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45 条记录 (耗时 0.022 秒)

    Pyrido�3,4-e!-as-triazines
    11.
    发明授权
    Pyrido�3,4-e!-as-triazines 失效
    吡啶并[3,4-e] -as-三嗪

    公开(公告)号：US4424351A

    公开(公告)日：1984-01-03

    申请号：US123807

    申请日：1980-02-22

    申请人： Pal Benko ,  Gyo/ rgyi nee Lax Kovanyi ,  Judit nee Gergely Timar ,  Maria nee Lakatos Sigmond ,  Lujza Petocz ,  Peter Go/ ro/ g ,  Ibolya Kosoczky ,  Eniko nee Kiszelly Szirt ,  Hristone Toncsev

    发明人： Pal Benko ,  Gyo/ rgyi nee Lax Kovanyi ,  Judit nee Gergely Timar ,  Maria nee Lakatos Sigmond ,  Lujza Petocz ,  Peter Go/ ro/ g ,  Ibolya Kosoczky ,  Eniko nee Kiszelly Szirt ,  Hristone Toncsev

    IPC分类号： A61K31/53 ,  A61P25/04 ,  A61P29/00 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： Acylated pyrido �3,4-e!-as-triazines of the formula (I), ##STR1## wherein R.sub.1 stands for alkyl, alkoxy, haloalkyl, furyl, pyridyl, phenyl, phenyl-(C.sub.1-4 alkyl) or phyenyl-(C.sub.2-4 alkenyl) optionally substituted. R.sub.2 stands for hydrogen or a group of the formula R.sub.1 --CO--, R.sub.3 stands for hydrogen, a phenyl group or a naphthy6l group optionally substituted, or a phenyl-(C.sub.1-4 alkyl) group, pyridyl group or a C.sub.1-20 alkyl group, and R.sub.4 stands for hydrogen or a group of the formula R.sub.1 --CO--, and R.sub.5 forms together with R.sub.2 or R.sub.4 a valence bond, wherein R.sub.2 or R.sub.4 taking part in forming said valence bond may not have the above meaning, and pharmaceutically acceptable acid addition salts thereof, which are prepared by reacting a pyrido �3,4-e!-as-triazine of the formula (II) or an acid addition salt thereof ##STR2## R.sub.6 stands for hydrogen, and R.sub.5 forms together with R.sub. and R.sub.4 a valence bond, with an acylating agent of the formula (III). R.sub.1 --CO--X (III) The compounds exert favourable effects on the central nervous system, and can be applied primarily as analgesic and antiphlogistic agents.

    摘要翻译： 式（I）的酰化吡啶并[3,4-e] -as-三嗪，其中R1代表烷基，烷氧基，卤代烷基，呋喃基，吡啶基，苯基，苯基 - （C1-4烷基）或 （烯基）（C 2-4烯基）任意取代。 R2代表氢或式R1-CO-的基团，R3代表氢，苯基或任选取代的萘基，或苯基 - （C 1-4烷基）基，吡啶基或C 1-20烷基， R4代表氢或式R1-CO-基团，R5与R2或R4一起形成价键，其中参与形成所述价键的R2或R4可能不具有上述含义，并且其药学上可接受的酸 通过使式（II）的吡啶并[3,4-e]-α-三嗪或其酸加成盐反应制备的加成盐，其中R6代表氢，R5与 兰德R4是价键，具有式（III）的酰化剂。 R1-CO-X（III）该化合物对中枢神经系统具有有利的作用，可主要用作镇痛药和消炎药。

    Condensed as-triazine derivatives and method of using the same
    12.
    发明授权
    Condensed as-triazine derivatives and method of using the same 失效
    缩合三嗪衍生物及其使用方法

    公开(公告)号：US4419355A

    公开(公告)日：1983-12-06

    申请号：US283971

    申请日：1981-07-16

    申请人： Ibolya Kosoczky ,  Eva Toncsev, nee Ravasz ,  Pal Benko ,  Laszlo Pallos ,  Lujza Petocz ,  Sandor Batori ,  Gyorgy Hajos ,  Andras Messmer ,  Katalin Grasser

    发明人： Ibolya Kosoczky ,  Eva Toncsev, nee Ravasz ,  Pal Benko ,  Laszlo Pallos ,  Lujza Petocz ,  Sandor Batori ,  Gyorgy Hajos ,  Andras Messmer ,  Katalin Grasser

