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    • 21. 发明授权
    • Benzotriazolyl-4,5-dihydro-3(2H)-pyridazinones
    • 苯并三唑基-4,5-二氢-3(2H) - 哒嗪酮
    • US4616018A
    • 1986-10-07
    • US749580
    • 1985-06-27
    • Norbert HauelVolkhard AustelJoachim HeiderManfred ReiffenWilli DiederenWalter Haarman
    • Norbert HauelVolkhard AustelJoachim HeiderManfred ReiffenWilli DiederenWalter Haarman
    • A61K31/50A61K31/501A61P7/02A61P9/12C07D237/04C07D249/18C07D401/14C07D403/04C07D403/02
    • C07D401/14C07D237/04C07D249/18C07D403/04Y10S514/822
    • Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; alkyl of 1 to 7 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; monosubstituted alkyl of 1 to 3 carbon atoms, where the substituent is pyridyl, methylpyridyl, phenyl, mono-, di- or trisubstituted phenyl, where the substituents on the phenyl ring, which may be identical to or different from each other, are selected from the group consisting of one amino, one dimethylamino, one to two hydroxyls, one to three methoxys and one to three halogens; .omega.-monosubstituted alkyl of 2 to 4 carbon atoms, where the substituent is hydroxyl or di(alkyl of 1 to 3 carbon atoms)amino; phenyl; monohalo-phenyl; unsubstituted or monosubstituted straight or branched alkanoyl of 1 to 6 carbon atoms, where the substituent is phenyl, methoxyphenyl or cycloalkyl of 3 to 7 carbon atoms; or unsubstituted or monosubstituted phenylsulfonyl, where the substituent is methyl or methoxy; and,R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics, hypotensives and antithrombotics.
    • 其中R 1是氢的式IMAMA的化合物; 1至7个碳原子的烷基; 3至7个碳原子的环烷基; 其中取代基是吡啶基,甲基吡啶基,苯基,单 - ,二 - 或三取代的苯基,其中可以相同或不同的苯环上的取代基选自 由一个氨基,一个二甲基氨基,一至两个羟基,一至三个甲氧基和一至三个卤素组成的组; 2至4个碳原子的ω-单取代的烷基,其中取代基是羟基或二(1至3个碳原子的烷基)氨基; 苯基; 单卤代苯基; 未取代的或单取代的1至6个碳原子的直链或支链烷酰基,其中取代基是苯基,甲氧基苯基或3-7个碳原子的环烷基; 或未取代或单取代的苯基磺酰基,其中取代基是甲基或甲氧基; R2为氢或1〜3个碳原子的烷基; 和无毒的,药学上可接受的酸加成盐。 化合物及其盐可用作强心剂,低血糖剂和抗血栓药物。
    • 22. 发明授权
    • 2-Phenyl-pyrimidones
    • 2-苯基 - 嘧啶酮
    • US4379788A
    • 1983-04-12
    • US327348
    • 1981-12-04
    • Joachim HeiderVolkhard AustelWolfgang EberleinRudolf KadatzChristian Lillie
    • Joachim HeiderVolkhard AustelWolfgang EberleinRudolf KadatzChristian Lillie
    • C07D239/88A61K31/513A61P9/00C07D213/82C07D239/91C07D265/22C07D471/04C07D498/04A61K31/505
    • C07D213/82C07D239/91C07D265/22C07D471/04
    • Compounds of the formula ##STR1## wherein A and B, together with each other and the respective carbon atoms to which they are attached, form a phenyl or pyridine ring;R.sub.1 is hydrogen, halogen, amino, nitro, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;R.sub.2 is hydrogen or alkoxy of 1 to 3 carbon atoms;D is alkylene of 3 to 4 carbon atoms or hydroxy(alkylene of 3 to 4 carbon atoms);R.sub.3 and R.sub.5, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.4 is hydrogen or alkoxy of 1 to 3 carbon atoms; andR.sub.6 is straight or branched alkyl of 1 to 6 carbon atoms or --E--R.sub.7 ;where E is straight alkylene of 2 to 4 carbon atoms or hydroxy-substituted straight alkylene of 2 to 4 carbon atoms, andR.sub.7 is ##STR2## where R.sub.8 and R.sub.9 are each hydrogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof formed with inorganic or organic acids; the compounds as well as their salts are useful as hypotensives, antiarrhythmics and .beta.-receptor-blockers.
