公开(公告)号：US4469692A

公开(公告)日：1984-09-04

申请号：US442451

申请日：1982-11-17

申请人： Endre Tihanyi ,  Ferenc Andrasi ,  Melinda Gal ,  Eleonora Sineger

发明人： Endre Tihanyi ,  Ferenc Andrasi ,  Melinda Gal ,  Eleonora Sineger

IPC分类号： C07D487/04 ,  A61K31/4162 ,  A61K31/4196 ,  A61K31/53 ,  A61P25/20 ,  A61P41/00 ,  C07D487/10 ,  A61K31/415

CPC分类号： C07D487/10

摘要： A spiro derivative of the pyrazolo [1,5-d] [1,2,4] triazine ring system of the formula I ##STR1## wherein R.sub.1 and R.sub.2 represent, independently from each other, a hydrogen atom or a C.sub.1-4 alkyl group,R.sub.3 stands for a hydrogen atom, an unbranched or branched C.sub.1-4 alkyl, C.sub.2-5 alkenyl or benzyl group,R.sub.4 represents a hydrogen atom, an unbranched or branched C.sub.1-4 alkyl, C.sub.4-6 cycloalkyl, an unsubstituted or mono-halo or polyhalo benzyl group, andn is a whole number from 4 to 8,wherein R stands for an unbranched or branched C.sub.1-4 alkyl, or C.sub.4-6 cycloalkyl, C.sub.2-5 alkenyl, an unsubstituted or a monohalogeno or polyhalogenobenzyl group, and X represents a halogen or a 4-methyl-phenylsulfonyloxy group. Compounds of the formula I exhibit valuable CNS activities.

摘要翻译： 式I的吡唑并[1,5-d] [1,2,4]三嗪环系的螺衍生物其中R 1和R 2彼此独立地表示氢原子或C 1-4 烷基，R3表示氢原子，无支链或支链C 1-4烷基，C 2-5烯基或苄基，R 4表示氢原子，无支链或支链C 1-4烷基，C 4-6环烷基，未取代或未取代的 单卤素或多卤代苄基，n为4至8的整数，其中R代表无支链或支链C 1-4烷基或C 4-6环烷基，C 2-5链烯基，未取代或单卤素或多卤代苄基 基团，X表示卤素或4-甲基 - 苯基磺酰氧基。 式I的化合物显示出有价值的CNS活性。

公开(公告)号：US5441948A

公开(公告)日：1995-08-15

申请号：US115688

申请日：1993-09-03

申请人： Ilona Bodi ,  Eva Gal ,  Melinda Gal ,  Laszlo Jaszlits ,  Andrea Jednakovits ,  Adrina Kiss ,  Aniko Miklos nee Kovacs ,  Gyorgy Mathe ,  Istvan Pallagi ,  Gyorgy Rabloczky ,  Antal Simai ,  Endre Tihanyi

发明人： Ilona Bodi ,  Eva Gal ,  Melinda Gal ,  Laszlo Jaszlits ,  Andrea Jednakovits ,  Adrina Kiss ,  Aniko Miklos nee Kovacs ,  Gyorgy Mathe ,  Istvan Pallagi ,  Gyorgy Rabloczky ,  Antal Simai ,  Endre Tihanyi

IPC分类号： A61K31/55 ,  A61P9/00 ,  C07D255/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07F7/08 ,  C07D403/06

CPC分类号： C07D401/06 ,  C07D255/04 ,  C07D401/12 ,  C07D403/12 ,  C07F7/0812

摘要： The invention relates to racemic or optically active 1,3,4-benzotriazepin-5(4H)-one derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said compounds for the treatment of diseases and for the preparation of pharmaceutical compositions containing the said compounds as active agent.The new compounds according to the invention correspond to the general formula (I), ##STR1## wherein R.sup.1 represents hydrogen or straight or branched chain C.sub.1-4 alkyl optionally carrying a pyridyl or a phenyl substituent;R.sup.2 stands for cyanoimino;R.sup.3 denotes hydrogen or straight or branched chain C.sub.1-4 alkyl;R.sup.4 stands for C.sub.1-4 alkyl; andthe dotted line does not represent a valency bond; orR.sup.2 stands for a group of the formula R.sup.9 R.sup.10 N, whereinR.sup.9 and R.sup.10 are independently hydrogen or straight or branched chain C.sub.1-10 alkyl, orR.sup.9 R.sup.10 N together form a 5- to 7-membered heterocyclic group; orR.sup.9 R.sup.10 N together form a group of the formula N.dbd.C(NR.sup.12 R.sup.13)NH.sub.2, wherein R.sup.12 and R.sup.13 are independently hydrogen or straight or branched chain C.sub.1-10 alkyl, orNR.sup.12 R.sup.13 together form a 5- to 7-membered heterocyclic group;R.sup.4 stands for C.sub.1-4 alkyl; andthe dotted line represents a valency bond, consequently substituent R.sup.1 is missing;with the proviso that if R.sup.9 and R.sup.10 are the same, they are other than hydrogen.The 1,3,4-benzotriazepin-5(4H)-one derivatives of the general formula (I) affect the circulatory system and possess antianginal, antihypertensive and peripheral vasodilating effects.

摘要翻译： 本发明涉及外消旋或光学活性的1,3,4-苯并三氮杂-5（4H） - 酮衍生物，其制备方法，含有该衍生物的药物组合物，涉及所述化合物用于治疗疾病和 用于制备含有所述化合物作为活性剂的药物组合物。 根据本发明的新化合物对应于通式（I），其中R 1表示氢或任选带有吡啶基或苯基取代基的直链或支链C 1-4烷基; R2代表氰基亚氨基; R3表示氢或直链或支链C 1-4烷基; R4代表C1-4烷基; 虚线不代表价债券; 或R 2表示式R9R 10 N的基团，其中R 9和R 10独立地为氢或直链或支链C 1-10烷基，或R 9 R 10 N一起形成5-至7-元杂环基; 或R9R10N一起形成式N = C（NR 12 R 13）NH 2的基团，其中R 12和R 13独立地为氢或直链或支链C 1-10烷基或NR 12 R 13一起形成5-至7-元杂环基; R4代表C1-4烷基; 虚线表示价键，因此取代基R1缺失; 条件是如果R9和R10相同，它们不是氢。 通式（I）的1,3,4-苯并三氮杂-5（4H） - 酮衍生物影响循环系统，具有抗心绞痛，抗高血压和外周血管扩张作用。