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11. 发明授权

US6066654A Methods for treating disorders associated with the central nervous system using optically pure (-) cisapride 失效
标题翻译：使用光学纯（ - ）西沙必利治疗与中枢神经系统相关疾病的方法
公开(公告)号：US6066654A
公开(公告)日：2000-05-23
申请号：US329328
申请日：1999-06-10
申请人： Nancy M. Gray , James W. Young
发明人： Nancy M. Gray , James W. Young
IPC分类号： C07D211/62 , A61K31/445 , A61K31/4468 , A61P1/00 , A61P1/08 , A61P1/10 , A61P1/14
CPC分类号： A61K31/445 , A61K31/4468
摘要： Methods are disclosed utilizing the optically pure (-) isomer of cisapride. The (-) isomer of cisapride also exhibits longer duration of action than does racemic cisapride and is useful for treatment of disorders of the central nervous system.
摘要翻译：公开利用西沙必利的光学纯（ - ）异构体的方法。西沙必利的（ - ）异构体也表现出比外消旋西沙必利更长的作用时间，并且可用于治疗中枢神经系统疾病。

12. 发明授权

US5698558A Methods for treating allergic disorders using optically pure (-) cetirizine 失效
标题翻译：使用光学纯（ - ）西替利嗪治疗过敏性疾病的方法
公开(公告)号：US5698558A
公开(公告)日：1997-12-16
申请号：US789502
申请日：1997-01-27
申请人： Nancy M. Gray
发明人： Nancy M. Gray
IPC分类号： C07D241/04 , A61K31/495 , A61P11/00 , A61P37/08
CPC分类号： A61K31/495
摘要： Methods are disclosed utilizing optically pure (-) cetirizine for the treatment of seasonal and perennial allergic rhinitis in humans while avoiding the concomitant liability of adverse effects associated with the racemic mixture of cetirizine. The optically pure (-) isomer is also useful for the treatment of allergic asthma.
摘要翻译：公开了利用光学纯（ - ）西替利嗪治疗人类季节性和常年性过敏性鼻炎的方法，同时避免与西替利嗪的外消旋混合物相关的副作用的伴随责任。光学纯的（ - ）异构体也可用于治疗过敏性哮喘。

13. 发明授权

US5474997A Methods and compositions of (2R,4S) itraconazole for treating fungal yeast and dermatophyte infections 失效
标题翻译：（2R，4S）伊曲康唑用于治疗真菌酵母和皮肤癣菌感染的方法和组成
公开(公告)号：US5474997A
公开(公告)日：1995-12-12
申请号：US341266
申请日：1994-11-17
申请人： Nancy M. Gray , Raymond L. Woosley
发明人： Nancy M. Gray , Raymond L. Woosley
IPC分类号： C07D405/14 , A61K31/495 , A61P31/04 , A61K31/50
CPC分类号： A61K31/495
摘要： Methods and compositions are disclosed utilizing the optically pure (2R,4S) isomer of itraconazole. This compound is a potent drug for the treatment of local and systemic fungal, yeast, and dermatophyte infections, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of itraconazole.
摘要翻译：公开利用伊曲康唑的光学纯的（2R，4S）异构体的方法和组合物。该化合物是治疗局部和全身真菌，酵母和皮肤癣菌感染的有效药物，同时避免与伊曲康唑外消旋混合物相关的副作用的伴随责任。

14. 发明授权

US5331000A Antipyretic and analgesic methods and compositions containing optically pure R(-) ketoprofen 失效
标题翻译：解热止痛方法和含有光学纯的R（ - ）酮洛芬的组合物
公开(公告)号：US5331000A
公开(公告)日：1994-07-19
申请号：US24728
申请日：1993-03-01
申请人： James W. Young , Nancy M. Gray , William J. Wechter
发明人： James W. Young , Nancy M. Gray , William J. Wechter
IPC分类号： A61K31/192 , A61K31/19 , A61P25/04 , A61P29/00
CPC分类号： A61K31/19
摘要： Methods and compositions are disclosed utilizing optically pure R(-) ketoprofen for the treatment of pain including, but not limited to, pain associated with toothaches, headaches, sprains, joint pain and post-surgical pain, for example dental pain and ophthalmic pain, while substantially reducing adverse effects including, but not limited to, gastrointestinal, renal and hepatic toxicities, and leukopenia, which are associated with the administration of racemic ketoprofen. Optically pure R(-) ketoprofen is also useful in treating pyrexia while substantially reducing the adverse effects associated with the administration of racemic ketoprofen.
摘要翻译：公开了使用光学纯的R（ - ）酮洛芬用于治疗疼痛的方法和组合物，包括但不限于与牙痛，头痛，扭伤，关节疼痛和手术后疼痛相关的疼痛，例如牙痛和眼痛，同时显着降低与外消旋酮洛芬的施用相关的不良反应，包括但不限于胃肠道，肾脏和肝脏毒性以及白细胞减少。光学纯的R（ - ）酮洛芬也可用于治疗发热，同时显着减少与外消旋酮洛芬的给药相关的不良反应。

