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公开(公告)号：US20240174605A1
公开(公告)日：2024-05-30
申请号：US18279985
申请日：2022-03-01
发明人： Yanan ZHANG , Dehui ZHANG
IPC分类号： C07C311/37 , A61K31/167 , A61K31/18 , A61K31/381 , A61K31/40 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4439 , A61K31/444 , A61K31/4453 , A61K31/4545 , A61K31/496 , A61P25/28 , C07C237/42 , C07D213/40 , C07D213/75 , C07D213/76 , C07D213/81 , C07D213/82 , C07D277/56 , C07D295/16 , C07D333/38 , C07D401/12 , C07D417/12
CPC分类号： C07C311/37 , A61K31/167 , A61K31/18 , A61K31/381 , A61K31/40 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4439 , A61K31/444 , A61K31/4453 , A61K31/4545 , A61K31/496 , A61P25/28 , C07C237/42 , C07D213/40 , C07D213/75 , C07D213/76 , C07D213/81 , C07D213/82 , C07D277/56 , C07D295/16 , C07D333/38 , C07D401/12 , C07D417/12 , C07C2601/02
摘要： The present disclosure provides novel arylsulfonamide compounds as embodiments of the present disclosure. The compounds are believed to be orexin receptor agonists, useful for the treatment of diseases and conditions caused by reduced activity of orexin.
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公开(公告)号：US20230348373A1
公开(公告)日：2023-11-02
申请号：US17626061
申请日：2020-07-10
发明人： Sol J. Barer , Yanchao Xin , Yaping Hong , Gang Zhou
IPC分类号： C07C323/52 , C07C323/41 , C07D295/16 , A61P35/00
CPC分类号： C07C323/52 , A61P35/00 , C07C323/41 , C07D295/16 , C07B2200/05
摘要： The invention provides new deuterated derivatives of 6,8-bis(benzylsulfanyl)octanoic acid, pharmaceutical compositions thereof, and methods for treating cancer with the new compositions.
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3.发明申请公开(公告)号：US20180327374A1
公开(公告)日：2018-11-15
申请号：US15774157
申请日：2016-11-07
申请人： Michael T. RUDD , Edward J. BRNARDIC , Yuntae KIM , Robert S. MEISSNER , Vanessa RADA , Shawn J. STACHEL , Celina V. ZERBINATTI , Merck Sharp & Dohme Corp.
发明人： Michael T. Rudd , Edward J. Brnardic , Yuntae Kim , Robert S. Meissner , Vanessa L. Rada , Shawn J. Stachel , Celina V. Zerbinatti
IPC分类号： C07D295/16 , C07D243/08 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/08 , C07D487/08 , C07D513/04 , A61P25/28 , A61P25/18 , A61P25/16 , A61P3/10
CPC分类号： C07D295/16 , A61K31/496 , A61P3/10 , A61P25/16 , A61P25/18 , A61P25/28 , C07D213/74 , C07D213/85 , C07D243/08 , C07D295/192 , C07D295/205 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08 , C07D487/08 , C07D487/18 , C07D513/04 , C07D515/04
摘要： In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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公开(公告)号：US10058550B2
公开(公告)日：2018-08-28
申请号：US15629567
申请日：2017-06-21
申请人： AMGEN INC.
发明人： Ning Chen , Xiaoqi Chen , Yinhong Chen , Zice Fu , Julie Anne Heath , Daniel B. Horne , Matthew R. Kaller , Aarif Yusuf Khakoo , David John Kopecky , Zhihua Ma , Jeffrey T. Mihalic , Gayathri Swaminath , Xiaodong Wang , Wen-Chen Yeh
IPC分类号： A61K31/506 , A61K31/497 , A61K45/06
CPC分类号： C07D401/14 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
摘要： Methods of treating heart failure include administering to a subject having heart failure an effective amount of a triazole compound that is an agonist of the APJ receptor, a pharmaceutically acceptable salt of the compound, or a mixture thereof. Compounds particularly useful in such methods are provided herein.
