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1. 发明申请

WO2007062184A2 PROCESSES FOR REDUCING CONTAMINATING MICHAEL ACCEPTOR LEVELS IN OXYCODONE AND OTHER COMPOSITIONS 审中-公开
标题翻译：减少氧化剂和其他组合物中污染微生物接收剂含量的方法
公开(公告)号：WO2007062184A2
公开(公告)日：2007-05-31
申请号：PCT/US2006045316
申请日：2006-11-22
申请人： CONTROLLED CHEMICALS INC , SHAFER JULES A , TELYATNIKOV VLADISLAV V , WANG HAO
发明人： SHAFER JULES A , TELYATNIKOV VLADISLAV V , WANG HAO
CPC分类号： A23L5/27 , A23V2002/00 , C07D489/02 , C07D489/08 , G01N30/74 , G01N33/02 , G01N33/15 , G01N2030/027
摘要： The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
摘要翻译：本发明涉及从某些组合物中除去迈克尔受体的方法，其中组合物在足以除去迈克尔受体和所得到的硫醇 - 迈克尔加合物的条件下用含硫醇的化合物处理。本发明的某些实施方案能够定量和/或去除迈克尔受体和/或迈克尔受体前体。

2. 发明申请

WO2011022460A8 NOVEL CATIONIC LIPIDS WITH VARIOUS HEAD GROUPS FOR OLIGONUCLEOTIDE DELIVERY 审中-公开
标题翻译：具有各种头发交付的各种头巾组
公开(公告)号：WO2011022460A8
公开(公告)日：2012-05-10
申请号：PCT/US2010045854
申请日：2010-08-18
申请人： MERCK SHARP & DOHME , CAMERON MARK , DAVIS JENNIFER R , GEISER ANDREA R , STANTON MATTHEW G , TELYATNIKOV VLADISLAV V , TIAN LU , WANG WEIMIN
发明人： CAMERON MARK , DAVIS JENNIFER R , GEISER ANDREA R , STANTON MATTHEW G , TELYATNIKOV VLADISLAV V , TIAN LU , WANG WEIMIN
IPC分类号： C07C229/00 , A61K9/127
CPC分类号： A61K9/1272 , A61K31/7088 , C07J41/0055 , C07J43/003
摘要： The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with siRNA, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo.
摘要翻译：本发明提供了可以与其它脂质组分如胆固醇和PEG-脂质组合使用以与siRNA形成脂质纳米颗粒以促进细胞摄取和内体逃逸以及在体外和体内。

3. 发明专利

JP2013079279A Processes for reducing michael acceptor levels mixed in oxycodone and other compositions 审中-公开
标题翻译：减少氧化剂和其他组合物中混合的MICHAEL接收剂水平的方法
公开(公告)号：JP2013079279A
公开(公告)日：2013-05-02
申请号：JP2013001763
申请日：2013-01-09
申请人： Controlled Chemicals Inc , コントロールド・ケミカルズ・インコーポレーテッド
发明人： SHAFER JULES A , TELYATNIKOV VLADISLAV V , WANG HAO
IPC分类号： C07D489/08 , A61K31/485 , A61P25/04
CPC分类号： A23L5/27 , A23V2002/00 , C07D489/02 , C07D489/08 , G01N30/74 , G01N33/02 , G01N33/15 , G01N2030/027
摘要： PROBLEM TO BE SOLVED: To provide processes for removing Michael acceptors mixed in oxycodone and other compositions.SOLUTION: A composition is treated with a thiol-containing compound under conditions sufficient to remove at least a portion of the at least one Michael acceptor and/or a thiol-Michael adduct which can form from addition of the thiol-containing compound to the at least one Michael acceptor. Subsequent to formation of thiol-Michael adduct at pH-6 in one embodiment of the process used to remove 14-hydroxycodeinone from oxycodone, the pH of the reaction mixture is increased to precipitate and/or extract oxycodone organic base from an aqueous solution with most of the thiol-Michael adduct and excess sodium thioglyclolate remaining in aqueous solution.
摘要翻译：要解决的问题：提供用于除去在羟考酮和其它组合物中混合的迈克尔受体的方法。解决方案：在足以除去至少一部分至少一种迈克尔受体和/或硫醇 - 迈克尔加合物的条件下，用含硫醇的化合物处理组合物，所述至少一种迈克尔受体和/或可通过加入含硫醇化合物形成的硫醇 - 至少一个迈克尔接受者。在用于从羟考酮中除去14-羟可待因酮的方法的一个实施方案中，在pH-6形成硫醇-MX加合物之后，增加反应混合物的pH以从水溶液中沉淀和/或提取羟考酮有机碱，最多的硫醇-MX加合物和剩余的水溶液中的过量硫代巯基丙酸钠。版权所有（C）2013，JPO＆INPIT

