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公开(公告)号:US10745402B2
公开(公告)日:2020-08-18
申请号:US16475251
申请日:2017-12-20
Applicant: PURDUE PHARMA L.P.
Inventor: Laykea Tafesse
IPC: C07D471/08 , A61P25/04
Abstract: The application is directed to compounds of formula (I): and pharmaceutically acceptable salts, radiolabeled isomers, solvates, or hydrates thereof, wherein R1, R2, R3, X, and n are defined as set forth in the specification. The application is also directed to compounds of formulae II, I-a, I-a1, I-a2, I-b, and I-b1 and the pharmaceutically acceptable salts, radiolabeled isomers, solvates, and hydrates thereof. The application is also directed to use of Compounds of the present disclosure to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain Compounds of the present disclosure are especially useful for treating pain. In one embodiment, Compounds of the present disclosure exhibit less opioid-induced side effects (such as, euphoria or drug-liking).
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公开(公告)号:US10138207B2
公开(公告)日:2018-11-27
申请号:US14075176
申请日:2013-11-08
Applicant: Purdue Pharma L.P.
Inventor: Jeffrey Lockman , Laykea Tafesse , Jiangchao Yao , Jianming Yu
IPC: A61K31/4353 , C07D417/12 , C07D221/26 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12
Abstract: The present invention is directed to Benzomorphan Analog compounds of the Formula I″, Formula IA″, Formula IB″, Formula IC″, or Formula ID″ as shown below; and related Formula I′, Formula IA′, Formula IB′, Formula IC′, or Formula ID′; Formula I, Formula IA, Formula IB, Formula IC, or Formula ID; wherein R1, R2a, R2b, R3 and R4 are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.
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公开(公告)号:US20180208575A1
公开(公告)日:2018-07-26
申请号:US15864750
申请日:2018-01-08
Applicant: Purdue Pharma L.P.
Inventor: Laykea Tafesse
IPC: C07D401/04 , C07D213/61 , C07D417/14 , C07D405/14 , C07D213/74 , C07D213/72 , C07D407/14 , C07D401/12 , C07D401/14 , C07D417/12
Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.
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公开(公告)号:US20180127374A1
公开(公告)日:2018-05-10
申请号:US15703453
申请日:2017-09-13
Applicant: Purdue Pharma L.P.
Inventor: Jae Hyun Park , David Rosen , Laykea Tafesse , Jianming Yu
IPC: C07D221/26 , C07D221/28 , C07D405/06
CPC classification number: C07D221/26 , C07D221/28 , C07D405/06
Abstract: The present invention is directed to Benzomorphan Analog compounds of the Formula (I), Formula (IA), Formula (IB), Formula (IC), or Formula (ID) as shown below, wherein R1, R2a, R2b, R3, R4, Z, and G are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.
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公开(公告)号:US20180111934A1
公开(公告)日:2018-04-26
申请号:US15318277
申请日:2015-06-12
Applicant: Purdue Pharma L.P.
Inventor: Laykea Tafesse , Mark A. Youngman
IPC: C07D471/08 , A61P25/04
CPC classification number: C07D471/08 , A61P25/04 , C07B2200/05
Abstract: The application is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, and Z are defined as set forth in the specification. In certain embodiments, the invention is also directed to compounds of Formula II-VII and the pharmaceutically acceptable salts and solvates thereof. The invention is also directed to use of compounds of Formula I to VII, and the pharmaceutically acceptable salts and solvates thereof, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the invention are especially useful for treating pain.
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公开(公告)号:US20170283392A1
公开(公告)日:2017-10-05
申请号:US15623120
申请日:2017-06-14
Applicant: Purdue Pharma L.P.
Inventor: Stephen M. Lynch , Laykea Tafesse
IPC: C07D401/04
CPC classification number: C07D401/04
Abstract: The present disclosure provides dibenzazepine derivatives having Formula I or I(A): and the pharmaceutically acceptable salts and solvates thereof, wherein R3a, R3b, R6, V1, V2, Z1, Z2, Z3, and G are defined as set forth in the specification. The present disclosure is also directed to the use of the compounds of Formula I or I(A), and the pharmaceutically acceptable salts or solvates thereof, to treat a disorder responsive to the blockade of one or more sodium channels. In one embodiment, the compounds of the present disclosure are useful for treating pain.
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公开(公告)号:US09765029B2
公开(公告)日:2017-09-19
申请号:US14824319
申请日:2015-08-12
Applicant: Purdue Pharma L.P.
Inventor: Don Kyle , Chiyou Ni , Minnie Park , Laykea Tafesse
IPC: C07D413/14 , C07D213/79 , C07D213/56 , C07D213/81 , C07D401/12 , C07D413/12 , C07B59/00
CPC classification number: C07D213/79 , C07B59/002 , C07D213/56 , C07D213/81 , C07D401/12 , C07D413/12 , C07D413/14
Abstract: The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein A1, X, A2, R1a, R1b, R1c, G, and z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
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公开(公告)号:US09718780B2
公开(公告)日:2017-08-01
申请号:US14961026
申请日:2015-12-07
Applicant: Purdue Pharma L.P.
Inventor: Laykea Tafesse , Jiangchao Yao
IPC: C07D213/24 , C07D239/24 , A61K31/47 , A61K31/505 , C07D213/50 , C07D213/81 , C07D213/30 , C07D213/46 , C07D213/56 , C07D213/57
CPC classification number: C07D213/50 , C07D213/24 , C07D213/30 , C07D213/46 , C07D213/56 , C07D213/57 , C07D213/81
Abstract: The invention relates to substituted pyridine and pyrimidine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1, R2a, R2b, A1, A2, X, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
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公开(公告)号:US20170210713A1
公开(公告)日:2017-07-27
申请号:US15481150
申请日:2017-04-06
Applicant: Purdue Pharma L.P.
Inventor: Jeffrey Lockman , Chiyou Ni , Jae Hyun Park , Minnie Park , Bin Shao , Laykea Tafesse , Jiangchao Yao , Mark A. Youngman
IPC: C07D239/42 , C07D403/12 , C07D401/04 , C07D413/04 , C07D401/12 , C07D471/08 , C07D401/14 , C07D405/14 , C07D487/08 , C07D403/14 , C07D413/14 , C07D403/04 , C07D405/12
CPC classification number: C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D471/08 , C07D487/08
Abstract: The present disclosure provides substituted pyrimidine carboxamides of Formula (I) and the pharmaceutically acceptable salts and solvates thereof wherein A1, X, A2, W1, W2, W3, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
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公开(公告)号:US09388162B2
公开(公告)日:2016-07-12
申请号:US14576718
申请日:2014-12-19
Applicant: Purdue Pharma L.P.
Inventor: Andrew Kassick , Jeffrey Lockman , Laykea Tafesse
IPC: C07D401/06 , C07D215/20 , C07D215/14 , C07D471/08
CPC classification number: C07D401/06 , C07D215/14 , C07D215/20 , C07D471/08
Abstract: The application is directed to compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4a, and R4b are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
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