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    • 64. 发明授权
    • Imidazo- and pyrimido[2,1-b]quinazolines and preparation thereof
    • 咪唑并嘧啶并[2,3-b]喹唑啉及其制备方法
    • US4179560A
    • 1979-12-18
    • US553676
    • 1975-02-27
    • Michihiro YamamotoShigeaki MorookaMasao KoshibaShigeho InabaHisao Yamamoto
    • Michihiro YamamotoShigeaki MorookaMasao KoshibaShigeho InabaHisao Yamamoto
    • A61K31/505A61P7/10A61P9/12A61P25/24A61P25/26C07D487/04C07D491/147A61K31/395
    • C07D487/04
    • Imidazo- and pyrimido[2,1-b]quinazolines of the formula, ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, trifluoromethyl, nitro, C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or R.sub.1 and R.sub.2 may together represent methylenedioxy; R.sub.3 is hydrogen, C.sub.1-4 alkyl, phenyl or substituted phenyl of the formula, ##STR2## (wherein R is halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy); R.sub.4 is hydrogen, C.sub.1-4 alkyl or aralkyl; and A is C.sub.2-3 alkylene wich may be optionally substituted by one or two C.sub.1-2 alkyl radicals, and pharmaceutically acceptable acid addition salts thereof, are prepared by reacting a compound of the formula, ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined above; and X is oxygen or sulfur, with a halogenating agent at a temperature of about 30.degree. C. to about 180.degree. C. In the above imidaxo- and pyrimido[2,1-b]quinazolines, those having C.sub.1-4 alkyl, or ##STR4## as R.sub.3 are novel compounds and show antidepressant and/or antihypertensive activities.
    • 其中R 1和R 2独立地为氢,卤素,三氟甲基,硝基,C 1-4烷基或C 1-4烷氧基,或者R 1和R 2可以一起代表下式的咪唑并 - 嘧啶并[2,3-b]喹唑啉, 亚甲二氧基; R 3是氢,C 1-4烷基,苯基或下式的取代的苯基,其中R是卤素,C 1-4烷基或C 1-4烷氧基; R4是氢,C1-4烷基或芳烷基; 并且A是可以任选被一个或两个C 1-2烷基取代的C 2-3亚烷基及其药学上可接受的酸加成盐,其通过使下式化合物,其中R1,R2,R3, R4和A如上所定义; 在上述酰胺基 - 和嘧啶并[2,1-b]喹唑啉中,具有C 1-4烷基的那些,或其中X是氧或硫,与卤化剂在约30℃至约180℃的温度下反应。 作为R3是新化合物并显示抗抑郁药和/或抗高血压活性的图像。
    • 65. 发明授权
    • .gamma.-Piperidinobutyrophenones
    • {65-哌啶基丁酰苯
    • US4148796A
    • 1979-04-10
    • US388561
    • 1973-08-15
    • Hisao YamamotoMasaru NakaoKikuo SasajimaIsamu MaruyamaShigenari Katayama
    • Hisao YamamotoMasaru NakaoKikuo SasajimaIsamu MaruyamaShigenari Katayama
    • C07D211/48C07D401/06C07D401/04C07D211/50
    • C07D401/06C07D211/48
    • Novel .gamma.-piperidinobutyrophenone derivatives of the formula, ##STR1## wherein R.sup.1 is halogen, amino, alkanoylamino, alkylamino or N-(alkanoyl)alkylamino;R.sup.2 is hydrogen or halogen, provided that when R.sup.1 is halogen, R.sup.2 must be halogen; andZ is a piperidino group having the formula (A), ##STR2## (wherein each of R.sub.a and R.sub.b is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; R.sup.3 is hydrogen or hydroxyl; and n is 1 or 2), or a piperidino group having the formula (B), ##STR3## (wherein R.sub.c is hydrogen or lower alkyl; and each of R.sub.d and R.sub.e is hydrogen, halogen, lower alkyl or lower alkoxy), provided that when R.sup.1 is amino and R.sup.2 is hydrogen, Z cannot be represented by the formula (A), and their pharmaceutically acceptable acid addition salts, which are useful as psychotropic, neuroleptic or analgesic agents.
    • 其中R1是卤素,氨基,烷酰基氨基,烷基氨基或N-(烷酰基)烷基氨基的新颖的γ-哌啶基丁酰苯衍生物, R2是氢或卤素,条件是当R1是卤素时,R2必须是卤素; Z为具有式(A),(A)的哌啶子基,其中R a和R b各自为氢,卤素,低级烷基,低级烷氧基或三氟甲基; R 3为氢或羟基; n为1或 2)或具有式(B)的哌啶子基,其中R c是氢或低级烷基;并且R d和R e各自是氢,卤素,低级烷基或低级烷氧基),条件是当 R1是氨基,R2是氢,Z不能由式(A)表示,它们的药学上可接受的酸加成盐可用作精神药物,精神抑制剂或止痛剂。
    • 69. 发明授权
    • Analgetic composition
    • 笔画组成
    • US4083981A
    • 1978-04-11
    • US773936
    • 1977-03-03
    • Hisao YamamotoToshiya InukaiYoshihiko Koga
    • Hisao YamamotoToshiya InukaiYoshihiko Koga
    • C07D209/28A61K31/40A61K31/403A61K31/404A61K31/405A61K31/435A61K31/445A61K31/485A61P25/04C07D211/64C07D221/28
    • A61K31/485A61K31/435A61K31/445
    • An analgetic composition which comprises, as an active ingredient, a therapeutically effective amount of a synergistic mixture of an indole-3-acetic acid derivative of the formula, ##STR1## wherein R is a halobenzoyl, piperonylcyl or cinnamoyl group and R.sub.1 is a 5-methoxy or 5,6-methylenedioxy group; and a narcotic or anti-narcotic analgesic selected from the group consisting of a compound of the formula, ##STR2## wherein R.sub.2 and R.sub.3 are each a C.sub.1 - C.sub.3 alkyl group and R.sub.4 is a 4-(4-fluorophenyl)-4-oxobutyl, cyclopropylmethyl or 3-methyl-2-butenyl group; a compound of the formula, ##STR3## wherein R.sub.5 is a hydrogen atom or a C.sub.1 - C.sub.3 alkyl group; a compound of the formula, ##STR4## and a compound of the formula, ##STR5## wherein R.sub.6 is a C.sub.1 - C.sub.3 alkyl group; and a pharmaceutically acceptable carrier or diluent and its preparation and a method of obtaining analgesia which comprises administering the same to a patient.
    • 一种止痛组合物,其包含作为活性成分的治疗有效量的下式的吲哚-3-乙酸衍生物,其中R是卤代苯甲酰基,胡烷基或肉桂酰基的吲哚-3-乙酸衍生物,R 1为5 - 甲氧基或5,6-亚甲二氧基; 以及选自由下式化合物组成的组的麻醉或抗麻醉止痛剂,其中R2和R3各自为C1-C3烷基,R4为4-(4-氟苯基)-4-氧代丁基 ,环丙基甲基或3-甲基-2-丁烯基; 下式的化合物,其中R 5是氢原子或C 1 -C 3烷基; 下式的化合物和下式的化合物,其中R 6是C 1 -C 3烷基; 和药学上可接受的载体或稀释剂及其制备方法和获得镇痛的方法,其包括将其施用于患者。