8-Chloro-6-(2-chlorophenyl)-1-methyl-2H,4 H-pyrrolo[3,4-d][2]benzazepine-3-carboxaldehyde | 81993-49-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: 8-Chloro-6-(2-chlorophenyl)-1-methyl-2H,4 H-pyrrolo[3,4-d][2]benzazepine-3-carboxaldehyde
• 英文别名: 8-chloro-6-(2-chlorophenyl)-1-methyl-2,4-dihydropyrrolo[3,4-d][2]benzazepine-3-carbaldehyde
• CAS: 81993-49-9
• 化学式: C₂₀H₁₄Cl₂N₂O
• 分子量: 369.25
• InChiKey: ASQKOWPSPOCCQP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  25
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  45.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  8-chloro-6-(2-chlorophenyl)-1-methyl-2H,4H-pyrrolo[3,4-d][2]benzazepine 在 三氯氧磷 作用下， 以 N-甲基乙酰胺 、 二氯甲烷 为溶剂， 生成 8-Chloro-6-(2-chlorophenyl)-1-methyl-2H,4 H-pyrrolo[3,4-d][2]benzazepine-3-carboxaldehyde
  参考文献：
  名称：

  Pyrrolo[3,4-d][2]benzazepines

  摘要：

  本发明涉及以下结构的化合物：其中R.sub.1从氢、较低的烷基、C.sub.3到C.sub.7烯基或炔基、羟甲基、羟基、烷氧基、氨基和单或双较低的烷基氨基中选择；R.sub.3从氢、较低的烷基、C.sub.3到C.sub.7烯基或炔基、羟甲基、氢、羟基、三卤甲基、烷氧基、氨基和单或双较低的烷基氨基中选择；R.sub.2从氢、较低的烷基、C.sub.3到C.sub.7烯基或炔基、较低的烷氧基、C.sub.2到C.sub.7羧酸及其酯和酰胺、羟基C.sub.2到C.sub.7烷基和氨基或单或双较低的烷基氨基C.sub.2到C.sub.7烷基中选择；R.sub.4从氢、酰氧基、直链较低的烷氧基和羟基中选择；R.sub.5是卤素或氢；R.sub.6是卤素，但如果R.sub.1或R.sub.3中的一个是羟甲基或羟基，则剩余取代基从氢、较低的烷基和C.sub.3到C.sub.7烯基或炔基中选择，R.sub.2是氢，进一步规定(A)当R.sub.4是酰氧基时，R.sub.1和R.sub.3是氢、较低的烷基、C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，R.sub.2是较低的烷氧基，(B)当R.sub.4是羟基时，R.sub.1和R.sub.3是氢、较低的烷基、C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，R.sub.2是氢或(C)当R.sub.4是烷氧基时，R.sub.1和R.sub.3是氢、较低的烷基、C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，以及其药学上可接受的盐。还公开了吡咯苯并蒽啉的某些5,6-二氢衍生物、N-氧化物和季铵盐。

  公开号：

  US04354973A1

文献信息

• Pyrrolo[3,4-d] [2] benzazepines
  申请人：Hoffmann-La Roche Inc.

  公开号：US04405518A1

  公开（公告）日：1983-09-20

  The present invention relates to compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the group ##STR2## wherein R.sub.11 is hydrogen, hydroxy, alkoxy, amino and mono- or di-lower alkylamino; and R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the group ##STR3## wherein R.sub.11 is hydrogen, hydroxy, trihalomethyl, alkoxy, amino and mono- or di-lower alkylamino; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, the group ##STR4## C.sub.2 to C.sub.7 carboxylic acids and the esters and amides thereof, hydroxy C.sub.2 to C.sub.7 alkyl and amino or mono- or di-lower alkyl amino C.sub.2 to C.sub.7 alkyl; R.sub.4 is selected from the group consisting of hydrogen, acyloxy, straight chain lower alkoxy and hydroxy; R.sub.5 is halogen or hydrogen; R.sub.6 is halogen with the proviso that if one of R.sub.1 or R.sub.3 is hydroxymethyl or the group - ##STR5## wherein R.sub.11 is as above then the remaining substituent is selected from the group consisting of hydrogen, lower alkyl and C.sub.3 to C.sub.7 alkenyl or alkynyl, and R.sub.2 is hydrogen and the further proviso that (A) when R.sub.4 is acyloxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and R.sub.2 is the group ##STR6## (B) when R.sub.4 is hydroxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and R.sub.2 is hydrogen or (C) when R.sub.4 is alkoxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and the pharmaceutically acceptable salts thereof. Also disclosed are certain 5,6 dihydro derivatives, N-oxides and quarternary iminium salts of the pyrrolobenzazepines.