    • 其中A和B与它们相连的相互连接的碳原子一起形成苯基或吡啶环; R 1是氢,卤素,氨基,硝基,1至3个碳原子的烷基或1至3个碳原子的烷氧基; R2是氢或1〜3个碳原子的烷氧基; D是3至4个碳原子的亚烷基或羟基(3至4个碳原子的亚烷基); R 3和R 5可以相同或不同,分别为氢或1-3个碳原子的烷基; R4是氢或1〜3个碳原子的烷氧基; R6是1-6个碳原子的直链或支链烷基或-E-R7; 其中E是2至4个碳原子的直链亚烷基或2至4个碳原子的羟基取代的直链亚烷基,并且R 7是R 8和R 9各自为氢,1至3个碳原子的烷基或1至 3个碳原子; 和与无机或有机酸形成的无毒的,药学上可接受的酸加成盐; 化合物及其盐可用作低血糖,抗心律失常药和β-受体阻滞剂。
    • 23. 发明授权
    • Pyridazinone-substituted benzimidazoles and salts
    • 哒嗪酮取代的苯并咪唑和盐
    • US4361563A
    • 1982-11-30
    • US259537
    • 1981-05-01
    • Volkhard AustelJoachim HeiderWolfgang EberleinWilli DiederenWalter Haarmann
    • Volkhard AustelJoachim HeiderWolfgang EberleinWilli DiederenWalter Haarmann
    • A61K31/50C07D235/18C07D237/04C07D403/04
    • C07D237/04A61K31/50C07D235/18Y10S514/822
    • Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; trifluoromethyl; alkyl of 1 to 11 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; hydroxyl; alkoxy of 1 to 6 carbon atoms; mercapto; (alkyl of 1 to 6 carbon atoms)-mercapto; phenyl-(alkyl of 1 to 3 carbon atoms); phenyl; or mono-, di- or tri-substituted phenyl, where the substituents, which may be identical to or different from each other, are each halogen, alkyl of 1 to 4 carbon atoms, (alkyl of 1 to 6 carbon atoms)-sulfinyl, hydroxyl, alkoxy of 1 to 6 carbon atoms, mercapto or (alkyl of 1 to 6 carbon atoms)-mercapto;R.sub.2 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms or phenyl-(alkyl of 1 to 3 carbon atoms); andR.sub.3 is alkyl of 1 to 6 carbon atoms; optically active antipodes thereof; and non-toxic, pharmaceutically acceptable acid addition salts of said compounds or of said optically active antiposed. The compounds are useful as cardiotonics and antithrombotics.
    • 其中R 1是氢的式IMAMA的化合物; 三氟甲基 1至11个碳原子的烷基; 3至7个碳原子的环烷基; 羟; 1至6个碳原子的烷氧基; 巯基 (1-6个碳原子的烷基) - 巯基; 苯基 - (1至3个碳原子的烷基); 苯基; 或单取代,二取代或三取代的苯基,其中可以相同或不同的取代基各自为卤素,具有1至4个碳原子的烷基,(1至6个碳原子的烷基) - 亚磺酰基 ,羟基,1至6个碳原子的烷氧基,巯基或(1至6个碳原子的烷基) - 巯基; R2是氢,1至6个碳原子的烷基,3至6个碳原子的环烷基或苯基 - (1至3个碳原子的烷基); 且R 3为1至6个碳原子的烷基; 光学活性对映体; 和所述化合物或所述光学活性药物的无毒的药学上可接受的酸加成盐。 这些化合物可用作强心剂和抗血栓药物。