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    Novel triazolo-pyrimidine derivatives
    13.
    发明授权
    Novel triazolo-pyrimidine derivatives 失效
    新型三唑衍生物衍生物

    公开(公告)号：US5064826A

    公开(公告)日：1991-11-12

    申请号：US487412

    申请日：1990-03-02

    申请人： Klara Reiter nee Esses ,  Jozsef Reiter ,  Zoltan Budai ,  Endre Rivo ,  Peter Trinka ,  Lujza Petocz ,  Gabor Gigler ,  Istvan Gyertyan ,  Istvan Gacsalyi

    发明人： Klara Reiter nee Esses ,  Jozsef Reiter ,  Zoltan Budai ,  Endre Rivo ,  Peter Trinka ,  Lujza Petocz ,  Gabor Gigler ,  Istvan Gyertyan ,  Istvan Gacsalyi

    IPC分类号： A61K31/505 ,  A61K31/519 ,  A61P25/04 ,  A61P25/24 ,  A61P25/26 ,  A61P29/00 ,  C07D249/14 ,  C07D495/14

    CPC分类号： C07D495/14

    摘要： This invention relates to novel triazolopyrimidine derivatives of formulae (Ia) and (Ib), ##STR1## wherein Q represents hydrogen, a heterocyclic group optionally substituted by a C.sub.1-4 alkyl group and containing one or more oxygen and/or nitrogen atoms or a group of formula--SR.sup.1 wherein R.sup.1 is alkyl or aralkyl, or a group of formula--NR.sup.2 R.sup.3 wherein R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl or a heterocyclic group,m and n are independently 0, 1, 2, 3 or 4, with the provision that if m stands for 0, then n is different from 0, and if both n and m are 1 or m stands for 0 and n is 2, the Q is different from methylthio or morpholino group, their mixtures or pharmaceutically acceptable salts. Furthermore, the invention relates to a process for preparing these compounds.The compounds of formulae (Ia) and (Ib) are able to inhibit the ptosis caused by tetrabenazine and they have analgetic activity.

    摘要翻译： 本发明涉及式（Ia）和（Ib）的新型三唑并嘧啶衍生物，其中Q表示氢，任选被C 1-4烷基取代并含有一个或多个氧和/ 或氮原子或式-SR1的基团，其中R 1是烷基或芳烷基，或式-NR 2 R 3基团，其中R 2和R 3独立地是氢，烷基，烯基，环烷基，芳烷基，芳基或杂环基，m和n是 独立地0,1,2,3或4，条件是如果m代表0，则n不同于0，并且如果n和m都是1或m代表0并且n是2，则Q不同 甲硫基或吗啉代基，它们的混合物或药学上可接受的盐。 此外，本发明涉及一种制备这些化合物的方法。 式（Ia）和（Ib）的化合物能够抑制由丁苯那嗪引起的下垂并具有止痛活性。

    Aminopropanol derivatives, process for their preparation and pharmaceutical compositions comprising the same
    15.
    发明授权
    Aminopropanol derivatives, process for their preparation and pharmaceutical compositions comprising the same 失效
    氨基丙醇衍生物，其制备方法和包含其的药物组合物

    公开(公告)号：US5234934A

    公开(公告)日：1993-08-10

    申请号：US876091

    申请日：1992-04-30

    申请人： Zoltan Budai ,  Klara Reiter nee Esses ,  Eniko Sziri nee Kiszelly ,  Gizella Zsila ,  Gabor Gigler ,  Lujza Petocz ,  Maria Szecsey nee Hegedus ,  Marton Fekete ,  Valeria Hoffmann ,  Laszlo Kapolnai

    发明人： Zoltan Budai ,  Klara Reiter nee Esses ,  Eniko Sziri nee Kiszelly ,  Gizella Zsila ,  Gabor Gigler ,  Lujza Petocz ,  Maria Szecsey nee Hegedus ,  Marton Fekete ,  Valeria Hoffmann ,  Laszlo Kapolnai

