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    Malonic acid di-salts and a method for preparing malonyl dihalides
    2.
    发明授权
    Malonic acid di-salts and a method for preparing malonyl dihalides 有权
    丙二酸二盐和一种制备丙二酰二卤化物的方法

    公开(公告)号：US09108965B2

    公开(公告)日：2015-08-18

    申请号：US14364340

    申请日：2012-12-13

    Applicant: E I DU PONT DE NEMOURS AND COMPANY

    Inventor： Wenming Zhang

    IPC: C07D471/04 ,  C07C57/34 ,  C07C51/60 ,  C07C55/36 ,  C07C57/36 ,  C07D213/55

    CPC classification number: C07D471/04 ,  C07C51/60 ,  C07C55/36 ,  C07C57/34 ,  C07C57/36 ,  C07D213/55 ,  C07C57/72

    Abstract: A compound of Formula 2 is disclosed wherein R1, MA and MB are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 1 wherein R1 and X are as defined in the disclosure comprising contacting a compound of Formula 2 with a halogenating agent. Also disclosed is a method for preparing a compound of Formula 4 wherein R1, R3 and R4 are as defined in the disclosure, comprising reacting a compound of Formula 5 wherein R3 and R4 are as defined in the disclosure with a compound of Formula 1, with a compound of Formula 1, the process of preparing the compound of Formula 4 includes the step of preparing the compound of Formula 1 from the compound of Formula 2 by the method disclosed above. Also disclosed is compound that is methyl 3,5-dichlorobenzeneethanimidate methyl 3,5-dichlorobenzeneethanimidate or ethyl 3,5-dichlorobenzeneethanimidate or salts thereof.

    Abstract translation: 公开了式2的化合物，其中R1，MA和MB如本公开所定义。 还公开了制备式1化合物的方法，其中R 1和X如本公开所定义，包括使式2的化合物与卤化剂接触。 还公开了制备式4化合物的方法，其中R 1，R 3和R 4如本公开内容所定义，包括使式5的化合物，其中R 3和R 4如本发明所定义的化合物与式1化合物与式 式1化合物，制备式4化合物的方法包括通过上述方法由式2化合物制备式1化合物的步骤。 还公开了3,5-二氯苯甲酰亚胺酸甲酯，3,5-二氯苯甲酰亚胺酸甲酯或3,5-二氯苯甲酰亚氨酸乙酯或其盐的化合物。

    MALONIC ACID DI-SALTS AND A METHOD FOR PREPARING MALONYL DIHALIDES
    3.
    发明申请
    MALONIC ACID DI-SALTS AND A METHOD FOR PREPARING MALONYL DIHALIDES 有权
    马来酸钠盐和制备丙二醛的方法

    公开(公告)号：US20140343284A1

    公开(公告)日：2014-11-20

    申请号：US14364340

    申请日：2012-12-13

    Applicant: E I DU PONT DE NEMOURS AND COMPANY

    Inventor： Wenming Zhang

    IPC: C07D471/04 ,  C07C55/36 ,  C07D213/55 ,  C07C57/36 ,  C07C51/60

    CPC classification number: C07D471/04 ,  C07C51/60 ,  C07C55/36 ,  C07C57/34 ,  C07C57/36 ,  C07D213/55 ,  C07C57/72

    Abstract: A compound of Formula 2 is disclosed wherein R1, MA and MB are as defined in the disclosure.Also disclosed is a method for preparing a compound of Formula 1 wherein RI and X are as defined in the disclosure comprising contacting a compound of Formula 2 with a halogenating agent.Also disclosed is a method for preparing a compound of Formula 4 wherein R1, R3 and R4 are as defined in the disclosure, comprising reacting a compound of Formula 5 wherein R3 and R4 are as defined in the disclosure with a compound of Formula 1, with a compound of Formula 1, the process of preparing the compound of Formula 4 includes the step of preparing the compound of Formula 1 from the compound of Formula 2 by the method disclosed above.Also disclosed is compound that is methyl 3,5-dichlorobenzeneethanimidate methyl 3,5-dichlorobenzeneethanimidate or ethyl 3,5-dichlorobenzeneethanimidate or salts thereof.

