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1. 发明授权

US06218434B1 Use of the naturally-occurring quinones thymoquinone and dithymoquinone as antineoplastic and cytotoxic agents 失效
标题翻译：使用天然存在的醌类thymoquinone和dithymoquinone作为抗肿瘤和细胞毒性剂
公开(公告)号：US06218434B1
公开(公告)日：2001-04-17
申请号：US09321832
申请日：1999-05-28
申请人： Peter A. Crooks , David R. Worthen , Omar A. Ghosheh
发明人： Peter A. Crooks , David R. Worthen , Omar A. Ghosheh
IPC分类号： A61K31115
CPC分类号： A61K31/122
摘要： Nigella sativa derivatives, thymoquinone (TM) and dithymoquinone (DIM) are used in treatment of parental and multi-drug resistant human cancers.
摘要翻译： Nigella sativa衍生物，thymoquinone（TM）和dithymoquinone（DIM）用于治疗亲代和多药耐药的人类癌症。

2. 发明申请

US20100152300A1 STABILIZED COMPOSITIONS OF ALKYLATING AGENTS AND METHODS OF USING SAME 有权
标题翻译：碱性化合物的稳定组合物及其使用方法
公开(公告)号：US20100152300A1
公开(公告)日：2010-06-17
申请号：US12687605
申请日：2010-01-14
申请人： Robert ALONSO , Martin Stogniew , Peter A. Crooks , Mark A. Pimley , Stuart R. Lessin , David R. Worthen
发明人： Robert ALONSO , Martin Stogniew , Peter A. Crooks , Mark A. Pimley , Stuart R. Lessin , David R. Worthen
IPC分类号： A61K31/131 , A61P17/00 , A61P35/00
CPC分类号： C07C217/08 , A61K9/0014 , A61K9/06 , A61K9/08 , A61K31/13 , A61K31/131 , A61K47/10
摘要： Provided are stable compositions comprising alkylating agents, including nitrogen mustards, that are suitable for topical use, and methods for treating skin disorders comprising topically administering the compositions.
摘要翻译：提供了包含适合局部使用的烷基化剂（包括氮芥）的稳定组合物，以及治疗包括局部施用组合物的皮肤病症的方法。

3. 发明授权

US08501818B2 Stabilized compositions of alkylating agents and methods of using same 有权
标题翻译：烷基化剂的稳定组合物及其使用方法
公开(公告)号：US08501818B2
公开(公告)日：2013-08-06
申请号：US12687605
申请日：2010-01-14
申请人： Robert Alonso , Martin Stogniew , Peter A. Crooks , Mark A. Pimley , David R. Worthen
发明人： Robert Alonso , Martin Stogniew , Peter A. Crooks , Mark A. Pimley , David R. Worthen
IPC分类号： A01N33/02 , A61K31/13
CPC分类号： C07C217/08 , A61K9/0014 , A61K9/06 , A61K9/08 , A61K31/13 , A61K31/131 , A61K47/10
摘要： Provided are stable compositions comprising alkylating agents, including nitrogen mustards, that are suitable for topical use, and methods for treating skin disorders comprising topically administering the compositions.
摘要翻译：提供了包含适合局部使用的烷基化剂（包括氮芥）的稳定组合物，以及治疗包括局部施用组合物的皮肤病症的方法。

