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：US20090281096A1

公开(公告)日：2009-11-12

申请号：US12420085

申请日：2009-04-08

Applicant: Puwen Zhang ,  Andrew Fensome ,  Eugene A. Terefenko ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley ,  Jay E. Wrobel ,  Mark A. Collins

Inventor： Puwen Zhang ,  Andrew Fensome ,  Eugene A. Terefenko ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley ,  Jay E. Wrobel ,  Mark A. Collins

IPC: A61K31/536 ,  C07D265/18 ,  C07D265/14 ,  A61P5/00

CPC classification number: A61K31/536 ,  A61K31/538 ,  C07D265/18 ,  C07D413/04

Abstract: Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1, R2, R3, R4, R5, and Q1 are defined herein.

Abstract translation: 提供使用孕酮受体激动剂用于避孕的化合物和单独或与雌​​激素受体激动剂或孕酮受体拮抗剂联合治疗孕激素相关性疾病的方法。 这些化合物具有以下结构：其中R1，R2，R3，R4，R5和Q1如本文所定义。

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。

公开(公告)号：US07517899B2

公开(公告)日：2009-04-14

申请号：US11091885

申请日：2005-03-28

Applicant: 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

Inventor： 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: A61K31/40 ,  A61K31/415 ,  C07D235/00 ,  C07D209/04

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。

公开(公告)号：US07414142B2

公开(公告)日：2008-08-19

申请号：US11522688

申请日：2006-09-18

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: C07D291/04 ,  C07D285/06 ,  C07D285/08 ,  C07D285/10 ,  C07D285/12 ,  C07D271/04 ,  C07D271/06 ,  C07D271/08 ,  C07D271/10 ,  C07D207/08

CPC classification number: C07D207/416 ,  C07C251/44 ,  C07C255/64

Abstract: Compounds of formula I, wherein R1-R9 and n are defined herein, 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 or formula II, wherein R3-R5, R10, and R11 are defined herein.

Abstract translation: 提供其中R 1〜R 9和n在本文中定义的式I化合物，以及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或式II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，其中R 3〜 本文定义的是5，R 10和R 11。

公开(公告)号：US20080194654A1

公开(公告)日：2008-08-14

申请号：US11955204

申请日：2007-12-12

Applicant: 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

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

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

Abstract: 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.

Abstract translation: 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

Applicant: 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

Inventor： 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: A61K31/433 ,  C07D285/14 ,  A61P15/00 ,  A61P25/00 ,  A61P1/00 ,  A61P3/00

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

Abstract: 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.

Abstract translation: 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：US07354915B2

公开(公告)日：2008-04-08

申请号：US11804831

申请日：2007-05-21

Applicant: Puwen Zhang ,  Jeffrey Kern

Inventor： Puwen Zhang ,  Jeffrey Kern

IPC: C07D279/08 ,  A61K31/5415

CPC classification number: A61K31/538 ,  A61K31/517 ,  C07D265/18

Abstract: Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or unsubstituted C1 to C4 alkyl, aryl, substituted or unsubstituted C1 to C4 alkoxy, substituted or unsubstituted C1 to C3 aminoalkyl; R2 and R3 are H, substituted or unsubstituted C1 to C6 alkyl, C1 to C6 perfluoroalkyl, substituted or unsubstituted C2 to C6 alkenyl, substituted or unsubstituted C2 to C6 alkynyl, substituted or unsubstituted C3 to C6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or R2 and R3 are fused to form spirocyclic rings; R4 is NHR7, OR7, NHSO2R7, or OSO2R7; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt, ester, or prodrug thereof. Such compounds are useful as progesterone receptor modulators and for treating progesterone receptor related conditions

Abstract translation: 提供了具有式I结构的化合物。 在式I中，R 1是H，OH，取代或未取代的C 1至C 3烷基，C 1或N 2 C 3至C 3全氟烷基或COR 6; R 6是H，取代或未取代的C 1至C 4烷基，芳基，取代或未取代的C 1〜 至C 4烷氧基，取代或未取代的C 1至C 3氨基烷基; R 2和R 3均为H，取代或未取代的C 1至C 6烷基，C 1至C 6烷基， C 6至C 6全氟烷基，取代或未取代的C 2至C 6链烯基，取代或未取代的C 2， 取代或未取代的C 3至C 6环烷基，取代或未取代的芳基或取代或未取代的杂环基; 或R 2和R 3 3稠合形成螺环; R 4是NHR 7，OR 7，NHSO 2 R 7，或 OSO 2 R 7; Q是O，S，NR 8或CR 9 R 10; 或其药学上可接受的盐，酯或前药。 这些化合物可用作孕酮受体调节剂和用于治疗孕酮受体相关病症

公开(公告)号：US07319152B2

公开(公告)日：2008-01-15

申请号：US11522862

申请日：2006-09-18

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: C07D207/30 ,  C07D263/30 ,  C07D261/06 ,  C07D333/08

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

Abstract: Compounds of formula I or II are provided, wherein R1-R8 are defined herein, and pharmaceutical compositions and kits containing these compounds. 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, wherein R1-R9 are defined herein:

Abstract translation: 提供式I或II的化合物，其中R 1 -R 8是本文定义的，以及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化合物诱导避孕的方法，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，其中R 1， 本文定义为：