Sesquiterpene derivatives having anti-complementary activity
    2.
    发明授权
    Sesquiterpene derivatives having anti-complementary activity 失效
    倍半萜衍生物具有抗互补活性

    公开(公告)号:US4229466A

    公开(公告)日:1980-10-21

    申请号:US906300

    申请日:1978-05-15

    摘要: A sesquiterpene derivative expressed by the general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group or a lower alkanoyl group; R.sup.2 and R.sup.3, which may be the same or different, each represents a formyl group, a hydroxymethyl group, a hydroxyl group, a carboxyl group, a lower alkanoyloxymethyl group, or a group of the formula --CH.dbd.CR.sup.7 R.sup.8, wherein R.sup.7 and R.sup.8, which may be the same or different, each represents a hydrogen atom, a cyano group, a lower alkoxycarbonyl group or a carboxyl group, or R.sup.2 and R.sup.3 may combine to form a lactone ring of the formula ##STR2## in which R.sup.9 represents a hydrogen atom or a hydroxyl group; R.sup.4 and R.sup.6, which may be the same or different, each represents a hydroxyl group or a lower alkanoyloxy group; R.sup.5 represents a hydrogen atom; R.sup.4 and R.sup.5 may together form an oxo group (.dbd.O); and R.sup.4 and R.sup.6 may combine to form a lower alkylidenedioxy group, the pharmaceutically acceptable salts thereof, processes for the production of the compounds of the general formula (I) and the salts thereof, pharmaceutical composition containing the compounds of the general formula (I) and the salts thereof, and method of use of the compounds of the general formula (I) and the salts thereof.

    摘要翻译: 由通式(I)表示的倍半萜衍生物:其中R 1表示氢原子,低级烷基或低级烷酰基; R2和R3可以相同或不同,分别表示甲酰基,羟甲基,羟基,羧基,低级烷酰氧基甲基或式-CH = CR7R8的基团,其中R7和R8 可以相同或不同,各自表示氢原子,氰基,低级烷氧基羰基或羧基,或者R 2和R 3可以结合形成式“IMAGE”的内酯环,其中R 9表示 氢原子或羟基; R 4和R 6可以相同或不同,分别表示羟基或低级烷酰氧基; R5代表氢原子; R4和R5可以一起形成氧代基(= O); 并且R4和R6可以结合形成低级亚烷基二氧基,其药学上可接受的盐,通式(I)化合物及其盐的制备方法,含有通式(I)化合物的药物组合物, 及其盐,以及通式(I)的化合物及其盐的使用方法。

    Hydrofluorene derivatives
    3.
    发明授权
    Hydrofluorene derivatives 失效
    氢氟芴衍生物

    公开(公告)号:US5017724A

    公开(公告)日:1991-05-21

    申请号:US532341

    申请日:1990-06-04

    摘要: Novel hydrofluorene derivatives and salts thereof represented by the formula (1) which possess excellent activities for improving anoxemic and hypoxic symptoms and syndromes accompanied therewith, therefore said derivatives are useful as cerebral activators, preventive agents for arrhythmia and heart failure caused by the shortage of oxygen and others. Furthermore, said hydrofluorene derivatives and salts thereof possess actions for scavenging active oxygen radicals, therefore, the derivatives are useful prophylactic and treating agents for various disturbances and diseases caused by the excessive formation of active oxygen radicals. In addition to the above, the hydrofluorene derivatives are useful as anti-oxidative agents for fats and oils.Yet, further, the hydrofluorene derivatives and salts thereof accelerate the uptaking of high-affinity choline in the central nerve system and/or the releasing of acetylcholine therefrom, therefore, the hydrofluorene derivatives and salts thereof are useful cholinergic nerve system activating agents.

