5-Thiazole-methane-amines, and their use as antilipolytics
    1.
    发明授权
    5-Thiazole-methane-amines, and their use as antilipolytics 失效
    5-噻唑 - 甲胺,和它们作为抗生素使用

    公开(公告)号:US4108994A

    公开(公告)日:1978-08-22

    申请号:US721370

    申请日:1976-09-08

    摘要: A 5-thiazole-methane-amine selected from the group consisting of (1) compounds having the formula ##STR1## wherein R.sub.1 represents an alkyl having from 1 to 6 carbon atoms and R.sub.2 and R.sub.3 represent members selected from the group consisting of hydrogen, alkyl having from 1 to 6 carbon atoms, hydroxyalkyl having 1 to 6 carbon atoms, and, taken together, alkylene having up to 5 carbon atoms, azaalkylene having up to 4 carbon atoms, alkylalkylene having up to 5 carbon atoms in the alkylene and 1 to 4 carbon atoms in the alkyl, and alkylazaalkylene having up to 4 carbon atoms in the azaalkylene and 1 to 4 carbon atoms in the alkyl which may be in any position, and (2) its acid addition salts with non-toxic, pharmaceutically-acceptible acids; as well as processes for the preparation of the compounds and a process for use of the compounds as an antilipolytic agent.

    Novel p-(4-tetrahydropyranyl)-phenoxy-compounds
    2.
    发明授权
    Novel p-(4-tetrahydropyranyl)-phenoxy-compounds 失效
    新型对 - (4-四氢吡喃基) - 苯氧基化合物

    公开(公告)号:US4078076A

    公开(公告)日:1978-03-07

    申请号:US690010

    申请日:1976-05-26

    CPC分类号: C07D309/04 C07D309/06

    摘要: Novel pyranic derivatives of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and cations of alkali metals, alkaline earth metals, aluminum, amines and ammonium R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and X is selected from the group consisting of hydrogen, chlorine and bromine having hypolipemic activity and reducing the level of total lipids in plasma.

    摘要翻译: 其中R选自氢,1至6个碳原子的烷基和碱金属,碱土金属,铝,胺和铵的阳离子的新颖的吡喃衍生物,其中R 1和R 2分别选自 由氢和1-4个碳原子的烷基组成的组,X选自具有降血脂活性的氢,氯和溴,并降低血浆中总脂质的含量。

    Treatment of gastric and gastro-duodenal disorders with derivatives of
phenyl aliphatic carboxylic acids
    3.
    发明授权
    Treatment of gastric and gastro-duodenal disorders with derivatives of phenyl aliphatic carboxylic acids 失效
    用苯基脂肪族羧酸衍生物治疗胃和胃十二指肠疾病

    公开(公告)号:US4436752A

    公开(公告)日:1984-03-13

    申请号:US368209

    申请日:1982-04-14

    摘要: Gastric and gastro-duodenal disorders are treated by administering a compound of formula (I) ##STR1## in which A and B together represent a double bond or else A represents a hydrogen atom and B represents a hydroxy radical, and in which R represents a hydrogen atom or an alkyl radical containing from 1 to 5 carbon atoms, in the various possible stereoisomeric forms, as well as the pharmaceutically acceptable alkali metal, alkaline earth metal or amine salts of the compound of formula (I) in which R represents a hydrogen atom.

    摘要翻译: 通过施用式(I)化合物(I),其中A和B一起表示双键或A表示氢原子,B表示羟基,治疗胃和胃十二指肠疾病,其中 R表示氢原子或含有1至5个碳原子的烷基,以各种可能的立体异构形式,以及式(I)化合物的药学上可接受的碱金属,碱土金属或胺盐,其中R 表示氢原子。

    Dopaminergically stimulating 4-substituted indoles
    4.
    发明授权
    Dopaminergically stimulating 4-substituted indoles 失效
    多巴胺能刺激4-取代吲哚

    公开(公告)号:US4332808A

    公开(公告)日:1982-06-01

    申请号:US221927

    申请日:1980-12-31

    CPC分类号: C07D401/04

    摘要: Novel indoles of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 12 carbon atoms, X is selected from the group consisting of hydrogen and alkyl of 1 to 18 carbon atoms, Y is selected from the group consisting of hydrogen and halogen, Z is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, hydroxy alkyl of 1 to 8 carbon atoms, aryloxyalkyl of 7 to 12 carbon atoms, arylalkyl of 7 to 12 carbon atoms optionally substituted with at least one member of the group consisting of halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, --OH, --CF.sub.3, --OCF.sub.3, --NO.sub.2 and NH.sub.2, cycloalkylalkyl of 4 to 12 carbon atoms, alkenyl of 3 to 8 carbon atoms and alkynyl of 3 to 8 carbon atoms, and a and b may each be hydrogen or form a double bond or a is hydrogen and b is selected from the group consisting of --OH and alkoxy of 1 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having dopaminergic stimulating properties optionally accompanied with adrenergic and serotoninergic activity and their preparation and novel intermediates.