    IPC分类号： C07C251/58 ,  C07D213/16 ,  C07D295/088

    CPC分类号： C07D213/16 ,  C07C251/58 ,  C07D295/088 ,  C07C2101/02 ,  C07C2101/08 ,  C07C2101/14 ,  C07C2101/18

    摘要： The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkyl-aminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a piperidine ring which is optionally substituted by a phenyl or benzyl group and, if desired, it comprises a double bond,R.sup.6 stands for hydrogen atom or benzoyl group, andn represents an integer from 3 to 6,acid-addition salts and quaternary ammonium derivatives thereof.Further the invention relates to processes for preparing these compounds.The compounds of the invention exert cardiac circulation controlling and/or improving, central nervous system tranquillizing and/or digestive system irregulations improving effects.

    摘要翻译： 本发明涉及式I的新型外消旋或光学活性氨基丙醇衍生物其中R和R 1独立地为氢原子，卤素原子，低级烷氧基或一起代表亚甲基二氧基，R2和R3一起表示化学键或 独立地代表氢原子，R4和R5独立地是氢原子，C3-7环烷基或任选被一个或多个二烷基氨基烷基，二甲氧基苯基或苯基取代的直链或支链，饱和或不饱和的C 1-12烷基，或R 4 和R5与相邻的氮原子一起形成任选地包含氧，硫或另外的氮原子的4至7元环，该环任选被苯基，苄基或C 1-3烷基取代，所述取代基可以携带 羟基，一个或两个甲氧基，卤素原子或三氟甲基，或R4和R5与相邻的氮原子一起形成哌啶环，其任选地是 由苯基或苄基构成，如果需要，它包含双键，R6代表氢原子或苯甲酰基，n代表3-6的整数，其酸加成盐和季铵衍生物。 本发明还涉及制备这些化合物的方法。 本发明的化合物发挥心脏循环控制和/或改善，中枢神经系统镇定和/或消化系统不调节改善作用。

    Oxime ethers and pharmaceutical compositions containing the same
    16.
    发明授权
    Oxime ethers and pharmaceutical compositions containing the same 失效
    肟醚和含有它的药物组合物

    公开(公告)号：US4395413A

    公开(公告)日：1983-07-26

    申请号：US162674

    申请日：1980-06-24

    申请人： Zoltan Budai ,  Aranka Lay nee Konya ,  Tibor Mezei ,  Lujza Petocz ,  Katalin Grasser ,  Ibolya Kosoczky ,  Eniko Szirt nee Kiszelly ,  Peter Gorog

    发明人： Zoltan Budai ,  Aranka Lay nee Konya ,  Tibor Mezei ,  Lujza Petocz ,  Katalin Grasser ,  Ibolya Kosoczky ,  Eniko Szirt nee Kiszelly ,  Peter Gorog

    IPC分类号： A61K31/15 ,  A61K31/495 ,  A61P25/04 ,  C07C67/00 ,  C07C239/00 ,  C07C249/10 ,  C07C251/58 ,  C07D295/02 ,  C07D295/088 ,  C07D295/08

    CPC分类号： C07D295/088 ,  Y10S514/926 ,  Y10S514/927

    摘要： The invention relates to novel oxime ethers of the general formula /I/ and acid addition salts and quaternary ammonium derivatives thereof, ##STR1## wherein A represents a C.sub.2-6 straight or branched alkylene chain,R and R.sup.1 each represent a C.sub.1-6 alkyl group or they form together with the adjacent nitrogen atom a heterocyclic ring containing 4 to 7 carbon atoms and optionally a further hetero atom, i.e. an oxygen, sulfur or nitrogen atom, and said ring may be optionally substituted by a C.sub.1-3 alkyl, phenyl or benzyl group,R.sup.2 and R.sup.3 each denote a hydrogen atom or together form a valency bond,R.sup.4 denotes a C.sub.1-10 alkyl or C.sub.2-10 alkenyl group, andn denotes an integer from 3 to 7.The compounds of the general formula /I/ are prepared according to the invention by reacting a cycloalkane derivative of the general formula /II/ ##STR2## wherein R.sup.2, R.sup.3, R.sup.4 and n have the same meaning as above, whereasY denotes an oxygen or sulphur atom or a .dbd.N--OH group with an aminoalkyl derivative of the general formula /III/ ##STR3## wherein R, R.sup.1 and A have the same meaning as stated above andZ means a halogen atom or a H.sub.2 N--O-- group or a salt thereof in the presence of a basic condensing agent.The new compounds of the general formula /I/ possess valuable nicotine-lethality inhibiting, local anaesthetic, analgesic effects, which are, in case of certain compounds, complemented by anti-hypertensive, maximum electroshock and tetracorspasm inhibiting, ulcus inhibiting and motility inhibiting effects, and can be applied to advantage in the therapy.

