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    Novel triazolo-pyrimidine derivatives
    1.
    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
    7.
    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。

    Triazolyl thioamide derivates
    8.
    发明授权
    Triazolyl thioamide derivates 失效
    三唑氧化物衍生物

    公开(公告)号：US5175163A

    公开(公告)日：1992-12-29

    申请号：US617126

    申请日：1990-11-21

    申请人： Jozsef Barkoczy ,  Jozsef Reiter ,  Laszlo Pongo ,  Lujza Petocz ,  Marton Fekete ,  Frigyes Gorgenyi ,  Gabor Gigler ,  Istvan Gacsalyi ,  Istvan Gyertyan

    发明人： Jozsef Barkoczy ,  Jozsef Reiter ,  Laszlo Pongo ,  Lujza Petocz ,  Marton Fekete ,  Frigyes Gorgenyi ,  Gabor Gigler ,  Istvan Gacsalyi ,  Istvan Gyertyan

    IPC分类号： A61K31/41 ,  A61K31/4196 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P13/06 ,  A61P25/08 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  A61P29/00 ,  C07D249/14 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14

    CPC分类号： C07D249/14

    摘要： The invention relates to novel triazolyl thioamides of the general formula (I), ##STR1## wherein Q represents hydrogen or a heterocyclic group optionally bearing one or more C.sub.1-4 alkyl substituent(s), or a group of the formula SR.sup.1, whereinR.sup.1 stands for straight or branched chained alkyl group comprising 1 to 6 carbon atom(s), or a group of the formula NR.sup.2 R.sup.3, whereinR.sup.2 and R.sup.3 each represent hydrogen, straight or branched chained C.sub.1-4 alkyl or C.sub.2-6 alkenyl group,Y denotes C.sub.1-4 alkyl optionally bearing one or more hydroxyl or C.sub.1-4 alkoxy substituent(s), phenyl-(C.sub.1-4 alkyl) optionally bearing on the phenyl ring one or more C.sub.1-4 alkoxy group(s), or phenoxy-(C.sub.1-4 alkyl) optionally substituted on the phenyl ring by a C.sub.1-4 alkyl bearing a heterocyclic group containing a nitrogen atom,and pharmaceutically acceptable acid addition salts thereof.Furthermore the invention relates to a process for preparing these compounds.The compounds according to the invention possess tranquillant, antidepressant, spacmolytic, antiinflammatory, analgesic and antiperistaltic effects.

    摘要翻译： 本发明涉及通式（I）的新型三唑基硫代酰胺，其中Q表示氢或任选带有一个或多个C 1-4烷基取代基的杂环基或式SR 1的基团 其中R1代表包括1至6个碳原子的直链或支链烷基或式NR2R3基团，其中R2和R3各自表示氢，直链或支链C 1-4烷基或C 2-6烯基 基团，Y表示任选带有一个或多个羟基或C 1-4烷氧基取代基的C 1-4烷基，任选地在苯环上带有一个或多个C 1-4烷氧基的苯基 - （C 1-4烷基） 或在苯环上被含有含有氮原子的杂环基的C 1-4烷基任选取代的苯氧基 - （C 1-4烷基）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。 根据本发明的化合物具有镇静，抗抑郁，间质，抗炎，止痛和抗静脉作用。

    Dihydropyrimidothiazine derivatives
    9.
    发明授权
    Dihydropyrimidothiazine derivatives 失效
    二氢咪唑衍生物

    公开(公告)号：US5071849A

    公开(公告)日：1991-12-10

    申请号：US555943

    申请日：1990-07-19

    申请人： Daniel Bozsing ,  Lujza Petocz ,  Maria Szecsey nee Hegedus ,  Peter Tompe ,  Gabor Gigler ,  Istvan Gacsalyi ,  Istvan Gyertyan

    发明人： Daniel Bozsing ,  Lujza Petocz ,  Maria Szecsey nee Hegedus ,  Peter Tompe ,  Gabor Gigler ,  Istvan Gacsalyi ,  Istvan Gyertyan

    IPC分类号： A61K31/519 ,  A61K31/54 ,  A61K31/542 ,  A61P29/00 ,  C07D239/00 ,  C07D239/22 ,  C07D239/40 ,  C07D279/00 ,  C07D513/04

    CPC分类号： C07D239/22 ,  C07D513/04

    摘要： The invention relates to new dihydropyrimidothiazine derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same and new intermediates useful in the preparation of the said dihydropyrimidothiazine derivatives.The new dihydropyrimidothiazine derivatives of the general formula I, ##STR1## wherein R.sup.1 represents C.sub.1-6 alkoxy, amino or phenylamino,R.sup.2 stands for C.sub.1-6 alkyl or phenyl,R.sup.3 represents hydrogen or C.sub.1-6 alkyl, andR.sup.4 denotes C.sub.1-11 alkyl or phenyl optionally bearing one or more identical or different substituent/s/ selected from halogen, nitro, amino, di-(C.sub.1-6 alkyl)-amino, C.sub.1-6 alkyl, C.sub.1-6 alkoxy and hydroxy,and pharmaceutically acceptable acid addition salts thereof exert valuable antianginal and/or antiinflammatory effect/s/ and are useful in therapy.

    摘要翻译： 本发明涉及新的二氢嘧啶并噻嗪衍生物，其制备方法，包含其的药物组合物和可用于制备所述二氢嘧啶并噻嗪衍生物的新中间体。 新的通式I的二氢嘧啶并噻嗪衍生物，其中R1代表C1-6烷氧基，氨基或苯基氨基，R2代表C1-6烷基或苯基，R3代表氢或C1-6烷基，R4代表C1- 11烷基或苯基，其任选带有一个或多个相同或不同的取代基，选自卤素，硝基，氨基，二（C 1-6烷基） - 氨基，C 1-6烷基，C 1-6烷氧基和羟基，以及药学上可接受的 其酸加成盐发挥有价值的抗心绞痛和/或抗炎作用，并且可用于治疗。