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    PROCESS FOR RECOVERING NOBLE PRODUCTS IN A PROCESS FOR PRODUCING DIALKYLAMINOALKYL (METH) ACRYLATES
    1.
    发明申请
    PROCESS FOR RECOVERING NOBLE PRODUCTS IN A PROCESS FOR PRODUCING DIALKYLAMINOALKYL (METH) ACRYLATES 有权
    二甲基亚氨基（甲基）丙烯酸酯生产方法中回收产品的方法

    公开(公告)号：US20140350291A1

    公开(公告)日：2014-11-27

    申请号：US14346802

    申请日：2012-09-11

    申请人： Jean-Michel Paul ,  Andre Levray

    发明人： Jean-Michel Paul ,  Andre Levray

    IPC分类号： C07C227/40 ,  C07C227/18 ,  C07C213/10

    CPC分类号： C07C227/40 ,  C07C67/327 ,  C07C213/06 ,  C07C213/10 ,  C07C227/18 ,  C07C69/54 ,  C07C219/20 ,  C07C215/08

    摘要： The invention relates to a process for recovery of noble products from heavy (meth)acrylic fractions generated during production of (meth)acrylic esters by transesterification, the heavy fractions comprising at least noble products and Michael adducts, the process comprising the steps of: (i) adding at least one antifouling agent and optionally a viscosity-reducing compound to the heavy fractions; (ii) submitting the mixture to temperature and distillation conditions sufficient to crack the Michael adducts into their components; and (iii) recovering the noble products in the form of a stream of distillate, and of a final residue that is sufficiently fluid to be transported by pump.

    摘要翻译： 本发明涉及从通过酯交换反应生产（甲基）丙烯酸酯的重质（甲基）丙烯酸部分中回收贵重产物的方法，所述重馏分至少包含贵重产物和迈克尔加合物，该方法包括以下步骤：（ i）向重馏分中加入至少一种防污剂和任选的降粘化合物; （ii）将混合物提供到足以将迈克尔加合物裂解成其组分的温度和蒸馏条件; 和（iii）以馏出物流的形式回收贵重产物，以及最终残留物，该残余物足够流动以便通过泵输送。

    Anticancer Agents Based on Regulation of Protein Prenylation
    5.
    发明申请
    Anticancer Agents Based on Regulation of Protein Prenylation 失效
    基于蛋白质磷酸化调节的抗癌剂

    公开(公告)号：US20060111329A1

    公开(公告)日：2006-05-25

    申请号：US11275662

    申请日：2006-01-23

    申请人： Seth Rose ,  Scott Lefler ,  Steven Ottersberg ,  Ann Kim ,  Karl Okolotowicz ,  Rosemarie Hartman

    发明人： Seth Rose ,  Scott Lefler ,  Steven Ottersberg ,  Ann Kim ,  Karl Okolotowicz ,  Rosemarie Hartman

    IPC分类号： A61K31/66 ,  C07F9/02 ,  C07C67/02 ,  C07D233/61

    CPC分类号： A61K31/66 ,  A61K31/20 ,  C07C69/63 ,  C07C217/46 ,  C07C219/20 ,  C07D303/32 ,  C07D303/48 ,  C07F9/091

    摘要： Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.

    摘要翻译： 已知当诸如Ras和RhoB的癌蛋白定位在癌细胞膜的内表面时，诸如Ras和RhoB的癌蛋白以无限制的方式诱导细胞分裂。 定位通过异戊烯化反应进行，由此在酶（例如法呢基蛋白转移酶）的存在下将疏水基团（例如法呢基）连接到蛋白质上。 因此，通过共价修饰来停用异戊烯基化酶可最终导致癌细胞生长的缓解和/或停止。 具有与异戊烯基化酶共价或基本上不可逆地键合的必需结构基团的各种异戊二烯基化抑制剂包括与疏水性底物模拟基团键合的羰基或硫代羰基化合物（或这些化合物的掩蔽型）和α氧代环氧化物。 羰基或硫代羰基化合物还含有核原子或基团以增强形成共价键的倾向。

    Method for purifying the azeotropic fraction generated during the synthesis of N,N-dimethyl aminoethyl acrylate
    7.
    发明授权
    Method for purifying the azeotropic fraction generated during the synthesis of N,N-dimethyl aminoethyl acrylate 有权
    纯化在合成N，N-二甲基氨基乙基丙烯酸酯期间产生的共沸馏分的方法

