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    • 4. 发明授权
    • Malononitrile compound and use thereof
    • 丙二腈化合物及其用途
    • US07439266B2
    • 2008-10-21
    • US10522764
    • 2003-08-26
    • Satoshi OkadaDaisuke OohiraKen Otaka
    • Satoshi OkadaDaisuke OohiraKen Otaka
    • A01N37/34C07C333/00C07C327/00C07C255/00
    • C07C255/23A01N37/34A01N43/08C07C255/19C07C327/22C07C2601/02C07C2601/14C07D307/33
    • 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.
    • 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。
    • 5. 发明授权
    • Taxol enhancer compounds
    • 紫杉醇增强剂化合物
    • US07037940B2
    • 2006-05-02
    • US10846152
    • 2004-05-14
    • Keizo KoyaLijun SunShoujun ChenNoriaki TatsutaYaming WuMitsunori Ono
    • Keizo KoyaLijun SunShoujun ChenNoriaki TatsutaYaming WuMitsunori Ono
    • A61K31/16A61K31/335C07C327/00C07D305/00
    • A61K47/48176A61K31/16A61K31/165A61K31/277A61K31/337A61K31/381A61K31/44A61K31/505A61K31/53A61K47/58C07C327/56C07C2601/02C07C2601/04C07C2601/08C07C2601/14C07D209/42C07D209/44C07D213/83C07D261/18C07D305/14C07D307/68C07D333/38C07D333/68C07D407/12
    • 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.
    • 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。