Process for preparing pyrrolo(1,2-A)azepinone derivatives
    1.
    发明授权
    Process for preparing pyrrolo(1,2-A)azepinone derivatives 失效
    制备吡咯(1,2-A)氮杂酮衍生物的方法

    公开(公告)号:US4826974A

    公开(公告)日:1989-05-02

    申请号:US116725

    申请日:1987-11-04

    CPC分类号: C07D487/04

    摘要: Pyrrolo[1,2-a]azepinone derivatives of formula: ##STR1## in which R.sub.3 is H or halogen and either (A) R is benzyl or phenylthio in which the phenyls are optionally substituted by one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl optionally substituted by dialkylamino in which the alkyls are optionally joined to form a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl ring substituted by alkyl, or alternatively R.sub.1 and R.sub.2 form a heterocyclic ring chosen from pyrrolidine, piperidine, morpholine and piperazine, substituted by alkyl, alkenyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, or (B) R is phenyl optionally substituted with one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals and R.sub.1 and R.sub.2 together form a piperazine or homopiperazine ring substituted by hydroxyalkyl (2 to 4 C), alkenyl (2 to 4 C), alkynyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CN, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, the said alkyls containing, except where otherwise stated, 1 to 4 C in a straight or branched chain, and the pharmaceutically acceptable salts thereof, are useful as antipsychotics.

    摘要翻译: 吡咯并[1,2-a]吖庚因酮衍生物,其中R 3为H或卤素,(A)R为苄基或苯硫基,其中苯基任选被一个或多个卤素或羟基取代 ,烷基,烷氧基或烷硫基,R 1和R 2可以相同或不同,表示任选被二烷基氨基取代的烷基,其中烷基任选地连接以形成被烷基取代的1-吡咯烷基,哌啶子基,吗啉代或1-哌嗪基环 或者R1和R2形成选自吡咯烷,哌啶,吗啉和哌嗪的杂环,被烷基,烯基(2至4 C),任选被卤素,烷基,烷氧基,烷硫基,CF 3,COOH取代的苄基或苯乙基取代, 羧基烷基,烷氧基羰基,烷氧基羰基烷基,羟基烷基或烷基羰氧基烷基,其中烷基羰基具有2至18个C,或(B)R是任选被一个或多个卤素或羟基,烷基,烷氧基或烷硫基取代的苯基, 和R2一起形成被羟烷基(2〜4 C),烯基(2〜4 C),炔基(2〜4 C),任选被卤素,烷基,烷氧基,烷硫基,CN取代的苄基或苯乙基取代的哌嗪或高哌嗪环 ,CF 3,COOH,羧基烷基,烷氧基羰基,烷氧基羰基烷基,羟基烷基或其中烷基羰基具有2〜18个碳原子的烷基羰氧基烷基,所述烷基除了另外说明的含有1〜4个C的直链或支链, 其盐可用作抗精神病药。

    Novel 1,3-disubstituted pyrrolo[1,2-a]azepinone derivatives having
anti-psychotic activity and pharmaceutical compositions containing them
    4.
    发明授权
    Novel 1,3-disubstituted pyrrolo[1,2-a]azepinone derivatives having anti-psychotic activity and pharmaceutical compositions containing them 失效
    具有抗精神病活性的新型1,3-二取代吡咯并[1,2-a]吖庚因衍生物和含有它们的药物组合物

    公开(公告)号:US4769366A

    公开(公告)日:1988-09-06

    申请号:US839101

    申请日:1986-03-13

    CPC分类号: C07D487/04

    摘要: Pyrrolo[1,2-a]azepinone derivatives of formula: ##STR1## in which R.sub.3 is H or halogen and either (A) R is benzyl or phenylthio in which the phenyls are optionally substituted by one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl optionally substituted by dialkylamino in which the alkyls are optionally joined to form a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl ring substituted by alkyl, or alternatively R.sub.1 and R.sub.2 form a heterocyclic ring chosen from pyrrolidine, piperidine, morpholine and piperazine, substituted by alkyl, alkenyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C,or (B) R is phenyl optionally substituted with one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals and R.sub.1 and R.sub.2 together form a piperazine or homopiperazine ring substituted by hydroxyalkyl (2 to 4 C), alkenyl (2 to 4 C), alkynyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CN, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, the said alkyls containing, except where otherwise stated, 1 to 4 C in a straight or branched chain,and the pharmaceutically acceptable salts thereof,are useful as antipsychotics.

