公开(公告)号：US20080161366A1

公开(公告)日：2008-07-03

申请号：US11955195

申请日：2007-12-12

申请人： Casey Cameron McComas ,  Stephen Todd Cohn ,  Matthew Lantz Crawley ,  Andrew Fensome ,  Joel Adam Goldberg ,  Douglas John Jenkins ,  Callain Younghee Kim ,  Paige Erin Mahaney ,  Charles William Mann ,  Michael Anthony Marella ,  David John O'Neill ,  Joseph Peter Sabatucci ,  Eugene Anthony Terefenko ,  Eugene John Trybulski ,  An Thien Vu ,  Richard Page Woodworth ,  Puwen Zhang

发明人： Casey Cameron McComas ,  Stephen Todd Cohn ,  Matthew Lantz Crawley ,  Andrew Fensome ,  Joel Adam Goldberg ,  Douglas John Jenkins ,  Callain Younghee Kim ,  Paige Erin Mahaney ,  Charles William Mann ,  Michael Anthony Marella ,  David John O'Neill ,  Joseph Peter Sabatucci ,  Eugene Anthony Terefenko ,  Eugene John Trybulski ,  An Thien Vu ,  Richard Page Woodworth ,  Puwen Zhang

IPC分类号： A61K31/433 ,  C07D285/14 ,  A61P15/00 ,  A61P25/00 ,  A61P1/00 ,  A61P3/00

CPC分类号： C07D417/04 ,  C07D285/14 ,  C07D417/06

摘要： The present invention is directed to aminoalkyl-substituted aryl sulfamide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.

摘要翻译： 本发明涉及式I的氨基烷基取代的芳基磺酰胺衍生物：或其药学上可接受的盐，立体异构体或互变异构体，它们是单胺再摄取抑制剂，含有这些衍生物的组合物及其用于预防和治疗病症的方法 ，包括血管舒缩症状，性功能障碍，胃肠道疾病和泌尿生殖器疾病，抑郁症，内源性行为障碍，认知障碍，糖尿病性神经病，疼痛和其他疾病或病症。

公开(公告)号：US20090093469A1

公开(公告)日：2009-04-09

申请号：US12335245

申请日：2008-12-15

申请人： Callain Younghee Kim ,  Paige Erin Mahaney ,  Eugene John Trybulski ,  Puwen Zhang ,  Eugene Anthony Terefenko ,  Casey Cameron McComas ,  Michael Anthony Marella ,  Richard Dale Coghlan ,  Gavin David Heffernan ,  Stephen Todd Cohn ,  An Thien Vu ,  Joseph Peter Sabatucci ,  Fei Ye

发明人： Callain Younghee Kim ,  Paige Erin Mahaney ,  Eugene John Trybulski ,  Puwen Zhang ,  Eugene Anthony Terefenko ,  Casey Cameron McComas ,  Michael Anthony Marella ,  Richard Dale Coghlan ,  Gavin David Heffernan ,  Stephen Todd Cohn ,  An Thien Vu ,  Joseph Peter Sabatucci ,  Fei Ye

IPC分类号： A61K31/5415 ,  C07D403/06 ,  A61K31/496 ,  C07D413/06 ,  A61K31/5377 ,  C07D209/04 ,  A61K31/404 ,  C07D401/06 ,  A61K31/4439 ,  A61K31/454 ,  C07D265/36 ,  A61K31/538 ,  C07D241/38 ,  A61K31/498 ,  C07D235/04 ,  A61K31/4184 ,  C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P25/00 ,  A61P25/24 ,  C07D409/06 ,  C07D209/96 ,  C07D279/16

CPC分类号： C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D235/06 ,  C07D241/42 ,  C07D265/36 ,  C07D471/04

摘要： The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

公开(公告)号：US20090099164A1

公开(公告)日：2009-04-16

申请号：US12335144

申请日：2008-12-15

申请人： Callain Younghee Kim ,  Paige Erin Mahaney ,  Eugene John Trybulski ,  Puwen Zhang ,  Eugene Anthony Terefenko ,  Casey Cameron McComas ,  Michael Anthony Marella ,  Richard Dale Coghlan ,  Gavin David Heffernan ,  Stephen Todd Cohn ,  An Thien Vu ,  Joseph Peter Sabatucci ,  Fei Ye

