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公开(公告)号:US11478438B2
公开(公告)日:2022-10-25
申请号:US16787052
申请日:2020-02-11
发明人: Zhiyuan Zhang , Xiaodong Wang , Yaning Su , Hanying Ruan , Yan Ren
IPC分类号: A61K31/165 , A61K31/10 , A61K31/167 , C07C233/01 , C07C235/38 , C07D231/02 , C07D263/04 , C07D205/04 , C07D265/30 , C07D207/12 , C07D211/70 , C07D231/04 , C07D231/08 , C07D233/38 , C07D405/04 , C07D409/04 , C07D241/04 , C07D417/04 , C07D261/02 , C07D263/22 , C07D203/18 , C07D205/08 , C07D207/06 , C07D207/08 , C07D207/20 , C07D207/24 , C07D207/27 , C07D207/333 , C07D211/16 , C07D211/82 , G01C19/5649 , G01C19/5747
摘要: The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
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公开(公告)号:US20220071935A1
公开(公告)日:2022-03-10
申请号:US17321928
申请日:2021-05-17
IPC分类号: A61K31/18 , C07D237/02 , C07D307/52 , C07D233/02 , C07D261/02 , C07D275/02 , C07D295/084 , C07D231/04 , C07D239/04 , C07C311/39 , C07D211/44 , C07D265/30 , C07D277/04 , C07D241/04 , C07D279/12 , C07D263/04 , A61K31/4355
摘要: The present invention provides bumetanide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide analogs and methods for their use. These analogs are believed useful for the treatment and/or prophylaxis of conditions that involve the Na+K+Cl− co-transporter or GABAA receptor.
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公开(公告)号:US20220016613A1
公开(公告)日:2022-01-20
申请号:US17276855
申请日:2019-09-19
发明人: Theodore Alexander Betley , Alexandre Mikhailine , Claudia Kleinlein , Yuyang Dong , Yunjung Baek
IPC分类号: B01J31/18 , B01J31/22 , C07D471/08 , C07D471/04 , C07D207/06 , C07D211/70 , C07D263/04 , C07D401/04 , C07D209/54 , C07D487/08 , C07D403/04 , C07D209/04 , C07D209/44
摘要: Disclosed are compounds, methods, reagents, systems, and kits for the preparation and utilization of monomeric or polymeric metal-based compounds. These metal-based compounds are organometallic catalysts composed of substituted dipyrrin ligands bound to transition metals. C—H bond functionalization catalysis can be performed with the disclosed organometallic catalysts to yield C—N bonds to generate substituted bicyclic, spiro, and fused nitrogen-containing heterocycles, all common motifs in various pharmaceutical and bioactive molecules.
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公开(公告)号:US20210206787A1
公开(公告)日:2021-07-08
申请号:US17207388
申请日:2021-03-19
发明人: Barbara SLUSHER , Rana RAIS , Lukas TENORA , Pavel MAJER , Andrej JANCARIK
IPC分类号: C07F9/24 , C07D209/18 , A61K31/404 , C07D317/40 , C07C227/14 , C07F9/6561 , C07C271/22 , C07C245/18 , C07D473/34 , C07D209/20 , C07D211/90 , C07H15/203 , C07H19/207 , C07D263/18 , A61P35/00 , C07D263/04 , C07D309/10 , C07D317/38 , C07K5/062 , C07K5/078 , C07K5/083
摘要: The disclosure provides compounds having formula (I): and the pharmaceutically acceptable salts thereof, wherein R1, R2, R2′, and X are as defined as set firth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.
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公开(公告)号:US20210078947A1
公开(公告)日:2021-03-18
申请号:US16702286
申请日:2019-12-03
发明人: Jean-Christophe ANDREZ , Philippe BERGERON , Paul Robert BICHLER , Sultan CHOWDHURY , Christoph Martin DEHNHARDT , Thilo FOCKEN , Wei GONG , Michael Edward GRIMWOOD , Abid HASAN , Ivan William HEMEON , Qi JIA , Brian Salvatore SAFINA , Shaoyi SUN , Michael Scott WILSON , Alla Yurevna ZENOVA
IPC分类号: C07D207/16 , C07D403/12 , C07D413/14 , C07D221/22 , C07D401/12 , C07D413/12 , C07C235/52 , C07D205/04 , C07D277/06 , C07D209/02 , C07D305/08 , C07D401/14 , C07D231/06 , C07D403/04 , C07D403/14 , C07D409/06 , C07D417/12 , C07D451/02 , C07D263/04 , C07D263/26 , C07C235/42 , C07C235/54 , C07D265/30 , C07D207/08 , C07D207/10 , C07D207/22 , C07D209/52 , C07D209/54 , C07D211/20 , C07D211/38 , C07D211/60 , C07D213/69 , C07D401/10 , C07D405/10 , C07D471/08
摘要: The invention provides compounds having the general Formula (I); and pharmaceutically acceptable salts thereof; wherein the variables RA, RAA, subscript n, subscript q, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, D and E have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
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公开(公告)号:US10738066B2
公开(公告)日:2020-08-11
申请号:US16454880
申请日:2019-06-27
发明人: Barbara Slusher , Rana Rais , Lukas Tenora , Pavel Majer , Andrej Jancarik
IPC分类号: C07D209/18 , C07F9/24 , A61K31/404 , C07D317/40 , C07C227/14 , C07F9/6561 , C07C271/22 , C07C245/18 , C07D473/34 , C07D209/20 , C07D211/90 , C07H15/203 , C07H19/207 , C07D263/18 , A61P35/00 , C07D263/04 , C07D309/10 , C07D317/38 , C07K5/062 , C07K5/078 , C07K5/083 , A61K38/00
摘要: The disclosure provides compounds having formula (I): and the pharmaceutically acceptable salts thereof, wherein R1, R2, R2′, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.
