Anti-spasmodic substituted quinolizidine and indolizidine compounds
    12.
    发明授权
    Anti-spasmodic substituted quinolizidine and indolizidine compounds 失效
    抗痉挛性取代喹嗪啶和吲哚嗪类化合物

    公开(公告)号:US4205074A

    公开(公告)日:1980-05-27

    申请号:US16515

    申请日:1979-03-01

    CPC分类号: C07D471/04 C07D455/02

    摘要: Phenyl- or thienyl-substituted quinolizidines and indolizidines as well as quaternary salts thereof are disclosed. These compounds are useful as pharmaceutical agents exhibiting strong spasmolytic, anti-ulcer, anti-histaminic and antiemetic activities with minimized side effects such as thirst and dilation of the pupil.Phenyl- or thienyl-substituted quinolizidine-methanols and indolizidine-methanols which are starting materials of the aforementioned quinolizidine and indolizidine compounds are also useful as having spasmolytic, anti-ulcer, anti-histaminic and anti-emetic activities.

    摘要翻译: 公开了苯基或噻吩基取代的喹嗪基和吲哚嗪及其季盐。 这些化合物可用作具有强的解痉,抗溃疡,抗组胺和止吐活性的药物,其最小化的副作用如瞳孔的口渴和扩张。 作为上述喹嗪基和吲哚嗪化合物的起始原料的苯基或噻吩基取代的喹嗪基 - 甲醇和吲哚来啶 - 甲醇也可用作具有解痉,抗溃疡,抗组胺和抗呕吐活性。

    Photostable aqueous solution comprising benzyl alcohol derivatives
    13.
    发明授权
    Photostable aqueous solution comprising benzyl alcohol derivatives 有权
    包含苯甲醇衍生物的光稳定水溶液

    公开(公告)号:US6162833A

    公开(公告)日:2000-12-19

    申请号:US292664

    申请日:1999-04-16

    摘要: Aqueous solution, including at least one of optically active (-)-(R)-.alpha.-((tert-butylamino)methyl)-2-chloro-4-hydroxybenzyl alcohol represented by the following formula: ##STR1## and pharmacologically acceptable salt thereof. The aqueous solution also includes at least one photostabilizer selected from the group consisting of saccharide, sugar alcohol, and polyalcohol. A content of the at least one of optically active (-)-(R)-.alpha.-((tert-butylamino)methyl)-2-chloro-4-hydroxybenzyl alcohol and pharmacologically acceptable salt thereof is 0.01 to 10% (w/v) based on a volume of the aqueous solution. A content of the at least one photostabilizer is 1 to 50% (w/v) based on the volume of the aqueous solution. The content of the at least one photostabilizer is at least 10% (w/w) based on a total weight of the at least one of optically active (-)-(R)-.alpha.-((tert-butylamino)methyl)-2-chloro-4-hydroxybenzyl alcohol and pharmacologically acceptable salt thereof. Method of making a stabilized aqueous solution.

    摘要翻译: 水溶液,包括由下式表示的光学活性( - ) - (R)-α-((叔丁基氨基)甲基)-2-氯-4-羟基苄醇中的至少一种:及其药理学上可接受的盐。 水溶液还包括至少一种选自糖,糖醇和多元醇的光稳定剂。 光学活性( - ) - (R)-α-((叔丁基氨基)甲基)-2-氯-4-羟基苄醇及其药学上可接受的盐中的至少一种的含量为0.01〜10%(w / v)基于一定体积的水溶液。 基于水溶液的体积,至少一种光稳定剂的含量为1至50%(w / v)。 至少一种光稳定剂的含量基于光学活性( - ) - (R)-α-((叔丁基氨基)甲基) - 2-氯-4-羟基苄醇及其药理学上可接受的盐。 制备稳定水溶液的方法

    Pyrazine-2-carboxamide derivatives useful in treating allergic disease
    15.
    发明授权
    Pyrazine-2-carboxamide derivatives useful in treating allergic disease 失效
    吡嗪-2-甲酰胺衍生物,用于治疗过敏性疾病

