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公开(公告)号：EP2590965B1
公开(公告)日：2016-04-20
申请号：EP11804370.2
申请日：2011-07-07
申请人： Ardelyx, Inc.
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
IPC分类号： C07D403/02 , C07D239/42 , C07D241/20 , A61K45/06 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/59 , A61P13/00 , A61P13/12
CPC分类号： A61K31/5377 , A61K31/497 , A61K31/506 , A61K31/59 , A61K45/06 , C07D239/42 , C07D241/20
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公开(公告)号：EP3390382A1
公开(公告)日：2018-10-24
申请号：EP16822870.8
申请日：2016-12-19
申请人： Ardelyx, Inc.
发明人： LEWIS, Jason G. , LEADBETTER, Michael Robert , CALDWELL, Jeremy , DRAGOLI, Dean , BELL, Noah , JACOBS, Jeffrey W. , FINN, Patricia , JAIN, Rakesh , CHEN, Tao , SIEGEL, Matthew
IPC分类号： C07D401/12 , C07D405/12 , C07D213/38 , A61K31/4418 , A61K31/4427 , A61P3/00 , A61P9/10 , A61P11/06
CPC分类号： C07H15/26 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K31/553 , A61K31/706 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D213/30 , C07D213/38 , C07D213/80 , C07D213/81 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/08 , C07H15/04 , C07H15/18 , C07H15/234
摘要： where R1, R2, R2′, R3, R4, X1, X2, X3, X4, Q, and n are described herein.
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公开(公告)号：EP2590656B1
公开(公告)日：2017-11-15
申请号：EP11834773.1
申请日：2011-07-07
申请人： Ardelyx, Inc.
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
IPC分类号： A61K31/506
CPC分类号： C07D213/81 , A61K31/44 , A61K31/4418 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/59 , A61K31/593 , A61K31/785 , A61K45/06 , C07D213/30 , C07D213/38 , C07D213/50 , C07D213/82 , C07D239/34 , C07D239/42 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14
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公开(公告)号：EP2591354A1
公开(公告)日：2013-05-15
申请号：EP11804371.0
申请日：2011-07-07
申请人： Ardelyx, Inc.
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric , DU, Xunxiang , OSLOB, Johan
CPC分类号： A61K33/24 , A61K31/19 , A61K31/415 , A61K31/4192 , A61K31/4418 , A61K31/4433 , A61K31/4439 , A61K31/4453 , A61K31/454 , A61K31/4545 , A61K31/465 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/522 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/706 , A61K31/785 , A61K33/10 , A61K45/06 , C07D213/81 , C07D295/155 , C07D401/12 , C07D405/12 , C07D417/12
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译： 公开了具有作为磷酸盐转运抑制剂的活性的化合物，更具体地说，具有肠顶膜Na /磷酸盐共转运的抑制剂。 还公开了与这些化合物的制备和使用有关的方法，以及包含这些化合物的药物组合物。
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公开(公告)号：EP2590656A2
公开(公告)日：2013-05-15
申请号：EP11834773.1
申请日：2011-07-07
申请人： Ardelyx, Inc.
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
IPC分类号： A61K31/506
CPC分类号： C07D213/81 , A61K31/44 , A61K31/4418 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/59 , A61K31/593 , A61K31/785 , A61K45/06 , C07D213/30 , C07D213/38 , C07D213/50 , C07D213/82 , C07D239/34 , C07D239/42 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, A, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译： 公开了具有作为磷酸盐转运抑制剂的活性的化合物，更具体地说，具有肠顶膜Na /磷酸盐共转运的抑制剂。 所述化合物具有以下结构（I）：包括其立体异构体，药学上可接受的盐和前药，其中X，Y，A，R 1和R 2如本文所定义。 还公开了与这些化合物的制备和使用有关的方法，以及包含这些化合物的药物组合物。
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公开(公告)号：EP4397366A2
公开(公告)日：2024-07-10
申请号：EP24159204.7
申请日：2018-08-06
申请人： Ardelyx, Inc.
