Antibiotic aminoglycosides, processes of preparation and pharmaceutical
compositions
    3.
    发明授权
    Antibiotic aminoglycosides, processes of preparation and pharmaceutical compositions 失效
    抗生素氨基糖苷类,制备方法和药物组合物

    公开(公告)号:US4031210A

    公开(公告)日:1977-06-21

    申请号:US630917

    申请日:1975-11-11

    CPC分类号: C07H15/234

    摘要: There are disclosed pharmaceutically-active aminoglycosides comprising 4-O-[2',6'-diamino 2',3',6'-tridesoxy .alpha.,D-ribohexopyranosyl] 6-O-[3"-methylamino 3",4",6"-tridesoxy .alpha.,D-xylohexopyranosyl] 2-desoxystreptamine of the formula: ##STR1## and the addition salts thereof with mineral acids or organic acids. Also disclosed are methods for preparation of the novel products as well as certain novel intermediate products. There are also disclosed pharmaceutical compositions in which the novel products are the active agents and a method for the treatment of bacteria infections in humans and animals.

    摘要翻译: 公开了含有4-O- [2',6'-二氨基2',3',6'-三酰氧基α,D-核糖六吡喃糖基] 6-O- [3“ - 甲基氨基3”的药学活性氨基糖苷类, 4“,6” - 三酰氧基α,D-木糖六吡喃葡糖基] 2-脱氧神经胺,其分子式如下:其与无机酸或有机酸的加成盐。 还公开了制备新产品以及某些新型中间产物的方法。 还公开了其中新产品是活性剂的药物组合物和用于治疗人和动物细菌感染的方法。

    Antibiotic aminoglycosides, processes of preparation and pharmaceutical
compositions
    5.
    发明授权
    Antibiotic aminoglycosides, processes of preparation and pharmaceutical compositions 失效
    抗生素氨基糖苷类,制备方法和药物组合物

    公开(公告)号:US4064339A

    公开(公告)日:1977-12-20

    申请号:US557310

    申请日:1975-03-11

    CPC分类号: C07H15/224 C07H15/234

    摘要: There are disclosed pharmaceutically-active aminoglycosides comprising 4-O-(2',6'-diamino 2',6'-didesoxy .alpha.,D-glucopyrannosyl) 6-O-(3"-amino 3",4",6"-tridesoxy .alpha., D-xylohexopyrannosyl) 2-desoxy streptamine of the formula: ##STR1## and the addition salts thereof with mineral acids or organic acids. Also disclosed are methods for preparation of the novel products as well as certain novel intermediate products. There are also disclosed pharmaceutical compositions in which the novel products are the active agents as well as methods for use of compositions as antibiotic agents.

    摘要翻译: 公开了包含4-O-(2',6'-二氨基2',6'-二脱氧-α,D-吡喃葡萄糖基)6-O-(3“ - 氨基3”,4“'的药学活性氨基糖苷类 ,6“ - 三酰氧基α,D-木糖六吡喃葡糖基)2-脱氧链霉胺,及其与无机酸或有机酸的加成盐。 还公开了制备新产品以及某些新型中间产物的方法。 还公开了其中新产品是活性剂的药物组合物以及用作组合物作为抗生素剂的方法。

    2,3-dihydro indoles
    6.
    发明授权
    2,3-dihydro indoles 失效
    2,3-二氢吲哚

    公开(公告)号:US4736042A

    公开(公告)日:1988-04-05

    申请号:US72359

    申请日:1987-07-13

    CPC分类号: C07D413/04 C07D209/08

    摘要: Novel racemic mixtures and optical isomers of 4-morpholinyl-1H-indoles of the formula: ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and R.sub.2 is selected from the group consisting of hydroxymethyl, alkylthiomethyl of 1 to 3 alkyl carbons, cyanomethyl and carboxy optionally esterified with an aliphatic alcohol of 1 to 5 carbon atoms or optionally amidified with an amine of the formula ##STR2## R.sub.3 is alkyl of 1 to 4 carbon atoms and R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having the ability to activate neurons and to protect the same against ischemic or anoxic aggressions.