    公开(公告)号:US4792547A

    公开(公告)日:1988-12-20

    申请号:US941918

    申请日:1986-12-15

    摘要: Novel pyrazine derivatives useful for treatment of bronchial asthma, allergic gastorenteric trouble, hay fever urticaria, allertic rhinitis, and allergic conjunctivitis, and pharmaceutical compositions thereof, are disclosed. The compounds have the formula I as follows: ##STR1## wherein R represents hydrogen or ##STR2## wherein R.sub.1 and R.sub.2 may be the same or different and each independently represents hydrogen, straight or branched-chain lower-alkyl, or cycloalkyl having three to six carbon atoms inclusive, phenyl which may be substituted with halogen, lower-alkyl, or lower-alkoxy, or wherein R.sub.1 and R.sub.2 together represent alkylene of four to six carbon atoms, inclusive, optionally interrupted by one or two nitrogen atoms or one oxygen atom and said ring being optionally substituted by straight or branched-chain lower-alkyl having one to six carbon atoms inclusive, hydroxy, or phenyl,and pharmaceutically-acceptable salts thereof.

    摘要翻译: 用于治疗支气管哮喘,过敏性胃炎,花粉荨麻疹,过敏性鼻炎和过敏性结膜炎的新颖吡嗪衍生物及其药物组合物。 化合物具有如下式I:其中R表示氢或者其中R 1和R 2可以相同或不同,并且各自独立地表示氢,直链或支链低级烷基或具有三个至 6个碳原子,可被卤素,低级烷基或低级烷氧基取代的苯基,或其中R 1和R 2一起代表四至六个碳原子的亚烷基,包括任选地被一个或两个氮原子或一个氧 所述环任选被具有1-6个碳原子的直链或支链低级烷基,羟基或苯基取代,及其药学上可接受的盐。

    1',4'-Dihydro-1-methyl-spiro [piperidine and
pyrrolidine-2,3'(2'H)quinoline]-2'-one compounds
    18.
    发明授权
    1',4'-Dihydro-1-methyl-spiro [piperidine and pyrrolidine-2,3'(2'H)quinoline]-2'-one compounds 失效
    1 {40,4 {40-二氢-1-甲基 - 螺(8)哌啶和吡咯烷-2,3(40(2(40H))喹啉{9-2 {

    公开(公告)号:US3936459A

    公开(公告)日:1976-02-03

    申请号:US531452

    申请日:1974-12-11

    CPC分类号: C07D471/10

    摘要: Spiro compounds having the structural formula ##SPC1##Where n is an integer of 1 or 2,Are disclosed. These compounds are useful as analgetic, antihistamine and spasmolytic agents. They are indicated in the management of conditions such as headache, seasonal allergies and the like.

    摘要翻译: 螺旋化合物具有结构式,其中N为1或2的整数,被披露。 这些化合物可用作止痛药,抗组胺药和解痉药。 它们在诸如头痛,季节性过敏等条件的管理中被指出。

    Piperidine derivative, method for preparation thereof, and a
pharmaceutical composition comprising the same
    20.
    发明授权
    Piperidine derivative, method for preparation thereof, and a pharmaceutical composition comprising the same 失效
    哌啶衍生物,其制备方法和包含其的药物组合物

    公开(公告)号:US5153207A

    公开(公告)日:1992-10-06

    申请号:US520064

    申请日:1990-05-03

    IPC分类号: C07D211/46 C07D211/54

    CPC分类号: C07D211/54 C07D211/46

    摘要: A piperidine derivative represented by the following general formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each independently represents a hydrogen atom, a halogen atom, a lower alkyl group, or a lower alkoxy group; R.sub.3 represents a hydrogen atom or a lower alkyl group; X represents an oxygen atom or a sulfur atom; Y represents an alkylene group having 1 to 7 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an --A--O--B-- group wherein A and B are the same or different and each independently represents an alkylene group having 1 to 3 carbon atoms which may be optionally substituted with a lower alkyl group is disclosed. Also disclosed are a pharmacologically acceptable salt of a compound of formula (I), an antihistaminic and antiallergic agent comprising a compound of formula (I), a pharmaceutical composition comprising a compound of formula (I), and a method for the treatment of an allergic disease by administering a compound of formula (I).