利索-全球专利检索

  1. 登录
  2. 注册
发明公开
CN104245694A 具有治疗活性的氨基亚甲基吡唑啉酮 有权 转让

具有治疗活性的氨基亚甲基吡唑啉酮
摘要：
一种具有式III的结构的化合物或其药学上可接受的加成盐，其用于恶性上皮肿瘤的治疗，尤其是用于延迟、预防或逆转前列腺癌的转移其中：X是NH或S；R1是H或(1C-4C)烷基；R2是(1C-4C)烷基、苯基或在环中具有一个或多个N-、O-或S-原子的单环芳族环，所述烷基、苯基或芳族环任选地被一个或多个选自(1C-4C)烷基、(1C-4C)烷氧基、卤代(1C-4C)烷基、卤代(1C-4C)烷氧基、苯氧基、苯硫基、卤素或硝基的基团取代；R3和R4各自独立地是H、(1C-6C)烷基、(2C-6C)烯基、(2C-6C)炔基、氰基、(3C-6C)环烷基、苯基、在环中具有一个或多个N-、O-或S-原子的单环芳族环、在环中具有一个或多个N-、O-或S-原子的单环非芳族环，其中的每个任选地被羟基、(1C-4C)烷氧基、苯基、环烷基、哌啶基、哌嗪基、呋喃基、噻吩基、吡嗪基、吡咯基、2H-吡咯基、吡唑基、异唑基、异噻唑基、吡咯烷酮基、吡咯啉基、咪唑啉基、咪唑基、在环中具有一个或多个N-、O-或S-原子的单环芳族环取代，其中这些任选取代基中的每个还任选地被(1C-4C)烷基、(1C-4C)烷氧基、卤代(1C-4C)烷基、卤代(1C-4C)烷氧基、卤素、硝基或形成环的(1C-2C)二氧基取代；或者R3和R4一起形成吡咯基、咪唑基、吡唑基、吡咯烷基、吡咯啉基咪唑烷基、咪唑啉基、哌啶基、哌嗪基吗啉基，其中的每个任选地被(1C-6C)烷基、苯基(1C-4C)烷基、苯基酮基(1C-4C)烷基取代；R5是H、Cl、F、Br、Me、NO2、叔丁基、OCF3、OCH3、CF3；R6是H、(1C-4C)烷基、(1C-4C)烷氧基、卤代(1C-4C)烷基、卤代(1C-4C)烷氧基、硝基或卤素；R7是H、F、Cl、Br、Me、NO2、叔丁基、OCF3、OCH3、CF3。
摘要（英）：

A compound having the structure according to formula III wherein: X is NH or S;R1 is H or (1C-4C)alkyl;R2 is (1C-4C)alkyl, phenyl or a monocyclic aromatic ring having one or more N-, O-or S-atoms in the ring, which alkyl, phenyl or aromatic ring is optionally substituted with one or more groups selected from (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, phenyloxy, phenylthio, halogen, or nitro;R3 and R4 are each independently H, (1C-6C)alkyl, (2C-6C) alkenyl, (2C-6C)alkynyl, cyano, (3C-6C)cycloalkyl, phenyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, a monocyclic non-aromatic ring having one or more N-, O- or S-atoms in the ring, each optionally substituted with hydroxyl, (1C-4C)alkoxy, phenyl, cycloalkyl, piperidyl, piperazinyl, furyl, thienyl, pirazinyl, pyrrolyl, 2H-pyrrolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyrrolidonyl, pyrrolinyl, imidazolinyl, imidazolyl, a monocyclic aromatic ring having one or more N-, O- or S- atoms in the ring, whereby each of these optional substituents is optionally further substituted with (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, halogen, nitro or (1C-2C)dioxol forming a ring;or R3 and R4 form together pyrrolyl, imidazolyl, pyrazolyl, pyrrolidinyl, pyrrolinylimidazolidinyl, imidazolinyl, piperidyl, piperazinylmorpholinyl, each optionally substituted with (1C-6C)alkyl, phenyl(1C-4C)alkyl, phenylketo(1C-4C)alkyl; R5 is H, Cl, F, Br, Me, NO2, t-butyl, OCF3, OCH3, CF3; R6 is H, (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, nitro or halogen;R7 is H,F, Cl, Br, Me, NO2, t-butyl, OCF3, OCH3, CF3; or pharmaceutically acceptable addition salts thereof for use in treatments of carcinoma, in particular to delay, prevent or reverse metastasis in prostate cancer.

公开/授权文献
0/0