公开(公告)号：US20090325916A1

公开(公告)日：2009-12-31

申请号：US12552604

申请日：2009-09-02

Applicant: Puwen Zhang ,  Jeffrey Curtis Kern ,  Eugene Anthony Terefenko ,  Eugene John Trybulski

Inventor： Puwen Zhang ,  Jeffrey Curtis Kern ,  Eugene Anthony Terefenko ,  Eugene John Trybulski

IPC: A61K31/58 ,  C07D207/30 ,  C07J71/00 ,  A61K31/40 ,  A61P15/18

CPC classification number: C07D207/34 ,  C07D261/08 ,  C07D333/22 ,  C07D333/28

Abstract: Compounds of formula I or II and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I, formula II, or formula III.

Abstract translation: 提供式I或II的化合物和含有这些化合物的药物组合物和试剂盒。 还提供了使用式I，式II或式III化合物诱导避孕，提供激素替代疗法，治疗周期相关症状或治疗或预防良性或恶性肿瘤疾病的方法。

公开(公告)号：US07671238B2

公开(公告)日：2010-03-02

申请号：US11866158

申请日：2007-10-02

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

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

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

CPC classification number: C07C215/28 ,  C07C217/64 ,  C07C217/84

Abstract: 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.

Abstract translation: 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：US20080167303A1

公开(公告)日：2008-07-10

申请号：US11955018

申请日：2007-12-12

Applicant: 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

Inventor： 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: A61K31/5377 ,  C07D285/06 ,  A61K31/433 ,  A61K31/496 ,  A61P13/00 ,  A61P25/02 ,  A61P25/00 ,  A61P15/00 ,  C07D403/06 ,  C07D417/06

CPC classification number: C07D417/04 ,  C07D285/14 ,  C07D417/06

Abstract: 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.

Abstract translation: 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：US20080153873A1

公开(公告)日：2008-06-26

申请号：US11954469

申请日：2007-12-12

Applicant: Puwen Zhang ,  Joseph Peter Sabatucci ,  Eugene Anthony Terefenko ,  Eugene John Trybulski

Inventor： Puwen Zhang ,  Joseph Peter Sabatucci ,  Eugene Anthony Terefenko ,  Eugene John Trybulski

IPC: A61K31/4709 ,  C07D405/04 ,  A61K31/4045 ,  A61K31/4184 ,  A61P1/00 ,  A61P25/02 ,  A61P25/00 ,  A61P25/24 ,  A61P13/00 ,  C07D307/83 ,  A61K31/343

CPC classification number: C07D307/83 ,  C07D405/04

Abstract: The present invention is directed to dihydrobenzofuranyl derivatives of formula I: or a pharmaceutically acceptable salt 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 disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.

Abstract translation: 本发明涉及式I的二氢苯并呋喃基衍生物或其药学上可接受的盐，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，尤其包括血管舒缩症状 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：US07192956B2

公开(公告)日：2007-03-20

申请号：US10601481

申请日：2003-06-23

Applicant: Andrew Fensome ,  Gary S. Grubb ,  Diane Deborah Harrison ,  Richard Craig Winneker ,  Puwen Zhang ,  Jeffrey Curtis Kern ,  Eugene Anthony Terefenko

Inventor： Andrew Fensome ,  Gary S. Grubb ,  Diane Deborah Harrison ,  Richard Craig Winneker ,  Puwen Zhang ,  Jeffrey Curtis Kern ,  Eugene Anthony Terefenko

IPC: A61K31/535 ,  A61K31/445 ,  A61K31/135

CPC classification number: A61K31/426 ,  A61K31/536 ,  A61K31/54 ,  A61K31/554 ,  A61K31/565 ,  A61K2300/00

Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I or formula II, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1–R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.

Abstract translation: 本发明提供诱导避孕的方法，其包括递送给女性含有式I或式II化合物或其互变异构体的组合物，其方案包括递送一种或多种选择性雌激素受体调节剂，其中式I为 ：其中R 1〜Z 5和Q 1如本文所述定义。 提供了提供激素替代疗法和治疗癌症，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症和多囊卵巢综合征的方法，其包括递送式I化合物和选择性雌激素受体调节剂。

公开(公告)号：US07687529B2

公开(公告)日：2010-03-30

申请号：US11529450

申请日：2006-09-27

Applicant: Casey Cameron McComas ,  Puwen Zhang ,  Eugene Anthony Terefenko ,  An Thien Vu ,  Stephen Todd Cohn

Inventor： Casey Cameron McComas ,  Puwen Zhang ,  Eugene Anthony Terefenko ,  An Thien Vu ,  Stephen Todd Cohn

IPC: A61K31/4184 ,  C07D235/04 ,  C07D209/04

CPC classification number: C07D209/96 ,  C07D209/08 ,  C07D209/34 ,  C07D235/26 ,  C07D235/30 ,  C07D277/68

Abstract: The present invention is directed to substituted propylamine 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.

Abstract translation: 本发明涉及式I的取代丙胺衍生物：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，其中尤其包括血管舒缩症状（VMS） 特别是那些选自重症抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛等症状的那些疾病 ，糖尿病性神经病，及其组合。

公开(公告)号：US20090093469A1

公开(公告)日：2009-04-09

申请号：US12335245

申请日：2008-12-15

Applicant: 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

Inventor： 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: 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 classification number: C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D235/06 ,  C07D241/42 ,  C07D265/36 ,  C07D471/04

Abstract: 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：US20100029641A1

公开(公告)日：2010-02-04

申请号：US12548844

申请日：2009-08-27

Applicant: 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

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

CPC classification number: C07D417/04 ,  C07D285/14 ,  C07D417/06

Abstract: 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.

Abstract translation: 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

Applicant: 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

Inventor： 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: A61K31/496 ,  A61K31/5377 ,  C07D413/06 ,  C07D403/06

CPC classification number: C07D417/04 ,  C07D285/14 ,  C07D417/06

Abstract: 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.

Abstract translation: 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：US20090099164A1

公开(公告)日：2009-04-16

申请号：US12335144

申请日：2008-12-15

Applicant: 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

Inventor： 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: 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 classification number: C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D235/06 ,  C07D241/42 ,  C07D265/36 ,  C07D471/04

Abstract: 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.

Abstract translation: 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。