    摘要翻译: 其中R选自氢,1至8个碳原子的烷基和7至12个碳原子的芳烷基的新颖的吲哚,其中R选自氢和1至18的烷基 Y选自氢和卤素,Z选自氢,1至8个碳原子的烷基,1至8个碳原子的羟基烷基,7至12个碳原子的芳氧基烷基, 任选被至少一个卤素,1-4个碳原子的烷氧基,1-4个碳原子的烷基,-OH,-CF 3,-OCF 3,-NO 2和NH 2取代的7-12个碳原子的芳基烷基 4至12个碳原子的环烷基烷基,3至8个碳原子的链烯基和3至8个碳原子的炔基,a和b可各自为氢或形成双键,或a为氢,b选自 的-OH和1至8个碳原子的烷氧基,并且它们是无毒的,药学上可接受的 具有任选伴随肾上腺素能和5-羟色胺能活性的多巴胺能刺激性质的酸加成盐及其制备和新型中间体。

    Novel 7-alkyl-steroids
    6.
    发明授权
    Novel 7-alkyl-steroids 失效
    新型7-烷基类固醇

    公开(公告)号:US4258039A

    公开(公告)日:1981-03-24

    申请号:US125891

    申请日:1980-02-29

    摘要: Novel 7-alkyl-.DELTA..sup.4 -17.alpha.-pregnene-3-ones of the formula ##STR1## wherein R is selected from the group consisting of saturated and unsaturated alkyl of 2 to 8 carbon atoms, cycloalkyl alkyl of 4 to 8 carbon atoms and arylalkyl of 7 to 12 carbon atoms and X and Y form the group ##STR2## or X is OH and Y is ##STR3## and M is selected from the group consisting of hydrogen, alkali metal and NH.sub.4 and the wavy line indicates the .alpha.- or .beta.-position or mixtures thereof having aldosterone antagonistic activity and increased hydrosodium diuresis with organic potassium conservation while devoid of secondary hormonal effects and their preparation.

    摘要翻译: 新型7-烷基-TATA4-17α-孕烯-3-酮,其中R选自2-8个碳原子的饱和和不饱和烷基,4-8个碳原子的环烷基烷基 7至12个碳原子的原子和芳基烷基,X和Y形成基团,或X是OH,Y是,M选自氢,碱金属和NH 4,波浪线表示 α-或β-位或其混合物具有醛固酮拮抗活性和增加的氢化钠利尿与有机钾保护,而没有次级激素作用及其制备。

    Novel 19-nor-steroids
    8.
    发明授权
    Novel 19-nor-steroids 失效
    新型19-类固醇

    公开(公告)号:US4263290A

    公开(公告)日:1981-04-21

    申请号:US98766

    申请日:1979-11-30

    摘要: Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 and R.sub.2 taken together form a cycloalkyl of 3 to 8 carbon atoms or are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms with the proviso that both cannot be hydrogen, R.sub.3 is alkyl of 2 to 4 carbon atoms, R.sub.4 ' is selected from the group consisting of hydrogen, hydroxyl, acyloxy of an organic carboxylic acid of 1 to 18 carbon atoms and ##STR2## and M is selected from the group consisting of hydrogen and alkali metal, having antagonistic properties to aldosterone and increasing sodium-water diuresis with conservation of organic potassium and a novel process and novel intermediates for their preparation.

    摘要翻译: 式Ⅰ'的新型19-去甲甾类化合物,其中R 1和R 2一起形成3至8个碳原子的环烷基或分别选自氢,1至4个碳原子的烷基和烯基,和 2至6个碳原子的炔基,条件是两者不能是氢,R3是2至4个碳原子的烷基,R4'选自氢,羟基,1至18碳的有机羧酸的酰氧基 原子和M选自氢和碱金属,对醛固酮具有拮抗作用,并增加钠 - 水利尿与保护有机钾的新方法和新的制备中间体。

    Antihypertensive 2H-indol-2-ones
    9.
    发明授权
    Antihypertensive 2H-indol-2-ones 失效
    降压2H-吲哚-2-酮

    公开(公告)号:US4224333A

    公开(公告)日:1980-09-23

    申请号:US21243

    申请日:1979-03-15

    CPC分类号: A61K31/44

    摘要: Novel optically active isomers or racemates of 1,3-dihydro-3-{1-[2-(2,3-dihydro-1,4-benzodioxin-2-yl)-2-hydroxyethyl]-piperidin-4-yl}-2H-indol-2-ones of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, chlorine, bromine, fluorine and alkoxy of 1 to 5 carbon atoms and R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antihypertensive activity and a novel process and intermediates for their preparation.

    摘要翻译: 新的旋光异构体或1,3-二氢-3- {1- [2-(2,3-二氢-1,4-苯并二恶英-2-基)-2-羟乙基] - 哌啶-4-基} -2H-吲哚-2-酮,其中R 1选自氢,氯,溴,氟和1至5个碳原子的烷氧基,R 2选自氢和 具有1至5个碳原子的烷基和它们的具有抗高血压活性的无毒的药学上可接受的酸加成盐以及用于制备的新方法和中间体。