4. 发明申请

WO2004082620A3 OXYCODONE CONJUGATES WITH LOWER THE ABUSE POTENTIAL AND EXTENDED DURATION OF ACTION 审中-公开
标题翻译：氧化还原能降低滥用潜力和延长治疗时间
公开(公告)号：WO2004082620A3
公开(公告)日：2005-09-15
申请号：PCT/US2004007910
申请日：2004-03-15
申请人： CONTROLLED CHEMICALS INC
发明人： SHAFER JULES A , TELYATNIKOV VLADISLAV V , GUO ZHIWEI
IPC分类号： A61K31/485 , A61K47/48
CPC分类号： C07D489/08 , A61K47/555 , A61K47/60
摘要： The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.
摘要翻译：降低生物可利用药物如鸦片止痛剂的滥用潜力，并且通过在制剂前将其转化为不良吸收的酯前药或其它前药衍生物来延长其作用时间。与活性药物的许多现有持续释放制剂不同，其中通过咀嚼，破碎或以其它方式破坏含有活性药剂的片剂或胶囊珠可以释放活性药剂，这种包含本发明前药的片剂或胶囊珠粒的机械加工既不释放活性药物也不妥协药物对药物的受控转化。此外，含有本发明前药或其他药物的片剂和胶囊珠可以用足够量的增稠剂如羟丙基甲基纤维素或羧甲基纤维素配制，以阻止不适用于这些给药模式的制剂的不适当的静脉内和鼻内施用。

5. 发明专利

CA2630703A1 PROCESSES FOR REDUCING CONTAMINATING MICHAEL ACCEPTOR LEVELS IN OXYCODONE AND OTHER COMPOSITIONS 未知
公开(公告)号：CA2630703A1
公开(公告)日：2007-05-31
申请号：CA2630703
申请日：2006-11-22
申请人： CONTROLLED CHEMICALS INC
发明人： WANG HAO , TELYATNIKOV VLADISLAV V , SHAFER JULES A
IPC分类号： C07D489/02
摘要： The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.

6. 发明专利

AU2006318445A1 Processes for reducing contaminating michael acceptor levels in oxycodone and other compositions 未知
公开(公告)号：AU2006318445A1
公开(公告)日：2007-05-31
申请号：AU2006318445
申请日：2006-11-22
申请人： CONTROLLED CHEMICALS INC
发明人： SHAFER JULES A , WANG HAO , TELYATNIKOV VLADISLAV V
IPC分类号： C07D489/02
摘要： The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.

7. 发明专利

MX345055B PROCEDIMIENTOS PARA REDUCIR NIVELES DE ACEPTOR DE MICHAEL CONTAMINANTES EN OXICODONA Y OTRAS COMPOSICIONES. 未知
公开(公告)号：MX345055B
公开(公告)日：2017-01-13
申请号：MX2012006612
申请日：2008-05-22
申请人： CONTROLLED CHEMICALS INC
发明人： SHAFER JULES A , TELYATNIKOV VLADISLAV V , WANG HAO
IPC分类号： C07D489/02
摘要： La presente invención se refiere a procedimientos para remover aceptores de Michael a partir de ciertas composiciones en donde la composición se trata con un compuesto que contiene tiol bajo condiciones suficientes para remover aceptores de Michael y los tiol-aductos de Michael resultantes; ciertas modalidades de la presente invención permiten la cuantificación y/o remoción de aceptores de Michael y/o precursores de aceptor de Michael.

8. 发明专利

CA2630703C PROCESSES FOR REDUCING CONTAMINATING MICHAEL ACCEPTOR LEVELS IN OXYCODONE AND OTHER COMPOSITIONS 未知
公开(公告)号：CA2630703C
公开(公告)日：2014-05-20
申请号：CA2630703
申请日：2006-11-22
申请人： CONTROLLED CHEMICALS INC
发明人： SHAFER JULES A , TELYATNIKOV VLADISLAV V , WANG HAO
IPC分类号： C07D489/02
摘要： The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors. The removal of the Michael acceptors using thio-containing compounds is characterized by the following reaction: (see above formula).

9. 发明专利

DE602004024963D1 未知
公开(公告)号：DE602004024963D1
公开(公告)日：2010-02-25
申请号：DE602004024963
申请日：2004-03-15
申请人： CONTROLLED CHEMICALS INC
发明人： SHAFER JULES A , TELYATNIKOV VLADISLAV V , GUO ZHIWEI
IPC分类号： A61K47/48 , A61K31/485
摘要： The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.

10. 发明专利

MX2008006710A PROCEDIMIENTOS PARA REDUCIR NIVELES DE ACEPTOR DE MICHAEL CONTAMINANTES EN OXICODONA Y OTRAS COMPOSICIONES. 未知
公开(公告)号：MX2008006710A
公开(公告)日：2008-12-16
申请号：MX2008006710
申请日：2006-11-22
申请人： CONTROLLED CHEMICALS INC
发明人： SHAFER JULES A , TELYATNIKOV VLADISLAV V , WANG HAO
IPC分类号： C07D489/02
摘要： La presente invención se refiere a un procedimiento para remoción de aceptores de Michael para ciertas composiciones, en donde la composición se trata con un compuesto que contiene tiol bajo condiciones suficientes para remover los aceptores de Michael y los aductos de tiol-de Michael resultantes; ciertas modalidades de la presente invención permiten la cuantificación y/o remoción de aceptores de Michael y/o precursores del aceptor de Michael.

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