Organosulfur Compounds, a Method of Making Organosulfur Compounds and their Use for Inhibiting the Growth of Tumour Cells
    2.
    发明申请
    Organosulfur Compounds, a Method of Making Organosulfur Compounds and their Use for Inhibiting the Growth of Tumour Cells 失效
    有机硫化合物,一种制备有机硫化合物的方法及其用于抑制肿瘤细胞生长的方法

    公开(公告)号:US20110190368A1

    公开(公告)日:2011-08-04

    申请号:US13057960

    申请日:2009-08-05

    摘要: Organosulfur compounds of the general formula (2) are described, wherein R1 and R2 are linear or branched C1-C5 alkyl; linear or branched C1-C5 alkenyl with the proviso that R1 is not prop-1-enyl (allyl); substituted linear or branched C1-C5 alkenyl or substituted linear or branched C1-C5 alkyl, in which the substituents are selected from OR3, NR4R5, COOR6, CON—R7R8, in which R3 is selected from H, COR9, para-methoxybenzyl and trialkylsilyl, in which R9 is alkyl or substituted alkyl; R4 N and R5 are alkyl or R4 and R5 together form a phthalimido group; R6 is alkyl or substituted alkyl; and R7 and R8 are alkyl or substituted alkyl; substituted or unsubstituted aromatic specifically where R1 and R2 are benzyl, para-methoxybenzyl and/or ortho,para-methoxybenzyl and substituted or unsubstituted heteroaromatic. The compounds can be used for inhibiting the growth of tumour cells and for treating cancer. A pharmaceutical composition and a method of preparing the compounds are also described.

    摘要翻译: 描述了通式(2)的有机硫化合物,其中R 1和R 2是直链或支链C 1 -C 5烷基; 直链或支链C 1 -C 5烯基,条件是R 1不是丙-1-烯基(烯丙基); 取代的直链或支链C 1 -C 5烯基或取代的直链或支链C 1 -C 5烷基,其中取代基选自OR 3,NR 4 R 5,COOR 6,CON-R 7 R 8,其中R 3选自H,COR 9,对甲氧基苄基和三烷基甲硅烷基 其中R9是烷基或取代的烷基; R4N和R5是烷基或R4和R5一起形成苯二甲酰亚氨基; R6是烷基或取代的烷基; 并且R 7和R 8是烷基或取代的烷基; 取代或未取代的芳族化合物,其中R 1和R 2是苄基,对甲氧基苄基和/或邻甲氧基苄基和取代或未取代的杂芳族。 该化合物可用于抑制肿瘤细胞的生长和治疗癌症。 还描述了药物组合物和制备该化合物的方法。

    Malononitrile compound and use thereof
    4.
    发明授权
    Malononitrile compound and use thereof 失效
    丙二腈化合物及其用途

    公开(公告)号:US07439266B2

    公开(公告)日:2008-10-21

    申请号:US10522764

    申请日:2003-08-26

    摘要: The present invention relates to a novel malononitrile compound represented by the formula (A): wherein, R1 represents C1 to C6 alkyl that may be substituted with halogen, C2 to C6 alkenyl that may be substituted with halogen, etc; R2 represents hydrogen atom or C1 to C6 alkyl that may be substituted with halogen; R3 represents hydrogen atom or C1 to C6 alkyl; R4 represents hydrogen atom or C1 to C6 alkyl; R5 represents C1 to C6 alkyl that may be substituted with halogen, C3 to C6 alkenyl that may be substituted with halogen, etc, or R4 and R5 may be combined at their terminal and represent ethylene that may be substituted with C1 to C3 alkyl or trimethylene that may be substituted with C1 to C3 alkyl; and Z1 and Z2, which are the same or different, represent oxygen atom or sulfur atom. The malononitrile compound has an efficient pesticidal activity and can control effectively pests such as insect pests, acarine pests, nematode pests and the like.

    摘要翻译: 本发明涉及由式(A)表示的新型丙二腈化合物:其中R 1表示可被卤素取代的C 1至C 6烷基,可被卤素取代的C 2至C 6烯基 等等 R 2表示氢原子或可被卤素取代的C 1至C 6烷基; R 3表示氢原子或C 1至C 6烷基; R 4表示氢原子或C 1至C 6烷基; R 5表示可被卤素取代的C 1至C 6烷基,可被卤素取代的C 3至C 6烯基,或R 4和R 5 可以在它们的末端结合并表示可被可被C1-C3烷基取代的C1-C3烷基或三亚甲基取代的乙烯; 和Z 1和Z 2 2相同或不同,表示氧原子或硫原子。 丙二腈化合物具有有效的杀虫活性,可有效控制害虫,如害虫,螨类害虫,线虫等。

    Taxol enhancer compounds
    5.
    发明授权
    Taxol enhancer compounds 失效
    紫杉醇增强剂化合物

    公开(公告)号:US07037940B2

    公开(公告)日:2006-05-02

    申请号:US10846152

    申请日:2004-05-14

    摘要: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5–R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2–C6 substituted or unsubstituted alkylene group. Z is ═0 or ═S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with taxol or an analog of taxol.

