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1. 发明授权

US07534894B2 Biphenyloxy-acids 失效
标题翻译：联苯氧基酸
公开(公告)号：US07534894B2
公开(公告)日：2009-05-19
申请号：US10947710
申请日：2004-09-23
申请人： Thomas Joseph Commons , Susan Christman Croce , Eugene John Trybulski , Hassan Mahmoud Elokdah , David LeRoy Crandall
发明人： Thomas Joseph Commons , Susan Christman Croce , Eugene John Trybulski , Hassan Mahmoud Elokdah , David LeRoy Crandall
IPC分类号： C07D257/06 , C07D333/02 , C07D333/50 , C07D307/02 , C07D307/77
CPC分类号： C07D405/12 , C07C233/60 , C07C233/75 , C07C235/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07D209/30 , C07D209/42 , C07D231/14 , C07D307/68 , C07D307/84 , C07D333/38 , C07D333/68 , C07D403/12
摘要： The present invention relates generally to substituted biphenyloxy acids (such as 4′-aryl-amido-biphenyl-4(3)-yloxy-acids and 4′-aryl-amidomethyl-biphenyl-4(3)-yloxy-acids) and methods of using them, for example, as PAI-1 inhibitors.
摘要翻译：本发明一般涉及取代的联苯氧基酸（例如4'-芳基 - 酰氨基 - 联苯-4（3） - 氧基酸和4'-芳基 - 酰氨基甲基 - 联苯-4（3） - 氧基酸）和方法使用它们，例如，作为PAI-1抑制剂。

2. 发明授权

US06589970B2 6-(aryl-amido or aryl-amidomethyl)-naphthalen-2-yloxy-acidic derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) 失效
标题翻译： 6-（芳基 - 酰胺基或芳基 - 酰氨基甲基） - 萘-2-基氧基 - 酸性衍生物作为纤溶酶原激活物抑制剂1型抑制剂（PAI-1）
公开(公告)号：US06589970B2
公开(公告)日：2003-07-08
申请号：US10170558
申请日：2002-06-13
申请人： Thomas Joseph Commons , Susan Christman Croce , Richard Page Woodworth , Eugene John Trybulski , Hassan Mahmoud Elokdah , David LeRoy Crandall
发明人： Thomas Joseph Commons , Susan Christman Croce , Richard Page Woodworth , Eugene John Trybulski , Hassan Mahmoud Elokdah , David LeRoy Crandall
IPC分类号： A61K31343
CPC分类号： C07D403/12 , C07C233/73 , C07C235/48 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D231/14 , C07D307/68 , C07D307/84 , C07D307/85 , C07D405/12
摘要： This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula: Wherein: Ar is phenyl, naphthyl, furanyl, benzofuranyl, indolyl, pyrazolyl, oxazolyl, fluorenyl, phenylcycloalkane where the cycloalkane can be cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl and Ar can be optionally substituted by 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, hydroxy, phenyl-(CH2)0-6—, phenyl-(CH2)0-6O—, C3-C6 cycloalkyl, —(CH2)—C3-C6 cycloalkyl, halogen, C1-C3 perflouroalkyl and C1-C3 perfluoroalkoxy where phenyl can be substituted with from 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, phenyl, halogen, trifluoromethyl or trifluoromethoxy; R1 is hydrogen, C1-C6 alkyl or phenyl-(CH2)1-6— where phenyl can be substituted with C1-C6 alkyl, C1-C6 alkoxy, halo, trifluoromethyl or trifluoromethoxy; R2 and R3 are H, C1-C6 alkyl, phenyl-(CH2)0-3—, halo and C1-C3 perfluoroalkyl where phenyl can be substituted with C1-C6 alkyl, C1-C6 alkoxy, halo, trifluoromethyl or trifluoromethoxy; R4 is —CHR5CO2H or —CH2-tetrazole where R5 is H or benzyl; and n=0 or 1; or a pharmaceutically acceptable salt or ester form thereof.
摘要翻译：本发明提供新的化合物，药物组合物和治疗哺乳动物血栓形成障碍的方法，具有下式的化合物：其中：Ar是苯基，萘基，呋喃基，苯并呋喃基，吲哚基，吡唑基，恶唑基，芴基，苯基环烷烃，其中环烷烃可以是环丙基，环丁基，环戊基或环己基，Ar可以任选被1至3个选自C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，苯基 - （CH 2）0-6-，苯基 - （CH 2），C 3 -C 6环烷基， - （CH 2）-C 3 -C 6环烷基，卤素，C 1 -C 3全芳基烷基和C 1 -C 3全氟烷氧基，其中苯基可以被1至3个选自C 1 -C 6烷基，C 1 -C 6烷氧基，苯基，卤素，三氟甲基或三氟甲氧基; R 1是氢，C 1 -C 6烷基或苯基 - （CH 2）1-6 - ，其中苯基可以被C 1 -C 6烷基，C 1 -C 6烷氧基，卤素，三氟甲基或三氟甲氧基取代; R 2和R 3是H，C 1 -C 6烷基，苯基 - （CH 2）0-3-，卤素和C 1 -C 3全氟烷基，其中苯基可以被C 1 -C 6烷基，C 1 -C 6烷氧基，卤素，三氟甲基或三氟甲氧基取代; R4是-CHR5CO2H或-CH2-四唑，其中R5是H或苄基; 并且n = 0或1; 或其药学上可接受的盐或酯形式。

