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公开(公告)号：US20230265200A1
公开(公告)日：2023-08-24
申请号：US17706028
申请日：2022-03-28
CPC分类号： C07K16/2866 , C07K16/2815 , C07K16/2812 , A61P35/00 , C07K16/2818 , C07K16/2827 , A61K2039/505
摘要： The present disclosure relates to a method of treating a solid tumour, wherein said method involves the use of an antibody to CD25. In particular, the antibody to CD25 is optimized for depletion of regulatory T cells (Treg) within tumours. The present invention also provides novel anti-CD25 antibodies and their combination with other anti-cancer drugs, such as immune checkpoint inhibitors, compounds that target cancer antigens or the inhibitory Fc receptor FcyRllb (CD32b).
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公开(公告)号：US12071429B2
公开(公告)日：2024-08-27
申请号：US17164045
申请日：2021-02-01
发明人： Gianni Chessari , Steven Howard , Ildiko Maria Buck , Benjamin David Cons , Christopher Norbert Johnson , Rhian Sara Holvey , David Charles Rees , Jeffrey David St. Denis , Emiliano Tamanini , Bernard Thomas Golding , Ian Robert Hardcastle , Celine Florence Cano , Duncan Charles Miller , Martin Edward Mäntylä Noble , Roger John Griffin , James Daniel Osborne , Joanne Peach , Arwel Lewis , Kim Louise Hirst , Benjamin Paul Whittaker , David Wyn Watson , Dale Robert Mitchell
IPC分类号： C07D405/14 , A61K31/4035 , A61P35/00 , C07D209/48 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/06 , C07D413/12 , C07F9/572
CPC分类号： C07D405/14 , A61K31/4035 , A61P35/00 , C07D209/48 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/06 , C07D413/12 , C07F9/5728 , C07B2200/05
摘要： The invention provides a compound of formula (I):
or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims.
Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.-
3.发明公开公开(公告)号：US20240254110A1
公开(公告)日：2024-08-01
申请号：US18461253
申请日：2023-09-05
发明人： Keith Jones , Carl Rye , Nicola Chessum , Matthew D. Cheeseman , Adele E. Pasqua , Kurt G. Pike , Paul F. Faulder
IPC分类号： C07D405/12 , C07D319/18 , C07D405/14 , C07D407/12 , C07D409/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/08 , C07D491/056
CPC分类号： C07D405/12 , C07D319/18 , C07D405/14 , C07D407/12 , C07D409/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/08 , C07D491/056
摘要： The present invention relates to compounds of formula I wherein A1, A2 R4 and Q are as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
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公开(公告)号：US20240132504A1
公开(公告)日：2024-04-25
申请号：US18312069
申请日：2023-05-04
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity:
wherein HET, bonds a, b, c and d, X1, X2, X3, X4, R2, and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.-
公开(公告)号：US11897877B2
公开(公告)日：2024-02-13
申请号：US17319231
申请日：2021-05-13
发明人： Swen Hoelder , Julian Blagg , Savade Solanki , Hannah Woodward , Sebastien Gaston Andre Naud , Vassilios Bavetsias , Peter Sheldrake , Paolo Innocenti , Kwai-Ming J. Cheung , Butrus Atrash
IPC分类号： C07D471/04 , C07D401/14 , C07D413/14 , C07D401/04 , C07D405/04 , C07D519/00 , A61K31/519
CPC分类号： C07D471/04 , A61K31/519 , C07D401/04 , C07D401/14 , C07D405/04 , C07D413/14 , C07D519/00
摘要： The present invention relates to compounds of formula I
wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.-
公开(公告)号：US11873341B2
公开(公告)日：2024-01-16
申请号：US16979932
申请日：2019-03-13
发明人： Anne Goubier , Beatriz Goyenechea Corzo , Josephine Salimu , Kevin Moulder , Pascal Merchiers , Sergio Quezada
IPC分类号： C07K16/28 , A61P35/02 , C12N15/85 , A61P35/00 , A61K39/395 , C07K14/55 , A61K45/06 , A61K39/00 , C07K14/05
CPC分类号： C07K16/2866 , A61K39/39533 , A61K39/39541 , A61K39/39558 , A61K39/39566 , A61K45/06 , A61P35/00 , A61P35/02 , C07K14/05 , C07K16/2818 , C07K16/2827 , C12N15/85 , A61K2039/505 , A61K2039/507 , C07K2317/20 , C07K2317/21 , C07K2317/24 , C07K2317/31 , C07K2317/32 , C07K2317/33 , C07K2317/34 , C07K2317/40 , C07K2317/41 , C07K2317/52 , C07K2317/54 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/567 , C07K2317/569 , C07K2317/60 , C07K2317/622 , C07K2317/73 , C07K2317/732 , C07K2317/74 , C07K2317/76 , C07K2317/92 , C12N2015/8518
摘要： The present disclosure provides antibody sequences found in antibodies that bind to human CD25, in particular an anti CD25-a-674 antibody which do not block the binding of CD25 to IL-2 or IL-2 signalling. The claimed antibody binds to the epitopes: YQCVQGYRALHRGP (150 to 163) or SVCKMTHGKTRWTQP (166 to 180) on CD25 Antibodies and antigen-binding portions thereof including such sequences can be used in pharmaceutical compositions and methods of treatment, in particular for treating cancer.