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公开(公告)号：US20180162812A1
公开(公告)日：2018-06-14
申请号：US15891304
申请日：2018-02-07
申请人： Araxes Pharma LLC
发明人： Pingda Ren , Yi Liu , Liansheng Li , Jun Feng , Tao Wu
IPC分类号： C07D205/04 , G01N33/58 , C07D213/74 , C07D401/04 , C07D295/16 , C07D487/04 , C07D213/64 , C07D211/62 , C07D487/10 , C07D403/12 , C07D211/60 , C07D211/58 , C07D211/56 , C07D285/16 , C07D471/04 , C07D419/12 , C07D405/06 , C07D403/06 , C07D237/04 , C07D403/04 , C07D401/12 , C07D231/40 , C07D285/14
CPC分类号： C07D205/04 , C07D211/56 , C07D211/58 , C07D211/60 , C07D211/62 , C07D213/64 , C07D213/74 , C07D231/40 , C07D237/04 , C07D285/14 , C07D285/16 , C07D295/16 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D419/12 , C07D471/04 , C07D487/04 , C07D487/10 , G01N33/58
摘要： Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
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公开(公告)号：US09926267B2
公开(公告)日：2018-03-27
申请号：US14933734
申请日：2015-11-05
申请人： Araxes Pharma LLC
发明人： Pingda Ren , Yi Liu , Liansheng Li , Jun Feng , Tao Wu
IPC分类号： C07D205/04 , C07D403/04 , A61K31/496 , C07D487/10 , C07D211/62 , C07D213/64 , C07D487/04 , C07D295/16 , C07D401/04 , C07D285/14 , G01N33/58 , C07D213/74 , C07D231/40 , C07D401/12 , C07D237/04 , C07D403/06 , C07D405/06 , C07D419/12 , C07D471/04 , C07D285/16 , C07D211/56 , C07D211/58 , C07D211/60 , C07D403/12
CPC分类号： C07D205/04 , C07D211/56 , C07D211/58 , C07D211/60 , C07D211/62 , C07D213/64 , C07D213/74 , C07D231/40 , C07D237/04 , C07D285/14 , C07D285/16 , C07D295/16 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D419/12 , C07D471/04 , C07D487/04 , C07D487/10 , G01N33/58
摘要： Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
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公开(公告)号：US09884812B2
公开(公告)日：2018-02-06
申请号：US15124748
申请日：2015-03-12
发明人： Andrew Easton , Phillip Gould , Andrew Marsh
IPC分类号： A61K31/535 , C07C275/30 , C07C275/42 , C07C275/40 , C07C323/44 , C07D213/75 , C07C317/42 , C07D239/42 , C07D295/16 , G01N33/573 , G01N33/53 , A61K31/5375
CPC分类号： C07C275/30 , A61K31/17 , A61K31/4402 , A61K31/505 , A61K31/5375 , C07C275/34 , C07C275/40 , C07C275/42 , C07C317/42 , C07C323/36 , C07C323/44 , C07C335/16 , C07C2601/14 , C07D213/72 , C07D213/75 , C07D239/42 , C07D295/16 , C12Q1/18 , C12Y306/04013 , G01N33/5308 , G01N33/56983 , G01N33/573 , G01N2333/135 , G01N2333/914 , G01N2500/02
摘要： The invention relates to a DDX3X inhibitor for use in the treatment of pneumovirus infection in a mammal, wherein the DDX3X inhibitor may be a compound of Formula (I) wherein y, Z, R1, X, L, Ra and Rb are as defined herein. The invention also relates to compounds of Formula (I).
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公开(公告)号：US09751864B2
公开(公告)日：2017-09-05
申请号：US15298434
申请日：2016-10-20
申请人： AMGEN INC.
