Indoles
    31.
    发明授权
    Indoles 失效
    吲哚

    公开(公告)号:US4105777A

    公开(公告)日:1978-08-08

    申请号:US758633

    申请日:1977-01-12

    CPC分类号: C07D209/12

    摘要: Indoles of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, halogen, --CF.sub.3, alkyl of 1 to 8 carbon atoms and alkoxy of 1 to 8 carbon atoms, R.sub.2 is in the 2,3 or 4 position and is selected from the group consisting of halogen, --CF.sub.3 and alkyl, alkoxy and alkylthio of 1 to 8 carbon atoms, A is selected from the group consisting of branched alkylene of 3 to 5 carbon atoms and --(CH.sub.2).sub.n -- and n is a number of 2 to 5 and R.sub.3 and R.sub.4 are alkyl of 1 to 8 carbon atoms or taken together with the nitrogen atom form a heterocyclic ring selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, piperazinyl and N-alkyl piperazinyl with 1 to 4 alkyl carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity and their preparation.

    摘要翻译: 式I的吲唑,其中R 1选自氢,卤素,-CF 3,1至8个碳原子的烷基和1至8个碳原子的烷氧基,R 2为2,3或4位 并且选自卤素,-CF 3和具有1至8个碳原子的烷基,烷氧基和烷硫基,A选自3至5个碳原子的支链亚烷基和 - (CH 2)n和n 是2至5的数,R3和R4是1至8个碳原子的烷基或与氮原子一起形成选自哌啶基,吡咯烷基,吗啉基,哌嗪基和N-烷基哌嗪基的杂环,其中1 至4个烷基碳原子及其无毒的药学上可接受的具有止痛活性的酸加成盐及其制备。

    Novel-3-(4-quinolylamino)-2-thiophene-carboxylates
    32.
    发明授权
    Novel-3-(4-quinolylamino)-2-thiophene-carboxylates 失效
    新型3-(4-喹啉基氨基)-2-噻吩 - 羧酸酯

    公开(公告)号:US4093724A

    公开(公告)日:1978-06-06

    申请号:US770304

    申请日:1977-02-22

    CPC分类号: C07D401/12

    摘要: Novel 3-(4-quinolylamino)-2-thiophene-carboxylates of the formula ##STR1## wherein X is in the 6, 7 or 8-position and is selected from the group consisting of hydrogen, halogen, --CF.sub.3 and alkyl and alkoxy of 1 to 8 carbon atoms, n is 2, 3, 4 or 5, Y is in the 2, 3 or 4-position and is selected from the group consisting of hydrogen, halogen, --CF.sub.3 and alkyl and alkoxy of 1 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity and process and intermediates for their preparation.

    摘要翻译: 式(VI)的新型3-(4-喹啉基氨基)-2-噻吩 - 羧酸酯,其中X为6,7或8-位,并且选自氢,卤素,-CF 3和烷基,和 1至8个碳原子的烷氧基,n为2,3,4或5,Y为2,3或4位,并且选自氢,卤素,-CF 3和1至 8个碳原子及其无毒的药学上可接受的具有镇痛活性的酸加成盐及其制备方法和中间体。

    Method of inducing immunostimulating activity
    34.
    发明授权
    Method of inducing immunostimulating activity 失效
    诱导免疫刺激活性的方法

    公开(公告)号:US4880803A

    公开(公告)日:1989-11-14

    申请号:US103919

    申请日:1987-10-01

    CPC分类号: A61K31/40

    摘要: A method of inducing immunostimulating activity in warm-blooded animals comprising administering to warm-blooded animals an immunostimulating amount of at least one maleo-pimaric acid compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 together with the nitrogen to which they are attached form an optionally substituted saturated heterocycle optionally containing at least one other heteroatom, Y is selected from the group consisting of hydrogen, amino, alkyl of 1 to 5 carbon atoms optionally substituted with at least one hydroxy, dialkylamino with alkyl of 1 to 5 carbon atoms, alkoxy carbonyl of 2 to 5 carbon atoms, acyl of an organic carboxylic acid of 1 to 5 carbon atoms and ##STR2## X is an alkylene of 1 to 5 carbon atoms and R.sub.1 and R.sub.2 have the above definition.