4. 发明授权

US07816407B2 Agmatine and agmatine analogs in the treatment of epilepsy, seizure, and electroconvulsive disorders 有权
标题翻译：丁胺和丁胺类似物治疗癫痫，癫痫发作和电惊厥性疾病
公开(公告)号：US07816407B2
公开(公告)日：2010-10-19
申请号：US09881215
申请日：2001-06-15
申请人： Peter A. Crooks , Aimee K. Bence , David R. Worthen
发明人： Peter A. Crooks , Aimee K. Bence , David R. Worthen
IPC分类号： A61K31/175
CPC分类号： A61K31/155
摘要： Pharmaceutical preparations containing of agmatine, congeners, analogs or derivatives thereof for use in preventing or treating epilepsy, seizures and other electroconvulsive disorders are provided. Embodiments include administering an effective amount of agmatine, an agmatine analog or a pharmaceutically acceptable salt thereof to a human subject in need of treatment or prevention of epilepsy, seizure or other electroconvulsive disorder to treat, reduce, or prevent the disorder in the subject.
摘要翻译：提供了含有用于预防或治疗癫痫，癫痫发作和其他电惊厥疾病的胍丁胺，同系物，类似物或其衍生物的药物制剂。实施方案包括向需要治疗或预防癫痫，癫痫发作或其它电惊厥疾病的人类受试者施用有效量的胍丁胺，胍丁胺类似物或其药学上可接受的盐以治疗，减少或预防受试者的病症。

5. 发明授权

US08501819B2 Stabilized compositions of volatile alkylating agents and methods of using thereof 有权
标题翻译：挥发性烷基化剂的稳定组合物及其使用方法
公开(公告)号：US08501819B2
公开(公告)日：2013-08-06
申请号：US12948593
申请日：2010-11-17
申请人： Robert Alonso , Peter A. Crooks , Mark A. Pimley
发明人： Robert Alonso , Peter A. Crooks , Mark A. Pimley
IPC分类号： A01N33/02 , A61K31/13
CPC分类号： C07C211/15 , A61K31/13 , A61K31/131 , Y10T428/13
摘要： A composition and method for treatment of cancer. The composition for treating a skin disorder, comprising: a Nitrogen Mustard or an HX salt of the Nitrogen Mustard, wherein the Nitrogen Mustard or the HX salt of the Nitrogen Mustard is in a non-aqueous vehicle or carrier that does not include petrolatum or ethanol does not include petrolatum or ethanol. The method comprises topically applying the composition of a Nitrogen Mustard or a HX salt of the Nitrogen Mustard to the affected skin, wherein the Nitrogen Mustard or the HX salt of the Nitrogen Mustard is in a non-aqueous vehicle or carrier that does not include petrolatum or ethanol.
摘要翻译：用于治疗癌症的组合物和方法。用于治疗皮肤病症的组合物，其包含氮芥末的氮芥或HX盐，其中所述氮芥的氮芥或HX盐在不包括凡士林或乙醇的非水载体或载体中不含凡士林或乙醇。该方法包括将氮芥末的氮芥或HX盐的组合物局部施用于受影响的皮肤，其中氮芥的氮芥或HX盐在不含凡士林的非水性载体或载体中或乙醇。

6. 发明授权

US08101779B2 Enantioselective synthesis of (+) and (–)-2-[1-(2,6-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene 有权
标题翻译：（+）和（ - ） - 2- [1-（2,6-二氯苯氧基） - 乙基] -1,3-二氮杂环戊烯-2-酮的对映选择性合成
公开(公告)号：US08101779B2
公开(公告)日：2012-01-24
申请号：US12574578
申请日：2009-10-06
申请人： Peter A. Crooks , Ashish Pramod Vartak
发明人： Peter A. Crooks , Ashish Pramod Vartak
IPC分类号： C07D233/22
CPC分类号： C07D233/22
摘要： Methods for the enantioselective synthesis of (+) and (−) lofexidine or 2-[1-(2,6)-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene involve converting (+) or (−) 1-methyl-1-[2,6-dichlorophenoxy]ethanamide to an (+) or (−) imino-ether intermediate by electrophilic attack of the amide oxygen by a trimethoxonium ion and, without isolation, converting the (+) or (−) imino-ether intermediate to (+) or (−) 2-[1-(2,6-dichlorophenoxy)-ethyl]1,3-diazacyclopent-2-ene by adding ethylene diamine; and optionally converting the (+) or (−) 2-[1-(2,6-dichlorophenoxy)-ethyl]1,3-diazacyclopent-2-ene into a pharmaceutically acceptable acid addition salt thereof.
摘要翻译：（+）和（ - ）洛非替西或2- [1-（2,6） - 二氯苯氧基） - 乙基] -1,3-二氮杂环戊烯-2-酮的对映选择性合成方法涉及转化（+）或（ - ） 1-甲基-1- [2,6-二氯苯氧基]乙酰胺与（+）或（ - ）亚氨基醚中间体反应，通过三甲氧基铵离子对酰胺氧的亲电攻击而不分离地将（+）或（ - - ）亚氨基醚中间体加入（+）或（ - ）2- [1-（2,6-二氯苯氧基） - 乙基] -1,3-二氮杂环戊烯-2-烯; 并且任选地将（+）或（ - ）2- [1-（2,6-二氯苯氧基） - 乙基] -1,3-二氮杂环戊烯-2-酮转化为其药学上可接受的酸加成盐。