发明人： Ning Chen , Xiaoqi Chen , Richard V. Connors , Jeffrey Deignan , Paul John Dransfield , Xiaohui Du , Zice Fu , Julie Anne Heath , Daniel B. Horne , Jonathan Houze , Matthew R. Kaller , David John Kopecky , Su-Jen Lai , Zhihua Ma , Lawrence R. McGee , Julio C. Medina , Jeffrey T. Mihalic , Nobuko Nishimura , Steven H. Olson , Vatee Pattaropong , Xiaodong Wang , Kevin Yang , Mikkel V. DeBenedetto , Robert P. Farrell , Simon J. Hedley , Ted C. Judd
IPC分类号： C07D401/04 , C07D401/14 , C07D417/14 , C07D471/04 , C07D413/14 , C07D413/04 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K45/06 , C07B57/00 , C07B59/00 , C07D211/54 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D241/12 , C07D241/24 , C07D249/08 , C07D405/14 , C07D401/12 , A61K31/695 , C07F7/08 , A61K31/437 , C07C311/13 , C07D213/61 , C07D239/34 , C07D241/18 , C07D295/16
CPC分类号： A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
摘要： Methods of preparing compounds of Formula VI, salts thereof, tautomers thereof, or salts of the tautomers include cyclizing compounds of Formula V, salts thereof, tautomers thereof, or salts of the tautomers. Compounds of Formula VI and Formula V have the following structures: where the definitions of the variables are provided herein.
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9.发明申请公开(公告)号：US20170246164A1
公开(公告)日：2017-08-31
申请号：US15457782
申请日：2017-03-13
发明人： Zhou Wang , Joel Byron Nelson , Minh Bao Nguyen , John S. Lazo , Paul A. Johnston , Peter Wipf
IPC分类号： A61K31/496 , A61K31/495 , A61K31/4188
CPC分类号： A61K31/496 , A61K31/407 , A61K31/4188 , A61K31/495 , A61K31/4965 , A61K31/58 , A61K45/06 , C07D235/02 , C07D241/04 , C07D261/04 , C07D261/08 , C07D295/16 , C07D401/04 , C07D403/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/08 , C07D487/04 , A61K2300/00
摘要： A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from: (a) a phenyl-substituted imidazole, or a pharmaceutically acceptable salt or ester thereof; or (b) a compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; R21 is an alkanediyl or a substituted alkanediyl; a is 0 or 1; c is 0 or 1; X is C or S; R22 is a moiety that includes at least one divalent amino radical; and R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group.
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公开(公告)号：US09718770B2
公开(公告)日：2017-08-01
申请号：US15105426
申请日：2014-12-18
发明人： Wu Zhong , Song Li , Yanqun Zeng , Junhai Xiao , Xinbo Zhou , Zhibing Zheng , Xingzhou Li , Xiaokui Wang
IPC分类号： A61K31/155 , A61K31/17 , C07C335/04 , C07C391/00 , C07D213/75 , C07C335/08 , C07C335/14 , C07C335/16 , C07C335/18 , C07D295/16 , C07C335/20 , C07D211/06
CPC分类号： C07C391/00 , C07C335/08 , C07C335/14 , C07C335/16 , C07C335/18 , C07C335/20 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07D211/06 , C07D213/75 , C07D295/16
摘要： The invention provides a compound of Formula I, an isomer, a pharmaceutically acceptable salt, or a solvate thereof, and use thereof in manufacture of a medicament for preventing and/or treating a drug-resistant tumor or disease or disorder caused by a drug-resistant bacterium, or use thereof in manufacture of a medicament for preventing and/or treating a tumor, a neurodegenerative disease, an allogeneic graft rejection, or an infection-associated disease or disorder; preferably, the tumor, neurodegenerative disease, allogeneic graft rejection, or infection-associated disease or disorder is a disease or disorder caused by Heat shock protein 70 (Hsp70). The compounds of the invention, which are a class of Hsp70 inhibitors having a novel structure and a high activity, solve the problem concerning drug resistance of tumors, enhance the effect of treating tumors, and provide a new medical strategy for treatment of tumors in clinic.
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