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    • 3. 发明申请
    • PYRROLOPYRIDAZINE DERIVATIVE
    • 吡咯烷酮衍生物
    • WO1995019980A1
    • 1995-07-27
    • PCT/JP1995000038
    • 1995-01-18
    • SANKYO COMPANY, LIMITEDUBE INDUSTRIES, LTD.KIMURA, TomioFUJIHARA, YoshimiSHIBAKAWA, NobuhikoFUJIWARA, HiroshiITOH, EtsuroMATSUNOBU, KeijiTABATA, KeiichiYASUDA, Hiroshi
    • SANKYO COMPANY, LIMITEDUBE INDUSTRIES, LTD.
    • C07D487/04
    • C07D487/04
    • A pyrrolopyridazine derivative represented by general formula (I) and a pharmacologically acceptable salt thereof, wherein R represents C2-C6 alkenyl, halogenated C2-C6 alkenyl, (C6-C10 aryl)-substituted C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, (C3-C7 cycloalkyl)-substituted C1-C6 alkyl, (C5-C7 cycloalkenyl)-substituted C1-C6 alkyl or halogenated C1-C6 alkyl; R and R represent each independently hydrogen, C1-C6 alkyl or C6-C10 aryl; R represents hydrogen or C1-C6 alkyl; R represents C6-C10 aryl or five- to ten-membered heteroaryl wherein heteroatom(s) is(are) selected from among nitrogen, oxygen and sulfur atoms; A represents C1-C3 alkylene; X represents imino, oxygen, sulfur or methylene; m represents 0 or 1; and n represents 0 or 1. The derivative has excellent effects of suppressing gastric secretion and protecting gastric mucosa and an excellent antibacterial activity against Helicobacter pylori, thus being useful as a preventive or remedy for ulcerative diseases and the like.
    • 由通式(I)表示的吡咯并哒嗪衍生物及其药理学可接受的盐,其中R 1表示C 2 -C 6烯基,卤代C 2 -C 6烯基,(C 6 -C 10芳基) - 取代的C 2 -C 6烯基,C 2 -C 6 炔基,C 3 -C 7环烷基,(C 3 -C 7环烷基) - 取代的C 1 -C 6烷基,(C 5 -C 7环烯基) - 取代的C 1 -C 6烷基或卤代C 1 -C 6烷基; R 2和R 3各自独立地表示氢,C 1 -C 6烷基或C 6 -C 10芳基; R 4表示氢或C 1 -C 6烷基; R 5表示C6-C10芳基或五至十元杂芳基,其中杂原子选自氮,氧和硫原子; A表示C1-C3亚烷基; X表示亚氨基,氧,硫或亚甲基; m表示0或1; n表示0或1.该衍生物具有抑制胃分泌和保护胃粘膜的优异效果,对幽门螺杆菌具有优异的抗菌活性,因此可用作溃疡性疾病等的预防或治疗方法。
    • 5. 发明申请
    • PYRIMIDINE COMPOUND
    • 吡嗪化合物
    • WO1994007890A1
    • 1994-04-14
    • PCT/JP1993001412
    • 1993-10-01
    • UBE INDUSTRIES, LTD.KIMURA, TomioKUROKI, YoshiakiFUJIWARA, HiroshiANPEIJI, Shigeharu
    • UBE INDUSTRIES, LTD.
    • C07D401/12
    • C07D401/12C07D401/14C07D405/14C07D409/14
    • A pyrimidine derivative represented by general formula (II) or (III) and a salt thereof, both having selective acetylcholine esterase inhibitor and type A monoamine oxidase inhibitor effects, thus being useful as antidepressant and senile dementia remedy. In said formulae, R1 and R2 represent each H, halogen, amino, nitro, (un)substituted alkyl, alkoxy or alkoxycarbonyl, provided that R1 and R2 may be combined together to represent (un)substituted alkylene; R3 represents aralkyl or heteroaryl-alkyl; R4 represents H or acyl; R5 represents H, OH or alkoxy; R6 represents H, halogen, alkyl or alkoxy; X represents -CH=, -CH=CH-(CH2)p-, -CH2- or -CH2CH2-(CH2)p-; Y represents =CH-(CH2)p-, -CH2-(CH2)p-, single bond or double bond; p represents 0 or 1; and symbol .(OVERSCORE).(OVERSCORE).(OVERSCORE).(OVERSCORE).(OVERSCORE) represents either single or double bond.
    • 由通式(II)或(III)表示的嘧啶衍生物及其盐均具有选择性乙酰胆碱酯酶抑制剂和A型单胺氧化酶抑制剂作用,因此可用作抗抑郁药和老年痴呆症药物。 在所述式中,R 1和R 2表示每个H,卤素,氨基,硝基,(未)取代的烷基,烷氧基或烷氧基羰基,条件是R 1和R 2可以组合在一起代表(未)取代的亚烷基; R3表示芳烷基或杂芳基 - 烷基; R4代表H或酰基; R5表示H,OH或烷氧基; R6表示H,卤素,烷基或烷氧基; X表示-CH =,-CH = CH-(CH 2)p - , - CH 2 - 或-CH 2 CH 2 - (CH 2)p - Y表示= CH-(CH 2)p - , - CH 2 - (CH 2)p - 单键或双键; p表示0或1; (OVERSCORE)(OVERSCORE)(OVERSCORE)(OVERSCORE)(OVERSCORE)(OVERSCORE)(OVERSCORE)(OVERSCORE)(OVERSCORE)。