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11. 发明申请

US20090062336A1 Methods of Diminishing Co-Abuse Potential 审中-公开
标题翻译：减少共同滥用潜力的方法
公开(公告)号：US20090062336A1
公开(公告)日：2009-03-05
申请号：US12269471
申请日：2008-11-12
申请人： Vikram Khetani , Herbert Faleck
发明人： Vikram Khetani , Herbert Faleck
IPC分类号： A61K31/4418 , A61K31/445 , A61P25/30
CPC分类号： A61K31/4458
摘要： Methods of diminishing or eliminating the co-abuse of a methylphenidate drug comprising identifying a patient or patient group suspected or likely to abuse said methylphenidate drug in combination with a substance known or suspected to give rise to l-ethylphenidate or psychotropic effect when ingested in the combination and making available to said patent or patient group said methylphenidate drug substantially free of l-threo methylphenidate.
摘要翻译：减少或消除哌甲酯药物的共同滥用的方法包括鉴定怀疑或可能滥用所述哌甲酯类药物的患者或患者组合与已知或怀疑产生1-乙酯或精神药效作用的物质组合，组合并提供给所述专利或患者组，所述哌甲酯药物基本上不含1-苏式哌甲酯。

12. 发明申请

US20060127421A1 Treatment using D-threo methylphenidate 审中-公开
标题翻译：使用D-苏式哌甲酯治疗
公开(公告)号：US20060127421A1
公开(公告)日：2006-06-15
申请号：US11298093
申请日：2005-12-08
申请人： Vikram Khetani
发明人： Vikram Khetani
IPC分类号： A61K31/445 , A61K9/00
CPC分类号： A61K9/0019 , A61K31/445
摘要： Methods for treating a disease responsive to the administration of methylphenidate and/or one or more isomers thereof, said method comprising identifying a patient suffering from a disease or disorder having a family history or diagnosis of tics or Tourette's Syndrome and administering to said patient a therapeutically effective amount of D-threo methylphenidate substantially free of the l-threo isomer and of erythro methylphenidates.
摘要翻译：用于治疗响应于哌甲酯和/或其一种或多种异构体的疾病的方法，所述方法包括鉴定患有家族史或Tico或Tourette综合征诊断的疾病或病症的患者，并且向所述患者施用治疗有效量的D-苏式哌甲酯基本上不含1-苏式异构体和红皮药哌啶类。

13. 发明申请

US20050239830A1 Methods of diminishing co-abuse potential 审中-公开
标题翻译：减少共同滥用潜力的方法
公开(公告)号：US20050239830A1
公开(公告)日：2005-10-27
申请号：US10832210
申请日：2004-04-26
申请人： Vikram Khetani , Herbert Faleck
发明人： Vikram Khetani , Herbert Faleck
IPC分类号： A61K31/445
CPC分类号： A61K31/4458
摘要： Methods of diminishing or eliminating the co-abuse of a methylphenidate drug comprising identifying a patient or patient group suspected or likely to abuse said methylphenidate drug in combination with a substance known or suspected to give rise to l-ethylphenidate or psychotropic effect when ingested in the combination and making available to said patent or patient group said methylphenidate drug substantially free of l-threo methylphenidate.
摘要翻译：减少或消除哌甲酯药物的共同滥用的方法包括鉴定怀疑或可能滥用所述哌甲酯类药物的患者或患者组合与已知或怀疑产生1-乙酯或精神药效作用的物质组合，组合并提供给所述专利或患者组，所述哌甲酯药物基本上不含1-苏式哌甲酯。

14. 发明授权

US06359139B1 Methods for production of piperidyl acetamide stereoisomers 有权
标题翻译：哌啶乙酰胺立体异构体的生产方法
公开(公告)号：US06359139B1
公开(公告)日：2002-03-19
申请号：US09707524
申请日：2000-11-07
申请人： Vikram Khetani , William Konnecke , Chuansheng Ge
发明人： Vikram Khetani , William Konnecke , Chuansheng Ge
IPC分类号： C07D21132
CPC分类号： C07D211/34
摘要： Synthetic methods are provided comprising the steps of racemizing l-threo-piperidyl acetamides to form a mixture of d-threo, l-threo, d-erythro, and l-erythro-piperidyl acetamides by reacting said l-threo-piperidyl acetamides with alkanoic acid.
摘要翻译：提供了合成方法，包括以下步骤：使1-苏式 - 哌啶基乙酰胺进行外消旋化以形成d-苏，1-苏，d-赤型和1-赤型 - 哌啶基乙酰胺的混合物，通过使所述1-苏 - 哌啶基乙酰胺与链烷酸酸。

