion thereof, and for assessing the severity of ulcerative colitis in a subject by analysing a colonoscopy video obtained from the subject. Analysing a colonoscopy video comprises using a first deep neural network classifier to classify image data from the subject colonoscopy video or portion thereof into at least a first severity class (more severe endoscopic lesions) and a second severity class (less severe endoscopic lesions), wherein the first deep neural network has been trained at least in part in a weakly supervised manner using training image data from a plurality of training colonoscopy videos, the training image data comprising multiple sets of consecutive frames from the plurality of training colonoscopy videos, wherein frames in a set have the same severity class label. Devices and methods for providing a tool for analysing colonoscopy videos are also described.
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12.发明授权公开(公告)号：US11577893B2
公开(公告)日：2023-02-14
申请号：US16831161
申请日：2020-03-26
发明人： Harald Heinlein
摘要： A vial stopper for closure of a lyophilization vial is disclosed. The vial stopper has a stopper body comprising a first circumferential sealing surface for hermetically sealing against an interior surface of a mouth of the vial in a first position of the vial stopper. The stopper body further comprises a second circumferential sealing surface for hermetically sealing against the interior surface of the mouth of the vial in a second position of the vial stopper. The second sealing surface is spaced apart from the first sealing surface in an axial direction of the stopper body. The stopper body further comprises an intermediate region in between the first and second sealing surfaces, the intermediate region having at least one venting element for venting an interior of the vial in at least one intermediate position of the stopper in between the first and second positions.
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公开(公告)号：US20230045262A1
公开(公告)日：2023-02-09
申请号：US17819867
申请日：2022-08-15
摘要： The invention relates to new bispecific antigen binding molecules, comprising at least one antigen binding domain capable of specific binding to 4-1BB, at least one moiety capable of specific binding to a target cell antigen, and a Fc domain composed of a first and a second subunit capable of stable association, and to methods of producing these molecules and to methods of using the same.
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![SYNTHESIS OF A BIS-MESYLATE SALT OF 4-AMINO-N-(1-((3-CHLORO-2-FLUOROPHENYL)AMINO)-6-METHYLISOQUINOLIN-5-YL)THIENO[3,2-D]PYRIMIDINE-7-CARBOXAMIDE AND INTERMEDIATES THERETO](/abs-image/US/2023/01/26/US20230028651A1/abs.jpg.150x150.jpg)
公开(公告)号：US20230028651A1
公开(公告)日：2023-01-26
申请号：US17852227
申请日：2022-06-28
发明人： Francis GOSSELIN , Stefan G. KOENIG , Eduardo V. MERCADO-MARIN , Andreas STUMPF , Daniel ZELL , Haiming ZHANG , Stephan BACHMANN , Diane E. CARRERA , Michael E. DALZIEL , Yonghui GE , Jie ZHANG , Raphael BIGLER , Laure Elizabeth Simone FINET , Regis Jean Georges MONDIERE , Yuki NAKAGAWA
IPC分类号： C07D495/04
摘要： A manufacturing process to a bis-mesylate salt 1b of the pan-RAF inhibitor 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide. The process features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2 and a highly chemoselective PtN/C-catalyzed nitro group reduction to access penultimate intermediate 7. The final amide coupling of 7 and 2 was accomplished by a mild and safe protocol employing N,N,N′,N′-tetramethylchloroformamidinium hexafluorophosphate (TCFH) as the coupling reagent, to produce a 1:1 adduct of the freebase and THF. The adduct afforded compound 1b with excellent yield, purity, and form stability on a multikilogram production scale after reaction with MsOH and recrystallization. The methods are able to produce a compound having upwards of 95% purity.
