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    • 1. 发明授权
    • Acylthiourea compound or salt thereof, and use thereof
    • 酰基硫脲化合物或其盐及其用途
    • US08304427B2
    • 2012-11-06
    • US12937312
    • 2009-04-09
    • Yoshimitsu SudaKosuke EgamiHidenori Fujita
    • Yoshimitsu SudaKosuke EgamiHidenori Fujita
    • A61K31/04C07D215/38
    • C07D215/48C07D401/12C07D405/12C07D409/12
    • Provided is a c-Met inhibitory antitumor agent which mitigates side effects by selectively affecting tumor cells in which c-Met is specifically expressed, having a formula (I) or its salt: wherein each of R1 and R2 are independently a hydrogen atom, an optionally substituted C1-6 alkyl, C3-10 cycloalkyl, C6-14 aromatic hydrocarbon, or saturated or unsaturated heterocyclic group, or R1 and R2 may form, together with the nitrogen atom to which they are attached, an optionally substituted nitrogen-containing heterocyclic ring; R3 is a C1-6 alkyl group; and R4, R5, and R6, are independently a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylamino group, an optionally substituted aromatic hydrocarbon group, or an optionally substituted saturated or unsaturated heterocyclic group, or R5 and R6 may form a ring together with the phenyl ring to which they are attached.
    • 本发明提供一种c-Met抑制性抗肿瘤剂,其通过选择性地影响c-Met特异性表达的具有式(I)或其盐的肿瘤细胞来减轻副作用:其中R1和R2各自独立地为氢原子, 任选取代的C 1-6烷基,C 3-10环烷基,C 6-14芳烃或饱和或不饱和杂环基,或R 1和R 2可以与它们所连接的氮原子一起形成任选取代的含氮杂环 环; R3是C1-6烷基; 和R 4,R 5和R 6独立地为氢原子,卤素原子,任选取代的C 1-6烷基,C 1-6烷氧基,C 1-6烷基氨基,任选取代的芳族烃基或 任选取代的饱和或不饱和杂环基,或R 5和R 6可以与它们所连接的苯环一起形成环。
    • 2. 发明申请
    • ACYLTHIOUREA COMPOUND OR SALT THEREOF, AND USE THEREOF
    • 乙酰化合物或其盐,及其用途
    • US20110034439A1
    • 2011-02-10
    • US12937312
    • 2009-04-09
    • Yoshimitsu SudaKosuke EgamiHidenori Fujita
    • Yoshimitsu SudaKosuke EgamiHidenori Fujita
    • A61K31/55C07D215/233A61K31/47A61K31/4709C07D413/12A61K31/5377C07D401/12A61P35/00
    • C07D215/48C07D401/12C07D405/12C07D409/12
    • To provide an antitumor agent which exhibits excellent c-Met inhibitory effect and mitigates side effects by virtue of selectively affecting to tumor cells in which c-Met is specifically expressed.The invention provides an acylthiourea compound represented by formula (I): (wherein each of R1 and R2, which may be the same or different, represents a hydrogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted C3-10 cycloalkyl group, an optionally substituted C6-14 aromatic hydrocarbon group, or an optionally substituted saturated or unsaturated heterocyclic group, or R1 and R2 may form, together with the nitrogen atom to which they are attached, an optionally substituted nitrogen-containing heterocyclic ring; R3 represents a C1-6 alkyl group; and each of R4, R5, and R6, which may be identical to or different from one another, represents a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylamino group, an optionally substituted aromatic hydrocarbon group, or an optionally substituted saturated or unsaturated heterocyclic group, or R5 and R6 may form a ring together with the phenyl ring to which they are attached) or a salt thereof.
    • 提供通过选择性地影响c-Met特异性表达的肿瘤细胞,其表现出优异的c-Met抑制作用并减轻副作用的抗肿瘤剂。 本发明提供由式(I)表示的酰基硫脲化合物:其中R 1和R 2各自可以相同或不同,表示氢原子,任选取代的C 1-6烷基,任选取代的C 3-10环烷基 基团,任选取代的C 6-14芳族烃基或任选取代的饱和或不饱和杂环基,或R 1和R 2可以与它们所连接的氮原子一起形成任选取代的含氮杂环; R 3 可以相同或不同的R4,R5,R6各自表示氢原子,卤素原子,任意取代的C1-6烷基,C1- C6烷氧基,C1-6烷基氨基,任选取代的芳族烃基或任选取代的饱和或不饱和杂环基,或者R 5和R 6可以与它们所代表的苯环一起形成环 e附着)或其盐。