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1. 发明申请

US20050187251A1 Substituted N-heterocycle derivatives and methods of their use 失效
标题翻译：取代的N-杂环衍生物及其使用方法
公开(公告)号：US20050187251A1
公开(公告)日：2005-08-25
申请号：US10962971
申请日：2004-10-12
申请人： Paige Mahaney , Lori Gavrin , Douglas Jenkins
发明人： Paige Mahaney , Lori Gavrin , Douglas Jenkins
IPC分类号： A61K31/40 , A61K31/4468 , A61K31/454 , A61K31/4545 , C07D207/14 , C07D209/14 , C07D211/46 , C07D211/48 , C07D211/58 , C07D213/38 , C07D215/12 , C07D295/084 , C07D307/52 , C07D307/81 , C07D309/10 , C07D317/58 , C07D333/28 , C07D333/58 , C07D333/62 , C07D409/06 , C07D413/02 , C07D43/02 , C07D49/02
CPC分类号： C07D333/58 , C07D207/14 , C07D209/14 , C07D211/46 , C07D211/48 , C07D211/58 , C07D213/38 , C07D215/12 , C07D295/092 , C07D307/52 , C07D307/81 , C07D309/10 , C07D317/58 , C07D333/28 , C07D333/62 , C07D409/06
摘要： The present invention is directed to substituted N-heterocycle 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N-杂环衍生物，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，胃肠道和泌尿生殖器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，糖尿病性神经病变及其组合的那些疾病，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。

2. 发明申请

US20050234058A1 Secondary amino-and cycloamino-cycloalkanol derivatives and methods of their use 失效
标题翻译：仲氨基和环氨基 - 环烷醇衍生物及其使用方法
公开(公告)号：US20050234058A1
公开(公告)日：2005-10-20
申请号：US10962899
申请日：2004-10-12
申请人： Paige Mahaney , Michael Webb , Lori Gavrin , Eugene Trybulski
发明人： Paige Mahaney , Michael Webb , Lori Gavrin , Eugene Trybulski
IPC分类号： A61K31/137 , A61K31/445 , A61K31/537 , C07C215/42 , C07D207/14 , C07D209/16 , C07D211/06 , C07D211/46 , C07D211/58 , C07D213/38 , C07D215/12 , C07D265/32 , C07D295/073 , C07D295/088 , C07D295/096 , C07D307/52 , C07D307/81 , C07D309/10 , C07D317/58 , C07D333/28 , C07D333/58 , C07D471/04
CPC分类号： C07C215/42 , C07C2601/04 , C07C2601/14 , C07D207/14 , C07D209/16 , C07D211/46 , C07D211/58 , C07D213/38 , C07D215/12 , C07D295/073 , C07D295/088 , C07D295/096 , C07D307/52 , C07D307/81 , C07D309/10 , C07D317/58 , C07D333/28 , C07D333/58 , C07D471/04
摘要： The present invention is directed to secondary amino- and cycloamino-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：本发明涉及仲氨基和环氨基 - 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，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，糖尿病性神经病变以及纤维肌痛症状其组合。

