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    Dithienylalkylamines and process for their production
    1.
    发明授权
    Dithienylalkylamines and process for their production 失效
    二噻烷基烷基胺及其生产方法

    公开(公告)号：US4281010A

    公开(公告)日：1981-07-28

    申请号：US56840

    申请日：1979-07-12

    申请人： Axel Kleemann ,  Ingomar Nubert ,  Fritz Stroman ,  Klaus Thiemer

    发明人： Axel Kleemann ,  Ingomar Nubert ,  Fritz Stroman ,  Klaus Thiemer

    IPC分类号： C07D333/24 ,  A61K31/38 ,  A61K31/381 ,  A61P9/08 ,  C07D333/16 ,  C07D333/20 ,  C07D409/06

    CPC分类号： C07D333/20 ,  C07D333/16

    摘要： There are prepared compounds of the formula ##STR1## where >A--B-- has either the structure >C(OH)--CH.sub.2 -- or the structure >C.dbd.CH, Alk is a straight or branched chain C.sub.1 --C.sub.5 --alkylene group and Y is ##STR2## where R is hydrogen or a C.sub.1 --C.sub.4 --alkyl group and T is hydrogen or a C.sub.2 --C.sub.6 --alkanoyl group ##STR3## where R' is hydrogen, phenyl, phenyl substituted once or twice. The compounds are effective in improving peripheral and cerebral circulation. There are also produced intermediate compounds of formula (II) where NHY is replaced by chlorine, bromine or iodine.

    摘要翻译： 制备式（Ⅰ）化合物，其中AB-具有> C（OH）-CH 2 - 或结构> C = CH的结构，Alk是直链或支链C 1 -C 5亚烷基 并且Y是，其中R是氢或C 1 -C 4烷基，T是氢或C 2 -C 6烷酰基，其中R'是氢，苯基，苯基取代一次或两次。 该化合物有效改善周围和脑部循环。 还制备式（II）的中间体化合物，其中NHY被氯，溴或碘代替。

    Dithienyl beta-haloethyl carbinols
    2.
    发明授权
    Dithienyl beta-haloethyl carbinols 失效
    二噻吩基β-卤乙基甲醇

    公开(公告)号：US4254269A

    公开(公告)日：1981-03-03

    申请号：US56838

    申请日：1979-07-12

    申请人： Axel Kleemann ,  Ingomar Nubert ,  Fritz Stroman ,  Klaus Thiemer

    发明人： Axel Kleemann ,  Ingomar Nubert ,  Fritz Stroman ,  Klaus Thiemer

    IPC分类号： C07D333/24 ,  A61K31/38 ,  A61K31/381 ,  A61P9/08 ,  C07D333/16 ,  C07D333/20 ,  C07D333/12

    CPC分类号： C07D333/20 ,  C07D333/16

    摘要： There are prepared compounds of the formula ##STR1## where >A--B-- has either the structure >C(OH)--CH.sub.2 -- or the structure >C.dbd.CH, Alk is a straight or branched chain C.sub.1 -C.sub.5 -alkylene group and Y is a C.sub.3 -C.sub.7 -cycloalkyl group, a benzyl group, a methylenedioxybenzyl group, a benzyl group having one, two or three C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy group substituents, a C.sub.1 -C.sub.6 -alkyl group, or a C.sub.1 -C.sub.6 -alkyl group substituted by an amino group, a di C.sub.1 -C.sub.4 -alkylamino group, a mono C.sub.1 -C.sub.4 -alkyl-amino group, a morpholino group, a piperazino group or a 4-(C.sub.1 -C.sub.4 -alkyl)-piperazino group, or Y is ##STR2## where R is hydrogen or a C.sub.1 -C.sub.4 -alkyl group and T is hydrogen or a C.sub.2 -C.sub.6 -alkanoyl group or where --NHY is ##STR3## where R' is hydrogen, phenyl, phenyl substituted once or twice by C.sub.1 -C.sub.4 -alkyl groups, a C.sub.1 -C.sub.4 -alkoxy group or by halogen atoms, a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.4 -hydroxyalkyl group or a phenalkyl group whose alkyl portion consists of 1-4 carbon atoms or such a phenalkyl group containing 1 to 3 C.sub.1 -C.sub.4 -alkoxy group substituents or when Alk has 2 to 5 carbon atoms the group --NHY is a di-C.sub.1 -C.sub.4 -alkylamino group or the group --NH--CH(R)--CH(OH)--C.sub.6 H.sub.5 and salts thereof. The compounds are effective in improving peripheral and cerebral circulation. There are also produced intermediate compounds of formula (II) where NHY is replaced by chlorine, bromine or iodine.

