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    3-(1-Pyrazolyl)-pyridazine derivatives
    2.
    发明授权
    3-(1-Pyrazolyl)-pyridazine derivatives 失效
    3-（1-吡唑基） - 哒嗪衍生物

    公开(公告)号：US4251658A

    公开(公告)日：1981-02-17

    申请号：US914084

    申请日：1978-06-09

    申请人： Geza Szilagyi ,  Endre Kasztreiner ,  Laszlo Tardos ,  Edit Kosa ,  Laszlo Jaszlits ,  Gyorgy Cseh ,  Andras Divald ,  Pal Tolnay ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

    发明人： Geza Szilagyi ,  Endre Kasztreiner ,  Laszlo Tardos ,  Edit Kosa ,  Laszlo Jaszlits ,  Gyorgy Cseh ,  Andras Divald ,  Pal Tolnay ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

    IPC分类号： C07D401/14 ,  A61K31/50 ,  A61K31/501 ,  A61P9/12 ,  A61P43/00 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14

    CPC分类号： C07D403/04

    摘要： 3-(1-Pyrazolyl)-pyridazine derivatives of the formula I, or pharmaceutically acceptable acid addition salts thereof, which decrease high blood pressure and inhibit catabolism or prostaglandins, ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl,R.sup.2 is hydrogen, cyano, carboxyl, carbamoyl, carbaxoyl or C.sub.1-4 alkoxycarbonyl,R.sup.3 is hydrogen or chlorine or --NR.sup.4 NHR.sup.5 or NR.sup.6 R.sup.7, wherein R.sup.4 and R.sup.5 are each hydrogen or C.sub.1-4 alkyl, wherein R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-5 alkyl, C.sub.1-5 hydroxyalkyl, C.sub.3-7 cycloalkyl, phenyl or benzyl, or benzyl or phenylethyl substituted with one or two chlorine atoms or methoxy groups, or a furylmethyl, pyridylmethyl, pyrrolidine or piperazine ring, or when R.sup.7 is hydrogen, R.sup.6 is --(CH.sub.2).sub.n --NR.sup.4 R.sup.5 wherein n is an integer from 1 to 3.

    摘要翻译： 降低高血压并抑制分解代谢或前列腺素的式I的3-（1-吡唑基） - 哒嗪衍生物或其药学上可接受的酸加成盐，其中R 1是氢或C 1-4烷基， R2是氢，氰基，羧基，氨基甲酰基，碳酰基或C1-4烷氧基羰基，R3是氢或氯或-NR4NHR5或NR6R7，其中R4和R5分别是氢或C1-4烷基，其中R6和R7各自是氢或C1 或烷基，C 1-5羟基烷基，C 3-7环烷基，苯基或苄基，或被一个或两个氯原子或甲氧基取代的苄基或苯乙基，或呋喃基甲基，吡啶基甲基，吡咯烷或哌嗪环，或者当R7为氢时， R 6为 - （CH 2）n -NR 4 R 5，其中n为1至3的整数。

    3-(1-Pyrazolyl)-pyridazine derivatives and hypotensive compositions thereof
    4.
    发明授权
    3-(1-Pyrazolyl)-pyridazine derivatives and hypotensive compositions thereof 失效
    3-（1-吡唑基） - 哒嗪衍生物及其低血压组合物

    公开(公告)号：US4224325A

    公开(公告)日：1980-09-23

    申请号：US923623

    申请日：1978-07-11

    申请人： Geza Szilagyi ,  Endre Kasztreiner ,  Laszlo Tardos ,  Edit Kosa ,  Laszlo Jaszlits ,  Gyorgy Cseh ,  Ilona Kovacs, nee Szabo ,  Pal Tolnay ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

    发明人： Geza Szilagyi ,  Endre Kasztreiner ,  Laszlo Tardos ,  Edit Kosa ,  Laszlo Jaszlits ,  Gyorgy Cseh ,  Ilona Kovacs, nee Szabo ,  Pal Tolnay ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

    IPC分类号： C07D403/04 ,  A61K31/50 ,  A61K31/501 ,  A61P9/12 ,  A61P43/00 ,  C07D403/14 ,  C07D521/00 ,  A61K31/535 ,  C07D413/14