    IPC分类号： C07D471/04 ,  A61K31/53 ,  A61P25/24 ,  A61P25/26 ,  C07D253/10 ,  C07D487/04 ,  C07D253/08

    CPC分类号： C07D487/04

    摘要： The invention relates to new condensed as-triazine derivatives of the general formula (I) ##STR1## wherein Z represents a buta-1,3-dienyl group or a group of the formula (a), (b), (c) or (d) ##STR2## R.sub.1 denotes a C.sub.1-10 alkyl group, an oxo group or a C.sub.6-10 aryl or C.sub.6-10 aryl-(C.sub.1-3 alkyl) group optionally substituted by one or more identical or different substituents selected from the group consisting of amino, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy and halogen,R.sub.2 stands for hydrogen, C.sub.1-10 alkyl or amino,R.sub.3 represents hydrogen, C.sub.1-10 alkyl or C.sub.6-10 aryl or C.sub.6-10 aryl-(C.sub.1-3 alkyl) optionally substituted by one or more identical or different substituents selected from the group consisting of nitro, amino, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy and halogen,X.sup.- denotes an anion, andn is 0 or 1,with the proviso that if n is O, R.sub.1 is other than an oxo group and R.sub.1 ' and R.sub.2 ' form together a double bond, and with the further provisos that if n is 1, R.sub.1 represents an oxo group and the symbols R.sub.1 ' and R.sub.2 ' are not present, and if Z is a buta-1,3-dienyl group and R.sub.1 denotes an oxo group, R.sub.3 is other than unsubstituted phenyl.The new compounds of the general formula (I) can be prepared by cyclizing the compounds of the general formula (II) or (V), wherein R.sub.1, Z, R.sub.3 and X.sup.- have the above defined meanings, R.sub.4 is a leaving group and R.sub.7 represents hydrogen or C.sub.1-10 alkyl.The new compounds of the general formula (I) possess a valuable antidepressant effect and can advantageously be used in the therapy.

    摘要翻译： 本发明涉及通式（I）的新的缩合的三嗪衍生物，其中Z代表丁-1,3-二烯基或式（a），（b），（ c）或（d）R1表示任选被一个或多个相同的C 1-6烷基，氧代基或C 6-10芳基或C 6-10芳基 - （C 1-3烷基） 或选自氨基，硝基，C 1-6烷基，C 1-6烷氧基，羟基和卤素的不同取代基，R 2代表氢，C 1-10烷基或氨基，R 3表示氢，C 1-10烷基或C 6- 芳基或任选被一个或多个相同或不同的选自硝基，氨基，C 1-6烷基，C 1-6烷氧基，羟基和卤素的取代基取代的芳基或C 6-10芳基 - （C 1-3烷基） 表示阴离子，n为0或1，条件是如果n为O，则R1不是氧代基，R1'和R2'一起形成双键，另外条件是，如果n为1， R1代表氧代基团， mbols R1'和R2'不存在，并且如果Z是丁-1,3-二烯基并且R 1表示氧代基，则R 3不是未取代的苯基。 通式（I）的新化合物可以通过使通式（II）或（V）的化合物环化来制备，其中R1，Z，R3和X具有上述定义，R4是离去基团， R 7表示氢或C 1-10烷基。 通式（I）的新化合物具有有价值的抗抑郁作用，可有利地用于治疗。

    Dibenzo[d,g][1,3,6]dioxazocine derivatives
    14.
    发明授权
    Dibenzo[d,g][1,3,6]dioxazocine derivatives 失效
    二苯并[d，g] [1,3,6]二氧杂吖庚因衍生物

    公开(公告)号：US4229350A

    公开(公告)日：1980-10-21

    申请号：US61042

    申请日：1979-07-26

    申请人： Laszlo Rozsa ,  Lujza Petocz ,  Katalin Grasser ,  Ibolya Kosoczky ,  Eniko Kiszelly ,  Jozsef Nagy

    发明人： Laszlo Rozsa ,  Lujza Petocz ,  Katalin Grasser ,  Ibolya Kosoczky ,  Eniko Kiszelly ,  Jozsef Nagy

    IPC分类号： A61K31/553 ,  C07D273/00 ,  C07D273/01 ,  C07D413/06

    CPC分类号： C07D273/00 ,  Y10S514/818

    摘要： This invention relates to novel dibenzo[d,g][1,3,6]dioxazocine derivatives represented by the general formula I ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, cyano or trifluoromethyl,Y stands for hydrogen or a group of formula ##STR2## wherein A stands for a straight or branched chained alkylene having from 2 to 5 carbon atoms andR.sub.3 and R.sub.4 independently stand for an alkyl having from 1 to 4 carbon atoms, orR.sub.3 and R.sub.4 together with the nitrogen atom they are attached to and optionally together with a further nitrogen atom or with an additional oxygen atom may form a five- or six-membered heterocyclic ring optionally substituted with an alkyl having from 1 to 4 carbon atoms,and pharmaceutically acceptable acid addition salts thereof formed with an inorganic or organic acid.A process for the preparation of these compounds is also within the scope of this invention.The above compounds possess valuable pharmaceutical properties, for instance they are effective local anaesthetics and can be used for treating Parkinson syndrome.

