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公开(公告)号：US10562878B2
公开(公告)日：2020-02-18
申请号：US15836261
申请日：2017-12-08
发明人： Liming Shao , Fengjiang Wang , Scott Christopher Malcolm , Michael Charles Hewitt , Larry R. Bush , Jianguo Ma , Mark A. Varney , Una Campbell , Sharon Rae Engel , Larry Wendell Hardy , Patrick Koch , John E. Campell
IPC分类号： C07D333/20 , C07C211/17 , C07C211/40 , C07C215/42 , C07C215/44 , C07C217/52 , C07C217/74 , C07C323/32 , C07D207/06 , C07D207/08 , C07D211/14 , C07D265/14 , C07D277/28 , C07D295/06 , C07D307/52 , C07D317/58 , C07D317/72 , C07D319/06 , C07D491/056 , C07C211/29 , C07D211/16
摘要： The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
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公开(公告)号：US10526287B2
公开(公告)日：2020-01-07
申请号：US15567978
申请日：2016-04-22
发明人： Brian K. Albrecht , James Edmund Audia , Alexandre Côté , Martin Duplessis , Victor S. Gehling , Jean-Christophe Harmange , Rishi G. Vaswani
IPC分类号： C07D211/22 , C07D211/26 , C07D309/20 , C07D215/44 , C07D317/28 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/04 , C07D239/30 , C07C215/44 , C07D417/06 , C07D263/32 , C07D205/12 , C07D207/32 , C07D211/36 , C07D213/64 , C07D305/06 , C07C255/58 , C07C211/09 , C07C211/36 , C07C211/40 , C07C215/14 , C07C217/08 , C07C229/10 , C07C229/38 , C07C229/46 , C07C233/41 , C07C237/06 , C07C255/24 , C07C215/42 , C07C255/30 , C07D211/58 , C07D211/76 , C07D213/38 , C07D213/69 , C07D213/73 , C07D295/195 , A61P35/00
摘要： Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with LSD1. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with LSD1.
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公开(公告)号：US20190233377A1
公开(公告)日：2019-08-01
申请号：US16379487
申请日：2019-04-09
发明人： Kevin Duane Bunker , Chuangxing Guo , Mark Charles Grier , Chad Daniel Hopkins , Joseph Robert Pinchman , Deborah Helen Slee , Peter Qinhua Huang , Mehmet Kahraman
IPC分类号： C07D213/89 , A61K45/06 , C07C317/30 , A61K31/13 , C07C233/14 , C07C233/05 , A61K31/444 , A61K31/27 , A61K31/164 , A61K31/16 , A61K31/145 , C07C211/38 , C07C215/42 , C07C233/06 , C07C233/23 , C07C233/13 , C07C233/09
CPC分类号： C07D213/89 , A61K31/13 , A61K31/145 , A61K31/16 , A61K31/164 , A61K31/27 , A61K31/444 , A61K45/06 , C07C211/38 , C07C215/42 , C07C233/05 , C07C233/06 , C07C233/09 , C07C233/13 , C07C233/14 , C07C233/23 , C07C317/30 , C07C2601/02 , C07C2602/38 , C07C2603/62 , A61K2300/00
摘要： Disclosed herein are compounds of Formulae (I) and (II), methods of synthesizing compounds of Formulae (I) and (II), and methods of using compounds of Formulae (I) and (II) as an analgesic.
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公开(公告)号：US20190076450A1
公开(公告)日：2019-03-14
申请号：US16188444
申请日：2018-11-13
发明人： Alaric J. Dyckman , T.G. Murali Dhar , Hai-Yun Xiao , John L. Gilmore , Michael G. Yang , Zili Xiao , David Marcoux
IPC分类号： A61K31/695 , C07F7/08 , A61K31/505 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/661 , C07F9/09 , C07F9/572 , C07F9/54 , C07C235/46 , C07C323/25 , C07C217/74 , C07C275/26 , C07D213/38 , C07D209/46 , C07C251/44 , C07C251/42 , C07C251/38 , C07C323/29 , C07D241/04 , C07D215/14 , A61K31/135 , C07D213/69 , C07D213/32 , C07C251/54 , C07C219/24 , C07C217/52 , C07D333/16 , C07D319/20 , C07D311/76 , C07D311/58 , C07D309/12 , C07D309/06 , C07D277/24 , C07D239/26 , C07D231/12 , C07D217/24 , C07C317/28 , C07C271/34 , C07C251/52 , C07C233/41 , C07C217/58 , C07C215/42 , C07F9/655 , C07F9/62 , C07D305/08 , C07D241/12 , C07D231/20 , C07D215/12 , C07D213/70
摘要： Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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公开(公告)号：US20190023709A1
公开(公告)日：2019-01-24
申请号：US16129586
申请日：2018-09-12