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The invention relates to compounds of general formula ##STR1## wherein R.sup.1 stands for a hydrogen atom or a C.sub.1-6 alkyl-, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl or a phenyl group,R.sup.2 stands for a hydrogen, fluorine, chlorine or bromine atom or a C.sub.1-6 alkyl, a C.sub.2-4 hydroxyalkyl, a nitro or an --NR.sup.5 R.sup.6 group, wherein R.sup.5 and R.sup.6 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-4 alkyl or a C.sub.2-4 hydroxyalkyl group,R.sup.3 stands for a hydrogen atom or a C.sub.1-6 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl or a phenyl group, a chlorine atom or a hydroxyl, amino or methoxy group,R.sup.4 stands for a carbamoyl, a cyano or an --NR.sup.7 --NHR.sup.8 group, wherein R.sup.7 and R.sup.8 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-4 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.1-4 alkoxycarbonyl or an --NR.sup.9 R.sup.10 group, wherein R.sup.9 and R.sup.10 may have the same or different meaning and stand each for a hydrogen atom or a C.sub.1-5 alkyl, a C.sub.2-4 hydroxyalkyl, a C.sub.3-6 cycloalkyl, a phenyl or a benzyl group, or --NR.sup.9 R.sup.10 may represent a morpholine, piperidine or piperazine ring,and their pharmaceutically acceptable acid-addition salts. Furthermore, the invention relates to a process for preparing these compounds.The novel compounds of general formula I have valuable pharmacological properties. Thus they show a considerable hypotensive effect and are capable to inhibit enzymes regulating the catabolism of prostaglandins.

    摘要翻译： 本发明涉及通式为“IMAGE”的化合物，其中R1代表氢原子或C1-6烷基，C2-4羟基烷基，C3-6环烷基或苯基，R2代表氢，氟， 氯或溴原子或C 1-6烷基，C 2-4羟基烷基，硝基或-NR 5 R 6基团，其中R 5和R 6可以具有相同或不同的含义，并且各自代表氢原子或C 1-4烷基或 C2-4羟基烷基，R3代表氢原子或C1-6烷基，C2-4羟烷基，C3-6环烷基或苯基，氯原子或羟基，氨基或甲氧基，R4代表 对于氨基甲酰基，氰基或-NR 7 -NHR 8基团，其中R 7和R 8可以具有相同或不同的含义，各自代表氢原子或C 1-4烷基，C 2-4羟烷基，C 1-4烷氧基羰基 或-NR 9 R 10基团，其中R 9和R 10可以具有相同或不同的含义，并且各自表示氢原子或C 1-5烷基，C 2-4的羟基烷基，C 3-6环烷基，苯基或苯基 或-NR9R10可以表示吗啉，哌啶或哌嗪环及其药学上可接受的酸加成盐。 此外，本发明涉及一种制备这些化合物的方法。 通式Ⅰ的新化合物具有有价值的药理学性质。 因此，它们显示出相当的降血压作用，并且能够抑制调节前列腺素分解代谢的酶。

    Acylated 2-aminothiazole derivatives
    8.
    发明授权
    Acylated 2-aminothiazole derivatives 失效
    酰化2-氨基噻唑衍生物

    公开(公告)号：US3963735A

    公开(公告)日：1976-06-15

    申请号：US518732

    申请日：1974-10-29

    申请人： Lajos Farkas ,  Endre Kasztreiner ,  Ferenc Andrasi ,  Jozsef Borsi ,  Istvan Elekes ,  Istvan Polgari

    发明人： Lajos Farkas ,  Endre Kasztreiner ,  Ferenc Andrasi ,  Jozsef Borsi ,  Istvan Elekes ,  Istvan Polgari

    IPC分类号： C07D277/20 ,  C07D277/46 ,  C07D295/14 ,  C07D417/04 ,  C07D417/14 ,  C07D213/56

    CPC分类号： C07D417/04 ,  C07D277/46 ,  C07D417/14 ,  Y10S514/927

    摘要： New acylated 2-aminothiazole derivatives of the general formula (I), ##SPC1##whereinR.sup.1 stands for phenyl group or a pyridyl group,R.sup.2 stands for hydrogen or lower alkyl,R.sup.3 stands for hydrogen, a lower alkyl group or benzyl group, andR.sup.4 and R.sup.5 each represent hydrogen, a C.sub.1-8 alkyl group, allyl group, a hydroxyalkyl group, a C.sub.3-6 cycloalkyl group, .beta.-dimethylaminoethyl group, .beta.-diethylaminoethyl group, benzyl group, 2-furylmethyl group, or a phenyl group having optionally a halogen, methyl, methoxy or trifluoromethyl substituent, orR.sup.4 and R.sup.5 may form, together with the adjacent nitrogen atom, a 5 to 8 membered polymethyleneimino group, morpholino group, piperazino group, N-methylpiperazino group or N-phenylpiperazino group, the compounds of formula I are anticholinergics.