    摘要翻译： 本发明涉及由通式I（I）表示的新的二苯并[d，g] [1,3,6]二氧杂吖庚因衍生物，其中R 1和R 2独立地表示氢，卤素，氰基或三氟甲基，Y代表氢 或一组式（I）其中A代表具有2至5个碳原子的直链或支链链状亚烷基，R3和R4独立代表具有1至4个碳原子的烷基，或R3和R4与氮原子一起 它们与另外的氮原子或与另外的氧原子连接并且可选地与另外的氧原子连接的原子可以形成任选被具有1至4个碳原子的烷基取代的五元或六元杂环，及其药学上可接受的酸加成盐 由无机或有机酸形成。 制备这些化合物的方法也在本发明的范围内。 上述化合物具有有价值的药物性质，例如它们是有效的局部麻醉剂，并且可用于治疗帕金森综合征。

    Nortropine-carbazate derivatives
    15.
    发明授权
    Nortropine-carbazate derivatives 失效
    阿托品 - 卡巴肼衍生物

    公开(公告)号：US4127576A

    公开(公告)日：1978-11-28

    申请号：US855705

    申请日：1977-11-29

    申请人： Gyula Mikite ,  Lujza Petocz ,  Ibolya Kosoczky ,  Katalin Grasser

    发明人： Gyula Mikite ,  Lujza Petocz ,  Ibolya Kosoczky ,  Katalin Grasser

    IPC分类号： C07D209/82 ,  A61K31/437 ,  A61K31/46 ,  A61P23/00 ,  A61P23/02 ,  A61P25/02 ,  C07D451/06 ,  C07D451/12 ,  C07D471/08

    CPC分类号： C07D451/06

    摘要： The invention relates to novel nortropine-carbazate derivatives of the general formula (I), ##STR1## wherein R.sub.1 is C.sub.1-4 alkyl, phenyl or halophenyl group,R.sub.2 is hydrogen or a C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl, C.sub.1-4 acyl, phenoxycarbonyl or C.sub.1-4 alkoxycarbonyl group, andR.sub.3 is hydrogen of a C.sub.1-4 alkyl or C.sub.1-4 acyl group, orR.sub.2 and R.sub.3 may form together a C.sub.1-10 alkylene group attachedTo the nitrogen atom with a double bond, as well as to pharmaceutically acceptable acid addition salts of said compounds.The above compounds are new and can be applied as narcosis potentiating agents.The compounds of the general formula (I) can be prepared by reacting a compound of the general formula (II), ##STR2## wherein R.sub.1 is as defined above and Q is halogen, C.sub.1-4 alkoxy or phenoxy, with a hydrazine compound of the general formula (III), ##STR3## wherein R.sub.2 and R.sub.3 are as defined above. According to another method a compound of the general formula (II), wherein R.sub.1 and Q are as defined above, is reacted with hydrazine or hydrazine hydrate, and the resulting compound of the general formula (I), wherein R.sub.2 and R.sub.3 are hydrogens and R.sub.1 is as defined above, is converted into the corresponding N-substituted derivatives by methods known in the art.

    摘要翻译： 本发明涉及通式（I），其中R 1为C 1-4烷基，苯基或卤代苯基，R 2为氢或C 1-4烷基，羟基-C 1〜C 1-4烷基的通式（I）的新戊酸carb嗪衍生物， C4烷基，C1-4酰基，苯氧基羰基或C1-4烷氧基羰基，R3是C1-4烷基或C1-4酰基的氢，或R2和R3可以一起形成连接到氮的C1-10亚烷基 具有双重粘合剂的ATOM，也适用于化学物质的接受酸的添加剂。

    Indazole-3-carboxylic acid hydrazides and a process for the preparation thereof
    16.
    发明授权
    Indazole-3-carboxylic acid hydrazides and a process for the preparation thereof 失效
    吲唑-3-羧酸酰肼及其制备方法

    公开(公告)号：US3956312A

    公开(公告)日：1976-05-11

    申请号：US497676

    申请日：1974-08-15

    申请人： Laszlo Magdanyi ,  Lujza Petocz ,  Eniko Kiszelly ,  Ibolya Kosoczky ,  Attila Varga

