知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

25 条记录 (耗时 0.013 秒)

    Process for preparing substituted urea derivatives
    3.
    发明授权
    Process for preparing substituted urea derivatives 失效
    制备取代脲衍生物的方法

    公开(公告)号：US4435567A

    公开(公告)日：1984-03-06

    申请号：US334470

    申请日：1981-12-28

    申请人： Gyorgy Lugosi ,  Antal Simay ,  Janos Bodnar ,  Laszlo Simandi ,  Eva Somfai

    发明人： Gyorgy Lugosi ,  Antal Simay ,  Janos Bodnar ,  Laszlo Simandi ,  Eva Somfai

    IPC分类号： C07D295/20 ,  C07C67/00 ,  C07C239/00 ,  C07C273/18 ,  C07C275/02 ,  C07C275/06 ,  C07C275/26 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07D213/75 ,  C07D217/06 ,  C07D235/32 ,  C07D275/06 ,  C07D277/82 ,  C07D285/12 ,  C07D285/135 ,  C07D295/215 ,  C07C127/00 ,  C07C127/15 ,  C07C127/17 ,  C07C127/19

    CPC分类号： C07D213/75 ,  C07C273/1809 ,  C07D217/06 ,  C07D235/32 ,  C07D277/82 ,  C07D285/135 ,  C07D295/215

    摘要： A process for the preparation of substituted urea derivatives, and compositions and concentrates for the same purpose are disclosed. According to the process the substituted urea derivatives of formula (I) ##STR1## wherein R is hydrogen, alkyl, aryl, cycloalkyl or aralkyl, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkinyl, alkoxy, oxyalkyl, cycloalkyl, aralkyl, alkoxycarbonylalkyl, aryl or heteroaryl, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom may form a saturated or unsaturated heterocycle, or a condensed and/or substituted ring system, and said heterocycle or said condensed and/or substituted ring system may contain also a sulfo group,can be manufactured by reacting an amine of formula (II) ##STR2## with an N-carbamoyl-benzoic acid sulfimide derivative of formula (III) ##STR3## The disclosed N-acylating composition comprises of from 3 to 60% by weight, preferably of from 5 to 50% by weight sulfimide derivative of formula (III), of from 97 to 40% by weight, preferably of from 95 to 50% by weight solvent, and if desired, an organic or inorganic base.The disclosed N-acylating concentrate comprises of from 60 to 95.5% by weight N-acylating agent of formula (III) and of from 4.5 to 40% by weight additives.

    摘要翻译： 公开了用于制备取代的脲衍生物的方法，以及用于相同目的的组合物和浓缩物。 根据该方法，式（I）的取代脲衍生物其中R是氢，烷基，芳基，环烷基或芳烷基，R1和R2是氢，烷基，烯基，炔基，烷氧基，烷氧基，环烷基，芳烷基，烷氧基羰基 ，芳基或杂芳基，或R 1和R 2与相邻的氮原子一起可以形成饱和或不饱和的杂环或稠合和/或取代的环系，并且所述杂环或所述缩合和/或取代的环系可以含有磺基 可以通过使式（II）的胺与式（III）的N-氨基甲酰基 - 苯甲酸硫酰亚胺衍生物反应来制备。所公开的N-酰化组合物包含3至60重量％ ，优选为5至50重量％的式（III）的亚磺酰亚胺衍生物，为97至40重量％，优选为95至50重量％的溶剂，如果需要，为有机或无机碱。 所公开的N-酰化浓缩物包含60至95.5重量％的式（III）的N-酰化剂和4.5至40重量％的添加剂。

    Psychostimulant agent
    7.
    发明授权
    Psychostimulant agent 失效
    精神刺激剂

    公开(公告)号：US5220068A

    公开(公告)日：1993-06-15

    申请号：US649239

    申请日：1991-01-29

    申请人： Jozsef Knoll ,  Antal Simay ,  Eva Szinnyei ,  Eva Somfai ,  Zoltan Torok ,  Karoly Mozsolits ,  Janos Bergmann

    发明人： Jozsef Knoll ,  Antal Simay ,  Eva Szinnyei ,  Eva Somfai ,  Zoltan Torok ,  Karoly Mozsolits ,  Janos Bergmann

    IPC分类号： A61K31/135

    CPC分类号： A61K31/135

    摘要： The present invention relates to a pharmaceutical composition comprising as active ingredient a compound of the Formula I ##STR1## wherein R.sup.1 stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; phenyl alkyl having 7 to 10 carbon atoms; phenyl; or cycloalkyl comprising 3 to 8 carbon atoms;R.sup.2 stands for straight or branched chain alkyl comprising 1 to 8 carbon atoms; alkyl comprising 1 to 8 carbon atoms substituted by halogen, hydroxy, alkoxy having 1 to 4 carbon atoms or by one or two phenyl groups; phenyl; or cycloalkyl having 3 to 8 carbon atoms,with the proviso that groups R.sup.1 and R.sup.2 together contain at least three carbon atoms. The invention also relates to a process for the preparation of compounds of the Formula I by methods known per se. The compounds of the Formula I are phychostimulants having a new spectrum of effect which can be used in therapy for increasing psychical activity (learning and retention) and for treating clinical patterns of depression and deficiencies of learning and retention like in Alzheimer's disease, and are void of side effects (e.g. due to catecholamine release) of known stimulants.