    摘要翻译： 新的通式（I）的酰化2-氨基噻唑衍生物，其中R1代表苯基或吡啶基，R2代表氢或低级烷基，R3代表氢，低级烷基或苄基，R4和R5 各自表示氢，C1-8烷基，烯丙基，羟基烷基，C3-6环烷基，β-二甲基氨基乙基，β-二乙基氨基乙基，苄基，2-呋喃基甲基或任选具有 卤素，甲基，甲氧基或三氟甲基取代基，或者R4和R5可以与相邻的氮原子一起形成5至8元多亚甲基亚氨基，吗啉代基，哌嗪基，N-甲基哌嗪基或N-苯基哌嗪基， 配方I是抗胆碱能药。

    Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives
    10.
    发明授权
    Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives 失效
    厌氧性4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑烷酮衍生物

    公开(公告)号：US4308278A

    公开(公告)日：1981-12-29

    申请号：US90450

    申请日：1979-11-01

    申请人： Geza Schneider ,  Ferenc Andrasi ,  Pal Berzsenyi ,  Arpad Lazar ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

    发明人： Geza Schneider ,  Ferenc Andrasi ,  Pal Berzsenyi ,  Arpad Lazar ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

    IPC分类号： A61K31/415 ,  A61K31/4166 ,  A61P1/00 ,  A61P3/04 ,  C07C45/71 ,  C07D233/32 ,  C07D233/34 ,  C07D233/38 ,  C07D233/78

    CPC分类号： C07C255/00 ,  C07C45/71 ,  C07D233/32 ,  C07D233/38 ,  C07D233/78 ,  Y10S514/91

    摘要： 4-[(3,4-Dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives having the formula I ##STR1## wherein R.sup.1 stands for a cycloalkyl group containing from 3 to 6 carbon atoms or benzyl group;R.sup.2 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.3 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.4 stands for hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms or an alkoxycarbonyl group containing from 1 to 4 carbon atoms; andR.sup.5 stands for hydrogen atom or an alkoxycarbonyl group containing from 1 to 4 carbon atoms,are prepared by(a) reducing a hydantoin derivative having the general formula II, wherein R.sup.1 and R.sup.2 are as defined above, with lithium aluminum hydride in a neutral organic solvent, or(b) hydrogenating catalytically an 1,3-dihydro-2H-imidazol-2-one derivative having the general formula III, wherein R.sup.1 and R.sup.3 are as defined above, while the meaning of R.sup.4 is hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, or(c) reacting a carbamate derivative having the general formula IV, wherein R.sup.1 is as defined above, while R.sup.6 stands for an alkyl group containing from 1 to 4 carbon atoms, with an organic or inorganic base.The compounds having the formula I possess valuable therapeutical properties, mainly anorexigenic activity.

    摘要翻译： 4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑啉酮衍生物，其具有式I其中R1代表含有3至6个碳原子的环烷基或苄基; R2代表氢原子或含有1至4个碳原子的烷基; R3代表氢原子或含有1至4个碳原子的烷基; R4表示氢原子或含有1至4个碳原子的烷基或含有1至4个碳原子的烷氧基羰基; 并且R5代表氢原子或含有1至4个碳原子的烷氧基羰基，是通过以下步骤制备的：（a）将具有通式II的乙内酰脲衍生物（其中R 1和R 2如上定义）与中性的氢化铝锂 有机溶剂，或（b）催化氢化具有通式III的1,3-二氢-2H-咪唑-2-酮衍生物，其中R 1和R 3如上所定义，而R 4的含义是氢原子或烷基 含有1至4个碳原子的基团，或（c）使具有通式IV的氨基甲酸酯衍生物与其中R 1如上定义，而R6代表含有1至4个碳原子的烷基，与有机或无机 基础。 具有式I的化合物具有有价值的治疗性质，主要是厌食症活性。