    摘要翻译: 公开了由结构式(I)表示的化合物:Y是共价键,亚苯基或取代或未取代的直链烃基。 此外,Y与它所键合的两个> C-Z基团一起是取代或未取代的芳族基团。 优选地,Y是共价键或-C(R 7 R 8) - 。 R 1和R 2分别独立地是芳基或取代的芳基,R 3和R 4是 独立的-H,脂族基团,取代的脂族基团,芳基或取代的芳基。 R 5 -R 6独立地是-H,脂族基团,取代的脂族基团,芳基或取代的芳基。 R 7和R 8各自独立地为-H,脂族或取代的脂族基团或R 7为-H, 8是取代或未取代的芳基,或者R 7和R 8一起是C2-C6取代或未取代的亚烷基。 Z是-O或-S。 还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。 还公开了通过向受试者施用结构式(I)的化合物与紫杉醇或紫杉醇的类似物组合治疗患有癌症的受试者的方法。

    Process for the preparation of hydroxy 4-methyl thiobutyric acid esters
    6.
    发明申请
    Process for the preparation of hydroxy 4-methyl thiobutyric acid esters 有权
    制备羟基-4-甲基硫代丁酸酯的方法

    公开(公告)号:US20010029308A1

    公开(公告)日:2001-10-11

    申请号:US09778191

    申请日:2001-02-07

    IPC分类号: C07C327/00

    CPC分类号: C07C319/20 C07C323/52

    摘要: A process, for the preparation of an ester of 2-hydroxy-4-methylthiobutyric acid which is substantially in the monomeric form, which process, being capable of industrial application and which comprises reacting 2-hydroxy-4-methylthiobutyric acid with an alcohol in the presence of water and an acid catalyst at a temperature of from 30 to 150null C. wherein the acid is the direct product of the hydrolysis of 2-hydroxy-4-methylthiobutyronitrile.

    摘要翻译: 一种制备基本上为单体形式的2-羟基-4-甲硫基丁酸酯的方法,该方法能够工业应用并且包括使2-羟基-4-甲硫基丁酸与醇反应 在30至150℃的温度下存在水和酸催化剂,其中酸是2-羟基-4-甲基硫代丁腈水解的直接产物。

    Polymerization catalyst promoter
    9.
    发明授权
    Polymerization catalyst promoter 失效
    聚合催化剂促进剂

    公开(公告)号:US5786504A

    公开(公告)日:1998-07-28

    申请号:US649736

    申请日:1996-05-15

    摘要: Compounds of the formula: ##STR1## wherein n is 1, 2, 3, or 4; X.sup.1 and X.sup.2 are each, independently, chlorine or bromine; A is O or S; R.sup.1 is hydrogen or C.sub.1 -C.sub.16 alkyl; R.sup.2 is C.sub.1 -C.sub.16 alkyl, C.sub.6 -C.sub.16 aryl, C.sub.1 -C.sub.4 alkylidene, or CH.sub.2 OR.sup.5 ; R.sup.3 is hydrogen, chlorine, bromine, or OR.sup.6 ; R.sup.4 is C.sub.1 -C.sub.16 alkyl, C.sub.7 -C.sub.16 aralkyl, C.sub.2 -C.sub.16 alkenyl, or C.sub.6 -C.sub.18 aryl; R.sup.5 is hydrogen, C.sub.1 -C.sub.16 alkyl, C.sub.7 -C.sub.16 aralkyl, C.sub.2 -C.sub.16 alkenyl, or C.sub.6 -C.sub.18 aryl; and R.sup.6 is hydrogen or C.sub.1 -C.sub.16 alkyl. These compounds by themselves and in combination with certain halo-but-2-enoic acids and esters are useful as catalyst promoters in ethylene polymerization processes.

    摘要翻译: 下式的化合物:其中n为1,2,3或4; X1和X2各自独立地为氯或溴; A是O或S; R1是氢或C1-C16烷基; R2是C1-C16烷基,C6-C16芳基,C1-C4亚烷基或CH2OR5; R3是氢,氯,溴或OR6; R4是C1-C16烷基,C7-C16芳烷基,C2-C16烯基或C6-C18芳基; R5是氢,C1-C16烷基,C7-C16芳烷基,C2-C16烯基或C6-C18芳基; 并且R 6是氢或C 1 -C 16烷基。 这些化合物本身并与某些卤代丁-2-烯酸和酯组合可用作乙烯聚合方法中的催化剂促进剂。

    Process to make .alpha.,.alpha.-difluoro-.beta.-hydroxyl thiol esters
    10.
    发明授权
    Process to make .alpha.,.alpha.-difluoro-.beta.-hydroxyl thiol esters 失效
    制备α,α-二氟-β-羟基硫醇酯的方法

    公开(公告)号:US5756775A

    公开(公告)日:1998-05-26

    申请号:US762622

    申请日:1996-12-09

    申请人: John A. Weigel

    发明人: John A. Weigel

    摘要: A process to make .alpha.,.alpha.-difluoro-.beta.-hydroxy thiol esters of formula (IIIA) ##STR1## comprising reacting a difluoroethanethioate of formula (IVA) ##STR2## with a second reactant selected from the group consisting of aldehydes, ketones, acid halides and esters; in a solvent and in the presence of a strong base; with the proviso that the process is conducted in the absence of a catalyst and in the absence of a silyl containing compound. These thiol esters are useful as intermediates in organic syntheses of pharmaceutical products.

    摘要翻译: 制备式(IIIA)的α,α-二氟-β-羟基硫羟酸酯(IIIA)的方法,包括使式(IVA)的二氟乙硫乙酸酯(IVA)与选自以下的第二反应物 的醛,酮,酰卤和酯; 在溶剂中并在强碱的存在下进行; 条件是该方法在不存在催化剂的情况下和在不存在含甲硅烷基的化合物的情况下进行。 这些硫醇酯可用作药物有机合成中的中间体。