Heterocyclic compounds
    1.
    发明授权
    Heterocyclic compounds 失效
    杂环化合物

    公开(公告)号:US4220646A

    公开(公告)日:1980-09-02

    申请号:US790801

    申请日:1977-04-25

    摘要: Heterocyclic compounds of the formula: ##STR1## wherein the pyrroline ring and the symbols R.sub.1 and R.sub.2 together form an isoindoline, 6,7-dihydro-5H-pyrrolo-[3,4-b]pyrazine, 2,3,6,7-tetrahydro-5H-1,4-oxathiino-[2,3-c]pyrrole or 2,3,6,7-tetrahydro-5H-1,4-dithiino-[2,3-c]pyrrole nucleus, Het represents an optionally substituted pyrid-2-yl, quinol-2-yl or 1,8-naphthyridin-2-yl radical, Z represents oxygen or sulphur and R represents hydrogen, alkyl or halo-substituted alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, optionally substituted phenyl, phenylalkyl, the phenyl ring of which may optionally be substituted, phenylalkenyl, the phenyl ring of which may optionally be substituted, or R represents a 5- or 6-membered heterocyclic radical containing one or two hetero-atoms selected from nitrogen, oxygen and sulphur, and, when the pyrroline ring and the symbols R.sub.1 and R.sub.2 together form an isoindoline nucleus, the residue of the isoindoline nucleus represented by R.sub.1 and R.sub.2 may optionally be substituted, possess pharmacological properties, and are especially useful as tranquillizers, anti-convulsant agents, decontracturants and agents to produce hypnosis.

    摘要翻译: 其中吡咯啉环和符号R1和R2一起形成异二氢吲哚,6,7-二氢-5H-吡咯并 - [3,4-b]吡嗪,2,3,6,7 - 四氢-5H-1,4-氧硫杂环丁烷并[2,3-c]吡咯或2,3,6,7-四氢-5H-1,4-二硫基 - [2,3-c]吡咯核,Het代表 任选取代的吡啶-2-基,喹啉-2-基或1,8-萘啶-2-基,Z表示氧或硫,R表示氢,烷基或卤素取代的烷基,烯基,炔基,环烷基,烷氧基 ,任选取代的苯基,苯基烷基,其苯基环可任选被取代,苯基烯基,其苯基环可任选被取代,或R表示含有一个或两个选自以下的杂原子的5-或6-元杂环基: 氮,氧和硫,并且当吡咯啉环和符号R1和R2一起形成异二氢吲哚核时,由R1和R2表示的异二氢吲哚核的残基可以任选地被取代 具有药理性质,特别适用于镇静剂,抗惊厥剂,脱保护剂和催眠剂。

    Naphtyridine derivatives
    2.
    发明授权
    Naphtyridine derivatives 失效
    萘啶衍生物

    公开(公告)号:US4131674A

    公开(公告)日:1978-12-26

    申请号:US843369

    申请日:1977-10-19

    CPC分类号: C07D471/04

    摘要: Heterocyclic compounds of the formula: ##STR1## wherein the pyrroline ring and the symbols X.sub.1 and X.sub.2 together form an unsubstituted or substituted isoindoline nucleus, or a 6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine or 2,3,6,7-tetrahydro-5H-1,4-oxathiino[2,3-c]pyrrole nucleus, the 1,8-naphthyridin-2-yl nucleus is unsubstituted or substituted, and the grouping --NR.sub.1 R.sub.2 is an amino or substituted amino group, are new compounds which are active as tranquillizers, hypnotics, anti-convulsant agents and anti-spasmodics.

    摘要翻译: 其中吡咯啉环和符号X1和X2一起形成未取代或取代的异吲哚啉核的6,7-二氢-5H-吡咯并[3,4-b]吡嗪6, 7-二氢-5H-吡咯并[3,4-b]吡啶或2,3,6,7-四氢-5H-1,4-氧硫杂环丁烷并[2,3-c]吡咯核,1,8-萘啶 - 2-基核是未取代或取代的,并且-NR1R2基团是氨基或取代的氨基,是作为镇静剂,催眠药,抗惊厥剂和抗痉挛剂起作用的新化合物。

    Naphthyridine derivatives
    5.
    发明授权
    Naphthyridine derivatives 失效
    萘啶衍生物

