公开(公告)号：US09000174B2

公开(公告)日：2015-04-07

申请号：US11665345

申请日：2005-10-14

申请人： Elfrida R. Benjamin ,  Zhengming Chen ,  Deyou Sha ,  Laykea Tafesse ,  Samuel F. Victory ,  John W. F. Whitehead

发明人： Elfrida R. Benjamin ,  Zhengming Chen ,  Deyou Sha ,  Laykea Tafesse ,  Samuel F. Victory ,  John W. F. Whitehead

IPC分类号： C07D211/58 ,  A61K31/4545 ,  A61K31/4468 ,  C07D401/06 ,  C07D211/96

CPC分类号： C07D401/06 ,  C07D211/58 ,  C07D211/96

摘要： The invention relates to piperidinyl compounds of Formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to an assay useful for identifying such compounds as N-type calcium channel modulators or blockers. The invention is also directed to the compounds of Formula (I) and compounds identified by the above assay, and the use of such compounds to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

公开(公告)号：US20120302619A1

公开(公告)日：2012-11-29

申请号：US13366219

申请日：2012-02-03

申请人： Phil SKOLNICK ,  Anthony Basile ,  Zhengming Chen ,  Joseph W. Epstein

发明人： Phil SKOLNICK ,  Anthony Basile ,  Zhengming Chen ,  Joseph W. Epstein

IPC分类号： A61K31/403 ,  A61P25/22 ,  A61P25/24 ,  C07D209/52 ,  A61P25/00

CPC分类号： A61K31/403 ,  C07D209/52

摘要： The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.

摘要翻译： 本发明提供新的多取代的1-芳基-3-氮杂双环[3.1.0]己烷，以及用于制备这些化合物的相关方法和中间体，以及使用这些化合物用于治疗和/或预防中枢的组合物和方法 神经系统（CNS）障碍，包括抑郁和焦虑。

公开(公告)号：US20090233978A1

公开(公告)日：2009-09-17

申请号：US12334432

申请日：2008-12-12

申请人： Phil Skolnick ,  Anthony Basile ,  Zhengming Chen ,  Joseph W. Epstein

发明人： Phil Skolnick ,  Anthony Basile ,  Zhengming Chen ,  Joseph W. Epstein

IPC分类号： A61K31/40 ,  C07D209/02 ,  A61P25/00

CPC分类号： A61K31/403 ,  C07D209/52

摘要： The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.

摘要翻译： 本发明提供新的多取代的1-芳基-3-氮杂双环[3.1.0]己烷，以及用于制备这些化合物的相关方法和中间体，以及使用这些化合物用于治疗和/或预防中枢的组合物和方法 神经系统（CNS）障碍，包括抑郁和焦虑。

公开(公告)号：US20090069374A1

公开(公告)日：2009-03-12

申请号：US12135053

申请日：2008-06-06

申请人： Phil Skolnick ,  Zhengming Chen

发明人： Phil Skolnick ,  Zhengming Chen

IPC分类号： A61K31/47 ,  A61K31/403 ,  A61K31/4439 ,  A61K31/428

CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04

摘要： The invention provides novel 1-heteroaryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety.

摘要翻译： 本发明提供新颖的1-杂芳基-3-氮杂双环[3.1.0]己烷，以及制备这些化合物的相关方法和中间体，以及使用这些化合物治疗和/或预防中枢神经系统（CNS）的组合物和方法 ）疾病，包括但不限于抑郁和焦虑。

公开(公告)号：US20080194696A1

公开(公告)日：2008-08-14

申请号：US11936722

申请日：2007-11-07

申请人： Phil Skolnick ,  Zhengming Chen ,  Ji Yang

发明人： Phil Skolnick ,  Zhengming Chen ,  Ji Yang

IPC分类号： A61K31/135 ,  C07C211/41

CPC分类号： C07C211/41 ,  C07B2200/07 ,  C07C2602/18

摘要： The invention provides novel arylbicyclo[3.1.0]hexylamines, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety.

