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    • 7. 发明申请
    • NOVEL 8-(2-AMINOALKOXY)FLUOROCHROMAN DERIVATIVE
    • 新型8-(2-氨基烷氧基)氟代吡啶衍生物
    • WO1994029293A1
    • 1994-12-22
    • PCT/JP1994000923
    • 1994-06-08
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.YASUNAGA, TomoyukiKIMURA, TakenoriNAITO, RyoKONTANI, ToruYAMAGUCHI, TokioWANIBUCHI, Fumikazu
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D311/22
    • C07D407/12C07D311/22
    • An 8-(2-aminoalkoxy)fluorochroman derivative represented by general formula (I) or a salt thereof, both having a selective affinity for 5-HT1A receptors and being useful for treating psychoneurotic diseases such as anxiety, manic-depressive state and schizophrenia, sex disorder, eating disorder, sleep disorder, and drug dependence: wherein R, R2 and R3 represent each lower alkoxy, etc., or R1 and R2 may be combined together to represent -O-(CH2)m-O- (wherein m is an integer of 1 to 3), etc.; R4 represents hydrogen, lower alkyl or aralkyl; R represent hydroxy, amino or lower alkoxy; R6 represents hydrogen or lower alkyl, provided R5, R6 and the carbon atom to which they are bonded are combined together to represent carbonyl; A represents an ethylene group which may be substituted by lower alkyl; and B represents optionally branched C1-C10 alkylene.
    • 对通式(I)表示的8-(2-氨基烷氧基)氟苯并喃喃衍生物或其盐对5-HT 1A受体具有选择性亲和力,可用于治疗焦虑,躁狂抑郁状态和精神分裂症等精神病性疾病, 性障碍,进食障碍,睡眠障碍和药物依赖性:其中R,R 2和R 3表示各个低级烷氧基等,或者R 1和R 2可以组合在一起代表-O-(CH 2)m O-(其中m是 1〜3的整数)等; R4代表氢,低级烷基或芳烷基; R 5代表羟基,氨基或低级烷氧基; R6表示氢或低级烷基,其中R5,R6和它们所键合的碳原子结合在一起代表羰基; A表示可被低级烷基取代的亚乙基; B表示任选支链的C 1 -C 10亚烷基。
    • 8. 发明申请
    • SERINE DERIVATIVE
    • 丝氨酸衍生物
    • WO1994025450A1
    • 1994-11-10
    • PCT/JP1994000697
    • 1994-04-26
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.NODA, IchioIWATA, MasahiroSAKAMOTO, ShuichiKOSHIYA, KazuoMORITA, TakumaKOHARA, Atsuyuki
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D307/52
    • C07D409/06C07D307/52C07D307/54C07D333/20C07D333/24Y02P20/55
    • A serine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, having an anti-PCP(phencyclidine) activity and being useful as a psychotropic, wherein X represents sulfur or oxygen; Y represents nitrogen or CH; R and R represent each independently hydrogen, lower alkyl or an amino-protecting group, or R and R may be combined together to form 4- to 9-membered nitrogenous cycloalkyl; R represents hydrogen, carboxy, protected carboxy, aralkyl, or lower alkyl which may be hydroxylated; R represents hydrogen or hydroxy; R represents hydrogen or lower alkyl; A represents lower alkylene; B represents (1) an (un)saturated 4- to 10-membered nitrogenous cycloalkyl group which may be substituted by lower alkyl or aralkyl, or (2) a bicyclic nitrogenous hydrocarbon ring group comprising a 4- to 8-membered nitrogenous cycloalkyl group and a benzene ring fused together; and . &cir& _. &cir& _. &cir& _ represents a single or a double bond.
    • 由通式(I)表示的丝氨酸衍生物或其药学上可接受的盐,具有抗PCP(苯环利定)活性,可用作精神药物,其中X表示硫或氧; Y表示氮或CH; R 1和R 2各自独立地表示氢,低级烷基或氨基保护基,或者R 1和R 2可以组合在一起形成4-至9-元含氮环烷基; R 3表示氢,羧基,保护的羧基,芳烷基或可被羟基化的低级烷基; R 4表示氢或羟基; R 5表示氢或低级烷基; A表示低级亚烷基; B表示(1)可被低级烷基或芳烷基取代的(未)饱和的4-至10-元含氮环烷基,或(2)包含4-至8-元含氮环烷基的双环含氮环烃基 和苯环稠合在一起; 和。 &cir&_。 &cir&_。 &cir&_代表单一或双重债券。