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公开(公告)号:US20230416266A1
公开(公告)日:2023-12-28
申请号:US18038367
申请日:2021-11-23
IPC分类号: C07D491/052 , A61P35/00
CPC分类号: C07D491/052 , A61P35/00
摘要: The disclosure provides compounds of Formula (I)
or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, CA, R1, R2a, and R2b are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.-
公开(公告)号:US11738010B2
公开(公告)日:2023-08-29
申请号:US17385258
申请日:2021-07-26
发明人: John P. Caldwell , Reynalda De Jesus , Fa-Xiang Ding , Charles J. Gill , Ginny Dai Ho , Sookhee N. Ha , Sandra J. Koseoglu , Marc A. Labroli , Sang Ho Lee , Christina Madsen-Duggan , Mihir Mandal , Terry Roemer , Jing Su , Christopher Michael Tan , Zheng Tan , Haifeng Tang , Hao Wang , Christine Yang , Shu-Wei Yang
IPC分类号: A61K31/4439 , A61P31/04 , A61K31/407 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/431 , A61K31/4375 , A61K31/438 , A61K31/4709 , A61K31/5377 , A61K31/5383 , C07D263/26 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/048 , C07D495/04 , C07D498/04
CPC分类号: A61K31/4439 , A61K31/407 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/431 , A61K31/438 , A61K31/4375 , A61K31/4709 , A61K31/5377 , A61K31/5383 , A61P31/04 , C07D263/26 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/048 , C07D495/04 , C07D498/04
摘要: Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a β-lactam antibiotic.
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公开(公告)号:US20230192876A1
公开(公告)日:2023-06-22
申请号:US17772229
申请日:2020-10-29
发明人: Elliot K. Chartash , Amy M. Beebe , Jason K. Cheung , Konstantin Dobrenkov , Claire H. Li , Richard Wnek
IPC分类号: C07K16/28 , A61P35/00 , A61K39/395 , A61K31/282 , A61K31/519
CPC分类号: C07K16/2878 , A61P35/00 , C07K16/2818 , C07K16/2827 , A61K39/3955 , A61K31/282 , A61K31/519 , A61K2039/505
摘要: The present invention relates to methods of treating cancer by administering an anti-CD27 antibody as a monotherapy or as a part of a combination thereof.
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公开(公告)号:US20230129710A1
公开(公告)日:2023-04-27
申请号:US17913920
申请日:2021-03-25
IPC分类号: C07H1/00 , C07H19/067
摘要: The present invention relates to methods and intermediates for the synthesis of nucleosides and nucleoside analogues (NAs). More specifically, the present invention relates to methods of synthesizing nucleosides and NAs, using simple achiral materials by a ‘one-pot’ proline-catalyzed halogenation of a heteroaryl-substituted acetaldehyde together with a tandem enantioselective aldol reaction followed by a reduction or organometallic addition and cyclization (annulation) reaction involving halide displacement.
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公开(公告)号:US11566051B2
公开(公告)日:2023-01-31
申请号:US16964118
申请日:2019-01-24
发明人: Lan Zhang , Arthur Fridman , Eberhard Durr , Andrew Bett
IPC分类号: C07K14/135 , A61K39/155 , C12N7/00 , A61K39/00
摘要: The disclosure relates to stable RSV F proteins and immunogenic compositions containing the same, as well as methods of using the immunogenic compositions and compositions comprising the RSV F proteins.
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公开(公告)号:US11545270B1
公开(公告)日:2023-01-03
申请号:US16748800
申请日:2020-01-21
摘要: A dossier change control management system periodically ingests data regarding a regulated product from multiple data stores. The dossier change control management system updates dossier data describing a dossier history for the regulated product using the received data. The dossier includes multiple documents in a standardized format and is updated based on a data mapping indicating correspondence between fields of the documents and portions of the received data. An out-of-expectation scenario for the dossier is identified based on regulatory requirements and an alert generated. A report with information about the out-of-expectation scenario is provided for display at a client device based on the alert.
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公开(公告)号:US11542505B1
公开(公告)日:2023-01-03
申请号:US17047271
申请日:2019-04-15
申请人: Merck Sharp & Dohme Corp. , Craig A. Parish , Hongwu Wang , Wonsuk Chang , Quang T. Truong , Tony Siu , Anne Mai Wassermann
发明人: Craig A. Parish , Hongwu Wang , Wonsuk Chang , Quang T. Truong , Tony Siu , Anne Mai Wassermann
IPC分类号: C12N15/113 , C07H21/02
摘要: This invention provides compositions, compounds, and uses thereof, wherein said compounds comprise a single strand oligonucleotide that may form a short oligonucleotide hairpin or stem loop molecule with self complementary base pairing of less than 12 base pairs that bind to RIG-I and activate the RIG-I pathway.
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公开(公告)号:US20220409724A1
公开(公告)日:2022-12-29
申请号:US17772468
申请日:2020-10-28
发明人: Yoichi OZAWA , Yasuhiro FUNAHASHI , Yu KATO
IPC分类号: A61K39/395 , A61P35/00 , A61K31/47 , A61K31/53
摘要: The present disclosure describes a combination therapy comprising an antagonist of Programmed Death 1 receptor (PD-1), a lenvatinib or a pharmaceutically acceptable salt thereof, and (6S,9aS)-N-benzyl-8-({6-[3-(4-ethylpiperazin-1-yl)azetidin-1-yl]pyridin-2-yl}methyl)-6-(2-fluoro-4-hydroxybenzyl)-4,7-dioxo-2-(prop-2-en-1-yl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide (E7386) or a pharmaceutically acceptable salt thereof,—and the use of the combination therapies for the treatment of a cancer.
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9.
公开(公告)号:US20220397570A1
公开(公告)日:2022-12-15
申请号:US17762210
申请日:2020-09-22
发明人: Lee J. Klein , Leia C. Epstein
摘要: An ultraviolet (UV) absorbance assay for measuring the concentration of large RNA molecules such as mRNA in suspensions comprising RNA-lipid nanoparticles (RNA-LNPs) is described.
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公开(公告)号:US20220380469A1
公开(公告)日:2022-12-01
申请号:US17762215
申请日:2020-09-23
发明人: Gursel Aktan , Roger Delemere Dansey , Vassiliki Karantza , Zifang Guo , Jaime A. Mejia , Shu-Chih Su , Jing Zhao , Xuan Zhou
摘要: The present invention relates to methods for treating metastatic triple negative breast cancer in a human patient which has been identified as having a PD-L1 enriched tumor comprising administering, as monotherapy, an anti-PD-1 antibody or antigen binding fragment thereof (e.g., pembrolizumab) in specific amounts to the patient about every three or six weeks, wherein the PD-L1 enriched tumor is a tumor identified as having a CPS score of ≥10.
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