Carbostyril compounds
    91.
    发明授权
    Carbostyril compounds 失效
    碳青霉烯化合物

    公开(公告)号:US4289883A

    公开(公告)日:1981-09-15

    申请号:US965535

    申请日:1978-11-30

    摘要: Carbostyril compounds represented by the formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group or a phenylalkyl group, R.sub.2 represents an alkenyl group, an alkoxyalkyl group, a hydroxyalkyl group, a carboxyalkyl group, an alkylcarbonyl group, a cycloalkylcarbonyl group, an alkylcarbonylalkyl group, an alkoxycarbonylalkyl group, an alkynyl group or a carbamoylalkyl group, R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom, an alkyl group, a cycloalkyl group, an alkoxyalkyl group, an alkenyl group, a phenylalkyl group, a phenoxyalkyl group or a phenyl group, and the 3,4-bond of the carbostyril nucleus represents a single or double bond, pharmaceutically acceptable salts thereof, and a process for preparing the same.

    摘要翻译: 由式(I)表示的卡博司坦化合物其中R1表示氢原子,烷基或苯基烷基,R2表示烯基,烷氧基烷基,羟烷基,羧基烷基,烷基羰基 基团,环烷基羰基,烷基羰基烷基,烷氧基羰基烷基,炔基或氨基甲酰基烷基,可以相同或不同的R 3和R 4各自表示氢原子,烷基,环烷基,烷氧基烷基 基团,烯基,苯基烷基,苯氧基烷基或苯基,喹诺酮环的3,4-键表示单键或双键,其药学上可接受的盐及其制备方法。

    Tetrazolylalkoxycarbostyril derivatives and pharmaceutical compositions
containing them
    92.
    发明授权
    Tetrazolylalkoxycarbostyril derivatives and pharmaceutical compositions containing them 失效
    四唑基烷氧基吡啶三唑衍生物和含有它们的药物组合物

    公开(公告)号:US4277479A

    公开(公告)日:1981-07-07

    申请号:US70710

    申请日:1979-08-29

    CPC分类号: C07D257/04 Y10S514/826

    摘要: Novel tetrazolylalkoxycarbostyril derivative of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a low alkenyl group, a lower alkanoyl group, a benzoyl group or phenylalkyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a group of the formula ##STR2## R.sup.3 is a lower alkyl group, a cycloalkyl group, a cycloalkylalkyl group, a phenyl group or a phenylalkyl group; A is a lower alkylene group; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is either single or double bond; and the substituted position of a group of the formula, ##STR3## in the carbostyril skeleton is either 4-, 5-, 6-, 7- or 8-position provided that the only one such group of the formula can be substituted in the whole carbostyril skeleton, thus when R.sup.2 in 4-position is a group of the formula ##STR4## then 5-, 6-, 7- or 8-position will have no such substituted group; furthermore, the phenyl group in the above-mentioned benzoyl group, phenylalkyl group or phenyl group may have substituted group(s).The above-mentioned novel tetrazolylalkoxycarbostyril derivatives have pharmacological activities such as platelet aggregation inhibitory action, antiinflammatory action, antiulcer action, vasodilatory action and phosphodiesterase inhibitory action and are useful as anti-thrombosis agent, cerebral blood flow improving agent, antiinflammatory agent, antiulcer agent, anti-hypertensive agent and anti-asthmatic agent.

    摘要翻译: 式(I)的新型四唑基烷氧基吡咯烷腈衍生物:其中R 1为氢原子,低级烷基,低级烯基,低级烷酰基,苯甲酰基或苯基烷基; R2是氢原子,低级烷基或下式的基团R3是低级烷基,环烷基,环烷基烷基,苯基或苯基烷基; A是低级亚烷基; 喹诺酮骨架中3-和4-位之间的碳 - 碳键是单键或双键; 并且喹诺酮骨架中的一组式()的取代位置是4-,5-,6-,7-或8-位,条件是式中唯一一个可以在 因此当4-位上的R2是式“IMAGE”的基团时,则5-,6-,7-或8-位将不具有这样的取代基; 此外,上述苯甲酰基中的苯基,苯基烷基或苯基可以具有取代基。 上述新型四唑基烷氧基吡咯烷腈衍生物具有药物活性,例如血小板聚集抑制作用,抗炎作用,抗溃疡作用,血管扩张作用和磷酸二酯酶抑制作用,可用作抗血栓形成剂,脑血流量改善剂,抗炎剂,抗溃疡剂, 抗高血压药和抗哮喘药。

    Carbostyril derivatives and process for preparing the same
    94.
    发明授权
    Carbostyril derivatives and process for preparing the same 失效
    卡波他特尔衍生物及其制备方法