  本发明涉及式为##STR1##的化合物，其中R.sub.1选择自羟基甲基，氢，低碳基，C.sub.3到C.sub.7烯基或炔基，羟甲基，##STR2##其中R.sub.11为氢，羟基，烷氧基，氨基和单或双低碳基氨基;和R.sub.3选择自氢，低碳基，C.sub.3到C.sub.7烯基或炔基，羟甲基，##STR3##其中R.sub.11为氢，羟基，三卤甲基，烷氧基，氨基和单或双低碳基氨基; R.sub.2选择自氢，低碳基，C.sub.3到C.sub.7烯基或炔基，##STR4##C.sub.2到C.sub.7羧酸及其酯和酰胺，羟基C.sub.2到C.sub.7烷基和C.sub.2到C.sub.7烷基的氨基或单或双低碳基氨基; R.sub.4选择自氢，酰氧基，直链低碳基烷氧基和羟基; R.sub.5选择自卤素或氢; R.sub.6选择自卤素，但如果R.sub.1或R.sub.3之一是羟甲基或-##STR5##其中R.sub.11如上所述，则其余取代基选择自氢，低碳基和C.sub.3到C.sub.7烯基或炔基，并且R.sub.2为氢，并且进一步规定当R.sub.4为酰氧基时，R.sub.1和R.sub.3为氢，低碳基，C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，而R.sub.2为##STR6##当R.sub.4为羟基时，R.sub.1和R.sub.3为氢，低碳基，C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，而R.sub.2为氢或当R.sub.4为烷氧基时，R.sub.1和R.sub.3为氢，低碳基，C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，以及其药学上可接受的盐。此外，还披露了某些吡咯并苯并氮杂环的5,6-二氢衍生物，N-氧化物和季铵盐。
• Pyrrolo[3,4-D][2]Benzazepines
  申请人：Hoffmann-La Roche Inc.

  公开号：US04409390A1

  公开（公告）日：1983-10-11

  The present invention relates to compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the group ##STR2## wherein R.sub.11 is hydrogen, hydroxy, alkoxy, amino and mono- or di-lower alkylamino; and R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the group ##STR3## wherein R.sub.11 is hydrogen, hydroxy, trihalomethyl, alkoxy, amino and mono- or di-lower alkylamino; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, the group ##STR4## C.sub.2 to C.sub.7 carboxylic acids and the esters and amides thereof, hydroxy C.sub.2 to C.sub.7 alkyl and amino or mono- or di-lower alkyl amino C.sub.2 to C.sub.7 alkyl; R.sub.4 is selected from the group consisting of hydrogen, acyloxy, straight chain lower alkoxy and hydroxy; R.sub.5 is halogen or hydrogen; R.sub.6 is halogen with the proviso that if one of R.sub.1 or R.sub.3 is hydroxymethyl or the group ##STR5## wherein R.sub.11 is as above then the remaining substituent is selected from the group consisting of hydrogen, lower alkyl and C.sub.3 to C.sub.7 alkenyl or alkynyl, and R.sub.2 is hydrogen and the further proviso that (A) when R.sub.4 is acyloxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and R.sub.2 is the group ##STR6## (B) when R.sub.4 is hydroxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and R.sub.2 is hydrogen or (C) when R.sub.4 is alkoxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and the pharmaceutically acceptable salts thereof. Also disclosed are certain 5,6 dihydro derivatives, N-oxides and quarternary iminium salts of the pyrrolobenzazepines.

