公开(公告)号：US20110201645A1

公开(公告)日：2011-08-18

申请号：US13093917

申请日：2011-04-26

申请人： Andrew L. Zeitlin ,  Maghsoud M. Dariani ,  David I. Stirling

发明人： Andrew L. Zeitlin ,  Maghsoud M. Dariani ,  David I. Stirling

IPC分类号： A61K31/4458 ,  A61P25/00

CPC分类号： A61K31/445 ,  A61K9/1676 ,  A61K9/2886 ,  A61K9/5078 ,  A61K9/5084 ,  A61K31/4458 ,  C07D211/34 ,  C12P17/12 ,  C12P41/006

摘要： Methods for treating Attention Deficit Disorder, Attention Deficit Hyperactivity Disorder, AIDS Dementia Complex and cognitive decline in HIV-AIDS while minimizing drug hypersensitivity, toxicity, side effects, euphoric effect, and drug abuse potential by administration of d-threo-methylphenidate or pharmaceutically acceptable salts thereof.

摘要翻译： 治疗注意力缺陷障碍，注意力缺陷多动障碍，艾滋病痴呆综合征和艾滋病毒/艾滋病认知衰退的方法，同时通过施用二硫代哌甲酯或药学上可接受的方式尽量减少药物过敏反应，毒性，副作用，欣欣乐效和药物滥用潜力 的盐。

公开(公告)号：US5169780A

公开(公告)日：1992-12-08

申请号：US549830

申请日：1990-07-09

申请人： David I. Stirling ,  Andrew L. Zeitlin ,  George W. Matcham ,  James D. Rozzell, Jr.

发明人： David I. Stirling ,  Andrew L. Zeitlin ,  George W. Matcham ,  James D. Rozzell, Jr.

IPC分类号： C12N9/10 ,  C12P7/26 ,  C12P41/00

CPC分类号： C12N9/1096 ,  C12P41/006 ,  C12P7/26

摘要： Amines in which the amino group is on a secondary carbon atom which is chirally substituted can be enantiomerically enriched by the action of an omega-amino acid transaminase which has the property of preferentially converting one of the two chiral forms to a ketone. The process can be used to stereoselectively sythesize one chiral form from ketones substantially to the exclusion of the other. An aqueous solution of chiral amines after being brought into contact with an omega-amino acid transaminase and an amino acceptor is treated with a water-immiscible organic solvent, the aqueous and organic phases are separated, and the aqueous phase can be recirculated for further contact with the transaminase.

摘要翻译： 其中氨基在手性取代的仲碳原子上的胺可通过ω-氨基酸转氨酶的作用而被对映体富集，该氨基酸转氨酶具有优先将两种手性形式之一转化为酮的性质。 该方法可用于立体选择性地将酮的一种手性形式基本上与另一种不同。 与ω-氨基酸转氨酶和氨基受体接触后手性胺的水溶液用水不混溶的有机溶剂处理，水相和有机相被分离，水相可再循环以进一步接触 与转氨酶。

公开(公告)号：US20100093797A1

公开(公告)日：2010-04-15

申请号：US12640734

申请日：2009-12-17

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： A61K31/445 ,  A61P15/00 ,  A61P35/04

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。

公开(公告)号：US5733756A

公开(公告)日：1998-03-31

申请号：US583317

申请日：1996-01-05

申请人： Andrew L. Zeitlin ,  David I. Stirling

发明人： Andrew L. Zeitlin ,  David I. Stirling

IPC分类号： C07D211/34 ,  C12P17/12 ,  C12P41/00 ,  C07D211/26

CPC分类号： C07D211/34 ,  C12P17/12 ,  C12P41/006

摘要： Novel lactams and processes for the preparation of chiral compounds having utility as intermediates in the synthesis of compounds with Central Nervous System stimulant activity.

摘要翻译： 新型内酰胺和制备手性化合物的方法，其具有在具有中枢神经系统兴奋剂活性的化合物的合成中作为中间体的作用。

公开(公告)号：US5346828A

公开(公告)日：1994-09-13

申请号：US844724

申请日：1992-03-02

申请人： David I. Stirling ,  Muppala S. Raju ,  Andrew L. Zeitlin

发明人： David I. Stirling ,  Muppala S. Raju ,  Andrew L. Zeitlin

IPC分类号： C07C227/04 ,  C07C315/06 ,  C07C317/48 ,  C07C319/28 ,  C07C323/63 ,  C12P7/24 ,  C12P11/00 ,  C12P13/04 ,  C12P41/00

CPC分类号： C07C315/06 ,  C07C319/28 ,  C12P11/00 ,  C12P13/04 ,  C12P41/00 ,  C12P7/24 ,  C07B2200/07 ,  Y02P20/55 ,  Y10S435/829

摘要： Mixtures of enantiomeric D,L-threo 2-amino-3-hydroxy-3-phenylpropionic acids can be stereoisomerically enriched by contacting the mixture with a D-threonine aldolase. In a typical embodiment, D- and L-threo 2-amino-3-hydroxy-3-(4-methylsulfonylphenyl)propionic acid is treated with D-threonine aldolase to produce L-threo 2-amino-3-hydroxy-3-(4-methylsulfonylphenyl)propionic acid with a high ee. The benzaldehyde and amino acid formed from the D-threo isomer can be recycled.

