Novel dibenzo(b,f)azepines as thymoanaleptics
    1.
    发明授权
    Novel dibenzo(b,f)azepines as thymoanaleptics 失效
    新的二苯并(b,f)吖庚因作为胸腺杀菌剂

    公开(公告)号:US3979515A

    公开(公告)日:1976-09-07

    申请号:US533846

    申请日:1974-12-18

    摘要: Novel 5-methyl-10-(.beta.-alkylaminoethyl)dibenzo(b,f) azepines of the formula ##SPC1##Wherein R is lower alkyl, R.sub.1 is selected from the group consisting of hydrogen and lower alkyl and X and X' are selected from the group consisting of hydrogen and halogen and their non-toxic, pharmaceutically acceptable acid addition salts having a superior thymoanaleptic activity and their preparation and use.

    摘要翻译: 式WHEREIN R的新型5-甲基-10-(β-烷基氨基乙基)二苯并(b,f)吖庚因是低级烷基,R 1选自氢和低级烷基,X和X'选自 由氢和卤素及其无毒的药学上可接受的酸加成盐组成,具有优异的胸腺杀伤活性及其制备和用途。

    Analgesic 4-hydroxy-3-quinolinecarboxamides
    2.
    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
    3.
    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
    4.
    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 benzoylphenylacetic acid esters
    5.
    发明授权
    Novel benzoylphenylacetic acid esters 失效
    新型苯甲酰苯乙酸酯

    公开(公告)号:US4192890A

    公开(公告)日:1980-03-11

    申请号:US15786

    申请日:1979-02-28

    摘要: Racemates [and optically active isomers of benzoylphenylacetic acid esters of the formula ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 7 carbon atoms, and the two benzene rings may be optionally substituted with at least one member of the group consisting of chlorine, fluorine, bromine, trifluoromethyl and alkyl and alkoxy and alkylthio of 1 to 7 carbon atoms], intermediates and process for their preparation and their use as analgesics and antiinflammatory agents.

    摘要翻译: 外消旋体[和具有式I的苯甲酰基苯基乙酸酯的旋光异构体,其中R选自氢和1至7个碳原子的烷基,并且两个苯环可以任选地被至少一个成员 由氯,氟,溴,三氟甲基和烷基和烷氧基和1至7个碳原子的烷硫基组成的组],其制备的中间体及其制备方法及其作为止痛剂和抗炎剂的用途。

    Dibenzo (b,f) azepines
    7.
    发明授权
    Dibenzo (b,f) azepines 失效
    二苯并(b,f)吖庚因

    公开(公告)号:US3931151A

    公开(公告)日:1976-01-06

    申请号:US403108

    申请日:1973-10-03

    IPC分类号: C07D223/22 C07D223/26

    CPC分类号: C07D223/26

    摘要: Novel dibenzo (b,f) azepines of the formula ##SPC1##Wherein R is alkyl of 1 to 4 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, n is 0, 1 or 2 and AlK is alkyl of 1 to 2 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antidepressant and neurosedative activity.

    摘要翻译: 新的二苯并(b,f)吖庚因式为WHEREIN R为1至4个碳原子的烷基,R 1选自氢和1至4个碳原子的烷基,n为0,1或2,AlK为 具有1至2个碳原子的烷基及其无毒的药学上可接受的酸加成盐,其具有抗抑郁和神经活性。

    Benzoxazine-4-one intermediates
    9.
    发明授权
    Benzoxazine-4-one intermediates 失效
    苯并恶嗪-4-酮中间体

    公开(公告)号:US4518775A

    公开(公告)日:1985-05-21

    申请号:US495475

    申请日:1983-05-17

    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 ' and R.sub.2 ' 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'和R 2'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C 存在氢,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。