  本发明涉及以下式的化合物：##STR1##其中R.sub.1从下列组中选择：氢、低碳基、C.sub.3到C.sub.7烯基或炔基、羟甲基、##STR2##其中R.sub.11为氢、羟基、烷氧基、氨基和单-或双-低碳基氨基；R.sub.3从下列组中选择：氢、低碳基、C.sub.3到C.sub.7烯基或炔基、羟甲基、##STR3##其中R.sub.11为氢、羟基、三卤甲基、烷氧基、氨基和单-或双-低碳基氨基；R.sub.2从下列组中选择：氢、低碳基、C.sub.3到C.sub.7烯基或炔基、##STR4##C.sub.2到C.sub.7羧酸及其酯和酰胺、羟基C.sub.2到C.sub.7烷基和氨基或单-或双-低碳基氨基C.sub.2到C.sub.7烷基；R.sub.4从下列组中选择：氢、酰氧基、直链低碳基氧基和羟基；R.sub.5为卤素或氢；R.sub.6为卤素，但如果R.sub.1或R.sub.3中的一个是羟甲基或##STR5##其中R.sub.11如上所述，则剩余的取代基从以下组中选择：氢、低碳基和C.sub.3到C.sub.7烯基或炔基，且R.sub.2为氢；进一步规定，当R.sub.4为酰氧基时，R.sub.1和R.sub.3为氢、低碳基、C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，R.sub.2为##STR6##当R.sub.4为羟基时，R.sub.1和R.sub.3为氢、低碳基、C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，R.sub.2为氢或当R.sub.4为烷氧基时，R.sub.1和R.sub.3为氢、低碳基、C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，以及其药学上可接受的盐。此外，本发明还公开了某些吡咯苯并莫匹啶的5,6-二氢衍生物、N-氧化物和季铵盐。
• Pyrrolo[3,4,-d][2]benzazepines
  申请人：Hoffmann-La Roche Inc.

  公开号：US04428879A1

  公开（公告）日：1984-01-31

  The present invention relates to compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the group ##STR2## wherein R.sub.11 is hydrogen, hydroxy, alkoxy, amino and mono- or di-lower alkylamino; and R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the group ##STR3## wherein R.sub.11 is hydrogen, hydroxy, trihalomethyl, alkoxy, amino and mono- or di-lower alkylamino; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, the group ##STR4## C.sub.2 to C.sub.7 carboxylic acids and the esters and amides thereof, hydroxy C.sub.2 to C.sub.7 alkyl and amino or mono- or di- lower alkyl amino C.sub.2 to C.sub.7 alkyl; R.sub.4 is selected from the group consisting of hydrogen , acyloxy, straight chain lower alkoxy and hydroxy; R.sub.5 is halogen or hydrogen; R.sub.6 is halogen with the proviso that if one of R.sub.1 or R.sub.3 is hydroxymethyl or the group ##STR5## wherein R.sub.11 is as above then the remaining substituent is selected from the group consisting of hydrogen, lower alkyl and C.sub.3 to C.sub.7 alkenyl or alkynyl, and R.sub.2 is hydrogen and the further proviso that (A) when R.sub.4 is acyloxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and R.sub.2 is the group ##STR6## (B) when R.sub.4 is hydroxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and R.sub.2 is hydrogen or (C) when R.sub.4 is alkoxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and the pharmaceutically acceptable salts thereof which exhibit activity as sedatives and anxiolytics. Also disclosed are certain 5,6 dihydro derivatives, N-oxides and quarternary iminium salts of the pyrrolobenzazepines.

  本发明涉及以下式的化合物：##STR1##其中R.sub.1选自由氢、较低烷基、C.sub.3到C.sub.7烯基或炔基、羟甲基、##STR2##其中R.sub.11为氢、羟基、烷氧基、氨基和单-或双-较低烷基氨基；R.sub.3选自由氢、较低烷基、C.sub.3到C.sub.7烯基或炔基、羟甲基、##STR3##其中R.sub.11为氢、羟基、三卤甲基、烷氧基、氨基和单-或双-较低烷基氨基；R.sub.2选自由氢、较低烷基、C.sub.3到C.sub.7烯基或炔基、##STR4##C.sub.2到C.sub.7羧酸及其酯和酰胺、羟基C.sub.2到C.sub.7烷基和C.sub.2到C.sub.7烷基的氨基或单-或双-较低烷基氨基；R.sub.4选自由氢、酰氧基、直链较低烷氧基和羟基；R.sub.5为卤素或氢；R.sub.6为卤素，但前提是如果R.sub.1或R.sub.3中的一个是羟甲基或##STR5##其中R.sub.11如上所述，那么剩余的取代基选自由氢、较低烷基和C.sub.3到C.sub.7烯基或炔基，而R.sub.2为氢，进一步前提是(A)当R.sub.4为酰氧基时，R.sub.1和R.sub.3为氢、较低烷基、C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，而R.sub.2为##STR6##(B)当R.sub.4为羟基时，R.sub.1和R.sub.3为氢、较低烷基、C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，而R.sub.2为氢或(C)当R.sub.4为烷氧基时，R.sub.1和R.sub.3为氢、较低烷基、C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，以及具有镇静和抗焦虑活性的药物可接受的盐。还公开了某些吡咯并苯并螺氮平的5,6-二氢衍生物、N-氧化物和季铵盐。
• 1H-Pyrrole-3-carbonitrile-4(2-benzoyl)phenyl derivatives as
  申请人：Hoffmann-La Roche Inc.