摘要翻译： 对映异构体D，L-苏氨酸2-氨基-3-羟基-3-苯基丙酸的混合物可以通过将该混合物与D-苏氨酸醛缩酶接触来进行立体异构富集。 在典型的实施方案中，用D-苏氨酸醛缩酶处理D-和L-苏氨酸2-氨基-3-羟基-3-（4-甲基磺酰基苯基）丙酸以产生L-苏氨酸2-氨基-3-羟基-3- （4-甲基磺酰基苯基）丙酸，高ee。 可以回收由D-苏糖异构体形成的苯甲醛和氨基酸。

公开(公告)号：US5908850A

公开(公告)日：1999-06-01

申请号：US827230

申请日：1997-04-02

申请人： Andrew L. Zeitlin ,  Maghsoud M. Dariani ,  David I. Stirling

发明人： Andrew L. Zeitlin ,  Maghsoud M. Dariani ,  David I. Stirling

IPC分类号： A61K31/4458 ,  A61K31/445

CPC分类号： A61K31/4458

摘要： Methods for treating Attention Deficit Disorder, Attention Deficit Hyperactivity Disorder, AIDS Dementia Complex and cognitive decline in HIV-AIDS while minimizing drug hypersensitivity, toxicity, side effects, euphoric effect, and drug abuse potential by administration of d-threo-methylphenidate or pharmaceutically acceptable salts thereof.

公开(公告)号：US4950606A

公开(公告)日：1990-08-21

申请号：US369723

申请日：1989-06-22

申请人： David I. Stirling ,  Andrew L. Zeitlin ,  George W. Matcham

发明人： David I. Stirling ,  Andrew L. Zeitlin ,  George W. Matcham

IPC分类号： C07C209/00 ,  C12N9/10 ,  C12P7/26 ,  C12P41/00

CPC分类号： C12N9/1096 ,  C12P41/006 ,  C12P7/26

摘要： Amines in which the amino group is on a secondary carbon atom which is chrially substituted can be enantiomerically enriched by the action of an omega-amino acid transaminase which has the property of preferentially converting one of the two chiral forms to a ketone. The process also can be used to stereoselectively synthesize one chiral form from ketones substantially to the exclusion of the other.

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。

公开(公告)号：US5300437A

公开(公告)日：1994-04-05

申请号：US959147

申请日：1992-10-09

申请人： David I. Stirling ,  George W. Matcham ,  Andrew L. Zeitlin

发明人： David I. Stirling ,  George W. Matcham ,  Andrew L. Zeitlin

IPC分类号： C12N9/10 ,  C12P7/26 ,  C12P41/00 ,  C12P13/02 ,  C12P7/38

CPC分类号： C12N9/1096 ,  C12P41/006 ,  C12P7/26

摘要： Amines in which the amino group is on a secondary carbon atom which is chirally substituted can be enantiomerically enriched by the action of an omega-amino acid transaminase which has the property of preferentially converting one of the two chiral forms to a ketone. The process also can be used to stereoselectively synthesize one chiral form from ketones substantially to the exclusion of the other.

摘要翻译： 其中氨基在手性取代的仲碳原子上的胺可通过ω-氨基酸转氨酶的作用而被对映体富集，该氨基酸转氨酶具有优先将两种手性形式之一转化为酮的性质。 该方法还可以用于立体选择性地从酮中合成一种手性形式，基本上排除另一种。

公开(公告)号：US07435726B2

公开(公告)日：2008-10-14

申请号：US09853617

申请日：2001-05-14

申请人： Jerome B. Zeldis ,  Andrew L. Zeitlin ,  Sol Barer

发明人： Jerome B. Zeldis ,  Andrew L. Zeitlin ,  Sol Barer

IPC分类号： A01N43/00 ,  A61K31/33 ,  A01N43/04 ,  A61K31/70

CPC分类号： A61K31/4745 ,  A61K31/454 ,  A61K31/47 ,  A61K31/7056 ,  A61K31/724 ,  A61K31/445 ,  A61K2300/00

摘要： This invention relates to compositions comprising thalidomide and another anti-cancer drug which can be used in the treatment or prevention of cancer. Preferred anti-cancer drugs are topoisomerase inhibitors. A particular composition comprises thalidomide, or a pharmaceutically acceptable salt, solvate, or clathrate thereof, and irinotecan. The invention also relates to methods of treating or preventing cancer which comprise the administration of a thalidomide and another anti-cancer drug to a patient in need of such treatment or prevention. The invention further relates to methods of reducing or avoiding adverse side effects associated with the administration of chemotherapy or radiation therapy which comprise the administration of thalidomide to a patient in need of such reduction or avoidance.

摘要翻译： 本发明涉及可用于治疗或预防癌症的沙利度胺和另一种抗癌药物的组合物。 优选的抗癌药物是拓扑异构酶抑制剂。 特定组合物包含沙利度胺或其药学上可接受的盐，溶剂合物或包合物和伊立替康。 本发明还涉及治疗或预防癌症的方法，其包括向需要这种治疗或预​​防的患者施用沙利度胺和另一种抗癌药物。 本发明还涉及减少或避免与化疗或放射治疗相关的不良副作用的方法，其包括向需要这种减少或避免的患者施用沙利度胺。