发明人： Callain Younghee Kim ,  Paige Erin Mahaney ,  Eugene John Trybulski ,  Puwen Zhang ,  Eugene Anthony Terefenko ,  Casey Cameron McComas ,  Michael Anthony Marella ,  Richard Dale Coghlan ,  Gavin David Heffernan ,  Stephen Todd Cohn ,  An Thien Vu ,  Joseph Peter Sabatucci ,  Fei Ye

IPC分类号： A61K31/538 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/498 ,  A61K31/437 ,  A61P25/24 ,  A61P15/00 ,  A61P1/00 ,  A61P25/22 ,  A61P29/00 ,  A61K31/4184 ,  A61K31/404 ,  A61K31/4439

CPC分类号： C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D235/06 ,  C07D241/42 ,  C07D265/36 ,  C07D471/04

摘要： The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

摘要翻译： 本发明涉及式I的苯基氨基丙醇衍生物：或其药学上可接受的盐，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，所述方法尤其包括血管舒缩症状（VMS） 特别是选自重度抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛等的那些情况，特别是选自以下的那些病症：血管紧张素转换酶，抑制性功能障碍，性功能障碍，胃肠道和泌尿生殖系统疾病，慢性疲劳综合征，纤维瘤病综合征，神经系统疾病及其组合， 糖尿病性神经病变及其组合。

公开(公告)号：US07517899B2

公开(公告)日：2009-04-14

申请号：US11091885

申请日：2005-03-28

申请人： Callain Younghee Kim ,  Paige Erin Mahaney ,  Eugene John Trybulski ,  Puwen Zhang ,  Eugene Anthony Terefenko ,  Casey McComas ,  Michael Anthony Marella ,  Richard Dale Coghlan ,  Gavin David Heffernan ,  Stephen Todd Cohn ,  An Thien Vu ,  Joseph Peter Sabatucci ,  Fei Ye

发明人： Callain Younghee Kim ,  Paige Erin Mahaney ,  Eugene John Trybulski ,  Puwen Zhang ,  Eugene Anthony Terefenko ,  Casey McComas ,  Michael Anthony Marella ,  Richard Dale Coghlan ,  Gavin David Heffernan ,  Stephen Todd Cohn ,  An Thien Vu ,  Joseph Peter Sabatucci ,  Fei Ye

IPC分类号： A61K31/40 ,  A61K31/415 ,  C07D235/00 ,  C07D209/04

CPC分类号： C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D235/06 ,  C07D241/42 ,  C07D265/36 ,  C07D471/04

摘要： The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

摘要翻译： 本发明涉及式I的苯基氨基丙醇衍生物：或其药学上可接受的盐，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，所述方法尤其包括血管舒缩症状（VMS） 特别是选自重度抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛等的那些情况，特别是选自以下的那些病症：血管紧张素转换酶，抑制性功能障碍，性功能障碍，胃肠道和泌尿生殖系统疾病，慢性疲劳综合征，纤维瘤病综合征，神经系统疾病及其组合， 糖尿病性神经病变及其组合。

公开(公告)号：US07671238B2

公开(公告)日：2010-03-02

申请号：US11866158

申请日：2007-10-02

申请人： An Thien Vu ,  Stephen Todd Cohn ,  Eugene Anthony Terefenko ,  William Jay Moore ,  Puwen Zhang ,  Paige Erin Mahaney ,  Eugene John Trybulski

发明人： An Thien Vu ,  Stephen Todd Cohn ,  Eugene Anthony Terefenko ,  William Jay Moore ,  Puwen Zhang ,  Paige Erin Mahaney ,  Eugene John Trybulski

IPC分类号： C07C215/00 ,  A01N33/02 ,  A61K31/135

CPC分类号： C07C215/28 ,  C07C217/64 ,  C07C217/84

摘要： The present invention is directed to arylamino-arylpropanolamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

摘要翻译： 本发明涉及式I的芳基氨基 - 芳基丙醇胺衍生物：或其药学上可接受的盐，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，所述方法尤其包括血管舒缩症状（ VMS），性功能障碍，胃肠道和泌尿生殖系统疾病，慢性疲劳综合征，纤维肌痛综合征，神经系统疾病及其组合，特别是选自重度抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛， 疼痛，糖尿病性神经病，及其组合。