  公开号：US04431823A1

  公开（公告）日：1984-02-14

  The present invention relates to compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the ##STR2## wherein R.sub.11 is hydrogen, hydroxy, alkoxy, amino and mono- or di-lower alkylamino; and R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the ##STR3## wherein R.sub.11 is hydrogen, hydroxy, trihalomethyl, alkoxy, amino and mono- or di-lower alkylamino; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, the ##STR4## C.sub.2 to C.sub.7 carboxylic acids and the esters and amides thereof, hydroxy C.sub.2 to C.sub.7 alkyl and amino or mono- or di-lower alkyl amino C.sub.2 to C.sub.7 alkyl; R.sub.4 is selected from the group consisting of hydrogen, acyloxy, straight chain lower alkoxy and hydroxy; R.sub.5 is halogen or hydrogen; R.sub.6 is halogen with the proviso that if one of R.sub.1 or R.sub.3 is hydroxymethyl or the ##STR5## wherein R.sub.11 is as above then the remaining substituent is selected from the group consisting of hydrogen, lower alkyl and C.sub.3 to C.sub.7 alkenyl or alkynyl, and R.sub.2 is hydrogen and the further proviso that (A) when R.sub.4 is acyloxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 C.sub.7 alkynyl, and R.sub.2 is the ##STR6## (B) when R.sub.4 is hydroxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and R.sub.2 is hydrogen or (C) when R.sub.4 is alkoxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and the pharmaceutically acceptable salts thereof. Also disclosed are certain 5,6 dihydro derivatives, N-oxides and quarternary iminium salts of the pyrrolobenzazepines.

  本发明涉及以下式的化合物：##STR1##其中R.sub.1选自氢，低碳基，C.sub.3到C.sub.7烯基或炔基，羟甲基，##STR2##其中R.sub.11为氢，羟基，烷氧基，氨基和单或双低碳基氨基；R.sub.3选自氢，低碳基，C.sub.3到C.sub.7烯基或炔基，羟甲基，##STR3##其中R.sub.11为氢，羟基，三卤甲基，烷氧基，氨基和单或双低碳基氨基；R.sub.2选自氢，低碳基，C.sub.3到C.sub.7烯基或炔基，##STR4##C.sub.2到C.sub.7羧酸及其酯和酰胺，羟基C.sub.2到C.sub.7烷基和氨基或单或双低碳基氨基C.sub.2到C.sub.7烷基；R.sub.4选自氢，酰氧基，直链低碳基烷氧基和羟基；R.sub.5为卤素或氢；R.sub.6为卤素，但若R.sub.1或R.sub.3中有一个为羟甲基或##STR5##其中R.sub.11如上所述，则剩余的取代基选自氢，低碳基和C.sub.3到C.sub.7烯基或炔基，R.sub.2为氢，并进一步规定：（A）当R.sub.4为酰氧基时，R.sub.1和R.sub.3为氢，低碳基，C.sub.3到C.sub.7烯基或C.sub.3 C.sub.7炔基，而R.sub.2为##STR6##（B）当R.sub.4为羟基时，R.sub.1和R.sub.3为氢，低碳基，C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，而R.sub.2为氢或（C）当R.sub.4为烷氧基时，R.sub.1和R.sub.3为氢，低碳基，C.sub.3到C.sub.7烯基或C.sub.3到C.sub.7炔基，以及其药学上可接受的盐。还公开了某些吡咯并苯并丙啶的5,6-二氢衍生物，N-氧化物和季铵盐。
• Pyrrolo(3,4-d)(2)benzazepine, Zwischenprodukte und Verfahren zu deren Herstellung sowie diese enthaltende Arzneimittel
  申请人：F. HOFFMANN-LA ROCHE & CO. Aktiengesellschaft

