Thiadiazinone derivatives
    1.
    发明授权
    Thiadiazinone derivatives 失效
    噻二嗪酮衍生物

    公开(公告)号:US5567699A

    公开(公告)日:1996-10-22

    申请号:US422916

    申请日:1995-04-17

    CPC分类号: C07D417/12

    摘要: This invention provides thiadiazinone derivatives represented by the following formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or C.sub.1 -C.sub.5 alkyl, R.sup.2 represents a 5- or 6-membered heterocyclic ring having (a) 1-3 nitrogen atoms, (b) a oxygen atom, (c) one sulfur atom, (d) 1-3 nitrogen atoms and one oxygen atom, or (e) 1-3 nitrogen atoms and one sulfur atom each of which rings may optionally be substituted by at least one substituent selected from the group consisting of C.sub.1 -C.sub.5 alkyl, cyano, hydroxy, C.sub.1 -C.sub.5 alkoxy, amino, C.sub.1 -C.sub.5 alkylamino, C.sub.2 -C.sub.6 dialkylamino, C.sub.2 -C.sub.5 acylamino, carboxyl, C.sub.2 -C.sub.5 alkoxycarbonyl and carbamoyl; or a pharmaceutically acceptable salt thereof. The compounds according to the present invention have an excellent cardiotonic activity, and are useful as active ingredients of a cardiotonic drug.

    摘要翻译: 本发明提供由下式(I)表示的噻二嗪酮衍生物其中R 1表示氢原子或C 1 -C 5烷基,R 2表示具有(a)1-3氮原子的5-或6-元杂环 原子,(b)氧原子,(c)一个硫原子,(d)1-3个氮原子和一个氧原子,或(e)1-3个氮原子和一个硫原子,其中每个环可以任选地被取代 通过至少一个选自C 1 -C 5烷基,氰基,羟基,C 1 -C 5烷氧基,氨基,C 1 -C 5烷基氨基,C 2 -C 6二烷基氨基,C 2 -C 5酰基氨基,羧基,C 2 -C 5烷氧基羰基和氨基甲酰基 ; 或其药学上可接受的盐。 根据本发明的化合物具有优异的强心活性,可用作强心药物的活性成分。

    Process for preparing steroid-carboxylates
    2.
    发明授权
    Process for preparing steroid-carboxylates 失效
    类固醇羧酸盐的制备方法

    公开(公告)号:US4265816A

    公开(公告)日:1981-05-05

    申请号:US145693

    申请日:1980-05-01

    CPC分类号: C07J21/003 C07J51/00

    摘要: An alkali metal salt of a 3-(17.beta.-hydroxyandrosten-3-one 3-acetal-17.alpha.-yl)propiolic acid which is useful as an intermediate in the preparation of 3-(3-oxo-7.alpha.-acetylthio-17.beta.-hydroxyandrost-4-en-17.alpha.-yl)-propiolactone (spironolactone) as antialdosteronic diuretics and hypotensive agents is prepared by reacting a 17.beta.-hydroxypregnen-20-yn-3-one 3-acetal (I) with an alkali metal dimsyl (II) to give an alkali metal salt of the 17.beta.-hydroxypregnen-20-yn-3-one 3-acetal (III), and reacting the compound (III) with carbon dioxide followed by hydrolysis.

    摘要翻译: 3-(3-氧代-7α-乙酰基硫基)丙酸的3-(17β-羟基和3-酮-3-缩醛-17α-基)丙炔酸的碱金属盐,可用作中间体, 17β-羟基雄甾-4-烯-17α-基) - 丙内酯(螺内酯)作为抗增殖利尿剂和降血糖药是通过使17β-羟基孕烯-20-炔-3-酮3-缩醛(I)与 碱金属二甲基(II),得到17β-羟基孕烯-20-炔-3-酮3-缩醛(III)的碱金属盐,并使化合物(III)与二氧化碳反应,然后水解。

    1-phenylalkyl-3-phenylurea derivatives
    8.
    发明授权
    1-phenylalkyl-3-phenylurea derivatives 失效
    1-苯甲基-3-苯基衍生物

    公开(公告)号:US5126483A

    公开(公告)日:1992-06-30

    申请号:US562337

    申请日:1990-08-03

    CPC分类号: C07C275/28 C07C273/1827

    摘要: Novel 1-phenylakyl-3-phenylurea derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 is an alkyl group of 1 to 8 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, R.sup.2 is an alkyl group of 1 to 15 carbon atoms, each of R.sup.3 and R.sup.4 is independently an alkyl group of 1 to 5 carbon atoms, m is an integer of 1 to 3, and n is 0 or 1, are provided.The compounds are potent in reducing the cholesterol level in serum, and useful for treating hyperlipemia and atherosclerosis.

    摘要翻译: 由下式(I)表示的新型1-苯基烷基-3-苯基脲衍生物:其中R 1为1〜8个碳原子的烷基,1〜5个碳原子的烷氧基或卤素原子 R 2为1〜15个碳原子的烷基,R 3和R 4各自独立地为1〜5个碳原子的烷基,m为1〜3的整数,n为1〜 是0或1。 该化合物有效降低血清中的胆固醇水平,可用于治疗高脂血症和动脉粥样硬化。

    Aminobenzenesulfonic acid derivatives
    10.
    发明授权
    Aminobenzenesulfonic acid derivatives 失效
    氨基苯磺酸衍生物

    公开(公告)号:US5053409A

    公开(公告)日:1991-10-01

    申请号:US497184

    申请日:1990-03-22

    IPC分类号: C07D295/096

    CPC分类号: C07D295/096

    摘要: There is disclosed an aminobenzenesulfonic acid derivative of the formula: ##STR1## wherein R.sub.1 represents hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a C.sub.1 -C.sub.4 halogenated alkyl group, a halogen atom or a C.sub.6 -C.sub.12 aryl group, R.sub.2 represents hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.7 -C.sub.12 aralkyl group which may have at least one substituent selected from cyano group, nitro group, C.sub.1 -C.sub.6 alkoxy groups, halogen atoms, C.sub.1 -C.sub.6 alkyl groups and amino groups, and n represents an integer of 1 to 4, of a pharmaceutically acceptable salt thereof.

    摘要翻译: 公开了下式的氨基苯磺酸衍生物:其中R 1表示氢原子,C 1 -C 6烷基,C 3 -C 7环烷基,C 1 -C 4卤代烷基,卤素原子或 C 6 -C 12芳基,R 2表示氢原子,可以具有至少一个选自氰基,硝基,C 1 -C 6烷氧基,卤素原子,C 1 -C 6烷氧基, C6烷基和氨基,n表示1至4的整数,其药学上可接受的盐。