公开(公告)号：US20080085938A1

公开(公告)日：2008-04-10

申请号：US11866158

申请日：2007-10-02

申请人： An Thien Vu ,  Stephen Todd Cohn ,  Eugene Anthony Terefenko ,  William Jay Moore ,  Puwen Zhang ,  Paige Erin Mahaney ,  Eugene John Trybulski

发明人： An Thien Vu ,  Stephen Todd Cohn ,  Eugene Anthony Terefenko ,  William Jay Moore ,  Puwen Zhang ,  Paige Erin Mahaney ,  Eugene John Trybulski

IPC分类号： A61K31/136 ,  A61P1/00 ,  A61P13/00 ,  A61P15/00 ,  A61P25/00 ,  C07C211/44

CPC分类号： C07C215/28 ,  C07C217/64 ,  C07C217/84

摘要： The present invention is directed to arylamino-arylpropanolamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

摘要翻译： 本发明涉及式I的芳基氨基 - 芳基丙醇胺衍生物：或其药学上可接受的盐，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，所述方法尤其包括血管舒缩症状（ VMS），性功能障碍，胃肠道和泌尿生殖系统疾病，慢性疲劳综合征，纤维肌痛综合征，神经系统疾病及其组合，特别是选自重度抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛， 疼痛，糖尿病性神经病，及其组合。

公开(公告)号：US07550456B2

公开(公告)日：2009-06-23

申请号：US12031187

申请日：2008-02-14

申请人： Eugene John Trybulski ,  Joseph Peter Sabatucci ,  An Thien Vu ,  Stephen Todd Cohn ,  Arthur Attilio Santilli ,  Lori Krim Gavrin ,  Fei Ye ,  Paige Erin Mahaney

发明人： Eugene John Trybulski ,  Joseph Peter Sabatucci ,  An Thien Vu ,  Stephen Todd Cohn ,  Arthur Attilio Santilli ,  Lori Krim Gavrin ,  Fei Ye ,  Paige Erin Mahaney

IPC分类号： A01N43/62 ,  C07D243/08

CPC分类号： C07D295/088 ,  C07D207/14 ,  C07D209/14 ,  C07D211/44 ,  C07D211/46 ,  C07D211/56 ,  C07D211/58 ,  C07D213/38 ,  C07D215/12 ,  C07D241/04 ,  C07D243/08 ,  C07D295/03 ,  C07D307/14 ,  C07D307/81 ,  C07D309/12 ,  C07D317/58 ,  C07D333/28 ,  C07D333/58

摘要： The present invention is directed to substituted aryl cycloalkanoyl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

摘要翻译： 本发明涉及取代的芳基环烷酰基衍生物，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，所述方法尤其包括血管舒缩症状（VMS），性功能障碍，胃肠道和泌尿生殖系统疾病 特别是选自重度抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛，糖尿病性神经病变及其组合的那些病症，慢性疲劳综合征，纤维肌痛综合征，神经系统疾病及其组合。

公开(公告)号：US07365076B2

公开(公告)日：2008-04-29

申请号：US10963111

申请日：2004-10-12

申请人： Eugene John Trybulski ,  Joseph Peter Sabatucci ,  An Thien Vu ,  Stephen Todd Cohn ,  Arthur Attilio Santilli ,  Lori Krim Gavrin ,  Fei Ye ,  Paige Erin Mahaney

发明人： Eugene John Trybulski ,  Joseph Peter Sabatucci ,  An Thien Vu ,  Stephen Todd Cohn ,  Arthur Attilio Santilli ,  Lori Krim Gavrin ,  Fei Ye ,  Paige Erin Mahaney

IPC分类号： A61K31/50 ,  A61K31/501 ,  C07D241/04 ,  C07D295/00

CPC分类号： C07D295/088 ,  C07D207/14 ,  C07D209/14 ,  C07D211/44 ,  C07D211/46 ,  C07D211/56 ,  C07D211/58 ,  C07D213/38 ,  C07D215/12 ,  C07D241/04 ,  C07D243/08 ,  C07D295/03 ,  C07D307/14 ,  C07D307/81 ,  C07D309/12 ,  C07D317/58 ,  C07D333/28 ,  C07D333/58