    摘要翻译: 由式(1)表示的新型氢芴衍生物及其盐,其具有改善缺氧症和缺氧症状及伴随症状的优异活性,因此所述衍生物可用作脑激活剂,由氧气不足引起的心律失常和心力衰竭的预防剂 和别的。 此外,所述氢芴衍生物及其盐具有清除活性氧自由基的作用,因此,该衍生物是用于由过度形成活性氧自由基引起的各种紊乱和疾病的预防和治疗剂。 除了上述之外,氢芴衍生物可用作脂肪和油的抗氧化剂。 此外,氢芴衍生物和其盐加速了中枢神经系统中高亲和力胆碱的吸收和/或乙酰胆碱的释放,因此,氢芴衍生物及其盐是有用的胆碱能神经系统活化剂。

    Carbostyril derivatives for inhibiting skin erythema and/or skin
pigmentation
    7.
    发明授权
    Carbostyril derivatives for inhibiting skin erythema and/or skin pigmentation 失效
    用于抑制皮肤红斑和/或皮肤色素沉着的碳青霉烯衍生物

    公开(公告)号:US06133264A

    公开(公告)日:2000-10-17

    申请号:US485454

    申请日:2000-02-10

    摘要: The present invention provides an agent for inhibiting skin erythema and/or skin pigmentation, containing at least one selected from the group consisting of the carbostyril derivative and salt thereof represented by the general formula, ##STR1## (wherein R.sup.1 is a hydrogen atom, a lower alkyl group or the like; R.sup.2 is a hydrogen atom, a lower alkyl group, a lower alkoxy group or the like; R.sup.3 and R.sup.4 are lower alkyl groups which may have hydroxyl groups as substituents or the like; the carbon--carbon bond between 3- and 4-positions in the carbostyril skeleton is a single bond or double bond).

    摘要翻译: PCT No.PCT / JP98 / 03657 Sec。 371日期2000年2月10日 102(e)日期2000年2月10日PCT提交1998年8月18日PCT公布。 第WO99 /​​ 09011号公报 日期1999年2月25日本发明提供一种抑制皮肤红斑和/或皮肤色素沉着的药剂,其含有选自由通式表示的喹诺酮衍生物及其盐的至少一种(其中,R 1为氢原子 ,低级烷基等; R 2为氢原子,低级烷基,低级烷氧基等; R 3和R 4为可具有羟基作为取代基的低级烷基等;碳 - 碳 喹诺酮骨架中3-和4-位之间的键是单键或双键)。

    Carbostyril derivatives
    8.
    发明授权
    Carbostyril derivatives 失效
    卡波他汀衍生物

    公开(公告)号:US5006528A

    公开(公告)日:1991-04-09

    申请号:US424719

    申请日:1989-10-20

    IPC分类号: C07D215/22 C07D215/227

    CPC分类号: C07D215/227

    摘要: A novel carbostyril derivative and salt thereof represented by the formula (1) ##STR1## (wherein R is a group of the formula ##STR2## ((wherein R.sup.1 is a C.sub.1- C.sub.3 alkoxy group)), a group of the formula ##STR3## ((wherein R.sup.2 and R .sup.3 are each, at the same time, a chlorine atom, a bromine atom; and R.sup.4 is a hydrogen atom or a chlorine atom)), 2-methyl-3-nitrophenyl group, 3,5-dichlorophenyl group, or a group of the formula ##STR4## ((wherein R.sup.5 is a chlorine atom or a bromine atom; and R.sup.6 is a methyl group)); the carbon-carbon bond between 3- and 4-position in the carbostyril skeleton is a single or double bond).

