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1. 发明授权

US07141563B2 Process for the preparation of 1, 2, 3, 4, 8, 9, 10, 10a-octahydro-7bH-cyclopenta[b] [1, 4]diazepino[6, 7, 1-hi] indole derivatives 失效
标题翻译：制备1,2,3,4,8,9,10,10a-八氢-7H-环戊二烯并[b] [1,4]二氮杂[6,7-i-hi]吲哚衍生物的方法
公开(公告)号：US07141563B2
公开(公告)日：2006-11-28
申请号：US10016418
申请日：2001-11-02
申请人： Gregory S. Welmaker , Joan E. Sabalski , Michael D. Smith
发明人： Gregory S. Welmaker , Joan E. Sabalski , Michael D. Smith
IPC分类号： C07D243/00 , C07D487/00
CPC分类号： C07D209/94 , C07D487/06
摘要： This invention provides processes for preparing compounds formula: wherein R is H, alkyl, acyl, aryl, aroyl or —C(O)R′; R′ is alkyl or aryl; R1, R2, R4 and R5 are H, —OH, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl or alkoxy, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, acyl, aryl or aroyl; R3 is H, alkyl, cycloalkyl, alkoxy, fluorinated alkyl, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; or a pharmaceutically acceptable salt thereof, as well as novel compounds useful in the synthesis of these compounds.
摘要翻译：本发明提供制备下式化合物的方法：其中R为H，烷基，酰基，芳基，芳酰基或-C（O）R'; R'是烷基或芳基; R 1，R 2，R 4和R 5是H，-OH，烷基，环烷基，烷氧基卤素，氟化烷基或烷氧基，-CN，-NH-SO 2 - 烷基，-SO 2 -NH-烷基，烷基酰胺，氨基，烷基氨基，二烷基氨基，酰基，芳基或芳酰基; R 3是H，烷基，环烷基，烷氧基，氟化烷基，-NH-SO 2 - 烷基，-SO 2 -NH-烷基，烷基酰胺，氨基，烷基氨基，二烷基氨基，氟化烷氧基，酰基，芳基或芳酰基; 或其药学上可接受的盐，以及可用于合成这些化合物的新化合物。

2. 发明授权

US07351839B2 Process for the preparation of 1,2,3,4,8,9,10, 10a-octahydro-7bH-cyclopenta[b][1,4]diazepino-[6,7,1-hi]indole derivatives 失效
标题翻译：制备1,2,3,4,8,9,10,10a-八氢-7H-环戊二烯并[b] [1,4]二氮杂 - [6,7,1-hi]吲哚衍生物的方法
公开(公告)号：US07351839B2
公开(公告)日：2008-04-01
申请号：US11602531
申请日：2006-11-21
申请人： Gregory S. Welmaker , Joan E. Sabalski , Michael D. Smith
发明人： Gregory S. Welmaker , Joan E. Sabalski , Michael D. Smith
IPC分类号： C07D209/82
CPC分类号： C07D209/94 , C07D487/06
摘要： This invention provides processes for preparing compounds formula: wherein R is H, alkyl, acyl, aryl, aroyl or —C(O)R′; R′ is alkyl or aryl; R1, R2, R4 and R5 are H, —OH, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl or alkoxy, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, acyl, aryl or aroyl; R3 is H, alkyl, cycloalkyl, alkoxy, fluorinated alkyl, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; or a pharmaceutically acceptable salt thereof, as well as novel compounds useful in the synthesis of these compounds.
摘要翻译：本发明提供制备下式化合物的方法：其中R为H，烷基，酰基，芳基，芳酰基或-C（O）R'; R'是烷基或芳基; R 1，R 2，R 4和R 5是H，-OH，烷基，环烷基，烷氧基卤素，氟化烷基或烷氧基，-CN，-NH-SO 2 - 烷基，-SO 2 -NH-烷基，烷基酰胺，氨基，烷基氨基，二烷基氨基，酰基，芳基或芳酰基; R 3是H，烷基，环烷基，烷氧基，氟化烷基，-NH-SO 2 - 烷基，-SO 2 -NH-烷基，烷基酰胺，氨基，烷基氨基，二烷基氨基，氟化烷氧基，酰基，芳基或芳酰基; 或其药学上可接受的盐，以及用于合成这些化合物的新化合物。

