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    • 1. 发明授权
    • Tricyclic compounds having ACAT inhibiting activity
    • 具有ACAT抑制活性的三环化合物
    • US5679703A
    • 1997-10-21
    • US523843
    • 1995-09-07
    • Masashi YanaseToshiaki KumazawaShiro ShirakuraEiko OishiKoji Yamada
    • Masashi YanaseToshiaki KumazawaShiro ShirakuraEiko OishiKoji Yamada
    • C07C275/28C07D313/12A61K31/335A61K31/38C07D337/12
    • C07C275/28C07D313/12C07C2103/32
    • Disclosed is a tricyclic compound represented by formula (I): ##STR1## where X.sup.1 -X.sup.2 represents CH.dbd.CH--CH.dbd.CH, CH.dbd.CH--CH.dbd.N or S--CH.dbd.CH; Y--Z represents CH.sub.2 --O or CH.sub.2 --S; then L--M represents C.dbd.CR.sup.9 (in which R.sup.9 represents hydrogen or lower alkyl) or CH--CR.sup.10 R.sup.11 (in which each of R.sup.10 and R.sup.11 independently represents hydrogen or lower alkyl); W represents NR.sup.4 (in which R.sup.4 represents hydrogen or lower alkyl) or O; each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen, lower alkyl, lower alkoxy, halogen, nitro, amino or mono or di-lower alkyl-substituted amino; R.sup.5 represents hydrogen or lower alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, halogen, lower alkyl or lower alkoxy; provided that when Y--Z represents CH.dbd.CH or CH.sub.2 CH.sub.2, then L--M represents C.dbd.CR.sup.9 (in which R.sup.9 has the same meaning as defined above),or CH--CR.sup.10a R.sup.11a (in which each of R.sup.10a and R.sup.11a represents lower alkyl of R.sup.10 and R.sup.11); and a pharmaceutically acceptable salt thereto. The compound and its salt have an ACAT inhibiting activity and are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.
    • 公开了由式(I)表示的三环化合物:其中X 1 -X 2表示CH = CH-CH = CH,CH = CH-CH = N或S-CH = CH; Y-Z表示CH 2 -O或CH 2 -S; 那么L-M表示C = CR9(其中R9表示氢或低级烷基)或CH-CR10R11(其中R10和R11各自独立地表示氢或低级烷基); W表示NR4(其中R4表示氢或低级烷基)或O; R 1,R 2和R 3各自独立地表示氢,低级烷基,低级烷氧基,卤素,硝基,氨基或单或二低级烷基取代的氨基; R5代表氢或低级烷基; R 6,R 7和R 8各自独立地表示氢,卤素,低级烷基或低级烷氧基; 条件是当YZ表示CH = CH或CH 2 CH 2时,LM表示C = CR 9(其中R9具有与上述相同的含义)或CH-CR10aR11a(其中R10a和R11a各自表示R10和R11的低级烷基) ; 和其药学上可接受的盐。 该化合物及其盐具有ACAT抑制活性,预期对高脂血症和动脉硬化具有预防和治疗作用。
    • 4. 发明申请
    • Piperidine derivatives
    • 哌啶衍生物
    • US20070185168A1
    • 2007-08-09
    • US11547810
    • 2005-04-07
    • Haruki TakaiShunji KunoriShiro ShirakuraKatsumi ShinodaAtsuko MizutaniKoji YamadaShinichiro TokiTomoyuki Nishikawa
    • Haruki TakaiShunji KunoriShiro ShirakuraKatsumi ShinodaAtsuko MizutaniKoji YamadaShinichiro TokiTomoyuki Nishikawa
    • A61K31/4439
    • C07D409/14
    • For example, a piperidine derivative represented by following formula (I) (wherein, —C(═O)-Z- represents —C(═O)—CH2—, —C(═O)—C(CH3)2—, —C(═O)—NH—, —C(═O)—O—, —C(═O)—S—, —C(═O)—CH2CH2—, —C(═O)—CH═CH—, —C(═O)—CH2O—, —C(═O)—CH2S—, —C(═O)—CH2CH2CH2— or —C(═O)—NR8CH2—; R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R2 represents a hydrogen atom or hydroxy; R3 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R5 represents a hydrogen atom, hydroxy, or the like; R6 represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkyl, or the like, etc.; R7 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like; n and k each independently represents an integer of 0 to 2; and ---- represents a single bond, or a double bond together with R4, where in case ---- is a single bond, R4 represents a hydrogen atom, hydroxy, or the like) or a pharmaceutically acceptable salt thereof and the like having an antagonistic activity for a glutamic acid receptor (NR2B/NMDA receptor) of an N-methyl-D-aspartic acid (NMDA) type containing an NR2B subunit are provided.
    • 例如,由下式(I)表示的哌啶衍生物(其中,-C(-O)-Z-表示-C(-O)-CH 2 - , - C( - -C(= O)-NH-, - C(-O)-O - , - C(-O) - S - , - C(-O)-CH 2 CH 2 - , - C(-O)-CH-CH - , - C(-O)-CH O - , - C(-O)-CH 2 S - , - C(-O)-CH 2 CH 2 2-CH 2 - 或-C( - )-NR 8 CH 2 - ; R 1 - SUP>表示氢原子,取代或未取代的低级烷基等; R 2表示氢原子或羟基; R 3表示氢原子,取代或未取代的 低级烷基等; R 5表示氢原子,羟基等; R 6表示氢原子,羟基,取代或未取代的低级烷基,或 R 7表示氢原子,卤素,取代或未取代的低级烷基等; n和k各自独立地表示0〜2的整数;< U STYLE = “ SINGLE“> ----表示单键,或与R 4连接的双键,其中如果是单键,则R” 对于N-甲基-D-葡萄糖酸的谷氨酸受体(NR2B / NMDA受体)具有拮抗作用的氨基酸或其药学上可接受的盐等) 提供了含有NR2B亚基的天冬氨酸(NMDA)型。