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公开(公告)号:US10555920B2
公开(公告)日:2020-02-11
申请号:US16153706
申请日:2018-10-06
发明人: Zhiyuan Zhang , Xiaodong Wang , Yaning Su , Hanying Ruan , Yan Ren
IPC分类号: A61K31/10 , A61K31/165 , A61K31/167 , C07D263/04 , C07D265/30 , C07D207/12 , C07D211/70 , C07D231/04 , C07D231/08 , C07D233/38 , C07D405/04 , C07D409/04 , C07D241/04 , C07D417/04 , C07D261/02 , C07D263/22 , C07D203/18 , C07D205/08 , C07D207/06 , C07D207/08 , C07D207/20 , C07D207/24 , C07D207/27 , C07D207/333 , C07D211/16 , C07D211/82 , C07D231/02 , C07C233/01 , C07C235/38 , C07D205/04
摘要: The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
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公开(公告)号:US09890177B2
公开(公告)日:2018-02-13
申请号:US14920156
申请日:2015-10-22
IPC分类号: C07D498/10 , A01N43/76 , A01N43/90 , C07C201/08 , C07C201/12 , C07C205/02 , C07C205/06 , C07C205/18 , C07C215/08 , C07C215/42 , C07C239/10 , C07D263/04 , C07D263/52 , C07D498/04 , C08G18/32 , C07C205/04 , C07C205/05 , C07C205/15 , C07C205/16 , C07C215/20 , C07C215/28
CPC分类号: C07D498/10 , A01N43/76 , A01N43/90 , C07C201/08 , C07C201/12 , C07C205/02 , C07C205/04 , C07C205/05 , C07C205/06 , C07C205/15 , C07C205/16 , C07C205/18 , C07C215/08 , C07C215/20 , C07C215/28 , C07C215/42 , C07C239/10 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D263/04 , C07D263/52 , C07D498/04 , C08G18/3271 , Y02P20/582
摘要: Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compounds, as well as novel nitrated compounds and derivatives, and methods of using the derivatives in various applications.
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公开(公告)号:US20170283402A1
公开(公告)日:2017-10-05
申请号:US15515773
申请日:2015-09-30
发明人: Alexei Tulin
IPC分类号: C07D405/14 , C07D207/06 , C07D263/04 , C07D405/06 , C07D317/28 , C07D319/06 , C07D295/15 , C07D317/72
CPC分类号: C07D405/14 , A61P35/00 , C07D207/06 , C07D263/04 , C07D295/15 , C07D317/28 , C07D317/72 , C07D319/06 , C07D405/06 , C07D407/04
摘要: Compounds that are not related to NAD, and which target PARP1-histone H4 interaction are provided, as well as compositions of these compounds, and methods for specific inhibition of poly(ADP-ribose) polymerase 1 (PARP-1) using these compounds are provided. These PARP-1 inhibitors may be used to treat cancer in which PARP-1 activation or biologic activity plays a role, including prostate cancer, breast cancer, kidney cancer, ovarian cancer, lymphoma, leukemia, and glioblastoma, among others.
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公开(公告)号:US09665002B2
公开(公告)日:2017-05-30
申请号:US14930869
申请日:2015-11-03
IPC分类号: G03F7/039 , G03F7/004 , G03F7/30 , G03F7/32 , G03F7/38 , G03F7/20 , C07D263/04 , C07D233/02 , C07D277/04 , C07D207/04 , C07D279/12 , C07D295/112 , C07D203/14 , C07D241/04 , C07D225/02 , C07D223/04 , C07D211/06 , C07D205/04 , C07D265/30 , C07D295/155 , C07D213/79 , C07D295/26 , C07C381/12 , G03F7/16 , C07C25/00 , C07C69/78 , C07C69/76 , C07C25/02
CPC分类号: G03F7/0397 , C07C25/00 , C07C25/02 , C07C69/76 , C07C69/78 , C07C381/12 , C07D203/14 , C07D205/04 , C07D207/04 , C07D211/06 , C07D213/79 , C07D223/04 , C07D225/02 , C07D233/02 , C07D241/04 , C07D263/04 , C07D265/30 , C07D277/04 , C07D279/12 , C07D295/112 , C07D295/155 , C07D295/26 , G03F7/0045 , G03F7/0046 , G03F7/11 , G03F7/168 , G03F7/2037 , G03F7/2041 , G03F7/30 , G03F7/322 , G03F7/325 , G03F7/38
摘要: Sulfonium and iodonium salts of a carboxylate having an aromatic ring to which a nitrogen-containing alkyl or cyclic structure is attached are novel. The onium salt functions as an acid diffusion controlling agent in a resist composition, enabling to form a pattern of good profile with high resolution, improved MEF, LWR and DOF.
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