    公开(公告)号:US4223137A

    公开(公告)日:1980-09-16

    申请号:US932572

    申请日:1978-08-10

    摘要: Carbostyril derivative represented by the formula (I): ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom, a cycloalkylcarbonyl group, a cycloalkylalkanoyl group, a benzoyl group, an alkanoyl group or a phenylalkylcarbonyl group; R.sup.4 represents a hydrogen atom or an alkyl group, R.sup.5 and R.sup.6, which may be the same or different, each represents a hydrogen atom, an alkyl group, a cycloalkyl group, or a phenylalkyl group, or R.sup.5 and R.sup.6 may, when taken together with the nitrogen atom to which they are attached, form a 5- or 6-membered substituted or unsubstituted heterocyclic ring containing 1 or 2 nitrogen or oxygen atoms as hetero atoms; and the ring A has a partial structure: ##STR2## wherein R.sup.3 represents a hydrogen atom, a cycloalkylcarbonyl group, a cycloalkylalkanoyl group, a benzoyl group, an alkanoyl group or a phenylalkylcarbonyl group, with the proviso that at least one of R.sup.1, R.sup.2 and R.sup.3 when R.sub.3 is present, or at least one of R.sub.1 and R.sub.2 when R.sub.3 is absent, represents a cycloalkylcarbonyl group, a cycloalkylalkanoyl group, a benzoyl group, an alkanoyl group or a phenylalkylcarbonyl group; the pharmaceutically acceptable acid addition salts of the above carbostyril compounds represented by the formula (I), and processes for preparing the above carbostyril compounds represented by the formula (I).

    摘要翻译: 由式(I)表示的卡博司坦衍生物:其中R 1和R 2可以相同或不同,各自表示氢原子,环烷基羰基,环烷基烷酰基,苯甲酰基,烷酰基 或苯基烷基羰基; R4表示氢原子或烷基,R5和R6可以相同或不同,各自表示氢原子,烷基,环烷基或苯基烷基,或者R5和R6可以一起 与它们所连接的氮原子形成含有1或2个氮原子或氧原子作为杂原子的5或6元取代或未取代的杂环; 环A具有部分结构:其中R 3表示氢原子,环烷基羰基,环烷基烷酰基,苯甲酰基,烷酰基或苯基烷基羰基,条件是R 1,R 2, 当R3不存在时,R 3和R 3和R 2中的至少一个表示环烷基羰基,环烷基烷酰基,苯甲酰基,烷酰基或苯基烷基羰基; 由式(I)表示的上述喹诺酮化合物的药学上可接受的酸加成盐以及由式(I)表示的上述喹诺酮化合物的制备方法。

    5-[1-Hydroxy-2-(substituted-amino)]alkyl-8-hydroxycarbostyril derivatives
    96.
    发明授权
    5-[1-Hydroxy-2-(substituted-amino)]alkyl-8-hydroxycarbostyril derivatives 失效
    5- {8-羟基-2-(取代 - 氨基){9烷基-8-羟基卡波特他尔衍生物

    公开(公告)号:US4026897A

    公开(公告)日:1977-05-31

    申请号:US536515

    申请日:1974-12-26

    摘要: 5-[1-Hydroxy-2-(substituted-amino)]alkyl -8-hydroxy-carbostyril derivatives represented by the formula (I) ##STR1## wherein R.sup.1 represents an alkyl group having 1 to 4 carbon atoms and R.sup.2 and R.sup.3, which may be the same or different, each represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an aralkyl group containing a straight or branched chain alkyl moiety having 1 to 4 carbon atoms or a cycloalkyl group having 4 to 6 carbon atoms, or R.sup.2 and R.sup.3 may, when taken together with the nitrogen atom to which they are attached, form a 5- or 6-membered substituted or unsubstituted heterocyclic ring containing 1 or 2 nitrogen, oxygen or sulfur atoms as hetero atoms, the pharmaceutically acceptable acid addition salts thereof, and a process for preparing the same.

    摘要翻译: 由式(I)表示的5- [1-羟基-2-(取代 - 氨基)]烷基-8-羟基喹诺酮衍生物其中R 1表示具有1至4个碳原子的烷基和R 2 和可以相同或不同的R 3各自表示氢原子,具有1〜4个碳原子的烷基,含有1〜4个碳原子的直链或支链烷基部分的芳烷基或具有4个碳原子的环烷基 至6个碳原子,或者R 2和R 3可以与它们所连接的氮原子一起形成含有1或2个氮,氧或硫原子作为杂原子的5或6元取代或未取代的杂环 ,其药学上可接受的酸加成盐及其制备方法。