    Carbostyril derivatives, and antihistaminic agents containing the same
    9.
    发明授权
    Carbostyril derivatives, and antihistaminic agents containing the same 失效
    卡波他汀衍生物和含有它们的抗组胺剂

    公开(公告)号:US4482560A

    公开(公告)日:1984-11-13

    申请号:US357769

    申请日:1982-03-12

    摘要: Novel carbostyril derivatives and their salts having antihistaminic effects and are useful as antihistaminic agents, represented by the general formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkenyl group, a lower alkynyl group or a lower alkyl group which may have phenyl group(s) as the substituted group(s); R.sup.2 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.3 is a lower alkyl group having phenyl group(s) as the substituted group(s), or a phenyl group which may have 1 to 3 substituted groups selected from the group consisting of halogen atoms, lower alkyl groups and lower alkoxy groups; R.sup.4 is a hydrogen atom, a hydroxyl group or a lower alkanoyl group; X is a halogen atom; Y is a lower alkylene group which may have hydroxyl group(s) as the substituent(s); n is 0, 1 or 2; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or double bond; provided that when R.sup.3 is a lower alkyl group having phenyl group(s) as the substituted group(s), then R.sup.4 should be neither a hydroxyl group nor a lower alkanoyl group.

    摘要翻译: 新颖的喹诺酮衍生物及其具有抗组胺作用的盐,可用作抗组胺剂,由通式(1)表示,其中R1是氢原子,低级烯基,低级炔基或低级炔基 可以具有苯基作为取代基的烷基; R2是氢原子,低级烷基或苯基; R3是具有苯基作为取代基的低级烷基或可具有1至3个选自卤素原子,低级烷基和低级烷氧基的取代基的苯基; R4是氢原子,羟基或低级烷酰基; X是卤原子; Y是可以具有羟基作为取代基的低级亚烷基; n为0,1或2; 喹诺酮骨架中3-和4-位之间的碳 - 碳键是单键或双键; 条件是当R3为具有苯基作为取代基的低级烷基时,则R4不应为羟基也不应为低级烷酰基。

    3,4-Dihydrocarbostyril derivatives and process for preparing the same
    10.
    发明授权
    3,4-Dihydrocarbostyril derivatives and process for preparing the same 失效
    3,4-二氢喹诺酮衍生物及其制备方法

    公开(公告)号:US4147869A

    公开(公告)日:1979-04-03

    申请号:US795042

    申请日:1977-05-09

    摘要: 3,4-Dihydrocarbostyril derivatives represented by the formula (I) ##STR1## wherein R.sub.1 represents an alkylcarbonyl group, a cycloalkylcarbonyl group, an alkylsulfonyl group, a phenylsulfonyl group, a carbamoyl group or an alkoxycarbonyl group, R.sub.2 and R.sub.3, which may be the same or different, each represents a hydrogen atom, an alkyl group, a phenylalkyl group or a phenoxyalkyl group, or R.sub.2 and R.sub.3 can form, when taken together with the nitrogen atom to which they are attached, a heterocyclic group selected from the group consisting of piperidino, pyrrolidino, morpholino and 1-piperazinyl which may be substituted with a phenyl group or an alkyl group having 1 to 4 carbon atoms, with the proviso that, when the group --NHR.sub.1 is attached to the 8-position of the 3,4-dihydrocarbostyril nucleus in which R.sub.1 represents an alkylcarbonyl group and one of R.sub.2 and R.sub.3 represents a hydrogen atom, then the other group of R.sub.2 and R.sub.3 cannot be an alkyl group, pharmaceutically acceptable acid addition salts thereof, and process for preparing the same.

    摘要翻译: 由式(I)表示的3,4-二氢吡咯烷子衍生物其中R1表示烷基羰基,环烷基羰基,烷基磺酰基,苯基磺酰基,氨基甲酰基或烷氧基羰基,R2和R3, 其可以相同或不同,各自表示氢原子,烷基,苯基烷基或苯氧基烷基,或者当与所连接的氮原子一起时,R 2和R 3可以形成选自下列的杂环基 由可以被苯基或具有1至4个碳原子的烷基取代的哌啶子基,吡咯烷子基,吗啉代和1-哌嗪基组成的组,条件是当基团-NHR1连接到8-位时 的3,4-二氢喹诺酮环,其中R 1表示烷基羰基,R 2和R 3中的一个表示氢原子,则另一组R 2和R 3不能为烷基,其药学上可接受的酸加成盐 及其制备方法。