    公开(公告)号:US4016274A

    公开(公告)日:1977-04-05

    申请号:US623359

    申请日:1975-10-17

    IPC分类号: C07D519/00 C07D401/14

    CPC分类号: C07D519/00

    摘要: Compounds of the formula: ##STR1## wherein one of the symbols =X-- represents =N-- and the other three each represent a group ##STR2## in which Y represents hydrogen, halogen, alkyl, alkoxy, cyano or nitro, at least two of the symbols representing hydrogen, Z represents hydrogen, halogen, alkyl, alkoxy, trifluoromethyl or nitro, and (i) n represents zero and R represents hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl or phenyl, or (ii) n represents 1 and R represents alkyl, hydroxyalkyl or phenyl, are new compounds possessing pharmacological properties; they are particularly active as tranquilizers and anti-convulsant agents.

    摘要翻译: 其中符号之一= X表示= N-,其余三个表示其中Y表示氢,卤素,烷基,烷氧基,氰基或硝基的基团,至少两个 表示氢的符号,Z表示氢,卤素,烷基,烷氧基,三氟甲基或硝基,(i)n表示0,R表示氢,烷基,烯基,炔基,羟烷基或苯基,或(ii)n表示1和 R代表烷基,羟基烷基或苯基,是具有药理学性质的新化合物; 它们作为镇静剂和抗惊厥药物是特别活跃的。

    Isoindolin-1-one derivatives
    7.
    发明授权
    Isoindolin-1-one derivatives 失效
    ISOINDOLIN-1-ONE衍生物

    公开(公告)号:US3987174A

    公开(公告)日:1976-10-19

    申请号:US527031

    申请日:1974-11-25

    CPC分类号: C07D209/48

    摘要: Isoindolin-1-one derivatives substituted on the nitrogen atom in the 2-position by an unsubstituted or substituted phenyl radical or a heterocyclic radical having aromatic characteristics, substituted in the 3-position by a 3-amino(or substituted amino)-2-hydroxy-propoxy group, and optionally substituted in the 5-and/or 6-positions by one or two alkoxy radicals or optionally substituted in the 5- and 6-positions by a methylenedioxy radical, possess pharmacodynamic properties, and are especially useful as anti-arrhythmic agents.

    1,2-Dithiole derivatives
    8.
    发明授权
    1,2-Dithiole derivatives 失效
    1,2-二硫杂衍生物

    公开(公告)号:US4138487A

    公开(公告)日:1979-02-06

    申请号:US855385

    申请日:1977-11-28

    摘要: 1,2-Dithiole derivatives of the formula: ##STR1## wherein Het represents an aromatic heterocyclic radical with six atoms in the ring two of which are nitrogen atoms, the heterocyclic radical optionally carrying a single substituent selected from halogen, alkyl, alkoxy, mercapto, alkylthio, dialkylamino, pyrrolidin-1-yl, piperidino, morpholino and 4-alkylpiperazin-1-yl, and R represents halogen, alkyl (optionally substituted by alkoxycarbonyl), carboxy, alkoxycarbonyl, carbamoyl, N-alkylcarbamoyl or a group R.sub.1 --CH(OH)-- in which R.sub.1 represents hydrogen or alkyl, the said alkyl, alkoxy and alkylthio radicals or alkyl or alkoxy moieties containing 1 to 4 carbon atoms except in the case of R.sub.1 which contains 1 to 3 carbon atoms when an alkyl radical, are new compounds useful in the treatment of bilharziasis.

    摘要翻译: 其中Het表示在其中两个为氮原子的六个原子的芳香族杂环基,杂环基任选地带有选自卤素,烷基,烷氧基,巯基的单个取代基的1,2-二硫杂衍生物 ,烷硫基,二烷基氨基,吡咯烷-1-基,哌啶子基,吗啉代和4-烷基哌嗪-1-基,R表示卤素,烷基(任选被烷氧基羰基取代),羧基,烷氧基羰基,氨基甲酰基,N-烷基氨基甲酰基或基团R1- CH(OH) - 其中R1代表氢或烷基,所述烷基,烷氧基和烷硫基或含有1-4个碳原子的烷基或烷氧基部分,除了当烷基含有1至3个碳原子的情况下, 是可用于治疗胆红病的新化合物。