Decahydroquinolines and central analgesic method of use thereof
    11.
    发明授权
    Decahydroquinolines and central analgesic method of use thereof 失效
    十氢喹啉和中枢镇痛药的使用方法

    公开(公告)号:US4877796A

    公开(公告)日:1989-10-31

    申请号:US084456

    申请日:1987-08-12

    CPC分类号: C07D215/40

    摘要: A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms of a decahydroquinoline of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 5 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen and akyl of 1 to 5 carbon atoms, A is selected from the group consisting of --(CH.sub.2).sub.n --, --CH.sub.2 O-- and alkylene substituted with alkyl having a total of 2 to 8 carbon atoms, n is an integer from 0 to 5, Z is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthyl, optionally substituted indenyl, optionally substituted heteromonocycle of 5 to 6 members and optionally substituted heterobicycle with the proviso that when Z is o-alkoxy-phenyl, A is not --(CH.sub.2).sub.n -- in which n is O, and their non-toxic, pharmaceutically acceptable acid addition salts and their quaternary ammonium salts and intermediates having analgesic, diuretic, hypotensive, anti-arrithmic and anti-cerebral-ischaemic properties.

    摘要翻译: 选自下式的化合物:其中R 1为1至5个碳原子的烷基,R 2选自氢和1至5个碳原子的烷基的所有对映异构体和非对映异构体形式的十氢喹啉的化合物 原子,A选自 - (CH 2)n - , - CH 2 O-和被具有总共2至8个碳原子的烷基取代的亚烷基,n是0至5的整数,Z选自 由任选取代的苯基,任选取代的萘基,任选取代的茚基,任选取代的5至6个成员的异单环和任选取代的杂双环,条件是当Z是邻 - 烷氧基 - 苯基时,A不是 - (CH2)n-,其中 n是O,它们的无毒的药学上可接受的酸加成盐及其季铵盐和具有止痛,利尿,降压,抗对数和抗脑缺血性质的中间体。

    8-amino decahydroquinolines and medicinal use thereof
    16.
    发明授权
    8-amino decahydroquinolines and medicinal use thereof 失效
    8-氨基十氢喹啉及其医药用途

    公开(公告)号:US4963567A

    公开(公告)日:1990-10-16

    申请号:US371995

    申请日:1989-06-27

    CPC分类号: C07D215/40

    摘要: A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms of a decahydroquinoline of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 5 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, A is selected from the group consisting of --(CH.sub.2).sub.n --, --CH.sub.2 O-- and alkylene substituted with alkyl having a total of 2 to 8 carbon atoms, n is an integer from 0 to 5, Z is selected from the group consisting of optionally substituted phenyl, optionally substituted naphthyl, optionally substituted indenyl, optionally substituted heteromonocycle of 5 to 6 members and optionally substituted hetero-bicycle with the proviso that when Z is o-alkoxy-phenyl, A is not --(CH.sub.2).sub.n -- in which n is O, and their non-toxic, pharmaceutically acceptable acid addition salts and their quaternary ammonium salts and intermediates having analgesic, diuretic, hypotensive, anti-arrithmic and anti-cerebral-ischaemic properties.

    4-OH-quinoline carboxylic acid amides having analgesic and
anti-inflammatory activity

    公开(公告)号:US4845105A

    公开(公告)日:1989-07-04

    申请号:US30680

    申请日:1987-03-24

    摘要: A compound selected from the group consisting of optical isomers and racemates of 4-hydroxy-3-quinoline carboxylates 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, --SCF.sub.3 and --OCF.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 thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl and tetrazolyl, all optionally substituted with alkyl of 1 to 4 carbon atoms and phenyl and phenyl substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --NO.sub.2 and halogen, A is either ##STR2## in which R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.5 is selected from the group consisting of aryl of 6 to 14 carbon atoms, heteroaryl of 3 to 14 carbon atoms, alkyl of 1 to 14 carbon atoms, alkyl substituted with --NH.sub.2, --NHAlk or ##STR3## alkenyl of 2 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms substituted with aryl of 6 to 14 carbon atoms, Alk and Alk' are alkyl of 1 to 6 carbon atoms or, when R.sub.1 is hydrogen, A is ##STR4## and R.sub.3a are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, aryl and ##STR5## or R.sub.2a and R.sub.3a together form acetonide, R.sub.4a is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.5a is selected from the group consisting of alkyl of 1 to 4 carbon atoms and aryl with the proviso that when X is 8--CF.sub.3, R.sub.1 and R.sub.3 are hydrogen, R.sub.2 is 2-thiazolyl, R.sub.4 is methyl, R.sub.5 is not methyl and their non-toxic, pharmaceutically acceptable salts with acids or bases having analgesic and anti-inflammatory activity.

