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    • 1. 发明申请
    • SUBSTITUTED HETEROCYCLIC DERIVATIVE HAVING SQUALENE EPOXIDASE INHIBITORY EFFECT AND USE THEREOF
    • 具有平均环氧化酶抑制作用的取代的杂环衍生物及其用途
    • WO1993024478A1
    • 1993-12-09
    • PCT/JP1993000723
    • 1993-05-28
    • BANYU PHARMACEUTICAL CO., LTD.TSUCHIYA, YoshimiNOMOTO, TakashiMITSUYA, MorihiroNONOSHITA, KatsumasaHAYASHI, MasahiroSATO, ToshihikoSAWASAKI, YoshioKAMEI, Toshio
    • BANYU PHARMACEUTICAL CO., LTD.
    • C07D333/16
    • C07D333/08C07D333/16C07D333/18C07D333/24
    • A substituted heterocyclic derivative represented by general formula (I), wherein R represents a 5- or 6-membered heterocyclic group containing one or two heteroatoms selected from among nitrogen and other atoms; Q represents (II), (III), -CH=CH-CH2-, etc., -CH2-O-CH2-, or thrimethylene; X and Y may be the same or different from each other and each represents methylene, oxygen, etc., or alternatively X and Y may be combined together to represent vinylene, etc.; Q represents either (a) a 5- or 6-membered aromatic group represented by (IV) wherein A &cir& _, B &cir& _, D &cir& _ and E &cir& _ represent each nitrogen, etc., or =CH-; and p represents an integer of 0 or 1, or (b) a group represented by -F &cir& _-G &cir& _-I &cir& _- wherein F &cir& _, G &cir& _ and I &cir& _ may be the same or different from each other and each represents oxygen, etc., or =CH-; R represents lowr alkyl, etc.; Q represents ethylene, etc.; Q represents vinylene, etc.; R and R may be the same or different from each other and each represents lower alkyl, or alternatively R and R are combined together with the adjacent carbon atom to represent cycloalkyl; and R represents hydrogen, lower alkyl, etc.
    • 由通式(I)表示的取代的杂环衍生物,其中R表示含有一个或两个选自氮原子和其它原子的杂原子的5-或6-元杂环基; Q 1表示(II),(III),-CH = CH-CH 2 - 等,-CH 2 -O-CH 2 - 或三亚甲基; X和Y可以相同或不同,各自表示亚甲基,氧等,或者X和Y可以组合在一起代表亚乙烯基等; Q 2表示(a)由(IV)表示的5或6元芳族基团,其中A 1和R 3各自表示每个氮等,或= CH- ; 并且p表示0或1的整数,或(b)由-F 1和R 3表示的基团,其中F 1和R 3可以相同或不同 彼此各自表示氧等,或= CH-; R 1表示低级烷基等; Q 3表示乙烯等。 Q 4表示亚乙烯基等; R 2和R 3可以彼此相同或不同,并且各自表示低级烷基,或者R 2和R 3与相邻的碳原子一起代表环烷基; R 4表示氢,低级烷基等。
    • 2. 发明申请
    • ARYLTHIOACETAMIDE DERIVATIVES
    • 三氯乙酰胺衍生物
    • WO1996026925A1
    • 1996-09-06
    • PCT/JP1996000412
    • 1996-02-23
    • BANYU PHARMACEUTICAL CO., LTD.ISHIKAWA, KiyofumiHAYAMA, TakashiKAMEI, ToshioNAGATA, Yasufumi
    • BANYU PHARMACEUTICAL CO., LTD.
    • C07D213/75
    • C07D213/75C07D239/58
    • Arylthioacetamide derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof, wherein Ar represents phenyl, naphthyl or pyridyl optionally having one to four substituents selected from the group consisting of lower alkyl, lower alkoxy and halogeno; R represents hydrogen or lower alkyl; R and R may be the same or different and each represents hydrogen, lower alkyl, lower alkoxy, lower alkylthio, mono(lower alkyl)amino or di(lower alkyl)amino, provided that the lower alkyl, lower alkoxy, lower alkylthio, mono(lower alkyl)amino or di(lower alkyl)amino may be substituted by pyrrolidino, etc. at arbitrary hydrogen atoms; n represents 0, 1 or 2; and X represents CH or N. The compounds inhibit ACAT to thereby suppress the formation of cholesterol esters, are expected to be usable as a remedy or preventive for hypercholesterolemia, hyperlipidemia, arteriosclerosis and cardiac diseases, etc. accompanying the same.
    • 通式(I)表示的芳基硫代乙酰胺衍生物或其药学上可接受的盐,其中Ar表示苯基,萘基或任选具有一至四个选自低级烷基,低级烷氧基和卤代的取代基的吡啶基; R 1表示氢或低级烷基; R 2和R 3可以相同或不同,各自表示氢,低级烷基,低级烷氧基,低级烷硫基,单(低级烷基)氨基或二(低级烷基)氨基,条件是低级烷基,低级 烷氧基,低级烷硫基,单(低级烷基)氨基或二(低级烷基)氨基可以在任意的氢原子被吡咯烷子基等取代; n表示0,1或2; 并且X表示CH或N.化合物抑制ACAT从而抑制胆固醇酯的形成,预期可用作补充或预防高胆固醇血症,高脂血症,动脉硬化和伴随其的心脏病等。