3. 发明申请

US20050192283A1 Fused-aryl and heteroaryl derivatives and methods of their use 失效
标题翻译：稠合芳基和杂芳基衍生物及其使用方法
公开(公告)号：US20050192283A1
公开(公告)日：2005-09-01
申请号：US10963064
申请日：2004-10-12
申请人： Eugene Trybulski , Paige Mahaney , Lori Gavrin , Joseph Sabatucci , Gary Stack
发明人： Eugene Trybulski , Paige Mahaney , Lori Gavrin , Joseph Sabatucci , Gary Stack
IPC分类号： A61K31/496 , C07D207/14 , C07D207/22 , C07D209/14 , C07D211/48 , C07D211/56 , C07D211/58 , C07D213/36 , C07D213/38 , C07D215/12 , C07D215/14 , C07D295/084 , C07D307/34 , C07D307/52 , C07D307/81 , C07D309/04 , C07D309/10 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/58 , C07D333/66 , C07D409/06 , C07D413/02 , C07D43/02 , C07D49/02
CPC分类号： C07D295/092 , A61K31/496 , C07D207/14 , C07D207/22 , C07D209/14 , C07D211/48 , C07D211/56 , C07D211/58 , C07D213/38 , C07D215/12 , C07D307/34 , C07D307/52 , C07D307/81 , C07D309/10 , C07D317/58 , C07D333/28 , C07D333/58 , C07D409/06
摘要： The present invention is directed to fused-aryl and heteroaryl 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：本发明涉及稠合芳基和杂芳基衍生物，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，其中尤其包括血管舒缩症状（VMS），性功能障碍，胃肠道和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，糖尿病性神经病变及其组合的那些病症，特别是选自下列的那些病症：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。

4. 发明申请

US20050171115A1 Alkanol and cycloalkanol-amine derivatives and methods of their use 失效
标题翻译：烷醇和环烷醇胺衍生物及其使用方法
公开(公告)号：US20050171115A1
公开(公告)日：2005-08-04
申请号：US10962880
申请日：2004-10-12
申请人： Eugene Trybulski , Paige Mahaney , Lori Gavrin , William Moore , Joseph Sabatucci
发明人： Eugene Trybulski , Paige Mahaney , Lori Gavrin , William Moore , Joseph Sabatucci
IPC分类号： A61K20060101 , A61K31/495 , A61K31/496 , C07D207/14 , C07D209/14 , C07D211/46 , C07D211/48 , C07D211/56 , C07D211/58 , C07D213/38 , C07D215/12 , C07D215/14 , C07D243/08 , C07D295/073 , C07D295/084 , C07D295/096 , C07D295/155 , C07D307/52 , C07D307/81 , C07D309/10 , C07D317/58 , C07D333/20 , C07D333/38 , C07D333/58 , C07D409/06 , C07D471/04 , C07D45/02
CPC分类号： C07D295/073 , C07D207/14 , C07D209/14 , C07D211/46 , C07D211/48 , C07D211/56 , C07D211/58 , C07D213/38 , C07D215/12 , C07D215/14 , C07D243/08 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/155 , C07D307/52 , C07D307/81 , C07D309/10 , C07D317/58 , C07D333/20 , C07D333/38 , C07D333/58 , C07D409/06 , C07D471/04
摘要： The present invention is directed to alkanoyl and cycloalkanoyl-amine 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：本发明涉及烷酰基和环烷酰胺衍生物，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，其中包括尤其是血管舒缩症状（VMS），性功能障碍，胃肠道和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，糖尿病性神经病变及其组合的那些病症，特别是选自下列的那些病症：泌尿生殖系疾病，慢性疲劳综合征，纤维瘤病综合征，神经系统疾病及其组合。

5. 发明申请

US20050143579A1 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：US20050143579A1
公开(公告)日：2005-06-30
申请号：US10963111
申请日：2004-10-12
申请人： Eugene Trybulski , Joseph Sabatucci , An Vu , Stephen Cohn , Arthur Santilli , Lori Gavrin , Fei Ye , Paige Mahaney
发明人： Eugene Trybulski , Joseph Sabatucci , An Vu , Stephen Cohn , Arthur Santilli , Lori Gavrin , Fei Ye , Paige Mahaney
IPC分类号： C07D207/14 , C07D209/14 , C07D211/44 , C07D211/46 , C07D211/56 , C07D211/58 , C07D213/38 , C07D215/12 , C07D241/04 , C07D243/08 , C07D295/02 , C07D295/03 , C07D295/088 , C07D307/14 , C07D307/81 , C07D309/12 , C07D317/58 , C07D333/28 , C07D333/58
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。

