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    Dihydropyrimidothiazine derivatives
    1.
    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。

    Aminopropanol derivatives, process for their preparation and pharmaceutical compositions comprising the same
    6.
    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。