    摘要翻译： 本发明涉及包含作为活性成分的式I化合物（I）的药物组合物，其中R1代表包含1至8个碳原子的直链或支链烷基; 具有7至10个碳原子的苯基烷基; 苯基; 或包含3至8个碳原子的环烷基; R2代表包含1至8个碳原子的直链或支链烷基; 被卤素，羟基，具有1至4个碳原子的烷氧基或一个或两个苯基取代的碳原子数为1〜8的烷基; 苯基; 或具有3至8个碳原子的环烷基，条件是基团R 1和R 2一起含有至少3个碳原子。 本发明还涉及通过本身已知的方法制备式I化合物的方法。 式I的化合物是具有新的效应谱的phychostimulants，其可用于增加心理活动（学习和保留）的治疗和用于治疗抑郁症的临床模式和学习和保留的缺陷，如阿尔茨海默病，并且是无效的 的已知兴奋剂的副作用（例如由于儿茶酚胺释放）。

    Sulfur-containing isoquinoline derivatives in pharmaceutical compositions and methods of use
    8.
    发明授权
    Sulfur-containing isoquinoline derivatives in pharmaceutical compositions and methods of use 失效
    含硫异喹啉衍生物在药物组合物和使用方法中的应用

    公开(公告)号：US4425349A

    公开(公告)日：1984-01-10

    申请号：US381775

    申请日：1982-05-25

    申请人： Kalman Takacs ,  Maria H. Papp ,  Gabor Kovacs ,  Ilona K. Ajzert ,  Antal Simay ,  Peter Literati Nagy ,  Marian E. Puskas ,  Gyula Sebestyen ,  Istvan Stadler ,  Zoltan Sumeghy

    发明人： Kalman Takacs ,  Maria H. Papp ,  Gabor Kovacs ,  Ilona K. Ajzert ,  Antal Simay ,  Peter Literati Nagy ,  Marian E. Puskas ,  Gyula Sebestyen ,  Istvan Stadler ,  Zoltan Sumeghy

    IPC分类号： C07D217/14 ,  C07D513/04 ,  A61K31/47

    CPC分类号： C07D513/04 ,  C07D217/14 ,  Y10S514/826 ,  Y10S514/869

    摘要： The invention concerns new sulfur-containing isoquinoline derivatives. More particularly, the invention relates to isoquinoline derivatives of the general formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbamoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.2 is a straight or branched chained alkylene group having 1 to 6 carbon atoms, andthe dotted line stands for a further carbon-carbon bond or hydrogen atoms in the 3- and 4-positions of the ring,and salts and cyclic amides thereof.The new compounds possess valuable pharmaceutical activities, more particularly, are potent diuretic, antiasthmatic, hypotensive and antiinflammatory agents. Thus another aspect of the invention is a pharmaceutical composition which comprises as active ingredient a pharmaceutically effective amount of at least one compound of the general formula (I) with at least one pharmaceutically inert carrier or diluent. The invention also relates to a process for preparing these compounds.

    摘要翻译： 本发明涉及新的含硫异喹啉衍生物。 更具体地说，本发明涉及通式（I）的异喹啉衍生物，其中R独立地表示氢，羟基或具有1至4个碳原子的烷氧基，R 1是氢，具有1至4个碳原子的烷基和 任选地被苯基取代，任选被一个或多个卤素或烷氧基取代的苯基，氰基或氨基甲酰基，R 2是任选被一个或多个卤素，烷氧基或羧基取代的苯基或通式A的基团，其中R 3是 氢，具有1至4个碳原子的直链或支链烷基或苯基，m和n独立地表示0,1或2，条件是m + n至少为1，R4为氢，苯基，羟基，酰氧基， 羧基，具有1至6个碳原子的烷氧基羰基，在烷基部分含有1至6个碳原子的氨基甲酰基，咔唑基或二烷基氨基，或者是具有1至6个碳原子的直链或支链的亚烷基，虚线代表 进一步c 环的3-和4-位的碳 - 碳键或氢原子，及其盐和环状酰胺。 新化合物具有有价值的药物活性，特别是有效的利尿，止喘，降压和抗炎药。 因此，本发明的另一方面是药物组合物，其包含作为活性成分的药学有效量的至少一种通式（I）的化合物与至少一种药学上惰性的载体或稀释剂。 本发明还涉及制备这些化合物的方法。