6. 发明申请

US20050143394A1 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：US20050143394A1
公开(公告)日：2005-06-30
申请号：US10963458
申请日：2004-10-12
申请人： Paige Mahaney , Eugene Trybulski , Lori Gavrin , An Vu
发明人： Paige Mahaney , Eugene Trybulski , Lori Gavrin , An Vu
IPC分类号： C07D295/088 , A61K31/495 , C07D241/04
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

US20070072897A1 Phenylaminopropanol derivatives and methods of their use 审中-公开
标题翻译：苯基氨基丙醇衍生物及其使用方法
公开(公告)号：US20070072897A1
公开(公告)日：2007-03-29
申请号：US11529441
申请日：2006-09-27
申请人： Paige Mahaney , Gavin Heffernan , Richard Coghlan , Stephen Cohn , Callain Kim , Douglas Jenkins , Michael Marella , Casey McComas , Joseph Sabatucci , Eugene Terefenko , Eugene Trybulski , An Vu , Fei Ye , Puwen Zhang
发明人： Paige Mahaney , Gavin Heffernan , Richard Coghlan , Stephen Cohn , Callain Kim , Douglas Jenkins , Michael Marella , Casey McComas , Joseph Sabatucci , Eugene Terefenko , Eugene Trybulski , An Vu , Fei Ye , Puwen Zhang
IPC分类号： A61K31/4745 , A61K31/4184 , A61K31/407 , A61K31/404 , A61K31/4439 , C07D403/02 , C07D471/02
CPC分类号： C07D209/08 , C07D209/10 , C07D209/12 , C07D209/34 , C07D209/96 , C07D235/26 , C07D241/42 , C07D401/12 , C07D471/04
摘要： The present invention is directed to phenylaminopropanol derivatives of formulae I, II, and III: 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, schizophrenia, and combinations thereof.
摘要翻译：本发明涉及式I，II和III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，血管舒缩症状（VMS），性功能障碍，胃肠道和泌尿生殖器疾病，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，精神分裂症及其组合。

8. 发明申请

US20070203207A1 Heteroaromatic glucokinase activators 审中-公开
公开(公告)号：US20070203207A1
公开(公告)日：2007-08-30
申请号：US11789105
申请日：2007-04-23
申请人： Fred Bizzarro , Wendy Corbett , Joseph Grippo , Nancy-Ellen Haynes , George Holland , Robert Kester , Paige Mahaney , Ramakanth Sarabu
发明人： Fred Bizzarro , Wendy Corbett , Joseph Grippo , Nancy-Ellen Haynes , George Holland , Robert Kester , Paige Mahaney , Ramakanth Sarabu
IPC分类号： A61K31/425 , C07C211/00 , C07C211/01 , C07C311/00 , C07D277/00
CPC分类号： C07D213/75 , C07C275/50 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07D213/80 , C07D213/82 , C07D233/88 , C07D237/20 , C07D237/22 , C07D239/42 , C07D239/47 , C07D241/20 , C07D253/07 , C07D261/14 , C07D263/48 , C07D277/46 , C07D277/56 , C07D277/58 , C07D285/135
摘要： 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

9. 发明申请

US20060160815A1 Pyrrolo[1,2-a]quinoxalin-5-(4H)-yl)sulfonyls and carbonyls and their use as estrogenic agents 失效
标题翻译：吡咯并[1,2-a]喹喔啉-5-（4H） - 基）磺酰基和羰基及其作为雌激素剂的用途
公开(公告)号：US20060160815A1
公开(公告)日：2006-07-20
申请号：US11305739
申请日：2005-12-16
申请人： Joseph Sabatucci , Fei Ye , Paige Mahaney
发明人： Joseph Sabatucci , Fei Ye , Paige Mahaney
IPC分类号： A61K31/498 , C07D487/02
CPC分类号： C07D487/04
摘要： This invention provides estrogen receptor modulators having the structure: wherein R1 to R7, R9 and R10 X, Y, and Z are as defined in the specification; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了具有以下结构的雌激素受体调节剂：其中R 1至R 7，R 9和R 10 X，Y和Z如说明书中所定义; 或其药学上可接受的盐。