3. 发明授权

US07601856B2 Benzofurans as potassium ion channel modulators 失效
标题翻译：苯并呋喃作为钾离子通道调节剂
公开(公告)号：US07601856B2
公开(公告)日：2009-10-13
申请号：US11828457
申请日：2007-07-26
申请人： Gregory S. Welmaker , Matthew A. Wilson , Geraldine McFarlane , Joan E. Sabalski , John A. Butera , Eugene J. Trybulski , David R. Herbst
发明人： Gregory S. Welmaker , Matthew A. Wilson , Geraldine McFarlane , Joan E. Sabalski , John A. Butera , Eugene J. Trybulski , David R. Herbst
IPC分类号： C07D307/90
CPC分类号： C07D307/91 , C07D307/93 , C07D405/12 , C07D407/12 , C07D409/12 , C07D491/113
摘要： The present invention is directed to compounds of Formula I: that are potassium channel modulators and pharmaceutical compositions thereof. The present invention is further directed to methods of treatment using the compounds and pharmaceutical compositions of the invention. The present invention is still further directed to synthetic processes for producing the compounds of the invention.
摘要翻译：本发明涉及式I化合物：其是钾通道调节剂及其药物组合物。本发明还涉及使用本发明的化合物和药物组合物的治疗方法。本发明还涉及用于制备本发明化合物的合成方法。

4. 发明授权

US07271163B2 Cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives 失效
标题翻译：环戊基[b] [1,4]二氮杂[6,7,1-hi]吲哚及其衍生物
公开(公告)号：US07271163B2
公开(公告)日：2007-09-18
申请号：US10898029
申请日：2004-07-23
申请人： Annmarie L. Sabb , Robert L. Vogel , James A. Nelson , Sharon J. Rosenzweig-Lipson , Gregory S. Welmaker , Joan E. Sabalski
发明人： Annmarie L. Sabb , Robert L. Vogel , James A. Nelson , Sharon J. Rosenzweig-Lipson , Gregory S. Welmaker , Joan E. Sabalski
IPC分类号： A61K31/55 , A61P25/00 , A61P25/24 , C07D243/00
CPC分类号： C07D209/94 , A61K31/55 , C07D487/06
摘要： This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing these compounds and methods for their use, including treatment of obsessive-compulsive disorder, panic disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.
摘要翻译：本发明提供下式的化合物：其中：R 1是氢，-C（O）CH 3或1-6个碳原子的烷基; R 2和R 3各自独立地为氢，1-6个碳原子的烷基，环烷基，1-6个碳原子的烷氧基，-CH 2 1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺，1-6个碳原子的烷基氨基，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1个碳原子的氟代烷氧基 -6个碳原子，2-7个碳原子的酰基，芳基或芳酰基; R 4和R 5各自独立地为氢，1-6个碳原子的烷基，1-6个碳原子的烷氧基，卤素，氟烷基，-CN，烷基 1-6个碳原子的磺酰胺，1-6个碳原子的烷基酰胺，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，1-6个碳原子的氟烷氧基，2- 7个碳原子或芳酰基; R 6和R 7各自独立地为氢，C 1 -C 6烷基或环烷基; 或其药学上可接受的盐，以及含有这些化合物的药物组合物及其使用方法，包括治疗强迫症，恐慌症，抑郁症，焦虑症，广泛性焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，肥胖，癫痫和脊髓损伤。

5. 发明授权

US07399778B2 Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole 失效
标题翻译：含有唑类的β-淀粉样蛋白产生的杂环磺酰胺抑制剂
公开(公告)号：US07399778B2
公开(公告)日：2008-07-15
申请号：US11035005
申请日：2005-01-13
申请人： Lynn Resnick , Donna M. Huryn , Joan E. Sabalski , Joshua D. Berkowitz , Anthony Frank Kreft , Dennis Martin Kubrak , Thomas Joseph Caggiano , Koi Michele Morris
发明人： Lynn Resnick , Donna M. Huryn , Joan E. Sabalski , Joshua D. Berkowitz , Anthony Frank Kreft , Dennis Martin Kubrak , Thomas Joseph Caggiano , Koi Michele Morris
IPC分类号： A61K31/415 , C07D233/00
CPC分类号： A61K31/416 , C07D231/12 , C07D409/12
摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.
摘要翻译：提供了可用于降低β淀粉样蛋白水平的化合物。化合物具有式Ia的结构：其中R 1是低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2， / 5> 5

