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公开(公告)号:US11583526B2
公开(公告)日:2023-02-21
申请号:US16998900
申请日:2020-08-20
发明人: Vijaykumar Reddy Rajasekhar , Brendan Mark Johnson , David B. MacLean , Lynn Seely , Paul N. Mudd, Jr.
IPC分类号: A61K31/517 , A61K31/4164 , A61P35/00 , A61K31/501 , A61K31/513 , A61K9/00 , A61K31/4166
摘要: Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof. Another method includes: administering once-daily to the subject in need thereof, an oral load dose formulation having from 240 mg to 480 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof; and thereafter administering once-daily to the subject, an oral maintenance dose formulation having 80 mg to 160 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.
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公开(公告)号:US20230028114A1
公开(公告)日:2023-01-26
申请号:US17753803
申请日:2020-09-15
申请人: Holger MONENSCHEIN , Sean MURPHY , Scott OLSEN , Natasha O'ROURKE , Holly REICHARD , Melinda DAVIS , Betty LAM , TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人: Holger MONENSCHEIN , Sean MURPHY , Scott OLSEN , Natasha O'ROURKE , Holly REICHARD , Melinda DAVIS , Betty LAM
IPC分类号: A61K31/5025 , C07D471/04
摘要: Disclosed are compounds of Formula (1) and pharmaceutically acceptable salts thereof, wherein α, β, n, R4, R5, R6, R8, R9, R10, R11, X1, X2, X3 and X7 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula (1), to pharmaceutical compositions comprising them, and to their use for treating diseases, disorders, and conditions associated with GPR139.
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公开(公告)号:US11560372B2
公开(公告)日:2023-01-24
申请号:US16606043
申请日:2018-04-17
发明人: Shinobu Sasaki , Masaki Seto , Kazuaki Takami , Haruhi Ando
IPC分类号: C07D405/14 , A61P1/10 , C07D405/04 , C07D409/14
摘要: The present invention aims to provide a compound that may be useful for the prophylaxis or treatment of constipation and the like. The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the specification, salt thereof.
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公开(公告)号:US20230000915A1
公开(公告)日:2023-01-05
申请号:US17778611
申请日:2020-11-24
发明人: Shin KANEKO , Suguru ARIMA , Maiko TAKIGUCHI , Yoshiaki KASSAI , Akira HAYASHI
IPC分类号: A61K35/17 , C12N5/0783 , C12N15/62 , C12N15/86 , C07K14/725 , C07K14/705 , A61P35/00
摘要: The present invention provides a system for providing a T cell product, including a T cell master cell bank and/or a T cell working cell bank.
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公开(公告)号:US20220411752A1
公开(公告)日:2022-12-29
申请号:US17773467
申请日:2020-10-30
发明人: Shin KANEKO , Hisashi YANO , Tokuyuki SHINOHARA
IPC分类号: C12N5/0783 , C12N15/90
摘要: Provided is an excellent method for producing an IL-4 non-secreting and IFN-γ secreting (Th1-type) or IFN-γ non-secreting and IL-4 secreting (Th2-type) CD4 single-positive T cell (CD4SP T cell). The method for producing the Th1-type or Th2-type CD4SP T cell of the present invention comprises a step of inducing a CD4 single-positive T cell from a hematopoietic stem cell (HSC) and/or a hematopoietic progenitor cell (HPC) substantially defective in a factor involved in IL-4 secretion or a factor involved in IFN-γ secretion.
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公开(公告)号:US20220411413A1
公开(公告)日:2022-12-29
申请号:US17872680
申请日:2022-07-25
发明人: Masami YAMADA , Shinkichi SUZUKI , Takahiro SUGIMOTO , Minoru NAKAMURA , Hiroki SAKAMOTO , Makoto KAMATA
IPC分类号: C07D405/14 , C07D209/46 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D401/06 , C07D405/04 , A61K31/4035 , A61K31/4155 , A61K31/4439 , A61K31/13 , A61K31/325 , A61K31/445 , A61K31/55 , A61K31/045 , A61K31/4406
摘要: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like.
The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the specification, or a salt thereof.-
公开(公告)号:US20220409734A1
公开(公告)日:2022-12-29
申请号:US17610391
申请日:2020-05-08
发明人: Dylan Bradley ENGLAND , Steve P. LANGSTON , Hong Myung LEE , Liting MA , Zhan SHI , Stepan VYSKOCIL , Jianing WANG , He XU , Yutaka NISHIMOTO , Yumiko ISHII
摘要: The present disclosure provides antibody drug conjugates comprising STING modulators. Also provided are compositions comprising the antibody drug conjugates. The compounds and compositions are useful for stimulating an immune response in a subject in need thereof. Formula (I):
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公开(公告)号:US20220401443A1
公开(公告)日:2022-12-22
申请号:US17866203
申请日:2022-07-15
发明人: Vijaykumar Reddy RAJASEKHAR , Brendan Mark JOHNSON , David B. MACLEAN , Lynn SEELY , Paul N. MUDD, JR.
IPC分类号: A61K31/501 , A61P35/00 , A61K31/513 , A61K9/00 , A61K31/4166
摘要: Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof. Another method includes: administering once-daily to the subject in need thereof, an oral load dose formulation having from 240 mg to 480 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof; and thereafter administering once-daily to the subject, an oral maintenance dose formulation having 80 mg to 160 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.
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公开(公告)号:US11524957B2
公开(公告)日:2022-12-13
申请号:US17044366
申请日:2019-04-01
发明人: Lei Zhu , John Daniel Bailey , Landon Durak , Joshua David Waetzig , Masahiro Mizuno , Kazuhiro Maeda , Tsuneo Yasuma , Hiroshi Yamaguchi , Koichiro Fukuoka , Kazuyuki Akiyama
IPC分类号: C07D453/02 , C07D409/04
摘要: The present invention provides processes and synthetic intermediates for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4 {3H)-one or a salt, hydrate, or tautomer thereof, or any combination thereof, which are Cdc7 kinase inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with Cdc7 activity.
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公开(公告)号:US20220331303A1
公开(公告)日:2022-10-20
申请号:US17642337
申请日:2020-09-12
IPC分类号: A61K31/445 , A61P25/26 , A61K45/06
摘要: Described herein are methyl 3-((methylsulfonyl)amino)-2-(((4-phenylcyclohexyl)oxy)methyl)-piperidine-1-carboxylate (Compound (I)), compositions comprising Compound (I), and the use of Compound (I) for the treatment of excessive sleepiness in a subject in need thereof.
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