摘要： The present invention is directed to substituted aryl cycloalkanoyl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

摘要翻译： 本发明涉及取代的芳基环烷酰基衍生物，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，所述方法尤其包括血管舒缩症状（VMS），性功能障碍，胃肠道和泌尿生殖系统疾病 特别是选自重度抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛，糖尿病性神经病变及其组合的那些病症，慢性疲劳综合征，纤维瘤病综合征，神经系统疾病及其组合。

公开(公告)号：US20080153826A1

公开(公告)日：2008-06-26

申请号：US12031187

申请日：2008-02-14

申请人： Eugene John Trybulski ,  Joseph Peter Sabatucci ,  An Thien Vu ,  Stephen Todd Cohn ,  Arthur Attilio Santilli ,  Lori Krim Gavrin ,  Fei Ye ,  Paige Erin Mahaney

发明人： Eugene John Trybulski ,  Joseph Peter Sabatucci ,  An Thien Vu ,  Stephen Todd Cohn ,  Arthur Attilio Santilli ,  Lori Krim Gavrin ,  Fei Ye ,  Paige Erin Mahaney

IPC分类号： A61K31/5375 ,  C07D241/04 ,  C07D265/30 ,  A61P25/22 ,  A61P25/24 ,  A61P15/12 ,  A61K31/4965

CPC分类号： C07D295/088 ,  C07D207/14 ,  C07D209/14 ,  C07D211/44 ,  C07D211/46 ,  C07D211/56 ,  C07D211/58 ,  C07D213/38 ,  C07D215/12 ,  C07D241/04 ,  C07D243/08 ,  C07D295/03 ,  C07D307/14 ,  C07D307/81 ,  C07D309/12 ,  C07D317/58 ,  C07D333/28 ,  C07D333/58

摘要： The present invention is directed to substituted aryl cycloalkanoyl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

摘要翻译： 本发明涉及取代的芳基环烷酰基衍生物，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，所述方法尤其包括血管舒缩症状（VMS），性功能障碍，胃肠道和泌尿生殖系统疾病 特别是选自重度抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛，糖尿病性神经病变及其组合的那些病症，慢性疲劳综合征，纤维肌痛综合征，神经系统疾病及其组合。

公开(公告)号：US20090131409A1

公开(公告)日：2009-05-21

申请号：US12255232

申请日：2008-10-21

申请人： John Francis Mehlmann ,  Joseph Theodore Lundquist, IV ,  Paige Erin Mahaney ,  Matthew Lantz Crawley ,  Callain Younghee Kim

发明人： John Francis Mehlmann ,  Joseph Theodore Lundquist, IV ,  Paige Erin Mahaney ,  Matthew Lantz Crawley ,  Callain Younghee Kim

IPC分类号： A61K31/55 ,  C07D487/04 ,  A61P3/00 ,  A61P9/00 ,  A61P25/00 ,  A61P35/00

CPC分类号： C07D487/04

摘要： Disclosed are chemical entities including compounds of Formula I and pharmaceutically acceptable salts thereof, wherein X is chosen from CN, CF3, CF2H, S(O)nR6, and S(O)2N(R9)R10; Y is chosen from CR11 and N; Z is chosen from O and NH; R3 is chosen from —C(O)R12 and —C(O)N(R9)R10; and n, R1, R2 and R4-R12 are defined herein; compositions comprising one or more such chemical entities; and methods of using one or more such chemical entities for modulating the activity of certain receptors (e.g., farnesoid X) or for the treatment or prevention of one or more symptoms of disease or disorder related to the activity of those receptors.

摘要翻译： 公开了包括式I化合物及其药学上可接受的盐的化学实体，其中X选自CN，CF 3，CF 2 H，S（O）n R 6和S（O）2 N（R 9）R 10; Y选自CR11和N; Z选自O和NH; R 3选自-C（O）R 12和-C（O）N（R 9）R 10; 且n，R 1，R 2和R 4 -R 12在本文中定义; 包含一种或多种这样的化学实体的组合物; 以及使用一种或多种这样的化学实体调节某些受体（例如法尼斯X）的活性或用于治疗或预防与这些受体的活性相关的一种或多种疾病或病症症状的方法。