    Novel thiophene-acetic acids
    18.
    发明授权
    Novel thiophene-acetic acids 失效
    新型噻吩 - 乙酸

    公开(公告)号:US4159986A

    公开(公告)日:1979-07-03

    申请号:US610110

    申请日:1975-09-04

    CPC分类号: C07D333/24 C07D333/22

    摘要: Novel thiophene-acetic acid derivatives of the formulae ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.1 is selected from the group consisting of lower alkyl of 1 to 4 carbon atoms and hydrogen and R.sub.2 is selected from the group consisting of hydrogen, lower alkyl of 1 to 7 carbon atoms and optionally substituted with at least one hydroxy group or an oxygen atoms-containing heterocycle,di-lower alkylamino-lower alkyl, N-heterocyclic alkyl, alkali metals, alkaline earth metals, aluminum and --H,NH (lower alkyl).sub.2 and Ar is selected from the group consisting of phenyl, optionally substituted with at least one member of the group consisting of halogen, trihalogenomethyl, lower alkyl, lower alkoxy and carboxyl, cyclohexyl, thienyl, furyl, tetrahydrofuryl and pyridyl, and in formula II, ArCO is attached to one of the positions .alpha. to the sulfur atom, which compounds have analgesic and anti-inflammatory activity and their preparations.

    摘要翻译: 式(I)< IMAGE> II的新型噻吩 - 乙酸衍生物,其中R选自氢和1至4个碳原子的烷基,R 1选自1至 4个碳原子和氢,R2选自氢,1至7个碳原子的低级烷基,任选被至少一个羟基或含氧原子的杂环取代,二低级烷基氨基 - 低级烷基,N - 杂环烷基,碱金属,碱土金属,铝和-H,NH(低级烷基)2和Ar选自苯基,任选被至少一个由卤素,三卤甲基,低级 烷基,低级烷氧基和羧基,环己基,噻吩基,呋喃基,四氢呋喃基和吡啶基,并且在式II中,ArCO与硫原子的α位置连接,该化合物具有镇痛和抗炎活性, 准备工作

    2-Alkyl-5-thiazole-carboxylic acid derivatives in hypolipemiant
compositions
    19.
    发明授权
    2-Alkyl-5-thiazole-carboxylic acid derivatives in hypolipemiant compositions 失效
    2-烷基-5-噻唑 - 羧酸衍生物在脱脂组合物中的应用

    公开(公告)号:US4045567A

    公开(公告)日:1977-08-30

    申请号:US662122

    申请日:1976-02-27

    IPC分类号: A61K31/425

    CPC分类号: A61K31/425

    摘要: Hypolipemiant compositions comprising an effective amount of at least one 2-alkyl-5-thiazole-carboxylic acid derivative of the formula ##STR1## wherein R is hydrogen, an alkali metal, ammonium, the monovalent residue of an organic base or a substituted or unsubstituted alkyl and where R'.sub.1 is a linear alkyl of 1 to 12 carbon atoms, and a major amount of a pharmaceutical carrier; as well as the method of reducing the amount of sanguine lipids in warm-blooded animals utilizing the above-hypolipemiant compositions.

    摘要翻译: 包含有效量的至少一种下式的2-烷基-5-噻唑 - 羧酸衍生物,其中R是氢,碱金属,铵,有机碱的一价残基或取代或未取代的低分子量组合物 烷基,其中R'1是1至12个碳原子的直链烷基,和主要量的药物载体; 以及利用上述降血脂组合物减少温血动物中血糖量的方法。