    公开(公告)号：US08940925B2

    公开(公告)日：2015-01-27

    申请号：US13146601

    申请日：2010-01-27

    申请人： Jean-Michel Paul ,  Coralie Graire ,  Audrey Riehl

    发明人： Jean-Michel Paul ,  Coralie Graire ,  Audrey Riehl

    IPC分类号： C07C213/06 ,  C07C231/10 ,  C07C213/10

    CPC分类号： C07C213/10 ,  C07C219/20

    摘要： The invention relates to a method for producing N,N-dimethylaminoethyl acrylate by the transesterification reaction of an alykl acrylate by N1N-dimethylaminoethanol, and more particularly relates to a method for purifying the azeotropic fraction generated during said reaction, thereby enabling the recycling thereof on the alkyl acrylate production unit. The aim of the method of the invention is in particular to remove the acetaldehyde and the dialkoxyethane contained in the azeotropic fraction, either by the direct distillation of the azeotropic fraction or by the distillation of the aqueous phase resulting from the water scrubbing of the azeotropic fraction.

    摘要翻译： 本发明涉及通过由N，N-二甲基氨基乙醇通过丙烯酸甲酯的酯交换反应制备N，N-二甲基氨基乙基丙烯酸酯的方法，更具体地说，涉及一种纯化所述反应过程中产生的共沸馏分的方法， 丙烯酸烷基酯生产单位。 本发明方法的目的是特别是通过直接蒸馏共沸馏分或通过蒸馏由共沸馏分进行水洗而产生的水相来除去共沸馏分中所含的乙醛和二烷氧基乙烷 。

    Anticancer agents based on regulation of protein prenylation
    9.
    发明授权
    Anticancer agents based on regulation of protein prenylation 失效
    基于蛋白异戊烯化调节的抗癌剂

    公开(公告)号：US07423170B2

    公开(公告)日：2008-09-09

    申请号：US11275662

    申请日：2006-01-23

    申请人： Seth D. Rose ,  Scott R. Lefler ,  Steven R. Ottersberg ,  Ann Y. Kim ,  Karl J. Okolotowicz ,  Rosemarie F. Hartman

    发明人： Seth D. Rose ,  Scott R. Lefler ,  Steven R. Ottersberg ,  Ann Y. Kim ,  Karl J. Okolotowicz ,  Rosemarie F. Hartman

    IPC分类号： C07C69/007 ,  C07C69/017 ,  A01N57/14 ,  A01N41/04 ,  A01N41/10

    CPC分类号： A61K31/66 ,  A61K31/20 ,  C07C69/63 ,  C07C217/46 ,  C07C219/20 ,  C07D303/32 ,  C07D303/48 ,  C07F9/091

    摘要： Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.

    摘要翻译： 已知当诸如Ras和RhoB的癌蛋白定位在癌细胞膜的内表面时，诸如Ras和RhoB的癌蛋白以无限制的方式诱导细胞分裂。 定位通过异戊烯化反应进行，由此在酶（例如法呢基蛋白转移酶）的存在下将疏水基团（例如法呢基）连接到蛋白质上。 因此，通过共价修饰来停用异戊烯基化酶可最终导致癌细胞生长的缓解和/或停止。 具有与异戊烯基化酶共价或基本上不可逆地键合的必需结构基团的各种异戊二烯基化抑制剂包括与疏水性底物模拟基团键合的羰基或硫代羰基化合物（或这些化合物的掩蔽型）和α氧代环氧化物。 羰基或硫代羰基化合物还含有核原子或基团以增强形成共价键的倾向。

    Method of producing oxybutynin and its derivatives
    10.
    发明申请
    Method of producing oxybutynin and its derivatives 审中-公开
    奥昔布宁及其衍生物的制备方法

    公开(公告)号：US20040006243A1

    公开(公告)日：2004-01-08

    申请号：US10438851

    申请日：2003-05-16

    申请人： THE UNIVERSITY OF TOKYO

    发明人： Masakatsu Shibasaki ,  Motomu Kanai

    IPC分类号： C07C229/34 ,  C07F009/80

    CPC分类号： C07F9/6552 ,  C07C219/20 ,  C07C2601/14 ,  C07F9/80

    摘要： An oxybutynin and its derivatives are produced by reacting a phenylketone with a silylcyanide in the presence of a specified asymmetric catalyst to obtain a siloxynitrile, and then reacting the siloxynitrile with a reducing agent and oxidizing the resulting aldehyde, or subjecting the siloxynitrile to a hydrolysis.

    摘要翻译： 奥昔布宁及其衍生物通过在特定的不对称催化剂存在下使苯基酮与甲硅烷基氰反应得到甲硅烷氧基腈，然后使甲硅烷氧基腈与还原剂反应并氧化得到的醛，或使甲硅烷氧基腈进行水解而制备。