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    • 1. 发明授权
    • MDR resistance treatment and novel pharmaceutically active
riminophenazines
    • MDR抗性治疗和新型药学活性的riminophenazines
    • US5763443A
    • 1998-06-09
    • US738473
    • 1996-10-28
    • Constance Elizabeth MedlenRonald AndersonJohn Francis O'Sullivan
    • Constance Elizabeth MedlenRonald AndersonJohn Francis O'Sullivan
    • A61K31/498C07D241/46A61K31/495
    • A61K31/498
    • The invention concerns the new use of riminophenazines in the treatment of a patient who has built up, or could build up, resistance to a therapeutically active substance, such as a patient requiring treatment for cancer. The riminophenazine conveniently may be of the general formula (I). ##STR1## R.sup.1 is a hydrogen atom, a halogen atom or a (C.sub.1 -C.sub.3) alkyl, (C.sub.1 -C.sub.3) alkoxy, fluoromethoxy or trifluoromethyl radical, R.sup.2 is a hydrogen or halogen atom, R.sup.3 is selected from hydrogen, (C.sub.1 -C.sub.4) alkyl, N,N-dialkylamino alkyl, (C.sub.3 -C.sub.12) cycloalkyl, methylcyclohexyl, hydroxycyclohexyl, cycloalkylmethyl, piperidyl, alkyl substituted piperidyl or N-benzyl-substituted pipperidyl, R.sup.4 is a hydrogen or halogen atom or a (C.sub.1 -C.sub.3) alkyl, (C.sub.1 -C.sub.3) alkoxy, fluoromethoxy or trifluoromethyl radical, and n is 1, 2 or 3. The invention also provides novel riminophenazines of general formula (I), their preparation, and compositions containing them.
    • 本发明涉及用于治疗已经建立或可能增加对治疗活性物质(例如需要治疗癌症的患者)的患者的治疗的患者的新用途。 方便地可以具有通式(I)的riminophenazine。 (C 1 -C 3)烷基,(C 1 -C 3)烷氧基,氟甲氧基或三氟甲基,R 2是氢或卤素原子,R 3选自氢,(C 1 -C 4)烷基,N,N-二烷基氨基烷基, (C 3 -C 12)环烷基,甲基环己基,羟基环己基,环烷基甲基,哌啶基,烷基取代的哌啶基或N-苄基取代的哌啶子基,R4是氢或卤素原子或(C1-C3)烷基,(C1-C3)烷氧基, 或三氟甲基,n为1,2或3.本发明还提供通式(I)的新型riminophenazine,其制备方法和含有它们的组合物。
    • 2. 发明授权
    • Anti-parasitic activity
    • 抗寄生虫活性
    • US5763442A
    • 1998-06-09
    • US591032
    • 1996-01-25
    • Constance Elizabeth MedlenRonald Anderson
    • Constance Elizabeth MedlenRonald Anderson
    • C07D241/46A61K31/495A61K31/498A61P33/02A61K31/50
    • A61K31/498A61K31/495
    • The invention provides the use of a riminophenazine in the manufacture of a medicament to treat parasitic infections. The riminophenazine may be used for the prophylactic treatments of maleria or for the therapeutic treatment of maleria. A known anti-maleria drug, e.g. chloroquine or mefloquine may be administered as well. The riminophenazine may be a compound of the general formula: ##STR1## wherein: R.sup.1 is selected from hydrogen atoms, halogen atoms, alkyl, alkoxy and trifluoromethyl radicals, R.sub.2 is selected from hydrogen or halogen atoms, R.sup.3 is selected from hydrogen atoms, alkyl, substituted alkyl, cycloalkyl, cycloalkylalkyl, unsubstituted heterocyclic radicals, substituted heterocyclic radicals, unsubstituted heterocyclicalkyl and substituted heterocyclicalkyl radicals.
    • 本发明提供了在制备用于治疗寄生虫感染的药物中使用边缘吩吩嗪的用途。 所述的林必泛嗪可用于预防性治疗恶性肿瘤或用于治疗恶性肿瘤。 已知的抗疟药物,例如, 也可以施用氯喹或甲氟喹。 边缘吩吩嗪可以是以下通式的化合物:其中:R 1选自氢原子,卤素原子,烷基,烷氧基和三氟甲基,R 2选自氢或卤素原子,R 3选自氢 原子,烷基,取代的烷基,环烷基,环烷基烷基,未取代的杂环基,取代的杂环基,未取代的杂环烷基和取代的杂环烷基。