    摘要翻译： 制备式（Ⅰ）化合物，其中AB-具有> C（OH）-CH 2 - 或结构> C = CH的结构，Alk是直链或支链C 1 -C 5亚烷基 Y为C 3 -C 7 - 环烷基，苄基，亚甲二氧基苄基，具有一个，两个或三个C 1 -C 4 - 烷基或C 1 -C 4 - 烷氧基取代基的苄基，C 1 -C 6烷基， 或被氨基取代的C1-C6-烷基，二C1-C4-烷基氨基，单C1-C4-烷基 - 氨基，吗啉代基，哌嗪基或4-（C1-C4- 烷基） - 哌嗪基，或Y是其中R是氢或C 1 -C 4 - 烷基，T是氢或C 2 -C 6烷酰基或其中R'是氢的-NHY是“ 苯基，被C 1 -C 4 - 烷基取代一次或两次的苯基，C 1 -C 4 - 烷氧基或卤素原子，C 1 -C 6 - 烷基，C 1 -C 4 - 羟基烷基或烷基部分由 1-4个碳原子的烷基或含1-3个C 1 -C 4 - 烷氧基的苯烷基 基团取代基，或当Alk具有2至5个碳原子时，基团-NHY是二-C 1 - C 4 - 烷基氨基或基团-NH-CH（R）-CH（OH）-C 6 H 5及其盐。 该化合物有效改善周围和脑部循环。 还制备式（II）的中间体化合物，其中NHY被氯，溴或碘代替。

    Dithienylpiperidines, pharmaceutical compositions thereof, and method of use thereof
    5.
    发明授权
    Dithienylpiperidines, pharmaceutical compositions thereof, and method of use thereof 失效
    二噻吩基哌啶，其药物组合物及其使用方法

    公开(公告)号：US4283405A

    公开(公告)日：1981-08-11

    申请号：US112099

    申请日：1980-01-14

    申请人： Jurgen Engel ,  Axel Kleemann ,  Fritz Stroman ,  Klaus Thiemer

    发明人： Jurgen Engel ,  Axel Kleemann ,  Fritz Stroman ,  Klaus Thiemer

    IPC分类号： C07D409/14 ,  A61K20060101 ,  A61K31/38 ,  A61K31/4433 ,  A61K31/445 ,  A61P7/06 ,  A61P9/02 ,  A61P25/04 ,  C07D20060101

    CPC分类号： A61K31/38 ,  A61K31/4433 ,  A61K31/445 ,  C07D409/14

    摘要： There are prepared compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or together represent a second bond between the carbon atom carrying R.sub.1 and R.sub.2, R.sub.1 also can be a hydroxy group, R.sub.3 is hydrogen, a C.sub.3 -C.sub.8 cycloalkyl group or a C.sub.1 -C.sub.20 alkyl group, which optionally can also contain one or two hydroxy groups and the groups R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and are hydrogen, C.sub.1 -C.sub.6 -alkyl groups or halogen atoms, their N-oxide, their quaternary salts and their acid addition salts. There are also described processes for their production. The compounds possess especially an antischemic and blood pressure increasing activity.

    摘要翻译： 制备式Ⅰ的化合物，其中R1和R2是氢或一起代表携带R1和R2的碳原子之间的第二个键，R1也可以是羟基，R3是氢，C3-C8环烷基 或C 1 -C 20烷基，其任选地还可以含有一个或两个羟基，并且基团R 4，R 5，R 6和R 7相同或不同，并且是氢，C 1 -C 6 - 烷基或卤素原子， 氧化物，它们的季盐和它们的酸加成盐。 还描述了其生产方法。 这些化合物特别具有抗缺血和增压活性。