15. 发明授权

US5215992A Ethanobicyclic amine derivatives for CNS disorders 失效
标题翻译：用于CNS障碍的乙二醇胺衍生物
公开(公告)号：US5215992A
公开(公告)日：1993-06-01
申请号：US801148
申请日：1991-12-02
申请人： Nancy M. Gray , Brian K. Cheng
发明人： Nancy M. Gray , Brian K. Cheng
IPC分类号： C07D295/02 , C07D295/033
CPC分类号： C07D295/033 , C07C2103/68 , C07C2103/72
摘要： Certain ethanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, phenalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.11 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.12 and R.sup.13 is independently selected from hydrido, hydroxy, alkyl phenalkyl, phenyl, alkoxy, fluoroalkyl and fluoro; wherein m is one or two; wherein p is a number selected from zero through four, inclusive; wherein each of q and r is a number independently selected from one through three, inclusive with the proviso that sum of q and r is a number from three through six, inclusive; with the further proviso that the nitrogen-containing cyclohetero moiety must be attached at one position selected from R.sup.3, R.sup.4, ring-position two, and ring-position three; or the pharmaceutically-acceptable salts thereof.
摘要翻译：描述了某些乙酰胆碱胺化合物用于治疗中枢神经系统疾病如精神病，抽搐，肌张力障碍和脑缺血。特别感兴趣的化合物具有式“IMAGE”，其中R 1，R 2，R 3，R 4，Y和Z各自独立地选自氢，羟基，烷基，环烷基，环烷基烷基，苯烷基，苯基，烷氧基，苯氧基，苯烷氧基，烷氧基烷基，卤素，卤代烷基和羟基烷基; 其中R 3和R 4可以一起形成氧代; 其中R 5，R 6，R 7，R 8，R 9和R 10各自独立地选自氢，烷基，环烷基，羟烷基，氟烷基，环烷基烷基，烷氧基烷基，苯烷基和苯基; 其中含氮环杂环部分中的G选自其中R 11选自氢，烷基，环烷基，环烷基烷基，苯基，苯烷基，烷氧基烷基和羟烷基; 其中R 12和R 13各自独立地选自氢，羟基，烷基苯基烷基，苯基，烷氧基，氟烷基和氟; 其中m是一个或两个; 其中p是选自0至4的数字，包括端值; 其中q和r各自独立地选自1至3个，其中q和r之和是3至6的数，包括3和6的数。进一步的条件是含氮环杂环部分必须连接在选自R3，R4，环2位和环3位的一个位置上; 或其药学上可接受的盐。

16. 发明授权

US5130330A Nitrogen-containing cyclohetero cycloalkylaminoaryl derivatives for CNS disorders 失效
标题翻译：用于CNS疾病的含氮环己基氨基胆碱衍生物
公开(公告)号：US5130330A
公开(公告)日：1992-07-14
申请号：US473008
申请日：1990-01-31
申请人： Brian R. de Costa , Kenner C. Rice , Nancy M. Gray , Patricia C. Contreras , Arthur E. Jacobson , Andrew Thurkauf , Lilian A. Radesca , Wayne D. Bowen
发明人： Brian R. de Costa , Kenner C. Rice , Nancy M. Gray , Patricia C. Contreras , Arthur E. Jacobson , Andrew Thurkauf , Lilian A. Radesca , Wayne D. Bowen
IPC分类号： A61K31/40 , A61K31/4025 , A61P25/00 , C07D295/12 , C07D295/135 , C07D405/12
CPC分类号： C07D295/135
摘要： Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders and convulsions. Compounds of particular interest are of the formula ##STR1## wherein R.sup.1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms, and loweralkenylloweralkyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and loweralkyl; wherein each of R.sup.4 through R.sup.7, R.sup.10 and R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is a number selected from four through six; wherein p is a number selected from zero through four; wherein q is a number selected from three through five; wherein A is selected from phenyl, naphthyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述某些含氮环杂环烷基氨基芳基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和惊厥。特别感兴趣的化合物具有下式：其中R 1选自4至6个碳原子的氢，低级烷基，环烷基烷基和低级链烯基低级烷基; 其中R2和R3各自独立地选自氢和低级烷基; 其中R 4至R 7，R 10和R 11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中n是选自四至六的数; 其中p是选自零至四的数字; 其中q是选自三至五的数; 其中A选自苯基，萘基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。或其药学上可接受的盐。