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公开(公告)号：US20240011037A1
公开(公告)日：2024-01-11
申请号：US18254324
申请日：2021-11-24
发明人： Monika Gullerova
IPC分类号： C12N15/113 , C12N9/22 , A61P35/00
CPC分类号： C12N15/1135 , C12N9/22 , C12Y301/26003 , A61P35/00 , C12N2310/531 , C12N2310/14 , C12N2320/31
摘要： The present invention relates to a method of inhibiting expression of a gene in a biological system. The method of the present invention comprises introducing a tRNA-derived polynucleotide into the biological system. The tRNA-derived polynucleotide of 5 the present invention comprises a sequence that is complementary to an intronic region or exonic region of the gene whose expression is to be inhibited.
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公开(公告)号：US11753405B2
公开(公告)日：2023-09-12
申请号：US17231164
申请日：2021-04-15
IPC分类号： C07D417/14
CPC分类号： C07D417/14
摘要： A compound of Formula (I):
or a pharmaceutically acceptable salt thereof, where: Q can be 1,2,4-triazin-3-yl, pyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R1 can be hydrogen, methoxy, trifluoromethoxy, oxetan-3-yl, 3-fluoroazetidin-1-yl, 3-methoxyazetidin-1-yl, or 3,3-difluoroazetidin-1-yl; R2 can be hydrogen or fluoro; R3 can be hydrogen or methoxy; and R4 can be methoxy, ethoxy, or methoxymethyl; provided that when R1 is hydrogen, methoxy or trifluoromethoxy, then R3 is not hydrogen, and/or R4 is methoxymethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.-
公开(公告)号：US11697688B2
公开(公告)日：2023-07-11
申请号：US16979935
申请日：2019-03-13
发明人： Anne Goubier , Beatriz Goyenechea Corzo , Josephine Salimu , Kevin Moulder , Pascal Merchiers , Mark Brown , James Geoghegan , Bianka Prinz , Sergio Quezada
IPC分类号： C07K16/28 , A61P35/02 , C12N15/85 , A61P35/00 , A61K39/395 , C07K14/55 , A61K45/06 , A61K39/00
CPC分类号： C07K16/2866 , A61K39/39533 , A61K39/39541 , A61K39/39558 , A61K39/39566 , A61K45/06 , A61P35/00 , A61P35/02 , C07K14/55 , C07K16/2818 , C07K16/2827 , C12N15/85 , A61K2039/505 , A61K2039/507 , C07K2317/20 , C07K2317/21 , C07K2317/24 , C07K2317/31 , C07K2317/32 , C07K2317/33 , C07K2317/34 , C07K2317/40 , C07K2317/41 , C07K2317/52 , C07K2317/54 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/567 , C07K2317/569 , C07K2317/60 , C07K2317/622 , C07K2317/73 , C07K2317/732 , C07K2317/74 , C07K2317/76 , C07K2317/92 , C12N2015/8518
摘要： The present disclosure provides antibody sequences found in antibodies that bind to human CD25, in particular an anti CD25-a-674 antibody which do not block the binding of CD25 to IL-2 or IL-2 signalling. The claimed antibody binds to the epitopes: QCVQGYRA and RWTQPQLICTG on CD25 Antibodies and antigen-binding portions thereof including such sequences can be used in pharmaceutical compositions and methods of treatment, in particular for treating cancer.
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公开(公告)号：US11680068B2
公开(公告)日：2023-06-20
申请号：US17738278
申请日：2022-05-06
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity:
wherein HET, bonds a, b, c and d, X1, X2, X3, X4, R2, and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.
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