    摘要翻译： 本发明涉及通式I I的新型肟醚及其酸加成盐和季铵衍生物，其中A表示C2-6直链或支链亚烷基链，R和R1各自表示C1 -6烷基，或者它们与相邻的氮原子一起与含有4至7个碳原子的杂环和任选的另外的杂原子（即氧，硫或氮原子）一起形成，并且所述环可以任选地被C 1-3 烷基，苯基或苄基，R2和R3各自表示氢原子或一起形成价键，R4表示C1-10烷基或C2-10烯基，n表示3至7的整数。 根据本发明通过使通式/ II / IMAGE / II /的环烷烃衍生物与其中R2，R3，R4和n具有与上述相同的含义反应制备通式/ I / I，而Y表示氧或 硫原子或a =具有氨基烷基衍生物的N-OH基团 通式/ III / / III /其中R，R 1和A具有与上述相同的含义，Z表示在碱性缩合剂存在下的卤素原子或H 2 N-O-基或其盐。 新型化合物/ I /具有有价值的尼古丁杀伤力抑制，局部麻醉，止痛作用，在某些化合物的情况下，补充有抗高血压，最大电休克和四疣抑制作用，抑制溃疡和运动抑制作用 ，并且可以在治疗中有利地应用。

    Pyrazolo[1,5-c]quinazoline derivatives and analgesic compositions containing them
    17.
    发明授权
    Pyrazolo[1,5-c]quinazoline derivatives and analgesic compositions containing them 失效
    吡唑并[1,5-c]喹唑啉衍生物和含有它们的镇痛组合物

    公开(公告)号：US4303660A

    公开(公告)日：1981-12-01

    申请号：US150349

    申请日：1980-05-16

    申请人： Edit Berenyi nee Poldermann ,  Eniko Szirt nee Kiszelly ,  Peter Gorog ,  Lujza Petocz ,  Ibolya Kosoczky ,  Agnes Kovacs nee Palotai ,  Gabriella rmos nee Lassu

    发明人： Edit Berenyi nee Poldermann ,  Eniko Szirt nee Kiszelly ,  Peter Gorog ,  Lujza Petocz ,  Ibolya Kosoczky ,  Agnes Kovacs nee Palotai ,  Gabriella rmos nee Lassu

    IPC分类号： A61K31/4162 ,  A61K31/4745 ,  A61K31/505 ,  A61K31/519 ,  A61P1/00 ,  A61P1/04 ,  A61P25/04 ,  A61P29/00 ,  C07D231/16 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D231/16

    摘要： The invention relates to novel pyrazolo[1,5-c]quinazoline derivatives of the general formula I ##STR1## wherein R represents a hydrogen atom, a C.sub.1-4 alkyl group or an acyl group,R.sub.1 represents a hydrogen atom, a C.sub.1-12 alkyl group, a C.sub.3-8 cycloalkyl group, a C.sub.2-4 alkenyl group, an aralkyl group, wherein the alkyl group has 1 to 4 carbon atoms, a phenylalkenyl group, wherein the alkenyl group has 2 to 4 carbon atoms, furthermore a carboxy group or a phenyl group optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C.sub.1-4 alkoxy, nitro or di(C.sub.1-4 alkyl)amino groups, orR and R.sub.1 may form together a valence bond,R.sub.2 represents a hydrogen atom, a C.sub.1-4 alkyl or a phenyl group, orR.sub.1 and R.sub.2 may form together a C.sub.2-7 alkylene group,R.sub.3 represents a nitro group, an amino group, an alkylamino group, a dialkylamino group, wherein the alkyl groups have 1 to 4 carbon atoms, an alkylideneimino group, wherein the alkylidene group has 1 to 4 carbon atoms, a benzylideneimino group or an acylamino group,and pharmaceutically acceptable acid addition salts thereof.The novel compounds of the general formula I can be employed primarily as analgesic agents.