发明人： LUEHR, Gary , DRAGOLI, Dean , LEADBETTER, Michael , CHEN, Tao , LEWIS, Jason
IPC分类号： A61P5/44
CPC分类号： C07J63/008 , G02B3/0056 , G02B5/0215 , G02B5/0268 , G02B5/0294 , G02B27/0018 , G02B2207/12320130101 , G02F1/133502 , G02F1/133524 , G02F1/133526
摘要： The present invention provides a compound of formula (I) or a salt thereof: (I) wherein X, L, V, R1, R2, R3 and R4, are as defined herein. These compounds are inhibitors of 11-hydroxysteroid dehydrogenase type 2 (11-HSD-2) and are used to treat hyperkalemia.
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公开(公告)号：EP2590510B1
公开(公告)日：2016-09-28
申请号：EP11804373.6
申请日：2011-07-07
申请人： Ardelyx, Inc.
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
IPC分类号： A01N43/38 , A61K31/405
CPC分类号： A61K31/5377 , A61K31/454 , A61K31/59 , A61K45/06 , C07D209/12 , C07D209/14
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公开(公告)号：EP2590655B1
公开(公告)日：2015-06-24
申请号：EP11804369.4
申请日：2011-07-07
申请人： Ardelyx, Inc.
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
IPC分类号： A61K31/506 , A61K31/4965 , C07D401/00 , C07D403/00 , C07D211/68 , C07D413/00
CPC分类号： A61K31/5377 , A61K31/415 , A61K31/454 , A61K31/4545 , A61K31/4965 , A61K31/505 , A61K31/59 , A61K45/06 , C07D211/68 , C07D231/40 , C07D233/88 , C07D249/14 , C07D255/02 , C07D277/46 , C07D285/135 , C07D401/12 , A61K2300/00
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公开(公告)号：EP2794576A1
公开(公告)日：2014-10-29
申请号：EP12814096.9
申请日：2012-12-21
申请人： Ardelyx, Inc.
发明人： LEWIS, Jason, G. , REICH, Nicholas , CHEN, Tao , JACOBS, Jeffrey W. , CHARMOT, Dominique , NAVRE, Marc , FINN, Patricia , CARRERAS, Christopher , SPENCER, Andrew
IPC分类号： C07D241/42 , C07D215/08 , C07D265/30 , C07D277/06 , C07D279/10 , C07D279/16 , C07C235/68 , C07C237/24 , C07D207/16 , C07D213/75 , C07D231/20 , C07D233/90 , C07D263/34
CPC分类号： C07D241/42 , A61K31/498 , A61K31/5377 , A61K31/541 , A61K31/675 , A61K45/06 , C07C235/68 , C07C237/24 , C07D207/16 , C07D213/75 , C07D277/06 , C07D307/79 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07F9/6547
摘要： Compounds of structure (I), or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R
1 , R
2 , R
3 , R
4 , R
8 , R
9 , R
10 , R
11 , R
12 , A
1 , A
2 , X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.-
公开(公告)号：EP4234016A3
公开(公告)日：2023-10-18
申请号：EP23164821.3
申请日：2020-02-06
申请人： Ardelyx, Inc.
发明人： DRAGOLI, Dean , LUEHR, Gary , CHEN, Tao , LEWIS, Jason , LEADBETTER, Michael
摘要： The present invention provides a compound of formula (I) or a salt thereof:
wherein X, L, V, R 1 , R 2 , R 3 and R 4 , are as defined herein. The claimed compounds inhibit the enzyme 11-hydroxysteroid dehydrogenase type 2 (11-HSD2) and as a result are useful in the treatment of hyperkalemia by preventing cortisol from being oxidised to cortisone and thus allowing it to occupy the mineralocorticoid receptor, thus stimulating potassium excretion
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