    Process for the production of [1,1-dithienyl-(3)-1-hydroxypropyl-(3)]-[1-phenyl-1-hydroxypropyl-(2)]-a mine and [1,1-dithienyl-(3)-propen-(1)-yl-(3)]-[1-phenylpropyl-(2)]-amine
    7.
    发明授权
    Process for the production of [1,1-dithienyl-(3)-1-hydroxypropyl-(3)]-[1-phenyl-1-hydroxypropyl-(2)]-a mine and [1,1-dithienyl-(3)-propen-(1)-yl-(3)]-[1-phenylpropyl-(2)]-amine 失效
    制备[1,1-二噻吩基 - （3）-1-羟基丙基 - （3）] - [1-苯基-1-羟丙基 - （2）] - 胺和[1,1-二噻吩基 - （3 ） - 丙烯 - （1） - 基 - （3）] - [1-苯基丙基 - （2）] - 胺

    公开(公告)号：US4175088A

    公开(公告)日：1979-11-20

    申请号：US867294

    申请日：1978-01-05

    申请人： Axel Kleemann ,  Reinhold Kiel ,  Ingomar Nubert

    发明人： Axel Kleemann ,  Reinhold Kiel ,  Ingomar Nubert

    IPC分类号： C07D333/14 ,  A61K31/382 ,  C07D333/16 ,  C07D333/20

    CPC分类号： C07D333/16 ,  C07D333/20

    摘要： [1,1-dithien-(3)-yl-1-hydroxy-(3)-propyl]-[1-phenyl-1-hydroxy-(2)-propyl]-amine is prepared by condensing thien-(3)-yl lithium with a .beta.-halogen propionic acid alkyl ester of the formula ##STR1## where R is a lower alkyl group and Hal is chlorine, bromine or iodine, in an inert medium at a temperature below -50.degree. C. to form a compound of the formula ##STR2## which is then reacted with 2-amino-1-hydroxy-1-phenylpropane in an inert medium in the presence of a basic compound. The product cn be converted to [1,1-dithien-(3)-yl-(1)-propen-(3)-yl]-[1-phenyl-(2)-propyl]-amine by dehydration.

    摘要翻译： 通过将噻吩（3） - （3） - （1） - 羟基 - （3） - 丙基] - [1-苯基-1-羟基 - （2） ） - 基锂与式（II）的β-卤代丙酸烷基酯反应，其中R是低级烷基，Hal是氯，溴或碘，在惰性介质中，温度低于-50℃ 形成式（III）的化合物，然后在碱性化合物的存在下，在惰性介质中与2-氨基-1-羟基-1-苯基丙烷反应。 通过脱水将产物转化为[1,1-二噻吩 - （3） - 基 - （1） - 丙烯 - （3） - 基] - [1-苯基 - （2） - 丙基] - 胺。

    1-[3-(3,4,5-Trimethoxyphenoxy)-2-hydroxy-propyl]-4- aryl-piperazine-derivatives having pharmaceutical activity
    8.
    发明授权
    1-[3-(3,4,5-Trimethoxyphenoxy)-2-hydroxy-propyl]-4- aryl-piperazine-derivatives having pharmaceutical activity 失效
    具有药物活性的1- [3-（3,4,5-三甲氧基苯氧基）-2-羟基 - 丙基] -4-芳基 - 哌嗪衍生物