3. 发明申请

US20090197878A1 SUBSTITUTED BENZO[d][1,3]OXAZIN-2(4H)-ONES AND RELATED DERIVATIVES AND THEIR USES FOR MODULATING THE PROGESTERONE RECEPTOR 审中-公开
标题翻译：取代的苄基[d] [1,3]氧化亚-2（4H） - 酮及相关衍生物及其用于调节前列腺素受体的用途
公开(公告)号：US20090197878A1
公开(公告)日：2009-08-06
申请号：US12361764
申请日：2009-01-29
申请人： Thomas Joseph Commons , Douglas John Jenkins , Eugene John Trybulski , Andrew Fensome
发明人： Thomas Joseph Commons , Douglas John Jenkins , Eugene John Trybulski , Andrew Fensome
IPC分类号： A61K31/536 , C07D215/227 , C07D265/18 , A61P15/00 , A61K31/537 , A61K31/4704
CPC分类号： C07D265/18 , C07D215/227 , C07D413/06
摘要： Compounds of formula (I), or pharmaceutically acceptable salts thereof, are provided, wherein R1-R6 and X are defined herein. Also provided are methods of preparing the compounds of formula (I), pharmaceutical compositions and kits containing a compound of formula (I), as are methods of treating endometriosis, hormone-dependent carcinomas, leiomyoma, fibroids, dysfunctional bleeding, polycystic ovary syndrome, and menopause related symptoms; methods of contraception; methods of providing hormone replacement therapy; methods of stimulating food intake; methods of synchronizing estrus; and methods of treating symptoms of premenstrual syndrome and premenstrual dysphoric disorder by administering to a mammal in need thereof a pharmaceutically effective amount of a compound of formula (I).
摘要翻译：提供式（I）化合物或其药学上可接受的盐，其中R 1 -R 6和X如本文所定义。还提供了制备式（I）化合物，含有式（I）化合物的药物组合物和试剂盒的方法，以及治疗子宫内膜异位，激素依赖性癌，平滑肌瘤，肌瘤，功能障碍性出血，多囊卵巢综合征，和更年期相关的症状; 避孕方法; 提供激素替代疗法的方法; 刺激食物摄入的方法; 发情同步的方法以及通过向有需要的哺乳动物施用药学有效量的式（I）化合物来治疗经前期综合征和经前期焦虑症的症状的方法。

4. 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。

5. 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。

6. 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。

7. 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。

8. 发明申请

US20090093469A1 Phenylaminopropanol Derivatives and Methods of Their Use 审中-公开
公开(公告)号：US20090093469A1
公开(公告)日：2009-04-09
申请号：US12335245
申请日：2008-12-15
申请人： 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
发明人： 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分类号： 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分类号： C07D209/08 , C07D209/30 , C07D209/42 , C07D235/06 , C07D241/42 , C07D265/36 , C07D471/04
摘要： 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.

9. 发明授权

US07326700B2 Cyclohexenyl phenyl carboxamides tocolytic oxytocin receptor antagonists 失效
标题翻译：环己烯基苯基甲酰胺溶血性催产素受体拮抗剂
公开(公告)号：US07326700B2
公开(公告)日：2008-02-05
申请号：US10119453
申请日：2002-04-10
申请人： Amedeo Arturo Failli , Eugene John Trybulski , Jay Scott Shumsky , William Jennings Sanders
发明人： Amedeo Arturo Failli , Eugene John Trybulski , Jay Scott Shumsky , William Jennings Sanders
IPC分类号： A61P15/00 , A61K31/55 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides tricyclic carboxamide compounds and methods and pharmaceutical compositions for their use in treatment, prevention, or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and/or suppression of preterm labor, suppression of labor at term prior to caesarean deliver, 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：本发明提供三环羧酰胺化合物及其用于治疗，预防或抑制可通过催产素拮抗剂活性补救或缓解的疾病的方法和药物组合物，包括预防和/或抑制早产，抑制术中的劳动在剖宫产之前，以及治疗痛经。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。

10. 发明授权

US06903087B2 Pyrido cyclohexenyl phenyl carboxamides tocolytic oxytocin receptor antagonists 失效
标题翻译：吡啶环己烯基苯基甲酰胺，溶解性催产素受体拮抗剂
公开(公告)号：US06903087B2
公开(公告)日：2005-06-07
申请号：US10119894
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： A61K31/194 , A61K31/5517 , A61P3/00 , A61P5/10 , A61P5/24 , A61P7/00 , A61P7/02 , A61P9/04 , A61P9/08 , A61P9/12 , A61P15/00 , A61P15/06 , A61P25/00 , A61P25/22 , A61P27/02 , A61P27/06 , A61P27/16 , A61P43/00 , C07D471/14 , C07D487/04 , A61K31/33 , A61K31/55 , C07D487/12
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention provides novel tricyclic pyridyl carboxamides as well as methods and pharmaceutical compositions utilizing them compounds 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 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：本发明提供新颖的三环吡啶羧酰胺以及利用它们的化合物用于治疗和/或预防和/或抑制可由催产素拮抗剂活性补救或缓解的疾病的方法和药物组合物，包括预防和/或抑制早产剖宫产分娩期间的劳动，劳动抑制和痛经治疗。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。

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