    摘要翻译: 一种在温血动物中诱导免疫刺激活性的方法,包括向温血动物施用免疫刺激量的至少一种下式的马来酸 - 海松酸化合物,其中R1和R2与它们所连接的氮一起 形成任选地含有至少一个其它杂原子的任选取代的饱和杂环,Y选自氢,氨基,任选被至少一个羟基,二烷基氨基与1至5个碳原子的烷基取代的1至5个碳原子的烷基 2至5个碳原子的烷氧基羰基,1至5个碳原子的有机羧酸的酰基,X是1至5个碳原子的亚烷基,R 1和R 2具有上述定义。

    Novel anti-inflammatory treatment
    35.
    发明授权
    Novel anti-inflammatory treatment 失效
    新型抗炎治疗

    公开(公告)号:US4614736A

    公开(公告)日:1986-09-30

    申请号:US718175

    申请日:1985-04-01

    CPC分类号: A61K31/57

    摘要: A novel method of treating inflammation of the colon and rectum of warm-blooded animals comprising administering to the colon and rectum of warm-blooded animals an anti-inflammatorily effective amount of 9.alpha.,11.beta.-dichloro-16.alpha.-methyl-21-oxycarbonyldicyclohexylmethoxy-.DELTA..sup.1,4 -pregnadiene-3,20-dione.

    摘要翻译: 一种治疗温血动物结肠和直肠炎症的新方法,包括向结肠和直肠的温血动物施用抗炎剂有效量的9α,11β-二氯-16α-甲基-21- 氧羰基二环己基甲氧基-TATA1,4-孕烯二烯-3,20-二酮。

    Analgesic 4-hydroxy-3-quinolinecarboxamides
    36.
    发明授权
    Analgesic 4-hydroxy-3-quinolinecarboxamides 失效
    止痛4-羟基-3-喹啉甲酰胺

    公开(公告)号:US4397856A

    公开(公告)日:1983-08-09

    申请号:US262952

    申请日:1981-05-12

    摘要: Novel compounds of the formula ##STR1## wherein X is in the 5,6,7 or 8 position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, CF.sub.3 O--, CF.sub.3 S-- and CF.sub.3 --, R.sub.1 ' is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.2 ' is selected from the group consisting of hydrogen or an optionally unsaturated ring able to contain one or more heteroatoms of the group consisting of --S--, --O-- and --N-- optionally substituted with one or more members of the group consisting of (a) halogens, (b) alkyl of 1 to 4 carbon atoms optionally substituted with NH.sub.2, --NHAlK or --N---(AlK).sub.2 and AlK is alkyl of 1 to 3 carbon atoms, (c) phenyl, (d) alkoxy of 1 to 4 carbon atoms, (e) --OH, (f) --CF.sub.3 and (g) --NO.sub.2 or R.sub.1 ' together with the nitrogen atom to which they are attached form an optionally unsaturated ring, the said ring then being connected to the nitrogen atom by a double bond, R.sub.3 is selected from the group consisting of hydrogen, halogen and alkyl of 1 to 4 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and halogen, R.sub.5 is a halogen with the proviso that R.sub.3, R.sub.4 and R.sub.5 can not all be fluorine and R.sub.6 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and an acyl of an organic carboxylic acid of 2 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts and their salts with non-toxic, pharmaceutically acceptable bases having a remarkable analgesic activity, a very weak anti-inflammatory activity and a good tolerance by the gastrointestinal system and their preparation and their intermediates.

    摘要翻译: 新颖的式(Ⅰ)化合物,其中X为5,6,7或8位,选自氢,卤素,1至5个碳原子的烷基,1至4个碳原子的烷氧基 ,CF 3 O-,CF 3 S-和CF 3 - ,R''选自氢和1至4个碳原子的烷基,R 2'选自氢或任选不饱和的环,其能够含有一个或多个 任选被一个或多个由(a)卤素,(b)任选被NH 2取代的1至4个碳原子的烷基取代的-S-,-O-和 - NHAlK或-N - (AlK)2,AlK是1至3个碳原子的烷基,(c)苯基,(d)1-4个碳原子的烷氧基,(e)-OH,(f)-CF3和( g)-NO 2或R 1'与它们所连接的氮原子一起形成任选的不饱和环,然后所述环通过双键与氮原子连接,R 3选自组 氢,卤素和1至4个碳原子的烷基,R4选自氢和卤素,R5是卤素,条件是R3,R4和R5不能全部是氟,R6选自 由氢,1-8个碳原子的烷基和2至8个碳原子的有机羧酸的酰基及其无毒的药学上可接受的酸加成盐和它们的盐与无毒的药学上可接受的碱组成的组,其具有 显着的止痛活性,非常弱的抗炎活性和良好的耐胃肠系统及其制备及其中间体。