6. 发明申请

US20080249150A1 HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION CONTAINING AN AZOLE 失效
标题翻译：含有氨基酸的淀粉酶生产的杂环磺酰胺抑制剂
公开(公告)号：US20080249150A1
公开(公告)日：2008-10-09
申请号：US12142306
申请日：2008-06-19
申请人： Lynn Resnick , Donna M. Huryn , Joan E. Sabalski , Joshua D. Berkowitz , Anthony Frank Kreft , Dennis Martin Kubrak , Thomas Joseph Caggiano , Koi Michele Morris
发明人： Lynn Resnick , Donna M. Huryn , Joan E. Sabalski , Joshua D. Berkowitz , Anthony Frank Kreft , Dennis Martin Kubrak , Thomas Joseph Caggiano , Koi Michele Morris
IPC分类号： A61K31/4196 , C07D409/02 , A61K31/415 , A61P25/28 , C07D231/12
CPC分类号： A61K31/416 , C07D231/12 , C07D409/12
摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.
摘要翻译：提供了可用于降低β淀粉样蛋白水平的化合物。化合物具有式Ia的结构：其中R 1是低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2， / 5> 5

7. 发明申请

US20100144812A1 Heterocyclic Sulfonamide Inhibitors of Beta Amyloid Production Containing an Azole 审中-公开
标题翻译：包含唑类的β淀粉样蛋白的杂环磺酰胺抑制剂
公开(公告)号：US20100144812A1
公开(公告)日：2010-06-10
申请号：US12708557
申请日：2010-02-19
申请人： Lynn Resnick , Donna M. Huryn , Joan E. Sabalski , Joshua D. Berkowitz , Anthony Frank Kreft , Dennis Martin Kubrak , Thomas Joseph Caggiano , Koi Michele Morris
发明人： Lynn Resnick , Donna M. Huryn , Joan E. Sabalski , Joshua D. Berkowitz , Anthony Frank Kreft , Dennis Martin Kubrak , Thomas Joseph Caggiano , Koi Michele Morris
IPC分类号： A61K31/4155 , A61K31/415 , A61K31/41 , A61K31/4178 , A61K31/4025 , A61P25/28 , A61P25/00 , C07D409/02 , C07D231/10
CPC分类号： A61K31/416 , C07D231/12 , C07D409/12
摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.
摘要翻译：提供了可用于降低β淀粉样蛋白水平的化合物。所述化合物具有式Ia的结构：其中，R 1为低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2 R 5; R5是苯基，取代的苯基，杂环，取代的杂环，烷基或取代的烷基; R2是低级烷基，取代的低级烷基，CF3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基或环烷基; R3是氢，低级烷基或取代的低级烷基; R4是苯基，取代的苯基，杂环，取代的杂环，噻吩或取代的噻吩; R 6是氢，低级烷基，取代的低级烷基，CF 3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基，环烷基或取代的环烷基; W，X和Y独立地为CR 7或N; 并且R 7是氢，卤素，低级烷基或取代的低级烷基。

8. 发明授权

US07674813B2 Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole 失效
标题翻译：含有唑类的β-淀粉样蛋白产生的杂环磺酰胺抑制剂
公开(公告)号：US07674813B2
公开(公告)日：2010-03-09
申请号：US12142306
申请日：2008-06-19
申请人： Lynn Resnick , Donna M. Huryn , Joan E. Sabalski , Joshua D. Berkowitz , Anthony Frank Kreft , Dennis Martin Kubrak , Thomas Joseph Caggiano , Koi Michele Morris
发明人： Lynn Resnick , Donna M. Huryn , Joan E. Sabalski , Joshua D. Berkowitz , Anthony Frank Kreft , Dennis Martin Kubrak , Thomas Joseph Caggiano , Koi Michele Morris
IPC分类号： A01N43/50 , A01N43/56 , C07D231/00
CPC分类号： A61K31/416 , C07D231/12 , C07D409/12
摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.
摘要翻译：提供了可用于降低β淀粉样蛋白水平的化合物。所述化合物具有式Ia的结构：其中，R 1为低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2 R 5; R5是苯基，取代的苯基，杂环，取代的杂环，烷基或取代的烷基; R2是低级烷基，取代的低级烷基，CF3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基或环烷基; R3是氢，低级烷基或取代的低级烷基; R4是苯基，取代的苯基，杂环，取代的杂环，噻吩或取代的噻吩; R 6是氢，低级烷基，取代的低级烷基，CF 3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基，环烷基或取代的环烷基; W，X和Y独立地为CR 7或N; 并且R 7是氢，卤素，低级烷基或取代的低级烷基。

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