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    • 7. 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。
    • 10. 发明授权
    • Carbacyclin analogs
    • Carbacyclin类似物
    • US4680307A
    • 1987-07-14
    • US574125
    • 1984-01-26
    • Masami MuraokaToshio NakamuraAkihiko SugieKeiichi OnoMichihiro Yamamoto
    • Masami MuraokaToshio NakamuraAkihiko SugieKeiichi OnoMichihiro Yamamoto
    • C07C69/708A61K31/16A61K31/19A61K31/215A61K31/557A61P43/00C07C33/14C07C51/00C07C59/125C07C59/46C07C59/62C07C59/72C07C67/00C07C69/73C07C231/00C07C231/02C07C231/12C07C235/06C07C235/16C07C405/00C07D307/20C07D309/12A61K31/185A61K31/235A61K31/35C07C69/734C07C69/78C07D315/00
    • C07C405/0083C07C309/00C07C33/14Y10S514/925
    • A compound of the formula: ##STR1## wherein X.sup.1 is a free or an esterified carboxyl group, or a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7 membered saturated heterocyclic group, Y.sup.1 is a group of the formula: ##STR3## (R.sup.6 is a hydrogen atom or C.sub.1 -C.sub.4 alkyl group), ##STR4## (R.sup.6 is as defined above), ##STR5## R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sup.1 and R.sup.2, when taken together, mean a shingle linkage to from a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sup.5 is a hydrogen atom, a C.sub.1 -C.sub.12 alkyl group, a C.sub.2 -C.sub.12 alkenyl group, a C.sub.2 -C.sub.12 alkynyl group, a C.sub.3 -C.sub.10 cycloalkyl group, a C.sub.4 -C.sub.10 cycloalkenyl group, a hydroxy C.sub.1 -C.sub.12 alkyl group, a C.sub.3 -C.sub.10 heterocyclic group, a phenyl group optionally substituted with a halogen atom; a hydroxyl group, a C.sub.1 -C.sub.4 alkyl group, a trifluoromethyl group, or a C.sub.1 -C.sub.4 alkyl group or a formula: A-B (A is a C.sub.1 -C.sub.7 alkylene chain and B is a C.sub.3 -C.sub.10 cycloalkyl group, a C.sub.4 -C.sub.10 cycloalkenyl group, a C.sub.1 -C.sub.12 alkoxy group, a C.sub.3 -C.sub.10 cycloalkoxy group, a C.sub.4 -C.sub.10 cycloalkenyloxy group, a C.sub.3 -C.sub.10 heterocyclic group, or a phenyl or phenoxy group optionally substituted with a halogen atom, a hydroxy group, a C.sub.1 -C.sub.4 alkyl group, a trifluoromethyl group or a C.sub.1 -C.sub.4 alkoxy group); or a non-toxic pharmaceutically acceptable salt thereof. Said compound have strong anti-ulcerous action or antithrombotic action, and are useful in treatment of ulcer or thrombosis.
    • 下式的化合物,其中X 1是游离的或酯化的羧基,或下式的基团:(R a和R b各自独立地是氢原子,C 1 -C 4烷基,C 3 -C 7环烷基,苄基,苯基,被卤素原子或C1-C4烷基取代的苯基,或者当与它们所连接的相邻氮原子一起时,它们表示5〜 7元饱和杂环基,Y 1是下式的基团:R 6是氢原子或C 1 -C 4烷基,R 6如上所定义,R 1是氢原子 ,羟基或被保护的羟基,R2是氢原子或R1和R2,当它们一起表示与它们所连接的碳原子之间的双键的键合键,R3是羟基或被保护的 羟基,R4是氢原子或C1-C4烷基,R5是氢原子,C1-C12烷基,C2-C12烯基,C2-C12烷基 辛基,C3-C10环烷基,C4-C10环烯基,羟基C1-C12烷基,C3-C10杂环基,任选被卤素原子取代的苯基; 羟基,C1-C4烷基,三氟甲基或C1-C4烷基或式:AB(A是C1-C7亚烷基链,B是C3-C10环烷基,C4-C10 环烯基,C1-C12烷氧基,C3-C10环烷氧基,C4-C10环烯基氧基,C3-C10杂环基或任选被卤素原子取代的苯基或苯氧基,羟基,C1 -C4烷基,三氟甲基或C1-C4烷氧基); 或其无毒的药学上可接受的盐。 所述化合物具有强的抗溃疡作用或抗血栓形成作用,可用于治疗溃疡或血栓形成。