Pyrrolealdehydes, their preparation and their use
    7.
    发明授权
    Pyrrolealdehydes, their preparation and their use 失效
    吡咯醛,其制备及其用途

    公开(公告)号:US5043348A

    公开(公告)日:1991-08-27

    申请号:US485277

    申请日:1990-02-26

    CPC分类号: C07D207/333 C07D403/06

    摘要: Pyrrolealdehydes of the formula I ##STR1## wherein R and R.sup.1 independently of one another denote hydrogen or alkyl with 1 to 4 C atoms, R.sup.2 denotes alkyl, which is substituted by acylamino of the formula II ##STR2## wherein X stands for an oxygen or sulphur atom and R.sup.3 denotes hydrogen, optionally substituted alkyl or alkylamino, cycloalkyl with 5 to 7 C atoms, optionally substituted phenyl, an amino group or an optionally substituted phenylamio group, and pharmaceutically acceptable acid addition salts thereof, and wherein R.sup.3 cannot represent hydrogen if R and R.sup.1 denote hydrogen and the pyrrole ring is formylated in the 3-position, their preparation and their use.

    摘要翻译: 式I的吡咯醛其中R和R 1彼此独立地表示氢或具有1至4个C原子的烷基,R 2表示被式II的酰基氨基取代的烷基(II),其中 X代表氧或硫原子,R3表示氢,任选取代的烷基或烷基氨基,具有5至7个C原子的环烷基,任选取代的苯基,氨基或任选取代的苯基氨基,及其药学上可接受的酸加成盐,以及 如果R和R 1表示氢并且吡咯环在3-位甲酰化,其制备及其用途,则R3不能表示氢。

    Pyrrole derivatives, their preparation and their use as pharmaceutical
active compounds
    8.
    发明授权
    Pyrrole derivatives, their preparation and their use as pharmaceutical active compounds 失效
    吡咯衍生物,其制备及其作为药物活性化合物的用途

    公开(公告)号:US4966901A

    公开(公告)日:1990-10-30

    申请号:US355993

    申请日:1989-05-23

    摘要: Pyrrole derivatives of the general formula I ##STR1## wherein R denotes alkyl which is substituted by --NH.sub.2 or acylamino, R.sup.1 and R.sup.2 independently of one another denote hydrogen or alkyl having 1 to 4 carbon atoms, R.sup.3 denotes hydrogen, alkyl having 1 to 4 carbon atoms or a carboxylic acid grouping, R.sup.4 denotes a carboxylic acid grouping, nitro, alkylsulphinyl having 1 to 4 carbon atoms, optionally substituted phenylsulphinyl, alkylsulphonyl having 1 to 4 carbon atoms, optionally substituted phenylsulphonyl, alkylcarbonyl having 1 to 6 carbon atoms in the alkyl part, trifluoromethylcarbonyl, optionally substituted phenylcarbonyl, dicyanomethylene, formylvinyl, alkoxycarbonylvinyl having 1 to 6 carbon atoms in the alkoxy part or a carbonyl group, which is substituted by an optionally substituted aliphatic or aromatic 5- to 7-membered heterocyclic radical having 1 or 2 hetero atoms from the series comprising N, O and S, and pharmaceutically acceptable salts or acid addition salts thereof which are useful pharmacological active compounds. The invention also relates to methods for preparing the present compounds. The invention also includes formulations containing effective amounts of such compounds, and methods for administering same to patients for the treatment of diseases caused by restriction in cerebral function and/or for the treatment of cerebral aging processes.

    摘要翻译: 通式I的吡咯衍生物其中R表示被-NH 2或酰氨基取代的烷基,R 1和R 2彼此独立地表示氢或具有1至4个碳原子的烷基,R 3表示氢,烷基具有1至 4个碳原子或羧酸基团,R4表示羧酸基团,硝基,具有1至4个碳原子的烷基亚磺酰基,任选取代的苯基亚磺酰基,具有1至4个碳原子的烷基磺酰基,任选取代的苯基磺酰基,具有1至6个碳原子的烷基羰基 烷基部分,三氟甲基羰基,任选取代的苯基羰基,二氰基亚甲基,甲酰基乙烯基,烷氧基部分中具有1至6个碳原子的烷氧基羰基乙烯基或羰基,其被任选取代的脂族或芳族5至7元杂环基团取代, 或包含N,O和S的系列的2个杂原子及其药学上可接受的盐或其酸加成盐 是有用的药理活性化合物。 本发明还涉及制备本发明化合物的方法。 本发明还包括含有有效量的这种化合物的制剂,以及将其给予患者以治疗由脑功能限制引起的疾病和/或治疗脑衰老过程的方法。

    Thienylpiperazinones, their preparation and their use
    9.
    发明授权
    Thienylpiperazinones, their preparation and their use 失效
    噻吩基哌嗪酮,其制备及其用途

    公开(公告)号:US4898866A

    公开(公告)日:1990-02-06

    申请号:US349540

    申请日:1989-05-09

    CPC分类号: C07D409/04

    摘要: 3-(Thien-2-yl)-piperazin-2-ones, substituted in the 3-position, of the general formula ##STR1## wherein R dentoes, for example, phenyl or (C.sub.1 -C.sub.6)-alkyl and R.sup.1 denotes 2-thienyl and pharmacologically tolerable acid addition salts thereof, which possess valuable nootropic properties. The invention also includes methods for making such compounds, formulations containing such compounds and methods for treating a host in need thereof.

    摘要翻译: 3-(噻吩-2-基) - 哌嗪-2-酮,其通式为其中R dentoes例如苯基或(C 1 -C 6) - 烷基和 R1表示2-噻吩基和其药理学上可耐受的酸加成盐,其具有有价值的特异性。 本发明还包括制备这种化合物的方法,含有这些化合物的制剂和用于治疗有需要的宿主的方法。

    Pharmaceutical composition comprising a sodium hydrogen exchange inhibitor and an angiotensin converting enzyme inhibitor
    10.
    发明授权
    Pharmaceutical composition comprising a sodium hydrogen exchange inhibitor and an angiotensin converting enzyme inhibitor 失效
    包含钠氢交换抑制剂和血管紧张素转化酶抑制剂的药物组合物

    公开(公告)号:US08088799B2

    公开(公告)日:2012-01-03

    申请号:US10910912

    申请日:2004-08-04

    摘要: This invention is directed to a pharmaceutical composition comprising the sodium-hydrogen exchanger (NHE) inhibitor cariporide and an angiotensin converting enzyme (ACE) inhibitor which exhibits unexpectedly efficacious properties for preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life, and to methods of preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life comprising administering pharmaceutically effective amounts of the sodium-hydrogen exchange inhibitor cariporide and an ACE inhibitor.

    摘要翻译: 本发明涉及一种药物组合物,其包含钠 - 氢交换剂(NHE)抑制剂卡立劳和血管紧张素转换酶(ACE)抑制剂,其显示出意想不到的有效性质用于预防心力衰竭和其他与年龄有关的器官功能障碍,年龄相关疾病和 用于延长寿命,以及预防心力衰竭和其他与年龄有关的器官功能障碍,年龄相关疾病和延长寿命的方法,包括给予药学有效量的钠 - 氢交换抑制剂卡立劳和ACE抑制剂。