17. 发明授权

US5098916A Propanobicyclic amine derivatives for CNS disorders 失效
标题翻译：中枢神经系统疾病的丙酰胆碱胺衍生物
公开(公告)号：US5098916A
公开(公告)日：1992-03-24
申请号：US501216
申请日：1990-03-29
申请人： Nancy M. Gray , Brian K. Cheng
发明人： Nancy M. Gray , Brian K. Cheng
IPC分类号： A61K31/445 , A61K31/495 , A61P9/10 , A61P25/00 , C07C211/38 , C07C211/42 , C07D295/02 , C07D295/03 , C07D295/033 , C07D295/08 , C07D295/088
CPC分类号： C07D295/088 , C07C211/42 , C07D295/03 , C07D295/033 , C07C2103/78
摘要： Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.17 is independently selected from hydrido, hydroxy, alkyl, phenalkyl, phenyl, alkoxy, fluoroalkyl and fluoro; wherein m is one or two; wherein p is a number selected from zero through four, inclusive; wherein each of q and r is a number independently selected from one through three, inclusive, with the proviso that sum of q and r is a number from three through six, inclusive; with the further proviso that the nitrogen-containing cyclohetero moiety must be attached at one position selected from R.sup.3, R.sup.4, ring-position two, ring-position three and ring-position four; or the pharmaceutically-acceptable salts thereof.

18. 发明授权

US5629328A Methods for treating gastro-esophageal reflux disease and other disorders associated with the digestive tract using optically pure (+) cisapride 失效
标题翻译：使用光学纯（+）西沙必利治疗胃食管反流病和与消化道相关的其他疾病的方法
公开(公告)号：US5629328A
公开(公告)日：1997-05-13
申请号：US135769
申请日：1993-10-12
申请人： Nancy M. Gray , James W. Young
发明人： Nancy M. Gray , James W. Young
IPC分类号： C07D211/62 , A61K31/445 , A61K31/4468 , A61P1/00 , A61P1/08 , A61P1/10 , A61P1/14
CPC分类号： A61K31/445 , A61K31/4468
摘要： Methods are disclosed utilizing the optically pure (+) isomer of cisapride. This compound is useful in treating emesis while substantially reducing adverse effects associated with racemic cisapride.
摘要翻译：公开利用西沙必利的光学纯（+）异构体的方法。该化合物可用于治疗呕吐，同时显着降低与西西沙必利素有关的不良反应。

19. 发明授权

US5618828A Methods for treating gastro-esophageal reflux disease and emesis with optically pure (-) cisapride 失效
标题翻译：用光学纯（ - ）西沙必利治疗胃食管反流病和呕吐的方法
公开(公告)号：US5618828A
公开(公告)日：1997-04-08
申请号：US135776
申请日：1993-10-12
申请人： Nancy M. Gray , James W. Young
发明人： Nancy M. Gray , James W. Young
IPC分类号： C07D211/62 , A61K31/445 , A61K31/4468 , A61P1/00 , A61P1/08 , A61P1/10 , A61P1/14
CPC分类号： A61K31/445 , A61K31/4468
摘要： Methods are disclosed utilizing the optically pure (-) isomer of cisapride. This compound is a potent drug for the treatment of gastro-esophageal reflux disease while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of cisapride. This compound is also useful in treating or preventing emesis while substantially reducing adverse effects associated with racemic cisapride.
摘要翻译：公开利用西沙必利的光学纯（ - ）异构体的方法。该化合物是用于治疗胃食管反流疾病的有效药物，同时显着减少与西沙必利的外消旋混合物相关的副作用的伴随的责任。该化合物也可用于治疗或预防呕吐，同时显着降低与西西沙必利素有关的不良反应。

20. 发明授权

US5510352A Methods of using (+) doxazosin for the treatment of hypertension 失效
标题翻译：使用（+）多沙唑嗪治疗高血压的方法
公开(公告)号：US5510352A
公开(公告)日：1996-04-23
申请号：US207802
申请日：1994-03-07
申请人： Nancy M. Gray
发明人： Nancy M. Gray
IPC分类号： C07D405/12 , A61K31/505 , A61P9/10 , A61K31/495
CPC分类号： A61K31/505
摘要： Methods are disclosed utilizing the optically pure (+) isomer of doxazosin. This compound is a potent drug for the treatment of hypertension while avoiding the concomitant liability of adverse effects associated with the racemic mixture of doxazosin.
摘要翻译：利用多沙唑嗪的光学纯（+）异构体公开了方法。该化合物是治疗高血压的有效药物，同时避免与多沙唑嗪的外消旋混合物相关的副作用的伴随责任。

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