    Novel carboxylic acids, benzoyl phenyl alkanoic acids and use thereof
    37.
    发明授权
    Novel carboxylic acids, benzoyl phenyl alkanoic acids and use thereof 失效
    新型羧酸,苯甲酰基苯基链烷酸及其应用

    公开(公告)号:US4337353A

    公开(公告)日:1982-06-29

    申请号:US875323

    申请日:1978-02-06

    摘要: Novel carboxylic acids of the formula ##STR1## wherein Z is an aliphatic hydrocarbon chain selected from the group consisting of --(CH.sub.2).sub.n -- and --CH.dbd.CH--(CH.sub.2).sub.n-2 -- where the double bond may be at any point in the chain, n is an integer from 5 to 10 and X, X.sub.1, X.sub.2 and X.sub.3 are individually selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 5 carbon atoms, alkylthio of 1 to 5 carbon atoms, CF.sub.3 --, CF.sub.3 O-- and CF.sub.3 S-- and their non-toxic, pharmaceutically acceptable organic and inorganic salts and esters having analgesic and anti-inflammatory activity and their preparation.

    摘要翻译: 式(Ⅰ)的新型羧酸,其中Z是选自 - (CH 2)n - 和-CH = CH-(CH 2)n-2-的脂族烃链,其中双键可以是任何 n为5至10的整数,X,X 1,X 2和X 3分别选自氢,卤素,1至5个碳原子的烷基,1至5个碳原子的烷氧基,烷硫基 1至5个碳原子,CF 3 - ,CF 3 O-和CF 3 S-及其无毒的药学上可接受的有镇痛和抗炎活性的有机和无机盐和酯及其制备。

    Novel derivatives of 2-(4-quinolinylamino)-5-fluoro-benzoic acids
    38.
    发明授权
    Novel derivatives of 2-(4-quinolinylamino)-5-fluoro-benzoic acids 失效
    2-(4-喹啉基氨基)-5-氟 - 苯甲酸的新衍生物

    公开(公告)号:US4233305A

    公开(公告)日:1980-11-11

    申请号:US966964

    申请日:1978-12-06

    CPC分类号: C07D215/44

    摘要: Derivatives of 2-(4-quinolinylamino)-5-fluorobenzoic acid compounds of the formula ##STR1## wherein X is selected from the group consisting of chlorine and --CF.sub.3 in the 7- or 8-position and R is selected from the group consisting of hydrogen, an esterifying group, alkali metals, alkaline earth metals, ammonium and non-toxic, pharmaceutically acceptable organic amines and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable analgesic properties and their preparation.

    摘要翻译: 式(I)的2-(4-喹啉基氨基)-5-氟苯甲酸化合物的衍生物,其中X选自7-或8-位的氯和-CF 3,R选自 由氢,酯化基团,碱金属,碱土金属,铵和无毒的药学上可接受的有机胺及其无毒的药学上可接受的酸加成盐组成,具有显着的镇痛特性及其制备。

    Novel .DELTA..sup.4 -androstenes
    39.
    发明授权
    Novel .DELTA..sup.4 -androstenes 失效
    新型DELTA 4雄甾烯

    公开(公告)号:US4233297A

    公开(公告)日:1980-11-11

    申请号:US52489

    申请日:1979-06-27

    摘要: Novel .DELTA..sup.4 -androstenes of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, Y is selected from the group consisting of hydrogen, fluorine and methyl, R.sub.2 is selected from the group consisting of saturated and unsaturated alkyl of 1 to 12 carbon atoms, --CF.sub.3, aryl of 6 to 12 carbon atoms and aralkyl of 7 to 12 carbon atoms and the dotted lines in the A and B rings indicate the optional presence of one or two double bonds in the 1(2) and 6(7)-positions with the proviso that when R.sub.1 is methyl, R.sub.2 is saturated or unsaturated alkyl and the B ring is saturated, Y is methyl having anti-inflammatory activity and novel intermediates.

    摘要翻译: 式(Ⅰ)的新型DELTA 4-雄甾烯衍生物,其中R1为1〜3个碳原子的烷基,Y选自氢,氟和甲基,R2选自饱和和不饱和的烷基 1至12个碳原子,-CF 3,6至12个碳原子的芳基和7至12个碳原子的芳烷基和A和B环中的虚线表示在1(2)中任选存在一个或两个双键, 和6(7) - 位,条件是当R1是甲基时,R2是饱和或不饱和的烷基,B环是饱和的,Y是具有抗炎活性的甲基和新的中间体。