IPC分类号： C07D473/34 , C07C261/04 , C07D233/60 , C07D213/64 , C07C225/10 , C07C233/23 , C07C233/74 , C07D207/06 , C07D213/38 , C07C35/21 , C07C62/32 , C07C59/46 , C07D307/68 , C07D213/36 , C07D213/30 , C07D213/04 , C07D295/096 , C07C255/31 , C07D209/08 , C07D207/416 , C07D207/335 , C07D207/08 , C07C235/48 , C07C235/46 , C07C235/44 , C07C235/30 , C07C233/60 , C07C233/18 , C07C335/10 , C07D249/08 , C07D241/28 , C07D241/18 , C07C215/52 , C07C215/50 , C07C215/42 , C07D239/34 , C07D235/14 , C07D235/06 , C07C311/04 , C07D233/72 , C07D231/12 , C07C291/04 , C07D317/58 , C07D317/46 , C07C279/08 , C07C275/34 , C07C275/24 , C07C275/10 , C07C35/32 , C07D213/82 , C07D213/81
摘要： Compounds of formula (I): where R1, R2, R3, R4a, R4b, R5, R6 and R7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
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公开(公告)号：US10166249B2
公开(公告)日：2019-01-01
申请号：US15648250
申请日：2017-07-12
发明人： Alaric J. Dyckman , T. G. Murali Dhar , Hai-Yun Xiao , John L. Gilmore , Michael G. Yang , Zili Xiao , David Marcoux
IPC分类号： A61K31/695 , C07C215/42 , C07C217/52 , C07C217/58 , C07C219/24 , C07C233/41 , C07C251/52 , C07C251/54 , C07C271/34 , C07C317/28 , C07D213/32 , C07D213/69 , C07D213/70 , C07D215/12 , C07D217/24 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F7/08 , C07F9/62 , C07F9/655 , A61K31/135 , C07D215/14 , C07D241/04 , C07C323/29 , C07C251/38 , C07C251/42 , C07C251/44 , C07D209/46 , C07D213/38 , C07C275/26 , C07C217/74 , C07C323/25 , C07C235/46 , C07F9/54 , C07F9/572 , C07F9/09 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/661
摘要： Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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公开(公告)号：US20180290976A1
公开(公告)日：2018-10-11
申请号：US15567978
申请日：2016-04-22
发明人： Brian K. Albrecht , James Edmund Audia , Alexandre Côté , Martin Duplessis , Victor S. Gehling , Jean-Christophe Harmange , Rishi G. Vaswani
IPC分类号： C07D211/26 , C07D211/58 , C07C211/40 , C07D213/38 , C07C229/10 , C07D213/73 , C07C255/58 , C07D211/76 , C07D401/06 , C07C215/42 , C07C233/41 , C07C217/08 , C07C237/06 , C07D295/195 , C07C229/38 , C07C255/30 , C07D213/69 , C07D305/06
CPC分类号： C07D211/26 , A61P35/00 , C07B2200/07 , C07C211/09 , C07C211/36 , C07C211/40 , C07C215/14 , C07C215/42 , C07C215/44 , C07C217/08 , C07C229/10 , C07C229/38 , C07C229/46 , C07C233/41 , C07C237/06 , C07C255/24 , C07C255/30 , C07C255/58 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/44 , C07D205/12 , C07D207/32 , C07D211/22 , C07D211/36 , C07D211/58 , C07D211/76 , C07D213/38 , C07D213/64 , C07D213/69 , C07D213/73 , C07D215/44 , C07D239/30 , C07D263/32 , C07D295/195 , C07D305/06 , C07D309/20 , C07D317/28 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/04 , C07D417/06
摘要： Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with LSD1. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with LSD1.
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公开(公告)号：US20180290964A1
公开(公告)日：2018-10-11
申请号：US16008952
申请日：2018-06-14
IPC分类号： C07C215/42
摘要： The present invention is generally directed to methods of using novel crystalline forms of the acetate salt of (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol and pharmaceutical compositions comprising same.
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公开(公告)号：US20180155273A1
公开(公告)日：2018-06-07
申请号：US15885387
申请日：2018-01-31
IPC分类号： C07C215/42
CPC分类号： C07C215/42 , C07B2200/13 , C07C2601/14 , C07C2602/08 , C07C2602/24
摘要： The present invention is generally directed to novel crystalline forms of the acetate salt of (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol and processes for their preparation.
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公开(公告)号：US20180127435A1
公开(公告)日：2018-05-10
申请号：US15860058
申请日：2018-01-02
IPC分类号： C07D498/10 , A01N43/76 , C07C215/28 , C07C205/04 , C07C205/05 , C07C205/15 , C07C205/16 , C07C215/20 , A01N43/90 , C07C201/08 , C07C201/12 , C07C205/02 , C07C205/06 , C07C205/18 , C07C215/08 , C07C215/42 , C07C239/10 , C07D263/04 , C07D263/52 , C08G18/32 , C07D498/04
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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