15. 发明申请

US20130053414A1 METHODS FOR TREATMENT OF COGNITIVE AND MENOPAUSAL DISORDERS WITH D-THREO METHYLPHENIDATE 审中-公开
标题翻译：用甲基苯甲酸D-THREO治疗认知障碍和男性疾病的方法
公开(公告)号：US20130053414A1
公开(公告)日：2013-02-28
申请号：US13661472
申请日：2012-10-26
申请人： Jerome B. Zeldis , Herbert J. Faleck , Vikram Khetani , Andrew L. Zeitlin , Maghsoud M. Dariani , David I. Stirling
发明人： Jerome B. Zeldis , Herbert J. Faleck , Vikram Khetani , Andrew L. Zeitlin , Maghsoud M. Dariani , David I. Stirling
IPC分类号： A61K31/4458 , A61P25/00 , A61P25/24 , A61P3/00
CPC分类号： C07D211/34 , A61K31/4458 , A61K45/06 , C12P17/12 , C12P41/006 , A61K2300/00
摘要： In one aspect, the present invention is directed to methods for treating fatigue, neurobehavioral slowing and other cognitive disorders and defects due to cancers and treatments associated with cancers, and similar conditions. In a further aspect, the present invention is directed to methods for treating disorders related to menopause, including executive function defects. The methods involve the administration of a composition comprising D-threo methylphenidate that is substantially free of L-threo methylphenidate and of erythro forms of methylphenidate.
摘要翻译：一方面，本发明涉及用于治疗疲劳，神经行为减缓以及由于与癌症相关的癌症和治疗以及类似病症引起的其他认知障碍和缺陷的方法。在另一方面，本发明涉及治疗与绝经相关的疾病的方法，包括执行功能缺陷。所述方法包括施用包含基本上不含L-苏雷哌甲酯的D-苏雷哌甲酯和红皮质哌甲酯的组合物。

16. 发明申请

US20120136028A1 Methods Of Diminishing Co-Abuse Potential 审中-公开
标题翻译：减少共同滥用潜力的方法
公开(公告)号：US20120136028A1
公开(公告)日：2012-05-31
申请号：US13370663
申请日：2012-02-10
申请人： Vikram Khetani , Herbert Faleck
发明人： Vikram Khetani , Herbert Faleck
IPC分类号： A61K31/4458 , A61P25/00
CPC分类号： A61K31/4458
摘要： Methods of diminishing or eliminating the co-abuse of a methylphenidate drug comprising identifying a patient or patient group suspected or likely to abuse said methylphenidate drug in combination with a substance known or suspected to give rise to l-ethylphenidate or psychotropic effect when ingested in the combination and making available to said patent or patient group said methylphenidate drug substantially free of l-threo methylphenidate.
摘要翻译：减少或消除哌甲酯药物的共同滥用的方法包括鉴定怀疑或可能滥用所述哌甲酯类药物的患者或患者组合与已知或怀疑产生1-乙酯或精神药效作用的物质组合，组合并提供给所述专利或患者组，所述哌甲酯药物基本上不含1-苏式哌甲酯。

17. 发明授权

US07115631B2 Methods for treatment of cognitive and menopausal disorders with D-threo methylphenidate 失效
公开(公告)号：US07115631B2
公开(公告)日：2006-10-03
申请号：US10195974
申请日：2002-07-16
申请人： Jerome B Zeldis , Herbert J. Faleck , Vikram Khetani , Andrew L. Zeitlin , Maghsoud M. Dariani , David Sterling
发明人： Jerome B Zeldis , Herbert J. Faleck , Vikram Khetani , Andrew L. Zeitlin , Maghsoud M. Dariani , David Sterling
IPC分类号： A61K31/445
CPC分类号： C07D211/34 , A61K31/4458 , A61K45/06 , C12P17/12 , C12P41/006 , A61K2300/00
摘要： In one aspect, the present invention is directed to methods for treating fatigue, neurobehavioral slowing and other cognitive disorders and defects due to cancers and treatments associated with cancers, and similar conditions. In a further aspect, the present invention is directed to methods for treating disorders related to menopause, including executive function defects. The methods involve the administration of a composition comprising D-threo methylphenidate that is substantially free of L-threo methylphenidate and of erythro forms of methylphenidate.