10. 发明申请

US20070135449A1 Process for selective synthesis of enantiomers of substituted 1-(2-amino-1-phenyl-ethyl)-cyclohexanols 失效
标题翻译：选择性合成取代的1-（2-氨基-1-苯基 - 乙基） - 环己醇的对映异构体的方法
公开(公告)号：US20070135449A1
公开(公告)日：2007-06-14
申请号：US11633207
申请日：2006-12-04
申请人： Paige Mahaney , Madelene Antane , Jerry Sun
发明人： Paige Mahaney , Madelene Antane , Jerry Sun
IPC分类号： A61K31/495 , C07D241/04 , C07C62/30
CPC分类号： C07C213/02 , C07B2200/07 , C07C59/72 , C07C235/34 , C07C2601/14 , C07D263/26 , C07D295/092 , C07D295/096 , C07D295/185 , C07C217/74
摘要： A process for the enantioselective synthesis of an (S)— or (R)-1-[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol and analogues or salt thereof are described. The method involves the steps of (a) reacting an (S) or (R) 4-benzyloxazolidinone with a mixed anhydride of a methyoxyphenylacetic acid under conditions which form a oxazolidinone, (4S)— or (4R)-4-benzyl-3-[methyoxyphenyl]acetyl]-oxazolidin-2-one, (b) treating the (4S)— or (4R)-4-benzyl-3-[(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one with an aprotic amine base and titanium chloride in a chlorinated solvent under conditions which permit formation of the corresponding anion, (c) mixing the corresponding anion with titanium chloride and cylcohexanone under conditions which permit an aldol reaction to form the corresponding (4S)— or (4R)-4-benzyl-3-[(2R)-2-(1-hydroxycyclohexyl)-2-(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one, (d) hydrolyzing the (4S)— or (4R)-4-benzyl-3-[(2R)-2-(1-hydroxycyclohexyl)-2-(methoxyphenyl)acetyl]-1,3-oxazolidin-2-one to form a chiral acid (2S or 2R)-(1-hydroxycyclohexyl)-methoxyphenyl)acetic acid, (e) coupling the chiral phenylacid to a secondary amine to form an amide, and (f) reducing the amide to form an (S) or (R) 1[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol or a salt thereof.
摘要翻译：描述了（S） - 或（R）-1- [2-二甲基氨基）-1-（甲氧基苯基）乙基]环己醇及其类似物或其盐的对映选择性合成方法。该方法包括以下步骤：（S）或（R）4-苄氧基恶唑烷酮与甲氧基苯乙酸的混合酸酐在形成恶唑烷酮，（4S） - 或（4R）-4-苄基-3 - [甲氧基苯基]乙酰基] - 恶唑烷-2-酮，（b）用（4S） - 或（4R）-4-苄基-3 - [（甲氧基苯基）乙酰] -1,3-恶唑烷-2-酮处理非质子胺基和氯化钛在氯化溶剂中，在允许形成相应阴离子的条件下，（c）在允许醛醇缩合反应形成相应的（4S） - 或（ 4R）-4-苄基-3 - [（2R）-2-（1-羟基环己基）-2-（甲氧基苯基）乙酰基] -1,3-恶唑烷-2-酮，（d）水解（4S） - 或（4R）-4-苄基-3 - [（2R）-2-（1-羟基环己基）-2-（甲氧基苯基）乙酰基] -1,3-恶唑烷-2-酮以形成手性酸（2S或2R） - （1-羟基环己基） - 甲氧基苯基）乙酸，（e）将手性苯基酸偶联至仲胺以形成（f）还原酰胺以形成（S）或（R）1 [2-二甲基氨基）-1-（甲氧基苯基）乙基]环己醇或其盐。

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