    摘要翻译: 4-吗啉基-1H-吲哚的新型外消旋混合物和旋光异构体,其分子式如下:其中R和R 1分别选自氢和1至4个碳原子的烷基,R 2选自 由羟甲基,1至3个烷基碳的烷硫基甲基,任选地被1至5个碳原子的脂族醇酯化的氰基甲基和羧基,或任选地与下式的胺酰胺化:具有1至4个碳原子的烷基和R 4 选自氢和1至4个碳原子的烷基及其无毒的药学上可接受的酸加成盐,其具有激活神经元的能力并保护其相对于缺血性或缺氧性侵袭。

    Hexapeptides
    8.
    发明授权
    Hexapeptides 失效
    六肽

    公开(公告)号:US4412988A

    公开(公告)日:1983-11-01

    申请号:US310392

    申请日:1981-10-09

    摘要: Novel hexapeptides of the formulaCys--X--Y--D--Lys--Z Iwherein X is a sequence selected from the group consisting of Ala--Ala and Glu--His, Y is selected from the group consisting of Cys and Phe and Z is Phe when Y is Cys or Z is Cys when Y is Phe, the two Cys groups in the molecule being joined by a disulfide bridge, and their functional derivatives such as their non-toxic, pharmaceutically acceptable acid addition salts, salts with bases, esters and amides and metallic complexes thereof having an influence on the memory process and their preparation.

    摘要翻译: 式Cys-XYD-Lys-Z I的新型六肽,其中X为选自Ala-Ala和Glu-His的序列,Y选自Cys和Phe,Z为Phe时,Y为 当Y为Phe时,Cys或Z为Cys,分子中的两个Cys基团通过二硫键连接,其功能衍生物如其无毒的药学上可接受的酸加成盐,与碱,酯和酰胺的盐和金属 其复合物对记忆过程及其制备有影响。

    2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepines
    9.
    发明授权
    2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepines 失效
    2,4-二氧代-5-苯基-2,3,4,5-四氢-1H-1,5-苯并二氮杂卓

    公开(公告)号:US4988692A

    公开(公告)日:1991-01-29

    申请号:US457237

    申请日:1989-12-27

    CPC分类号: C07D403/12 C07D243/12

    摘要: A compound in all possible isomeric forms and mixtures thereof of the formula ##STR1## wherein X and X' are individually selected from the group consisting of hydrogen, halogen, cyano, --NO.sub.2, --CF.sub.3 and alkyl and alkoxy of 1 to 8 carbon atoms, R is hydrogen or alkyl of 1 to 8 carbon atoms and Ar is selected from the group consisting of an unsubstituted or substituted aryl of 6 to 14 carbon atoms, an unsubstituted or substituted aromatic heterocyclic or a heterocyclic united with an unsubstituted or substituted aryl having cholecystokinine antagonistic activity.

    摘要翻译: 具有式I的所有可能的异构体形式的化合物及其混合物,其中X和X'分别选自氢,卤素,氰基,-NO 2,-CF 3和1至8碳的烷基和烷氧基 原子,R为氢或1至8个碳原子的烷基,Ar选自未取代或取代的6至14个碳原子的芳基,未取代或取代的芳族杂环或杂环与未取代或取代的芳基 具有胆囊收缩素拮抗作用。

    4-morpholinyl-1H-indoles, pharmaceutical compositions and use
    10.
    发明授权
    4-morpholinyl-1H-indoles, pharmaceutical compositions and use 失效
    4-吗啉基-1H-吲哚,药物组合物和用途

    公开(公告)号:US4699907A

    公开(公告)日:1987-10-13

    申请号:US941037

    申请日:1986-12-12

    CPC分类号: C07D413/04 C07D209/08

    摘要: Novel racemic mixtures and optical isomers of 4-morpholinyl-1H-indoles of the formula: ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and R.sub.2 is selected from the group consisting of hydroxymethyl, alkylthiomethyl of 1 to 3 alkyl carbons, cyanomethyl and carboxy optionally esterified with an aliphatic alcohol of 1 to 5 carbon atoms or optionally amidified with an amine of the formula ##STR2## R.sub.3 is alkyl of 1 to 4 carbon atoms and R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having the ability to activate neurons and to protect the same against ischemic or anoxic aggressions.

    摘要翻译: 4-吗啉基-1H-吲哚的新型外消旋混合物和光学异构体,其具有下式:其中R和R 1分别选自氢和1至4个碳原子的烷基,R 2选自 由羟甲基,1至3个烷基碳的烷硫基甲基,任选地被1至5个碳原子的脂族醇酯化的氰基甲基和羧基,或任选地与下式的胺酰胺化:具有1至4个碳原子的烷基和R 4 选自氢和1至4个碳原子的烷基及其无毒的药学上可接受的酸加成盐,其具有激活神经元的能力并保护其相对于缺血性或缺氧性侵袭。