    Abstract translation: 公开了式2的化合物，其中R1，MA和MB如本公开所定义。 还公开了制备式1化合物的方法，其中R 1和X如本公开所定义，包括使式2的化合物与卤化剂接触。 还公开了制备式4化合物的方法，其中R 1，R 3和R 4如本公开内容所定义，包括使式5的化合物，其中R 3和R 4如本发明所定义的化合物与式1化合物与式 式1化合物，制备式4化合物的方法包括通过上述方法由式2化合物制备式1化合物的步骤。 还公开了3,5-二氯苯甲酰亚胺酸甲酯，3,5-二氯苯甲酰亚胺酸甲酯或3,5-二氯苯甲酰亚氨酸乙酯或其盐的化合物。

    Supermolecular carboplatinum derivatives, their preparation and pharmaceutical composition containing tem as active ingredient and applications of the compositions
    4.
    发明申请
    Supermolecular carboplatinum derivatives, their preparation and pharmaceutical composition containing tem as active ingredient and applications of the compositions 失效
    超分子卡铂衍生物，其制备方法和药物组合物含有作为活性成分的组合物和组合物的应用

    公开(公告)号：US20050165093A1

    公开(公告)日：2005-07-28

    申请号：US10497081

    申请日：2001-11-30

    Applicant: Jingzun Wang ,  Huisheng Qu ,  Lei Wang ,  Ting Wang

    Inventor： Jingzun Wang ,  Huisheng Qu ,  Lei Wang ,  Ting Wang

    IPC: A61P35/00 ,  A61K31/282 ,  C07C57/36 ,  C07C59/245 ,  C07C59/255 ,  C07C59/265 ,  C07C61/04 ,  C07F15/00 ,  A61K31/28

    CPC classification number: C07F15/0093

    Abstract: The present invention relates to a novel class of supermolecular carboplatin derivatives represented by general formula (I), wherein B is a polycarboxylic acid represented by general formula (II), wherein R1, R2 and n are defined as in the description. The present invention also relates to a process for preparing the same, pharmaceutical compositions containing the same as active ingredient and the use of the derivatives in the preparation of pharmaceutical compositions which are useful in treating various cellular cancers including hepatoma, stomach cancer, lung cancer and the like. The derivatives have stable cage-like chemical structures and constitutions in solid and in aqueous solution. The derivatives can not only kill cancer cells at a rate significantly higher than that by carboplatin, in particular, in the case of hepatoma cells, at a rate one to two times higher than that by carboplatin, but also produce little side effects such as vomit, baldness, decreases of leucocytes and platelets, and the like, which can be induced by administration of other chemotherapeutics. In the acute toxicity tests on mice, the lethal dose (LD50) of the present derivatives is about 300 mg/kg and 260 mg/kg body weight for a subcutaneous(sc) and an intraperitoneal(ip) administration, respectively. Therefore, the present derivatives are a novel class of cis-platium which can be widely used as anticancer agents.

    Abstract translation: 本发明涉及由通式（I）表示的新一类超分子卡铂衍生物，其中B是由通式（II）表示的多元羧酸，其中R 1，R 2 ＆lt; / SUB＆gt;和n如在说明书中所定义。 本发明还涉及其制备方法，其含有与活性成分相同的药物组合物和该衍生物在制备药物组合物中的用途，所述药物组合物可用于治疗各种细胞癌，包括肝癌，胃癌，肺癌和 类似。 该衍生物在固体和水溶液中具有稳定的笼状化学结构和结构。 衍生物不仅可以以比卡铂显着更高的速率杀死癌细胞，特别是在肝癌细胞的情况下，其比率高于卡铂的一至二倍，而且还产生很少的副作用，例如呕吐 ，秃发，白细胞和血小板的减少等，其可以通过施用其它化学治疗剂诱导。 在对小鼠的急性毒性试验中，本发明衍生物的致死剂量（LD 50 N）为皮下（sc）和腹膜内（ip）为约300mg / kg和260mg / kg体重 ）管理。 因此，本发明的衍生物是可广泛用作抗癌剂的新型顺铂。

    Process for preparing alkyl- and arylmalonic acids
    6.
    发明授权
    Process for preparing alkyl- and arylmalonic acids 失效
    制备烷基和芳基丙二酸的方法

