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1. 发明授权

US07601744B2 Benzothiadiazolylphenylalkylamine derivatives and methods of their use 失效
标题翻译：苯并噻二唑基苯基烷基胺衍生物及其使用方法
公开(公告)号：US07601744B2
公开(公告)日：2009-10-13
申请号：US11528792
申请日：2006-09-27
申请人： Casey Cameron McComas , Puwen Zhang , Eugene John Trybulski , An Thien Vu , Eugene Anthony Terefenko
发明人： Casey Cameron McComas , Puwen Zhang , Eugene John Trybulski , An Thien Vu , Eugene Anthony Terefenko
IPC分类号： A61K31/41 , C07D285/06
CPC分类号： C07D285/14
摘要： The present invention is directed to benzothiadiazolylphenylalkylamine 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的苯并噻二唑基苯基烷基胺衍生物：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）特别是选自重症抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛等的那些病症，其中，所述疾病，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，糖尿病性神经病变及其组合。

2. 发明申请

US20080153826A1 SUBSTITUTED ARYL CYCLOALKANOL DERIVATIVES AND METHODS OF THEIR USE 失效
标题翻译：取代的芳基环烷醇衍生物及其使用方法
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。

3. 发明申请

US20080085938A1 Arylamino-Arylpropanolamine Derivatives and Methods of Their Use 失效
标题翻译：芳基氨基 - 芳基丙醇胺衍生物及其使用方法
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。

4. 发明授权

US07202239B2 Cyclohexylphenyl carboxamides tocolytic oxytocin receptor antagonists 失效
标题翻译：环己基苯基甲酰胺溶血性催产素受体拮抗剂
公开(公告)号：US07202239B2
公开(公告)日：2007-04-10
申请号：US10119994
申请日：2002-04-10
申请人： Amedeo Arturo Failli , Eugene John Trybulski , Jay Scott Shumsky , John Paul Dusza , Kevin Anthony Memoli
发明人： Amedeo Arturo Failli , Eugene John Trybulski , Jay Scott Shumsky , John Paul Dusza , Kevin Anthony Memoli
IPC分类号： A61P15/06 , A61K31/55 , C07D487/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D487/04
摘要： The present invention provides novel tricyclic benzodiazepine carboxamides compounds and methods and pharmaceutical compositions utilizing them for the treatment and/or prevention and/or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and/or suppression suppression of preterm labor, suppression of labor at term prior to caesarean delivery, and for the treatment of dysmenorrhea. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.
摘要翻译：本发明提供了新型的三环苯并二氮杂甲酰胺化合物及其利用它们的方法和药物组合物，用于治疗和/或预防和/或抑制可通过催产素拮抗剂活性补救或减轻的疾病，包括预防和/或抑制早产的抑制剖宫产分娩期间的劳动抑制以及痛经的治疗。这些化合物也可用于提高生育率，提高农场动物的生存率和发情同步; 并且可用于预防和治疗包括强迫症（OCD）和神经精神障碍在内的催产素系统在中枢神经系统中的功能障碍。

5. 发明授权

US07671238B2 Arylamino-arylpropanolamine derivatives and methods of their use 失效
标题翻译：芳基氨基 - 芳基丙醇胺衍生物及其使用方法
公开(公告)号：US07671238B2
公开(公告)日：2010-03-02
申请号：US11866158
申请日：2007-10-02
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。

6. 发明授权

US07531543B2 Phenylpiperazine cycloalkanol derivatives and methods of their use 失效
标题翻译：苯基哌嗪环烷醇衍生物及其使用方法
公开(公告)号：US07531543B2
公开(公告)日：2009-05-12
申请号：US10963458
申请日：2004-10-12
申请人： Paige Erin Mahaney , Eugene John Trybulski , Lori Krim Gavrin , An Thien Vu
发明人： Paige Erin Mahaney , Eugene John Trybulski , Lori Krim Gavrin , An Thien Vu
IPC分类号： A61K31/4965 , C07D223/00 , C07D225/00 , C07D241/00 , C07D241/02 , C07D243/00 , C07D245/00
CPC分类号： C07D295/088
摘要： The present invention is directed to phenylpiperazine cycloalkanol 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：本发明涉及苯基哌嗪环烷醇衍生物，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，纤维肉瘤病综合征，神经系统疾病及其组合。

7. 发明申请

US20080167303A1 ARYL SULFAMIDE DERIVATIVES AND METHODS OF THEIR USE 失效
标题翻译： ARYL SULFAMIDE衍生物及其使用方法
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。

8. 发明申请

US20080153873A1 DIHYDROBENZOFURANYL DERIVATIVES AND METHODS OF THEIR USE 审中-公开
标题翻译： DIHYDROBENZOFURANYL衍生物及其使用方法
公开(公告)号：US20080153873A1
公开(公告)日：2008-06-26
申请号：US11954469
申请日：2007-12-12
申请人： Puwen Zhang , Joseph Peter Sabatucci , Eugene Anthony Terefenko , Eugene John Trybulski
发明人： Puwen Zhang , Joseph Peter Sabatucci , Eugene Anthony Terefenko , Eugene John Trybulski
IPC分类号： A61K31/4709 , C07D405/04 , A61K31/4045 , A61K31/4184 , A61P1/00 , A61P25/02 , A61P25/00 , A61P25/24 , A61P13/00 , C07D307/83 , A61K31/343
CPC分类号： C07D307/83 , C07D405/04
摘要： 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.
摘要翻译：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。

9. 发明授权

US07365076B2 Substituted aryl cycloalkanol derivatives and methods of their use 失效
标题翻译：取代的芳基环烷醇衍生物及其使用方法
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。

10. 发明授权

US07022699B2 Cyclohexenyl phenyl diazepines vasopressin and oxytocin receptor modulators 失效
标题翻译：环己烯基苯基二氮杂加压素和催产素受体调节剂
公开(公告)号：US07022699B2
公开(公告)日：2006-04-04
申请号：US10119611
申请日：2002-04-10
申请人： Amedeo Arturo Failli , William Jennings Sanders , Eugene John Trybulski
发明人： Amedeo Arturo Failli , William Jennings Sanders , Eugene John Trybulski
IPC分类号： A61P15/06 , A61K31/55 , C07D487/12
CPC分类号： C07D487/04
摘要： The present invention provides novel tricyclic diazepine compounds and methods and pharmaceutical compositions utilizing them for the treating or preventing disorders including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, congestive heart failure or for inducing temporary delay of urination, and in conditions with increased vascular resistance and coronary vasoconstriction; and for the treating or preventing disorders remedied or alleviated by oxytocin antagonist activity, including suppression of preterm labor, dysmenorrhea, endometritis, and for suppressing labor at term prior to caesarean delivery. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.
摘要翻译：本发明提供了新型的三环二氮杂化合物和利用它们用于治疗或预防包括尿崩症，夜间遗尿，夜尿症，尿失禁，出血和凝血障碍，充血性心力衰竭或引起排尿暂时延迟的疾病的方法和药物组合物，以及在具有增加的血管阻力和冠状动脉血管收缩的条件下; 以及用于治疗或预防由催产素拮抗剂活性治疗或缓解的疾病，包括抑制早产，痛经，子宫内膜炎，以及在剖宫产分娩前的期间抑制劳动。这些化合物也可用于提高生育率，提高农场动物的生存率和发情同步; 以及治疗中枢神经系统中催产素系统的功能障碍，包括强迫症（OCD）和神经精神障碍。

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