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    • 52. 发明申请
    • PYRIDO[2, 3-D] PYRIMIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS THEREOF
    • 吡咯并[2,3-D]吡啶衍生物及其药物组合物
    • WO1997019078A1
    • 1997-05-29
    • PCT/JP1996003389
    • 1996-11-20
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.TAKAYAMA, KazuhisaHISAMICHI, HiroyukiIWATA, MasahiroKUBOTA, HidekiAOKI, Motonori
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D471/04
    • C07D471/04
    • Compounds represented by general formula (I) or pharmaceutically acceptable salts thereof which have the effect of inhibiting the activity of type IV phosphodiesterases and are usable as drugs, in particular, type IV phosphodiesterase inhibitors or preventives and remedies for diseases in association with the sthenic type IV phosphodiesterase activity, in particular, respiratory diseases such as bronchial asthma. In said formula (I), X represents oxygen or sulfur; R represents lower alkyl, cycloalkyl(lower alkyl) or cycloalkyl; R represents hydrogen, halogeno, lower alkyl, halo(lower alkyl), hydroxy(lower alkyl), mercapto(lower alkyl), (lower alkoxy)(lower alkyl), (lower alkylthio)(lower alkyl), (lower alkanoyloxy)(lower alkyl), (lower alkanoylthio)(lower alkyl), (lower alkanoyl)(lower alkyl), hydroxyimino(lower alkyl), (lower alkoxyimino)(lower alkyl), cycloalkyl, aryl or lower alkanoyl; R represents hydrogen, halogeno or lower alkyl; R represents hydrogen, or lower alkyl; R represents cycloalkyl optionally substituted by the same group as R ; naphthyl optionally substituted by the same group as R ; a 5- or 6-membered monocyclic heterocycle optionally substituted by the same group as R , optionally fused with a benzene ring and having one to four heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur atoms; or a group of formula (a); and R represents halogeno, lower alkyl, halo(lower alkyl), hydroxy, lower alkoxy, cyano or nitro.
    • 具有抑制IV型磷酸二酯酶活性的通式(I)表示的化合物或其药学上可接受的盐,可用作药物,特别是IV型磷酸二酯酶抑制剂或预防药物以及与该类型相关的疾病的治疗方法 IV磷酸二酯酶活性,特别是呼吸道疾病如支气管哮喘。 在所述式(I)中,X表示氧或硫; R 1表示低级烷基,环烷基(低级烷基)或环烷基; R 2表示氢,卤代低级烷基,卤代(低级烷基),羟基(低级烷基),巯基(低级烷基),(低级烷氧基)(低级烷基),(低级烷硫基) (低级烷基),(低级烷酰基)(低级烷基),(低级烷酰基)(低级烷基),羟基亚氨基(低级烷基),(低级烷氧基亚氨基)(低级烷基),环烷基,芳基或低级烷酰基。 R 3表示氢,卤代或低级烷基; R 4表示氢或低级烷基; R 5表示任选被与R 6相同的基团取代的环烷基; 任选被与R 6相同基团取代的萘基; 任选地被与R 6相同的基团取代的5-或6-元单环杂环,任选地与苯环稠合并具有一至四个选自氮,氧和硫原子的杂原子; 或一组式(a); 和R 6表示卤代,低级烷基,卤代(低级烷基),羟基,低级烷氧基,氰基或硝基。
    • 58. 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。
    • 59. 发明申请
    • 5-HT3 RECEPTOR AGONIST, NOVEL THIAZOLE DERIVATIVE, AND INTERMEDIATE THEREFOR
    • 5-HT3受体激动剂,新型噻唑衍生物及其中间体
    • WO1995024399A1
    • 1995-09-14
    • PCT/JP1995000385
    • 1995-03-09
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.IWAOKA, KiyoshiANAN, HidekiIMANISHI, NaokiKAZUTA, KenichiKOSHIO, HiroyukiSUZUKI, TakeshiITAHANA, HirotsuneITO, HiroyukiMIYATA, KeijiOHTA, Mitsuaki
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D277/28
    • C07D277/60C07D417/04C07D417/06C07D417/14C07D471/04C07D471/08C07D487/04C07D487/08C07D513/04Y02P20/55
    • A 5-HT3 receptor agonist containing a thiazole derivative represented by general formula (I) as the active ingredient, a specified compound useful as a 5-HT3 receptor agonist, and a specified thioamide derivative useful as an intermediate therefor, wherein ring A represents one of the following rings which may be substituted by at least one substituent selected from the group consisting of halogen, lower alkyl and lower alkoxy: (1) a benzene ring, and (2) a 5- or 6-membered unsaturated heterocycle having one or two heteroatoms selected from among nitrogen, oxygen and sulfur; one of L and L represents a single bond, and the other of them is absent, or represents C1-C4 alkylene or C2-C5 alkenylene; R represents a group represented by any of general formulae: (1), (2), (3) and (4); L represents lower alkylene; L represents a single bond or lower alkylene; R and R represent each independently hydrogen, lower alkyl or an amino-protecting group; R represents hydrogen, lower alkyl, oxo or optionally protected amino; R is absent, or represents hydrogen, lower alkyl, aralkyl or an amino-protecting group; ring B represents one of the following rings which are either monocyclic or bicyclic and may bear an oxygen atom(s): (1) a nitrogenous saturated heterocycle bearing four to sixteen ring atoms, and (2) a nitrogenous heterocycle having a double bond and bearing four to sixteen ring atoms: and ring D represents a saturated carbocycle bearing four to eight ring atoms; provided the nitrogen atom of R may form an unsubstituted quaternary ammonium salt.
    • 含有由通式(I)表示的噻唑衍生物作为活性成分的5-HT 3受体激动剂,可用作5-HT 3受体激动剂的特定化合物和用作其中间体的特定硫代酰胺衍生物,其中环A表示1 可以被选自卤素,低级烷基和低级烷氧基的至少一个取代基取代的以下环:(1)苯环,和(2)具有一个或多个的一个或多个的5-或6-元不饱和杂环, 选自氮,氧和硫的两个杂原子; L 1和L 2之一表示单键,另一个不存在,或表示C1-C4亚烷基或C2-C5亚烯基; R表示由通式(1),(2),(3)和(4)中的任一个表示的基团。 L 3表示低级亚烷基; L 4代表单键或低级亚烷基; R 1和R 2各自独立地表示氢,低级烷基或氨基保护基; R 3表示氢,低级烷基,氧代或任选保护的氨基; R 4不存在,或表示氢,低级烷基,芳烷基或氨基保护基; 环B表示单环或双环的以下环之一,并且可以带有氧原子:(1)具有4至16个环原子的含氮饱和杂环,和(2)具有双键的含氮杂环和 具有四至十六个环原子:环D表示带有四至八个环原子的饱和碳环; 条件是R的氮原子可以形成未取代的季铵盐。