公开(公告)号：US20070179141A1

公开(公告)日：2007-08-02

申请号：US11729660

申请日：2007-03-28

申请人： Zhengming Chen

发明人： Zhengming Chen

IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  C07D413/14 ,  C07D403/14

CPC分类号： C07D401/04 ,  C07D211/64 ,  C07D401/14

摘要： 4-Tetrazolyl-4-phenylpiperidine Compounds, compositions comprising an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound, methods for treating or preventing pain or diarrhea in an animal comprising administering to an animal in need thereof an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound and methods for stimulating opioid-receptor function in a cell comprising contacting a cell capable of expressing an opioid receptor with an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound are disclosed.

公开(公告)号：US20070082940A1

公开(公告)日：2007-04-12

申请号：US11493431

申请日：2006-07-25

申请人： Phil Skolnick ,  Anthony Basile ,  Zhengming Chen ,  Joseph Epstein

发明人： Phil Skolnick ,  Anthony Basile ,  Zhengming Chen ,  Joseph Epstein

IPC分类号： A61K31/403

CPC分类号： A61K31/403 ,  C07D209/52

摘要： The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.

摘要翻译： 本发明提供新的多取代的1-芳基-3-氮杂双环[3.1.0]己烷，以及用于制备这些化合物的相关方法和中间体，以及使用这些化合物用于治疗和/或预防中枢的组合物和方法 神经系统（CNS）障碍，包括抑郁和焦虑。

公开(公告)号：US20050009854A1

公开(公告)日：2005-01-13

申请号：US10448627

申请日：2003-05-29

申请人： Zhengming Chen ,  Sam Victory

发明人： Zhengming Chen ,  Sam Victory

IPC分类号： C07D471/10 ,  A61K31/4747

CPC分类号： C07D471/10

摘要： Triazaspiro Compounds, compositions comprising a Triazaspiro Compound, methods for treating or preventing pain in an animal comprising administering to an animal in need thereof an effective amount of a Triazaspiro Compound and methods for stimulating opioid-receptor function in a cell comprising contacting a cell capable of expressing an opioid receptor with an effective amount of a Triazaspiro Compound are disclosed.

摘要翻译： 三唑类化合物，包含三氮唑类化合物的组合物，用于治疗或预防动物疼痛的方法，包括向有需要的动物施用有效量的三氮嘧啶化合物和刺激细胞中阿片受体功能的方法，包括使能够 公开了表达具有有效量的三氮唑螺化合物的阿片受体。

公开(公告)号：US5948933A

公开(公告)日：1999-09-07

申请号：US893921

申请日：1997-07-11

申请人： Peter C. Meltzer ,  Bertha K. Madras ,  Paul Blundell ,  Zhengming Chen

发明人： Peter C. Meltzer ,  Bertha K. Madras ,  Paul Blundell ,  Zhengming Chen

IPC分类号： A61K31/18 ,  A61K31/198 ,  A61K31/35 ,  A61K31/405 ,  A61K31/46 ,  A61K38/00 ,  A61K51/04 ,  A61P25/00 ,  A61P25/30 ,  A61P43/00 ,  C07C33/34 ,  C07C41/00 ,  C07C49/105 ,  C07C49/115 ,  C07C69/74 ,  C07C69/753 ,  C07C205/00 ,  C07C233/00 ,  C07C255/00 ,  C07D311/00 ,  C07D451/02 ,  C07D451/06 ,  C07D471/08 ,  C07D493/08 ,  C07F7/22

CPC分类号： C07D451/02 ,  A61K31/18 ,  A61K31/198 ,  A61K31/405 ,  A61K51/0448 ,  C07C69/753 ,  C07D451/06 ,  C07D471/08 ,  C07D493/08 ,  A61K2123/00 ,  A61K38/00 ,  C07C2102/44

摘要： New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

公开(公告)号：US20130345439A1

公开(公告)日：2013-12-26

申请号：US13887367

申请日：2013-05-05

申请人： Phil SKOLNICK ,  Anthony Basile ,  Zhengming Chen ,  Joseph W. Epstein

发明人： Phil SKOLNICK ,  Anthony Basile ,  Zhengming Chen ,  Joseph W. Epstein

IPC分类号： C07D209/52

CPC分类号： A61K31/403 ,  C07D209/52

摘要： The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.