    摘要翻译: 吡咯并[1,2-a]吖庚因酮衍生物,其中R 3为H或卤素,(A)R为苄基或苯硫基,其中苯基任选被一个或多个卤素或羟基取代 ,烷基,烷氧基或烷硫基,R 1和R 2可以相同或不同,表示任选被二烷基氨基取代的烷基,其中烷基任选地连接以形成被烷基取代的1-吡咯烷基,哌啶子基,吗啉代或1-哌嗪基环 或者R1和R2形成选自吡咯烷,哌啶,吗啉和哌嗪的杂环,被烷基,烯基(2至4 C),任选被卤素,烷基,烷氧基,烷硫基,CF 3,COOH取代的苄基或苯乙基取代, 羧基烷基,烷氧基羰基,烷氧基羰基烷基,羟基烷基或烷基羰氧基烷基,其中烷基羰基具有2至18个C,或(B)R是任选被一个或多个卤素或羟基,烷基,烷氧基或烷硫基取代的苯基, 和R2一起形成被羟烷基(2〜4 C),烯基(2〜4 C),炔基(2〜4 C),任选被卤素,烷基,烷氧基,烷硫基,CN取代的苄基或苯乙基取代的哌嗪或高哌嗪环 ,CF 3,COOH,羧基烷基,烷氧基羰基,烷氧基羰基烷基,羟基烷基或其中烷基羰基具有2至18个C的烷基羰氧基烷基,所述烷基除了另外说明的含有1至4个C的直链或支链以外, 其盐可用作抗精神病药。

    Antibiotic 27,706 RP and salt thereof
    7.
    发明授权
    Antibiotic 27,706 RP and salt thereof 失效
    抗生素27,706 RP及其盐

    公开(公告)号:US3970641A

    公开(公告)日:1976-07-20

    申请号:US219065

    申请日:1972-01-19

    IPC分类号: C07H15/252 C07H15/00

    CPC分类号: C07H15/252

    摘要: Antibiotics 20,798 RP and 27,706 RP of the general formula: ##SPC1##(wherein R represents a hydrogen atom or a hydroxy group) or acid addition salts thereof are prepared by reduction of a corresponding compound wherein the --CHOH--CH.sub.2 --R group is replaced by ##EQU1## The antibiotics of general formula I have valuable anti-tumour properties; that wherein R is hydroxy (27,706 RP) is new.

    摘要翻译: 抗生素20,798 RP和27,706 RP通式:

    Thiazolothienopyridines and anti-viral compositions thereof
    9.
    发明授权
    Thiazolothienopyridines and anti-viral compositions thereof 失效
    噻唑并噻吩并及其抗病毒组合物

    公开(公告)号:US4261999A

    公开(公告)日:1981-04-14

    申请号:US100523

    申请日:1979-12-05

    CPC分类号: C07D495/04 C07D513/14

    摘要: Thienopyridine derivatives of the formula: ##STR1## wherein the symbol A represents pyrid-3-yl, isoquinol-5-yl, or a 3-alkylisoquinol-5-yl group in which the alkyl radical is of 1 through 10 carbon atoms, and one of the symbols X and Y represents a single bond and the other represents the vinylene radical, are new compounds possessing useful pharmacological properties. They are particularly useful as anti-viral agents and, in certain cases, as analgesics, anti-inflammatory agents and anti-pyretics.

    摘要翻译: 下式的噻吩并吡啶衍生物:其中符号A表示吡啶-3-基,异喹啉-5-基或其中烷基为1至10个碳原子的3-烷基异喹啉-5-基,以及 符号X和Y之一表示单键,另一个表示亚乙烯基,是具有有用药理特性的新化合物。 它们特别可用作抗病毒剂,并且在某些情况下,作为止痛剂,抗炎剂和抗热解剂是特别有用的。