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    • 2. 发明申请
    • N-(3-PYRROLIDINYL)BENZAMIDE DERIVATIVE
    • N-(3-吡咯烷基)苯甲酰胺衍生物
    • WO1995029891A1
    • 1995-11-09
    • PCT/JP1995000818
    • 1995-04-26
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.OHMORI, JunyaMAENO, KyoichiHIDAKA, KazuyukiNAKATO, KazuhiroSAKAMOTO, ShuichiTSUKAMOTO, Shin-ichi
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D207/14
    • C07D207/14
    • An N-(3-pyrrolidinyl)benzamide derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof and a medicine containing the same, having a potent and selective antagonism against dopamine D3 and/or D4 receptors and useful as a psychotropic agent, schizophrenia remedy, and so forth. In said formula, R represents hydrogen, lower alkyl, aralkyl, or three- to eight-membered cycloalkyl or cycloalkyl-lower alkyl; R represents four- to sixteen-membered bi- or tricyclic bridged hydrocarbon group; R represents lower alkoxy, amino, or mono- or di(lower alkyl)amino; R represents hydrogen, halogen, optionally hydroxylated lower alkyl, lower alkoxy, cyano, nitro, amino, mono- or di(lower alkyl)amino, acyl or -S(O)m-R ; R represents lower alkyl, amino or mono- or di(lower alkyl)amino; m represents 0, 1 or 2; X represents a bond, -O-, -S(O)n-, -NH- or -CONH-; and n represents 0, 1 or 2; provided when R represents cycloalkyl, the case where X represents -CONH-, R represents lower alkoxy and R represents halogen is excepted.
    • 由通式(I)表示的N-(3-吡咯烷基)苯甲酰胺衍生物或其药学上可接受的盐和含有它们的药物,具有对多巴胺D3和/或D4受体的有效和选择性拮抗作用并用作精神药物 ,精神分裂症补救等等。 在所述式中,R 1表示氢,低级烷基,芳烷基或三至八元环烷基或环烷基 - 低级烷基; R 2表示四至十六元的二环或三环桥连烃基; R 3表示低级烷氧基,氨基或单或二(低级烷基)氨基; R 4表示氢,卤素,任选羟基化的低级烷基,低级烷氧基,氰基,硝基,氨基,单或二(低级烷基)氨基,酰基或-S(O)m -R 5。 R 5表示低级烷基,氨基或一或二(低级烷基)氨基; m表示0,1或2; X表示键,-O - , - S(O)n - , - NH-或-CONH-; n表示0,1或2; 当R 1表示环烷基时,其中X表示-CONH-,R 3表示低级烷氧基,R 4表示卤素的情况除外。
    • 5. 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。
    • 8. 发明申请
    • 1,2,3,4-TETRAHYDROQUINOXALINDIONE DERIVATIVE
    • 1,2,3,4-四氢喹啉酮衍生物
    • WO1996010023A1
    • 1996-04-04
    • PCT/JP1995001922
    • 1995-09-25
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.SHISHIKURA, Jun-ichiINAMI, HiroshiSAKAMOTO, ShuichiTSUKAMOTO, Shin-ichiSASAMATA, MasaoOKADA, MasamichiFUJII, Mitsuo
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D403/04
    • C07D231/12C07D233/56C07D241/44C07D249/08
    • A 1,2,3,4-tetrahydroquinoxalindione derivative represented by general formula (I) or a salt thereof, an NMDA-glycine receptor and/or AMPA receptor antagonist and a kainate neurocytotoxicity inhibitor each containing the same, and a medicinal composition comprising the above-mentioned compound and pharmaceutically acceptable carriers: wherein X represents N or CH; R represents imidazolyl or di(lower alkyl)amino; R represents (1) halogeno, nitro, cyano, carboxy, amino, mono- or di(lower alkyl)amino, lower alkanoyl, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, or carbamoyl, (2) lower alkyl or lower alkoxy which may be substituted by halogeno, carboxy or aryl, or (3) phenyloxy which may be substituted by lower alkoxycarbonyl or carboxy; R represents hydroxy, lower alkoxy, amino, or mono- or di(lower alkyl)amino; and A represents optionally substituted alkylene or -O-B- (B being lower alkylene); provided the case wherein R represents imidazolyl, R represents cyano, A represents ethylene and R represents hydroxy is excepted.
    • 由通式(I)表示的1,2,3,4-四氢喹喔啉二酮衍生物或其盐,NMDA-甘氨酸受体和/或AMPA受体拮抗剂和各自含有它们的红藻氨酸神经细胞毒素抑制剂,以及药物组合物, 上述化合物和药学上可接受的载体:其中X表示N或CH; R代表咪唑基或二(低级烷基)氨基; R 1表示(1)卤代,硝基,氰基,羧基,氨基,单或二(低级烷基)氨基,低级烷酰基,低级烷硫基,低级烷基亚磺酰基,低级烷基磺酰基或氨基甲酰基,(2)低级烷基或低级 可被卤素,羧基或芳基取代的烷氧基,或(3)可被低级烷氧基羰基或羧基取代的苯氧基; R 2表示羟基,低级烷氧基,氨基或单或二(低级烷基)氨基; 和A表示任选取代的亚烷基或-O-B-(B是低级亚烷基); 条件是其中R表示咪唑基,R 1表示氰基,A表示亚乙基,R 2表示羟基。