7. 发明申请

US20110065803A1 STABILIZED COMPOSITIONS OF VOLATILE ALKYLATING AGENTS AND METHODS OF USING THEREOF 有权
标题翻译：挥发性碱性化合物的稳定组合物及其使用方法
公开(公告)号：US20110065803A1
公开(公告)日：2011-03-17
申请号：US12948593
申请日：2010-11-17
申请人： Robert Alonso , Peter A. Crooks , Mark A. Pimley
发明人： Robert Alonso , Peter A. Crooks , Mark A. Pimley
IPC分类号： A61K31/131 , A61P17/06 , A61P17/00
CPC分类号： C07C211/15 , A61K31/13 , A61K31/131 , Y10T428/13
摘要： A composition and method for treatment of cancer. The composition for treating a skin disorder, comprising: a Nitrogen Mustard or an HX salt of the Nitrogen Mustard, wherein the Nitrogen Mustard or the HX salt of the Nitrogen Mustard is in a non-aqueous vehicle or carrier that does not include petrolatum or ethanol, wherein the non-aqueous vehicle or carrier that does not include petrolatum or ethanol does not include petrolatum or ethanol. The method comprises topically applying the composition of a Nitrogen Mustard or a HX salt of the Nitrogen Mustard to the affected skin, wherein the Nitrogen Mustard or the HX salt of the Nitrogen Mustard is in a non-aqueous vehicle or carrier that does not include petrolatum or ethanol, wherein the non-aqueous vehicle or carrier does not include petrolatum or ethanol.
摘要翻译：用于治疗癌症的组合物和方法。用于治疗皮肤病症的组合物，其包含氮芥末的氮芥或HX盐，其中所述氮芥的氮芥或HX盐在不包括凡士林或乙醇的非水载体或载体中其中不含凡士林或乙醇的非水性载体或载体不包括凡士林或乙醇。该方法包括将氮芥末的氮芥或HX盐的组合物局部施用于受影响的皮肤，其中氮芥的氮芥或HX盐在不含凡士林的非水性载体或载体中或乙醇，其中非水性载体或载体不包括凡士林或乙醇。

8. 发明申请

US20100121061A1 COMPOUNDS CAPABLE OF ACTIVATING CHOLINERGIC RECEPTORS 审中-公开
标题翻译：可激活胆碱受体的化合物
公开(公告)号：US20100121061A1
公开(公告)日：2010-05-13
申请号：US12633308
申请日：2009-12-08
申请人： William S. Caldwell , Gary M. Dull , Balwinder S. Bhatti , Srishailkumar B. Hadimani , Haeil Park , Jared M. Wagner , Peter A. Crooks , Patrick M. Lippiello , Merouane Bencherif
发明人： William S. Caldwell , Gary M. Dull , Balwinder S. Bhatti , Srishailkumar B. Hadimani , Haeil Park , Jared M. Wagner , Peter A. Crooks , Patrick M. Lippiello , Merouane Bencherif
IPC分类号： C07D239/26 , C07D213/55 , C07D213/65 , C07D213/73 , C07D213/02
CPC分类号： C07D239/26 , A61K31/44 , A61K31/505 , C07D213/38 , C07D213/61 , C07D213/65 , C07D213/73 , C07D403/06
摘要： The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed.
摘要翻译：本发明一般涉及以芳基取代的烯属化合物形式的烟碱化合物，以及前药，N-氧化物，代谢产物和药学上可接受的盐形式。还公开了通过施用化合物，前药，N-氧化物和/或药学上可接受的盐调节神经递质释放的方法。