18. 发明授权

US06486177B2 Methods for treatment of cognitive and menopausal disorders with D-threo methylphenidate 失效
标题翻译：用D-threo哌甲酯治疗认知和绝经障碍的方法
公开(公告)号：US06486177B2
公开(公告)日：2002-11-26
申请号：US09903803
申请日：2001-07-12
申请人： Jerome B. Zeldis , Herbert Faleck , Vikram Khetani
发明人： Jerome B. Zeldis , Herbert Faleck , Vikram Khetani
IPC分类号： A61K31445
CPC分类号： C07D211/34 , A61K31/4458 , A61K45/06 , C12P17/12 , C12P41/006 , A61K2300/00
摘要： In one aspect, the present invention is directed to methods for treating fatigue, neurobehavioral slowing and other cognitive disorders and defects due to cancers and treatments associated with cancers, and similar conditions. In a further aspect, the present invention is directed to methods for treating disorders related to menopause, including executive function defects. The methods involve the administration of a composition comprising D-threo methylphenidate that is substantially free of L-threo methylphenidate and of erythro forms of methylphenidate.
摘要翻译：一方面，本发明涉及用于治疗疲劳，神经行为减缓以及由于与癌症相关的癌症和治疗以及类似病症引起的其他认知障碍和缺陷的方法。在另一方面，本发明涉及治疗与绝经相关的疾病的方法，包括执行功能缺陷。所述方法包括施用包含基本上不含L-苏雷哌甲酯的D-苏雷哌甲酯和红皮质哌甲酯的组合物。

19. 发明授权

US5965734A Processes and intermediates for preparing 2-substituted piperidine stereoisomers 失效
标题翻译：制备2-取代的哌啶立体异构体的方法和中间体
公开(公告)号：US5965734A
公开(公告)日：1999-10-12
申请号：US792661
申请日：1997-01-31
申请人： Sowmianarayanan Ramaswamy , Vikram Khetani
发明人： Sowmianarayanan Ramaswamy , Vikram Khetani
IPC分类号： C07D211/34 , C07B61/00 , C07D211/26 , C07D213/40 , C07D211/32
CPC分类号： C07D211/34
摘要： Processes and intermediates for preparing 2-substituted piperidines such as 2-substituted d-threo piperidines are provided. In preferred embodiments, the processes of the invention comprise the steps of reacting a 2-substituted pyridine with hydrogen in the presence of a catalyst in an alkanoic acid, and adding an alkyl alkanoate to the resulting mixture of threo and erythro 2-piperidine stereoisomers to precipitate alkanoate salts of the erythro stereoisomers preferentially with respect to alkanoate salts of the threo stereoisomers. The erythro salts then are reacted with aqueous base to form the corresponding mixture of erythro amide free bases, which are reacted with a suitable organic acid resolving agent in an alkyl alcohol solvent to form acid salts of the l-erythro stereoisomers preferentially with respect to the d-erythro stereoisomers. The 1-erythro acid salts are then reacted with aqueous base to form the 1-erythro piperidine amide free base which, in turn, is epimerized to produce the desired d-threo product by treating it in an organic solvent with an alkali metal alkoxide.
摘要翻译：提供了制备2-取代的哌啶类的方法和中间体，例如2-取代的d-苏式哌啶。在优选的实施方案中，本发明的方法包括以下步骤：使2-取代的吡啶与氢在催化剂存在下在链烷酸中反应，并将烷基链烷酸酯加到得到的苏氨酸和赤式2-哌啶立体异构体的混合物中相对于苏立立体异构体的链烷酸盐，优选赤式立体异构体的链烷酸盐沉淀。然后将红藻酸盐与碱水溶液反应以形成相应的红酰胺游离碱混合物，其与烷基醇溶剂中的合适的有机酸拆分剂反应，以优先地形成1-赤型立体异构体的酸式盐 d-erythro立体异构体。然后将1-赤藓酸盐与碱水溶液反应以形成1-赤型哌啶酰胺游离碱，其依次通过在碱金属醇盐的有机溶剂中处理而产生所需的d-苏糖产物。

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