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    • 10. 发明授权
    • Quinuclidine derivative having tricyclic hetero condensed ring
    • 具有三环杂环稠环的奎宁环衍生物
    • US5830902A
    • 1998-11-03
    • US894549
    • 1997-08-21
    • Masahiko IsakaTsukasa IshiharaKoyo MatsudaHirotoshi KakutaHiroshi Moritani
    • Masahiko IsakaTsukasa IshiharaKoyo MatsudaHirotoshi KakutaHiroshi Moritani
    • C07D453/02A61K31/435C07D401/12C07D413/12C07D417/12
    • C07D453/02
    • A quinuclidine derivative represented by the following general formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, which has strong squalene synthase inhibiting activity and is useful as a cholesterol lowering agent without causing side effects. ##STR1## (Symbols in the formula represent the following meanings; R.sub.1 : a hydrogen atom, a halogen atom or a lower alkyl group, R.sub.2 : a hydrogen atom, a hydroxyl group or a lower alkoxy group, . . : a single bond or a double bond, with the proviso that R.sub.2 does not exist when . . . is a double bond, X and Y: the same or different from each other and each represents a bond, an oxygen atom (--O--), a carbonyl group (--CO--), a group represented by the formula --S(O).sub.p -- or a group represented by the formula --NR.sub.3 --, p: 0, 1 or 2, R.sub.3 : a hydrogen atom or a lower alkyl group which may have a substituent, A: a saturated or unsaturated lower alkylene group, a group of the formula --(CH.sub.2).sub.m Z(CH.sub.2).sub.n -- or a group of the formula --(CH.sub.2).sub.m Z(CH.sub.2).sub.n CR.sub.4 =, Z: an oxygen atom (--O--), a group of the formula --S(O).sub.q --, a carbonyl group (--CO--) or a group of the formula --NR.sub.5 --, R.sub.4 : a hydrogen atom, a halogen atom or a lower alkyl group, R.sub.5 : a hydrogen atom or a lower alkyl group, m and n: the same or different from each other and each is 0 or an integer of 1 to 5, m+n: an integer of 1 to 5 q: 0, 1 or 2, with the proviso that, when either one of X and Y is a bond, A is a group represented by the formula --(CH.sub.2).sub.m Z(CH.sub.2).sub.n CR.sub.4 =.)
    • PCT No.PCT / JP96 / 00491 Sec。 371日期1997年8月21日 102(e)日期1997年8月21日PCT 1996年3月1日PCT公布。 WO96 / 26938 PCT公开 日期1996年9月6日由以下通式(I)表示的奎宁环衍生物,其药学上可接受的盐,其水合物或溶剂合物,具有强的角鲨烯合酶抑制活性,可用作胆固醇降低剂而不引起侧 效果。 (I)(式中的符号表示以下含义; R1:氢原子,卤素原子或低级烷基,R2:氢原子,羟基或低级烷氧基,+ E,ovs ... + EE:单键或双键,条件是当+ E,ovs ... EE是双键时,R2不存在,X和Y彼此相同或不同 代表键,氧原子(-O-),羰基(-CO-),由式-S(O)p-表示的基团或由式-NR3-表示的基团,p:0, 1或2,R3:氢原子或可具有取代基的低级烷基,A:饱和或不饱和的低级亚烷基,式 - (CH2)mZ(CH2)n-的基团或 式 - (CH 2)m Z(CH 2)n CR 4 =,Z:氧原子(-O-),式-S(O)q-的基团,羰基(-CO-)或式 -NR5-,R4:氢原子,卤素原子或低级烷基,R5:氢原子或低级烷基,m和n:相同或不同 各自为0或1〜5的整数,m + n:1〜5的整数q:0,1或2,条件是当X和Y中的任一个为键时, A是由式 - (CH2)mZ(CH2)nCR4 =表示的基团。