9. 发明申请

US20080132531A1 SYNERGISTIC COMBINATIONS OF NORKETAMINE AND OPIOID ANALGESICS 审中-公开
标题翻译：诺卡胺和阿片类药物的协同联合
公开(公告)号：US20080132531A1
公开(公告)日：2008-06-05
申请号：US11558782
申请日：2006-11-10
申请人： Joseph R. Holtman , Peter A. Crooks
发明人： Joseph R. Holtman , Peter A. Crooks
IPC分类号： A61K31/439 , A61P29/00 , A61P25/00 , A61K31/135 , A61K31/445 , A61K31/4355
CPC分类号： A61K31/473 , A61K31/485 , A61K45/06 , A61K2300/00
摘要： The present invention relates to methods of alleviating pain with the administration of norketamine with a narcotic. More particularly, the invention provides a method of alleviating pain through the administration of a dose of norketamine, which, if administered alone would provide sub-optimal analgesic relief, yet provides analgesic relief when combined with a narcotic. In some embodiments, the combination of norketamine with a narcotic, further allows for the administration of a dose narcotic, which would be sub-optimal if used alone, but provides adequate pain relief in combination with norketamine. The invention relates to self-management of pain on an outpatient basis comprising administering via conventional routes, including transdermal, nasal, rectal, oral, transmucosal, intravenous, intramuscular, and other routes, one or more doses of norketamine/opioid compositions effective to alleviate pain to a subject suffering from pain. Uses of norketamine/opioid compositions would also apply, to treating headaches, drug abuse, mood and anxiety disorders, as well as other, neuropsychiatric disorders, both motoric and cognitive, such as Alzheimer's disease, Parkinson's syndrome, which are thought to be caused by neurodegeneration.
摘要翻译：本发明涉及通过麻醉剂施用诺可泰胺来缓解疼痛的方法。更具体地，本发明提供了一种通过施用一剂剂量的诺卡胺来减轻疼痛的方法，如果单独给予，它将提供次优的止痛缓解，但当与麻醉剂组合时提供镇痛缓解。在一些实施方案中，诺替卡胺与麻醉剂的组合进一步允许施用剂量麻醉剂，其如果单独使用则为次优，但与诺替胺组合提供足够的疼痛缓解。本发明涉及门诊患者疼痛的自我管理，包括通过常规途径给药，包括透皮，鼻，直肠，口服，经粘膜，静脉内，肌内和其他途径，一种或多种剂量的有效减轻的诺尔et胺/阿片样物质组合物疼痛痛苦的受试者。诺卡胺/阿片样物质组合物的使用也适用于治疗头痛，药物滥用，情绪和焦虑症，以及其他神经精神障碍，包括运动和认知，如阿尔茨海默氏病，帕金森综合征，被认为是由神经退行性疾病

10. 发明授权

US07045538B2 Compounds capable of activating cholinergic receptors 失效
公开(公告)号：US07045538B2
公开(公告)日：2006-05-16
申请号：US10971543
申请日：2004-10-22
申请人： William S. Caldwell , Gary M. Dull , Balwinder S. Bhatti , Srishailkumar B. Hadimani , Haeil Park , Jared M. Wagner , Peter A. Crooks , Patrick M. Lippiello , Merouane Bencherif
发明人： William S. Caldwell , Gary M. Dull , Balwinder S. Bhatti , Srishailkumar B. Hadimani , Haeil Park , Jared M. Wagner , Peter A. Crooks , Patrick M. Lippiello , Merouane Bencherif
IPC分类号： C07D213/38 , A61K31/44 , A61P29/02
CPC分类号： C07D239/26 , A61K31/44 , A61K31/505 , C07D213/38 , C07D213/61 , C07D213/65 , C07D213/73 , C07D403/06
摘要： The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed.

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