    摘要翻译： 本发明涉及通式I（XIX）的新颖的吡唑并[1,5-c]喹唑啉衍生物，其中R表示氢原子，C1-4烷基或酰基，R1表示氢原子， C1-12烷基，C3-8环烷基，C2-4烯基，其中烷基具有1至4个碳原子的芳烷基，苯基烯基，其中烯基具有2至4个碳原子 此外，羧基或任选被一个或多个选自卤素，羟基，C 1-4烷氧基，硝基或二（C 1-4烷基）氨基的取代基取代的苯基，或R和R 1可以一起形成 价键，R2表示氢原子，C1-4烷基或苯基，或R1和R2可以一起形成C2-7亚烷基，R3表示硝基，氨基，烷基氨基，二烷基氨基 基团，其中烷基具有1至4个碳原子，亚烷基亚氨基，其中亚烷基具有1至4个碳 n原子，亚苄基亚氨基或酰氨基，及其药学上可接受的酸加成盐。 通式I的新化合物可以主要用作止痛剂。

    Optically active 2-chloro-12-(3-dimethylamino-2-methyl-propyl)-12H-dibenzo[d.g] [1,3,6] dioxazocines and a process for the preparation thereof
    20.
    发明授权
    Optically active 2-chloro-12-(3-dimethylamino-2-methyl-propyl)-12H-dibenzo[d.g] [1,3,6] dioxazocines and a process for the preparation thereof 失效
    光学活性的2-氯-12-（3-二甲基氨基-2-甲基 - 丙基）-12H-二苯并[d] [1,3,6]二氧杂吖庚因及其制备方法

    公开(公告)号：US4906622A

    公开(公告)日：1990-03-06

    申请号：US195691

    申请日：1988-05-18

    申请人： Laszlo Rozsa ,  Lujza Petocz ,  Eniko Szirt nee Kiszelly ,  Peter Tompe ,  Gabor Gigler

    发明人： Laszlo Rozsa ,  Lujza Petocz ,  Eniko Szirt nee Kiszelly ,  Peter Tompe ,  Gabor Gigler

    IPC分类号： A61K31/395 ,  A61P25/00 ,  A61P25/16 ,  C07D273/00 ,  C07D273/01

    CPC分类号： C07D273/00

    摘要： The invention relates to optically active 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]dioxazocine of the Formula ##STR1## and pharmaceutically acceptable acid additional salts thereof. The enantiomers are especially active against Parkinsion's disease.The optically active enantiomers are prepared by(a) resolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxazocine with a optically active organic acid and separating the enantiomers; or(b) dissolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxazocine in an organic solvent, crystallizing and isolating one of the enantiomers, optionally dissolving additional racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxazocine in the mother liquor obtained and crystallizing and isolating the other enantiomer, and, if desired, repeating the whole process.

    摘要翻译： 本发明涉及式（I）的光学活性2-氯代 - 12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6]二恶唑辛嗪和药学上 其可接受的酸性附加盐。 对映异构体对帕金森氏病特别活跃。 旋光对映异构体通过以下步骤制备：（a）用光学拆分外消旋的2-氯代 - 12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6] 活性有机酸并分离对映异构体; 或（b）将外消旋的2-氯代 - 12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6] - 二氧杂吖嗪在有机溶剂中溶解， 的对映异构体，任选地将另外的外消旋的2-氯-12-（3-二甲基氨基-2-甲基丙基）-12H-二苯并[d，g] [1,3,6] - 二氧杂吖嗪应用于所获得和结晶的母液中， 分离另一个对映体，如果需要，重复整个过程。