    公开(公告)号：US5849949A

    公开(公告)日：1998-12-15

    申请号：US64005

    申请日：1998-04-21

    Applicant: Klaus-Dieter Steffen

    Inventor： Klaus-Dieter Steffen

    IPC: C07C27/02 ,  C07C51/09 ,  C07C51/48 ,  C07C55/02 ,  C07C57/36 ,  C07C61/04 ,  C07C61/09 ,  C07C51/00

    CPC classification number: C07C51/09

    Abstract: Alkyl- and arylmalonic acids of the formula I ##STR1## where R.sup.1 =H, C.sub.1 -C.sub.12 -alkyl, phenyl, C.sub.1 -C.sub.4 -alkylphenyl, C.sub.2 -C.sub.4 -dialkylphenyl, R.sup.2 =C.sub.1 -C.sub.12 -alkyl, phenyl, C.sub.1 -C.sub.4 -alkylphenyl, C.sub.2 -C.sub.4 -dialkylphenyl or R.sup.1 +R.sup.2 =--CH.sub.2 --CH.sub.2 --, are prepared by alkaline saponification by hydrolyzing the corresponding C.sub.1 -C.sub.4 -alkyl esters of the malonic acid of formula I, with alkali metal hydroxide dissolved in an aqueous alkali metal salt solution containing salt at 90-100% of saturation, acidifying the hydrolysis product with a mineral acid, removing the precipitated alkali metal salt which forms upon acidification, and extracting the alkyl- and arylmalonic acid formed from the aqueous solution with the aid of an organic solvent.

    Abstract translation: 式I的烷基和芳基丙二酸（I）其中R1 = H，C1-C12-烷基，苯基，C1-C4-烷基苯基，C2-C4-二烷基苯基，R2 = C1-C12-烷基，苯基， C 1 -C 4 - 烷基苯基，C 2 -C 4 - 二烷基苯基或R 1 + R 2 = -CH 2 -CH 2 - ，是通过碱溶解通过水解相应的式I的丙二酸的C 1 -C 4烷基酯与碱金属氢氧化物 在含有90-100％饱和盐的碱金属盐水溶液中，用无机酸酸化水解产物，除去在酸化时形成的沉淀的碱金属盐，并提取由水溶液形成的烷基和芳基丙二酸 借助有机溶剂。

    Alkylated or alkenylated malonic acid or its derivatives having a fluorine
    7.
    发明授权
    Alkylated or alkenylated malonic acid or its derivatives having a fluorine 失效
    烷基化或链烯基化的丙二酸或其具有氟的衍生物

    公开(公告)号：US4578503A

    公开(公告)日：1986-03-25

    申请号：US528134

    申请日：1983-08-31

    Applicant: Nobuo Ishikawa ,  Takeshi Nakai ,  Yoshio Inouye

    Inventor： Nobuo Ishikawa ,  Takeshi Nakai ,  Yoshio Inouye

    IPC: C07C69/65 ,  C07C69/716 ,  C07C67/317 ,  C07C57/36 ,  C07C69/612

    CPC classification number: C07C69/65 ,  C07C69/716

    Abstract: An alkylated or alkenylated malonic ester having a fluorine containing aliphatic substituent and derivatives thereof as expressed by the following general formula: ##STR1## where R.sub.f is a fluorine containing aliphatic group, R is an aliphatic group, or hydrogen or alkali metal atom, and R' is an unsubstituted or substituted aliphatic group.And a method to trap the enolate ion of a malonic ester having a fluorine containing aliphatic substituent as expressed by the following general formula,R.sub.f CH(CO.sub.2 R).sub.2where R.sub.f is a fluorine containing aliphatic group and R is an aliphatic group, hydrogen or alkali metal atom, wherein said malonic ester is converted under the action of a weaker base and/or fluoride ion to a fluorine containing enolate ion to be trapped as expressed by the following general formula:R.sub.f C.sup..crclbar. (CO.sub.2 R).sub.2where R.sub.f and R are the same as above.

    Abstract translation: 具有含氟脂肪族取代基的烷基化或链烯基化丙二酸酯及其衍生物，由以下通式表示：其中Rf是含氟脂族基团，R是脂族基团或氢或碱金属原子，R '是未取代或取代的脂族基团。 和捕获具有含氟脂肪族取代基的丙二酸酯的烯醇化物离子的方法，其由以下通式表示：RfCH（CO2R）2，其中Rf是含氟脂族基团，R是脂族基团，氢或碱金属 原子，其中所述丙二酸酯在较弱碱和/或氟离子的作用下转化为要被捕获的含氟烯醇化物离子，如以下通式表示：RfC（ - ）（CO 2 R）2，其中Rf和R为 与上述相同。

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