    公开(公告)号：US4335126A

    公开(公告)日：1982-06-15

    申请号：US193482

    申请日：1980-10-03

    申请人： Axel Kleemann ,  Vladimir Jakovlev ,  Klaus Thiemer ,  Jurgen Engel

    发明人： Axel Kleemann ,  Vladimir Jakovlev ,  Klaus Thiemer ,  Jurgen Engel

    IPC分类号： C07D295/092 ,  A61K31/495 ,  C07D295/08

    CPC分类号： C07D295/088

    摘要： There are prepared compounds corresponding to the general formula ##STR1## in which R.sup.1 is a hydrogen atom, a C.sub.2 to C.sub.6 -alkanoyl group, a C.sub.3 to C.sub.6 -alkenoyl group, a C.sub.3 to C.sub.6 -cycloalkyl carbonyl group, a benzoyl group, an alkoxybenzoyl group, a nicotinoyl group, a thienyl carbonyl group, a furyl carbonyl group, a phenylacetyl group or a C.sub.1 to C.sub.4 -alkoxyphenyl acetyl group and R.sup.2 represents a phenyl, naphthyl or pyridyl group or such group substituted by the groups R.sup.3 and R.sup.4, the groups R.sup.3 and R.sup.4, which may be the same or different, each representing hydrogen, hydroxyl, fluorine, chlorine, bromine, a nitro group, a trifluoromethyl group, a C.sub.1 to C.sub.6 -alkyl group, a C.sub.1 to C.sub.6 -alkoxy group, a C.sub.1 to C.sub.6 -alkyl thio group, a C.sub.1 to C.sub.6 -alkyl sulphonyl group, a C.sub.2 to C.sub.6 -alkanoyl group, an amino group, an acylamino group or an acyloxy group in which the acyl is of the type defined in respect to R.sup.1, and their salts. The compounds are pharmacodynamically active.

    摘要翻译： 制备相应于通式Ⅰ的化合物，其中R 1为氢原子，C 2至C 6烷酰基，C 3至C 6链烯酰基，C 3至C 6环烷基羰基，苯甲酰基， 烷氧基苯甲酰基，烟酰基，噻吩基羰基，呋喃基羰基，苯乙酰基或C1〜C4烷氧基苯基乙酰基，R2表示苯基，萘基或吡啶基，或被基团R3和R4取代的基团 ，可以相同或不同的各自表示氢，羟基，氟，氯，溴，硝基，三氟甲基，C1至C6烷基，C1至C6-烷氧基的基团R3和R4 ，C 1至C 6烷基硫基，C 1至C 6烷基磺酰基，C 2至C 6烷酰基，氨基，酰氨基或酰氧基，其中酰基是关于 R1及其盐。 该化合物具有药效学活性。

    N-Alkoxy-dithienylpiperidines, pharmaceutical compositions thereof and methods of use thereof
    9.
    发明授权
    N-Alkoxy-dithienylpiperidines, pharmaceutical compositions thereof and methods of use thereof 失效
    N-烷氧基 - 二噻吩基哌啶，其药物组合物及其使用方法

    公开(公告)号：US4263308A

    公开(公告)日：1981-04-21

    申请号：US112100

    申请日：1980-01-14

    申请人： Jurgen Engel ,  Axel Kleemann ,  Ute-Achterrath Tuckermann ,  Klaus Thiemer

    发明人： Jurgen Engel ,  Axel Kleemann ,  Ute-Achterrath Tuckermann ,  Klaus Thiemer

    IPC分类号： C07D409/14 ,  A61K31/4433 ,  A61K31/445 ,  C07D333/00 ,  C07D417/14

    CPC分类号： C07D333/00

    摘要： There are prepared compounds of the formula ##STR1## where R.sub.1 is hydrogen or hydroxy, R.sub.2 is hydrogen or R.sub.1 and R.sub.2 together represent a second bond between the carbon atoms carrying R.sub.1 and R.sub.2, Alk is a C.sub.2 -C.sub.6 alkylene group, R.sub.3 is a C.sub.3 -C.sub.8 -cycloalkyl group, a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.6 -hydroxyalkyl group or a C.sub.2 -C.sub.6 -hydroxyalkoxy-C.sub.1 -C.sub.6 -alkyl group and the groups R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and are hydrogen, C.sub.1 -C.sub.6 -alkyl group or halogen atoms, their N-oxides, their quaternary salts and their acid addition salts. There are also described processes for their production. The compounds have a strong bronchospasmolytic activity, antianaphylactic activity and an antihistamine-antiserotonine activity.

    摘要翻译： 制备式为“IMAGE”的化合物，其中R 1为氢或羟基，R 2为氢或R 1和R 2一起代表携带R1和R2的碳原子之间的第二个键，Alk为C2-C6亚烷基，R3为 C 3 -C 8 - 环烷基，C 1 -C 6烷基，C 1 -C 6羟基烷基或C 2 -C 6羟基烷氧基-C 1 -C 6 - 烷基，R 4，R 5，R 6和R 7基团相同或 不同的是氢，C 1 -C 6烷基或卤原子，它们的N-氧化物，它们的季盐和它们的酸加成盐。 还描述了其生产方法。 该化合物具有强的支气管痉挛分解活性，抗过敏活性和抗组织胺 - 抗血清素活性。