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![HYDROPYRIDO[1,2-a]PYRAZINE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE](/abs-image/US/2023/01/26/US20230022297A1/abs.jpg.150x150.jpg)
公开(公告)号：US20230022297A1
公开(公告)日：2023-01-26
申请号：US17780161
申请日：2020-12-01
发明人： Jianguo CHEN , Fabian DEY , Hongtao XU , Weixing ZHANG , Wei ZHU
IPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds act as antagonists of the toll-like receptors TLR7, TLR8 and/or TLR9 and are thus useful in the treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
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公开(公告)号：US20230016472A1
公开(公告)日：2023-01-19
申请号：US17856912
申请日：2022-07-01
IPC分类号： G06V10/774 , G06V10/82 , G06T7/00
摘要： Described herein are systems, methods, and programming for analyzing and classifying digital pathology images. Some embodiments include receiving whole slide images (WSIs) and dividing each of the WSIs into tiles. For each WSI, a random subset of the tiles may be selected and augmented views of each of the selected tiles may be generated. For each of the selected tiles, a first convolutional neural network (CNN) may be trained to: generate, using a first one of the augmented views corresponding to the selected tile, a first representation of the selected tile, and predict a second representation of the selected tile to be generated by a second CNN, wherein the second representation is generated based on a second one of the augmented views of the selected tile.
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公开(公告)号：US20230013602A1
公开(公告)日：2023-01-19
申请号：US17349888
申请日：2021-06-16
发明人： Jean-Baptiste BLANC , Nawaz KHAN , Christian KRAMER , Christian LERNER , Philippe PFLIEGER , Theodor STOLL , Song YANG
IPC分类号： C07D487/04 , A61P31/04 , B01J31/12
摘要： Provided are novel imidazopyrazine derivatives having the general formula (I), wherein A and R1 to R14 are as described herein and pharmaceutically acceptable salts thereof.
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.-
公开(公告)号：US11555067B2
公开(公告)日：2023-01-17
申请号：US16244378
申请日：2019-01-10
发明人： Tilman Schlothauer
摘要： Herein is reported a polypeptide comprising a first polypeptide and a second polypeptide each comprising in N-terminal to C-terminal direction at least a portion of an immunoglobulin hinge region, which comprises one or more cysteine residues, an immunoglobulin CH2-domain and an immunoglobulin CH3-domain, wherein the first, the second, or the first and the second polypeptide comprise the mutation Y436A (numbering according to the EU index).
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公开(公告)号：US11547748B2
公开(公告)日：2023-01-10
申请号：US16314117
申请日：2017-06-30
发明人： Christian Klein , Claudio Sustmann , Gerhard Niederfellner , Martina Geiger , Stefan Endres , Sebastian Kobold
IPC分类号： A61K39/00 , C07K16/28 , C07K16/30 , C07K14/71 , C12N5/0783 , A61P35/00 , A61K39/395
摘要： The present invention generally relates to T-cells, such as CD8+ T-cells, CD4+ T-cells, CD3+ T-cells, γδ T-cells or natural killer (NK) T-cells, transfected/transduced with a fusion protein which is recruited by the use of trivalent, bispecific antibody molecule which specifically binds to/interacts with the extracellular domain of the fusion protein. More precisely, the present invention relates to a kit comprising the nucleic acid molecules, vectors and/or the fusion proteins of the present invention and the trivalent, bispecific antibody molecules of the present invention. Further aspects of the inventions are expression vectors comprising nucleic acid molecules encoding the fusion proteins as well as the trivalent, bispecific antibody molecules. Further, a process for the production of the trivalent, bispecific antibody molecules of the invention and a medicament/pharmaceutical composition comprising said trivalent, bispecific antibody molecules are described. The invention also provides the use of said trivalent, bispecific antibody molecules in a method for the treatment of particular diseases as well as a pharmaceutical compositions/medicament comprising said trivalent, bispecific antibody molecules, wherein said trivalent, bispecific antibody molecule(s) is (are) to be administered in combination with transduced T-cells comprising the fusion protein of the invention. The invention also provides a method for the treatment of particular diseases.
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