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    • 7. 发明申请
    • PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR HYPERLIPIDEMIA
    • 高效药物和/或治疗药物
    • US20100069433A1
    • 2010-03-18
    • US12593356
    • 2008-03-28
    • Toshiaki TakizawaNoriyuki InoueKatsutoshi Miyosawa
    • Toshiaki TakizawaNoriyuki InoueKatsutoshi Miyosawa
    • A61K31/47A61K31/42
    • C07D263/58A61K31/423A61K31/47
    • The present invention provides a therapeutic agent for hyperlipidemia having an excellent effect of lowering the cholesterol and triglyceride level in blood plasma.The present invention relates to a prophylactic and/or therapeutic agent for hyperlipidemia, a prophylactic and/or therapeutic agent for obesity or diabetes mellitus, and a prophylactic and/or therapeutic agent for metabolic syndrome, each agent including a compound represented by the following formula (1): , wherein: R1 and R2, which may be identical or different, each represent a hydrogen atom, a methyl group or an ethyl group; R3a, R3b, R4a and R4b, which may be identical or different, each represent a hydrogen atom, a halogen atom, a nitro group, a hydroxyl group, a C1-4 alkyl group, a trifluoromethyl group, a C1-4 alkoxy group, a C1-4 alkylcarbonyloxy group, a di-C1-4 alkylamino group, a C1-4 alkylsulfonyloxy group, a C1-4 alkylsulfonyl group, a C1-4 alkylsulfinyl group, or a C1-4 alkylthio group, or R3a and R3b, or R4a and R4b are joined to represent an alkylenedioxy group; X represents an oxygen atom, a sulfur atom or N—R5 (wherein R5 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkylsulfonyl group, or a C1-4 alkyloxycarbonyl group); Y represents an oxygen atom, a S(O)l group (l represents a number from 0 to 2), a carbonyl group, a carbonylamino group, an aminocarbonyl group, a sulfonylamino group, an aminosulfonyl group, or an NH group; Z represents CH or N; n represents a number from 1 to 6; and m represents a number from 2 to 6, or a salt thereof, and a statin, particularly pitavastatin, in combination.
    • 本发明提供了具有降低血浆中胆固醇和甘油三酯水平的优异效果的高脂血症治疗剂。 本发明涉及高脂血症的预防和/或治疗剂,肥胖症或糖尿病的预防和/或治疗剂,以及代谢综合征的预防和/或治疗剂,每种试剂包括由下式表示的化合物 (1)表示:其中:R 1和R 2可以相同或不同,各自表示氢原子,甲基或乙基; R3a,R3b,R4a和R4b可以相同或不同,分别表示氢原子,卤素原子,硝基,羟基,C1-4烷基,三氟甲基,C1-4烷氧基 ,C 1-4烷基羰基氧基,二-C 1-4烷基氨基,C 1-4烷基磺酰氧基,C 1-4烷基磺酰基,C 1-4烷基亚磺酰基或C 1-4烷硫基,或R 3a和R 3b ,或R4a和R4b连接以代表亚烷基二氧基; X表示氧原子,硫原子或N-R5(其中,R5表示氢原子,C1-4烷基,C1-4烷基磺酰基或C1-4烷氧基羰基)。 Y表示氧原子,S(O)1基(l表示0〜2的数),羰基,羰基氨基,氨基羰基,磺酰基氨基,氨基磺酰基或NH基。 Z表示CH或N; n表示1〜6的数; m代表2至6的数,或其盐,他汀类,特别是匹伐他汀组合。