    发明人： Laszlo Magdanyi ,  Lujza Petocz ,  Eniko Kiszelly ,  Ibolya Kosoczky ,  Attila Varga

    IPC分类号： C07D231/54 ,  A61K31/13 ,  A61K31/395 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/445 ,  A61P1/04 ,  A61P25/24 ,  A61P25/26 ,  C07D231/56 ,  C07D401/12 ,  C07D405/12

    CPC分类号： C07D231/56 ,  A61K31/415

    摘要： New compounds of the general formula (I) ##SPC1##and salts thereof were prepared by reacting a compound of the general formula (II) ##SPC2##with a compound of the general formula (III) or (IV) ##EQU1## and optionally saturating the --C=N-- bond. In the above formulaeR.sup.1 and R.sup.2 are always the same and represent a C.sub.1-4 alkyl group,R.sup.3 stands for hydrogen,R.sup.4 and R.sup.5 each represent hydrogen or a straight-chained or branched C.sub.1-16 alkyl group optionally having an unsubstituted or substituted phenyl, furyl or naphthyl substituent, wherein said substituted aryl groups may contain up to 3 alkyl, C.sub.1-3 alkoxy, benzyloxy, nitro, amino, lower alkylamino, di-lower alkylamino, methylenedioxy, alkylmercapto, alkylsulfonyl or halogen substituents, orR.sup.4 and R.sup.5 may form together with the adjacent carbon atom a C.sub.3-12 cycloalkyl or C.sub.3-12 cycloalkylidene group, one of the methylene ring members of which being optionally replaced by an imino, lower alkylimino, or phenyl-lower alkylimino group, andR.sup.6 and R.sup.7 may stand for hydrogen, or R.sup.6 and R.sup.7 may form together a valence bond, andThe R.sup.8 groups may each represent hydrogen, lower alkyl or alkanoyl, or the two R.sup.8 groups may form together a lower alkylene or alkanoylene group.The compounds of the general formula (I) possess primarily gastric acid secretion inhibiting and central nervous activities, furthermore they exert favourable action on the development of certain microorganisms which can be utilized in therapy.

    摘要翻译： 通式（I）的新化合物及其盐通过使通式（II）的化合物与通式（III）或（IV）的化合物反应，R 5 = C（R）R 8 R 5 R 5 （IV）R8OR4并且任选地饱和-C = N-键。

    Pharmaceutical compositions with antianginal activity
    18.
    发明授权
    Pharmaceutical compositions with antianginal activity 失效
    具有抗心绞痛活性的药物组合物

    公开(公告)号：US4621101A

    公开(公告)日：1986-11-04

    申请号：US751623

    申请日：1985-07-02

    申请人： Zoltan Budai ,  Tibor Mezei ,  Aranka Lay nee Konya ,  Lujza Petocz ,  Katalin Grasser ,  Zsuzsanna Orr

    发明人： Zoltan Budai ,  Tibor Mezei ,  Aranka Lay nee Konya ,  Lujza Petocz ,  Katalin Grasser ,  Zsuzsanna Orr

    IPC分类号： A61K31/15 ,  A61P43/00 ,  C07C251/38

    CPC分类号： C07C251/58 ,  C07C2101/14 ,  C07C2101/18

    摘要： The invention relates to pharmaceutical compositions possessing valuable antianginal activity. These compositions show higher activity and more favorable therapeutic indices than the reference compound Prenylamine. Preparation of different kinds of pharmaceutical compositions, such as tablets, dragees, capsules and injectable solutions, containing compounds of general formula (I) ##STR1## or their acid addition salts as active ingredients, is disclosed, wherein in formula (I)R is phenyl or 4-chlorophenyl;R.sup.1 and R.sup.2 each represent hydrogen, methyl or isopropyl;R.sup.3 and R.sup.4 are hydrogen, or together form a chemical bond;n is an integer from 4 to 6;A means trimethylene, if n is 4 or 6; or ethylene, if n is 5.

    摘要翻译： 本发明涉及具有有价值的抗心绞痛活性的药物组合物。 这些组合物显示比参考化合物Prenylamine更高的活性和更有利的治疗指数。 公开了含有通式（I）化合物或其酸加成盐作为活性成分的不同种类的药物组合物如片剂，硫化物，胶囊和可注射溶液的制备，其中在式（I）中R是 苯基或4-氯苯基; R1和R2各自表示氢，甲基或异丙基; R3和R4是氢，或一起形成化学键; n为4-6的整数; 如果n为4或6，则表示三亚甲基; 或乙烯，如果n为5。