公开(公告)号：US6121459A

公开(公告)日：2000-09-19

申请号：US355227

申请日：1999-12-23

申请人： Mark Alan Schwindt ,  Lloyd Charles Franklin ,  Haile Tecle

发明人： Mark Alan Schwindt ,  Lloyd Charles Franklin ,  Haile Tecle

IPC分类号： A61K31/439 ,  A61P25/28 ,  C07D453/02 ,  C07D487/08

CPC分类号： C07D487/08 ,  C07D453/02

摘要： Biologically active O-substituted azabicyclo oximes having the Z configuration may be isolated simply, without chromatographic separation, and in high yield and Z/E purity through the coupling of a 1-azabicyclo-3-one with an O-substituted hydroxylamine in acidic aqueous solution and conversion of E-configured isomer to Z-isomer without requiring purification or separation. Neutralization and subsequent isolation of the free base followed by precipitation of the salt allows separation of the Z-isomer with high Z/E purity.

摘要翻译： PCT No.PCT / US97 / 23872 Sec。 371 1999年12月23日第 102（e）1999年12月23日PCT 1997年12月29日PCT PCT。 出版物WO98 / 32758 日期1998年7月30日具有Z构型的生物活性O-取代的氮杂双环肟可以简单地分离，无色谱分离，通过1-氮杂双环-3-酮与O- 在酸性水溶液中取代羟胺，并将E构型异构体转化为Z-异构体，无需纯化或分离。 中和并随后分离游离碱，随后沉淀盐允许以高Z / E纯度分离Z-异构体。

公开(公告)号：US06342529B1

公开(公告)日：2002-01-29

申请号：US09243946

申请日：1999-02-04

申请人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

发明人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

IPC分类号： A61K31195

CPC分类号： A61K31/197 ,  C07C69/34 ,  C07C69/675 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07C2601/14 ,  C07D263/22 ,  C07D263/26 ,  G11B20/1426 ,  G11B27/3027

摘要： A compound of the formula wherein R1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R2 is hydrogen or methyl; and R3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

摘要翻译： 式R 1的化合物是具有1至6个碳原子的直链或支链烷基，苯基或具有3至6个碳原子的环烷基; R2是氢或甲基; 并且R 3是氢，甲基或羧基; 其用于治疗癫痫发作。 公开了用于制备化合物的方法。 还公开了在合成化合物期间制备的中间体。

公开(公告)号：US06359169B1

公开(公告)日：2002-03-19

申请号：US08732065

申请日：1996-10-16

申请人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

发明人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

IPC分类号： C07C6934

CPC分类号： A61K31/197 ,  C07C69/34 ,  C07C69/675 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07C2601/14 ,  C07D263/22 ,  C07D263/26 ,  G11B20/1426 ,  G11B27/3027

摘要： A compound of the formula wherein R1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R2 is hydrogen or methyl; and R3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

公开(公告)号：US5710304A

公开(公告)日：1998-01-20

申请号：US733102

申请日：1996-10-16

申请人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

发明人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

IPC分类号： A61K31/197 ,  C07C69/34 ,  C07C69/675 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07D263/22 ,  C07D263/26 ,  G11B20/14 ,  G11B27/30 ,  C07C303/00

CPC分类号： A61K31/197 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07C69/34 ,  C07C69/675 ,  C07D263/22 ,  C07D263/26 ,  G11B20/1426 ,  G11B27/3027 ,  C07C2101/14

摘要： A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

公开(公告)号：US06414024B1

公开(公告)日：2002-07-02

申请号：US09244700

申请日：1999-02-04

申请人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

发明人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

IPC分类号： A61K31195

CPC分类号： A61K31/197 ,  C07C69/34 ,  C07C69/675 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07C2601/14 ,  C07D263/22 ,  C07D263/26 ,  G11B20/1426 ,  G11B27/3027

摘要： A compound of the formula wherein R1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R2 is hydrogen or methyl; and R3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

公开(公告)号：US06117906A

公开(公告)日：2000-09-12

申请号：US244699

申请日：1999-02-04

申请人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

发明人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

IPC分类号： A61K31/197 ,  C07C69/34 ,  C07C69/675 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07D263/22 ,  C07D263/26 ,  G11B20/14 ,  G11B27/30 ,  A61K31/195

CPC分类号： A61K31/197 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07C69/34 ,  C07C69/675 ,  C07D263/22 ,  C07D263/26 ,  G11B20/1426 ,  G11B27/3027 ,  C07C2101/14

摘要： A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

摘要翻译： 下式化合物其中R 1是具有1至6个碳原子的直链或支链烷基，苯基或具有3至6个碳原子的环烷基; R2是氢或甲基; 并且R 3是氢，甲基或羧基; 其用于治疗癫痫发作。 公开了用于制备化合物的方法。 还公开了在合成化合物期间制备的中间体。

公开(公告)号：US5684189A

公开(公告)日：1997-11-04

申请号：US420576

申请日：1995-04-12

申请人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

发明人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

IPC分类号： A61K31/197 ,  C07C69/34 ,  C07C69/675 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07D263/22 ,  C07D263/26 ,  G11B20/14 ,  G11B27/30 ,  C07C205/00

CPC分类号： A61K31/197 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07C69/34 ,  C07C69/675 ,  C07D263/22 ,  C07D263/26 ,  G11B20/1426 ,  G11B27/3027 ,  C07C2101/14

摘要： A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

公开(公告)号：US06525096B1

公开(公告)日：2003-02-25

申请号：US09244313

申请日：1999-02-04

申请人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

发明人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

IPC分类号： A61K31195

CPC分类号： A61K31/197 ,  C07C69/34 ,  C07C69/675 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07C2601/14 ,  C07D263/22 ,  C07D263/26 ,  G11B20/1426 ,  G11B27/3027

摘要： A compound of the formula wherein R1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R2 is hydrogen or methyl; and R3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

公开(公告)号：US06255345B1

公开(公告)日：2001-07-03

申请号：US09244676

申请日：1999-02-04

申请人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

发明人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

IPC分类号： A61K31195

CPC分类号： A61K31/197 ,  C07C69/34 ,  C07C69/675 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07C2601/14 ,  C07D263/22 ,  C07D263/26 ,  G11B20/1426 ,  G11B27/3027

摘要： A compound of the formula wherein R1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R2 is hydrogen or methyl; and R3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

公开(公告)号：US5847151A

公开(公告)日：1998-12-08

申请号：US891470

申请日：1997-07-10

申请人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

发明人： Richard B. Silverman ,  Ryszard Andruszkiewicz ,  Po-Wai Yuen ,  Denis Martin Sobieray ,  Lloyd Charles Franklin ,  Mark Alan Schwindt

IPC分类号： A61K31/197 ,  C07C69/34 ,  C07C69/675 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07D263/22 ,  C07D263/26 ,  G11B20/14 ,  G11B27/30 ,  C07D263/04

CPC分类号： A61K31/197 ,  C07C229/08 ,  C07C229/24 ,  C07C229/28 ,  C07C229/34 ,  C07C247/12 ,  C07C309/73 ,  C07C69/34 ,  C07C69/675 ,  C07D263/22 ,  C07D263/26 ,  G11B20/1426 ,  G11B27/3027 ,  C07C2101/14

摘要： A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

摘要翻译： 式Ⅰ化合物，其中R1是具有1至6个碳原子的直链或支链烷基，苯基或具有3至6个碳原子的环烷基; R2是氢或甲基; 并且R 3是氢，甲基或羧基; 其用于治疗癫痫发作。 公开了用于制备化合物的方法。 还公开了在合成化合物期间制备的中间体。