公开(公告)号：US20100029641A1

公开(公告)日：2010-02-04

申请号：US12548844

申请日：2009-08-27

申请人： Casey Cameron McComas ,  Stephen Todd Cohn ,  Andrew Fensome ,  Joel Adam Goldberg ,  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, JR. ,  Puwen Zhang

发明人： Casey Cameron McComas ,  Stephen Todd Cohn ,  Andrew Fensome ,  Joel Adam Goldberg ,  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, JR. ,  Puwen Zhang

IPC分类号： A61K31/5377 ,  C07D285/14 ,  C07D417/06 ,  A61K31/41 ,  A61K31/454 ,  A61P15/00 ,  A61P1/00 ,  A61P25/00 ,  A61P7/12

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

摘要： The present invention is directed to 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，其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， 尤其是血管舒缩症状，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，疼痛和其它疾病或病症。

公开(公告)号：US07601722B2

公开(公告)日：2009-10-13

申请号：US11955018

申请日：2007-12-12

申请人： Casey Cameron McComas ,  Stephen Todd Cohn ,  Andrew Fensome ,  Joel Adam Goldberg ,  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, Jr. ,  Puwen Zhang

发明人： Casey Cameron McComas ,  Stephen Todd Cohn ,  Andrew Fensome ,  Joel Adam Goldberg ,  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, Jr. ,  Puwen Zhang

IPC分类号： A61K31/496 ,  A61K31/5377 ,  C07D413/06 ,  C07D403/06

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

摘要： The present invention is directed to 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，其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， 尤其是血管舒缩症状，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，疼痛和其它疾病或病症。

公开(公告)号：US20080194654A1

公开(公告)日：2008-08-14

申请号：US11955204

申请日：2007-12-12

申请人： Casey Cameron McComas ,  Andrew Fensome ,  Joel Adam Goldberg ,  Charles William Mann ,  David John O'Neill ,  Joseph Peter Sabatucci ,  Eugene Anthony Terefenko ,  Eugene John Trybulski ,  An Thien Vu ,  Puwen Zhang

发明人： Casey Cameron McComas ,  Andrew Fensome ,  Joel Adam Goldberg ,  Charles William Mann ,  David John O'Neill ,  Joseph Peter Sabatucci ,  Eugene Anthony Terefenko ,  Eugene John Trybulski ,  An Thien Vu ,  Puwen Zhang

IPC分类号： A61K31/433 ,  C07D285/14 ,  A61P15/00 ,  A61P1/00 ,  A61P21/00 ,  A61P25/24 ,  A61P7/12 ,  A61P29/00

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

摘要： The present invention is directed to hydroxy-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的羟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：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：US20080167303A1

公开(公告)日：2008-07-10

申请号：US11955018

申请日：2007-12-12

申请人： Casey Cameron McComas ,  Stephen Todd Cohn ,  Andrew Fensome ,  Joel Adam Golderg ,  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 ,  Andrew Fensome ,  Joel Adam Golderg ,  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： A61K31/5377 ,  C07D285/06 ,  A61K31/433 ,  A61K31/496 ,  A61P13/00 ,  A61P25/02 ,  A61P25/00 ,  A61P15/00 ,  C07D403/06 ,  C07D417/06

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

摘要： The present invention is directed to 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，其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， 尤其是血管舒缩症状，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，疼痛和其它疾病或病症。

公开(公告)号：US20100184786A1

公开(公告)日：2010-07-22

申请号：US12622058

申请日：2009-11-19

申请人： Jeremy Mark Travins ,  Ronald Charles Bernotas ,  Jay Edward Wrobel ,  David Harry Kaufman ,  Baihua Hu ,  James Winfield Jetter ,  David John O'Neill ,  Charles William Mann

发明人： Jeremy Mark Travins ,  Ronald Charles Bernotas ,  Jay Edward Wrobel ,  David Harry Kaufman ,  Baihua Hu ,  James Winfield Jetter ,  David John O'Neill ,  Charles William Mann

IPC分类号： A61K31/517 ,  C07D239/74 ,  A61P9/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P29/00 ,  A61Q19/08 ,  A61K8/49

CPC分类号： C07D239/72

摘要： Disclosed are polar quinazoline-based modulators of Liver X receptors (LXRs) and related methods. The modulators include compounds of formula (I): in which, R1, R2, R3, R4, R5, R6, R22, R23, R24, R25, R26, R27, R28, R29, W, W1, W2, Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh, Ri, Rj, Rm, Rn, Ro, Rp, Rq, Rr, Rs, Rt, Ru, and n can be as defined anywhere herein. In general, these compounds can be used for treating or preventing one or more diseases, disorders, conditions or symptoms mediated by LXRs.

摘要翻译： 公开了基于极性喹唑啉的肝脏X受体调节剂（LXR）及相关方法。 调节剂包括式（I）化合物：其中R1，R2，R3，R4，R5，R6，R22，R23，R24，R25，R26，R27，R28，R29，W，W1，W2，Ra，Rb ，Rc，Rd，Re，Rf，Rg，Rh，Ri，Rj，Rm，Rn，Ro，Rp，Rq，Rr，Rs，Rt，Ru和n可以如本文任何地方所定义。 通常，这些化合物可用于治疗或预防由LXR介导的一种或多种疾病，病症，病症或症状。

公开(公告)号：US20100120778A1

公开(公告)日：2010-05-13

申请号：US12614167

申请日：2009-11-06

申请人： Baihua Hu ,  Jay Edward Wrobel ,  James Winfield Jetter ,  David John O'Neill ,  Charles William Mann ,  Rayomand Jal Unwalla

发明人： Baihua Hu ,  Jay Edward Wrobel ,  James Winfield Jetter ,  David John O'Neill ,  Charles William Mann ,  Rayomand Jal Unwalla

IPC分类号： A61K31/498 ,  C07D241/36 ,  A61P1/16 ,  A61P9/10 ,  A61P9/00 ,  A61P3/04 ,  A61P3/06 ,  A61P25/28 ,  A61P3/10 ,  A61P29/00 ,  A61P19/04

CPC分类号： C07D241/44 ,  C07D241/42

摘要： Disclosed are quinoxaline-based modulators of Liver X receptors (LXRs) and related methods. The modulators include compounds of formula (I): wherein: each of L1 and L2 is, independently, a bond, —O— or —NH—; R2 is C6-C10 aryl or heteroaryl including 5-10 atoms, each of which is (i) substituted with 1 R9, and (ii) optionally further substituted with from 1-4 Re; and each of R4 and R5 is, independently (i) hydrogen; or (ii) halo; or (iii) C1-C6 alkyl or C1-C6 haloalkyl, each of which is optionally substituted with from 1-3 Ra; and R1, R3, R6, R9, Ra and Re are defined herein. In general, these compounds can be used for treating or preventing one or more diseases, disorders, conditions or symptoms mediated by LXRs.

摘要翻译： 公开了基于喹喔啉的肝脏X受体调节剂（LXR）和相关方法。 调节剂包括式（I）的化合物：其中：L1和L2各自独立地是键，-O-或-NH-; R 2是包括5-10个原子的C 6 -C 10芳基或杂芳基，其各自为（i）被1个R9取代，和（ii）任选地被1-4个Re取代; 并且R 4和R 5各自独立地是（i）氢; 或（ii）卤素; 或（iii）C 1 -C 6烷基或C 1 -C 6卤代烷基，其各自任选被1-3个R a取代; 并且R1，R3，R6，R9，Ra和Re在本文中定义。 通常，这些化合物可用于治疗或预防由LXR介导的一种或多种疾病，病症，病症或症状。