  公开号：EP0045519A2

  公开（公告）日：1982-02-10

  Die Pyrrolo[3,4-d][2]benzazepine der allgemeinen Formel worin A eine der Gruppen worin A eine der Gruppen R. Wasserstoff, niederes Alkyl, C3 - bis C7-Alkenyl, C7-bis C7-Alkinyl, Hydroxymethyl oder die Gruppe -ClOR11, R11 Wasserstoff, Hydroxy, Alkoxy oder Amino oder mono- oder di-niederes Alkylamino, R3 Wasserstoff, niederes Alkyl, C3- bis C7-Alkenyl, C3- bis C7- Alkinyl, Hydroxymethyl oder die Gruppe -COR111, R", Wasserstoff, Hydroxy, Trihalomethyl, Alkoxy oder Aminc oder mono- oder di-niederes Alkylamino, R2 Wasserstoff, niederes Alkyl, C3- bis C7-Alkenyl, C3- bis C7-Alkinyl, die Gruppe -COO-niederes Alkyl, eine C2- bis C7-Carbonsäure und die Ester und Amide davon, Hydro- xv-C2- bis C7-Alkyl oder Amino- oder mono- oder di-niederes Alkylamino-C2-bis C7-Alkyl, R4 Wasserstoff, Acyloxy, geradkettiges niederes Alkoxy oder Hydroxy, R6 Halogen mit einer Ordnungszahl, welche nicht grös- set als 35 ist, oder Wasserstoff, R6 Halogen mit einer Ordnungszahl, welche nicht grösser als 35 ist, R95 niederes Alkyl und Z⊖ das Anion einer Säure bedeuten, mit der Massgabe, dass wenn einer der Reste R, und R3 Hydroxymethyl oder die Gruppe -COR11 oder -COR111 bedeutet, und R11 und R111 obige Bedeutung besitzen, der verbleibende Rest Wasserstoff, niederes Alkyl, C3- bis C7-Alkenyl oder C3- bis C7-Alkinyl und R2 Wasserstoff bedeuten, und mit der weiteren Massgabe, dass (A) wenn R4 Acyloxy bedeutet, R1 und R3 Wasserstoff, niederes Alkyl, C3- bis C7-Alkenyl oder C3- bis C7-Alkinyl und R2 die Gruppe -CO-niederes Alkoxy bedeuten, (B) wenn R4 Hydroxy bedeutet, R1 und R3 Wasserstoff, niederes Alkyl, C3- bis C7-Alkenyl oder C3- bis C7-Alkinyl und R2 Wasserstoff bedeuten, (C) wenn R4 geradkettiges niederes Alkoxy bedeutet, R, und R3 Wasserstoff, niederes Alkyl, C3- bis C7-Alkenyl oder C3- bis C7-Alkinyl bedeuten, (D) wenn A die obige Gruppe (b), (c), (d) oder (e) bedeutet, R4 Wasserstoff bedeutet, und (E) wenn A die obige Gruppe (b) oder (e) bedeutet, R2 eine von Amino- oder mono- oder di-niederes Alkylamino-C2- bis C7-Alkyl verschiedene Bedeutung besitzt, und pharmazeutisch annehmbare Säureadditionssalze von Verbindungen der Formel I, worin A die Gruppe (a) bedeutet, sind neue Verbindungen. Sie sind nützliche Wirkstoffe und zeichnes sich durch sedative und anxiolytische Eigenschaften aus Sie können in Form von herkömmlichen pharmazeutischer Dosierungsformen verwendet werden und können ausgehend von teilweise neuen Ausgangsstoffen hergestellt werder.

  通式如下的吡咯并[3,4-d][2]苯并氮杂卓 其中 A 为基团之一 其中 A 为基团之一 R.氢、低级烷基、C3-至 C7-烯基、C7-至 C7-炔基、羟甲基或基团-ClOR11，R11 是氢、羟基、烷氧基或氨基或单或双低级烷基氨基，R3 是氢、低级烷基、C3-至 C7-烯基、羟甲基或基团-ClOR11、R3为氢、低级烷基、C3-至 C7-烯基、羟甲基或基团-COR11，R2为氢、低级烷基、C3-至 C7-烯基、C3-至 C7-炔基、基团-COO-低级烷基、C2-至 C7-羧酸及其酯和酰胺，羟基-C2-至 C7-烷基或氨基或单或二低级烷基氨基-C2-至 C7-烷基，R4 氢、酰氧基、直链低级烷氧基或羟基，R6 原子序数不大于 35 的卤素、或氢，R6 是原子序数不大于 35 的卤素，R95 是低级烷基，Z⊖ 是酸的阴离子，但如果 R 和 R3 自由基之一是羟甲基或基团 -COR11 或 -COR111、且 R11 和 R111 如上文所定义，则其余基为氢、低级烷基、C3-至 C7-烯基或 C3-至 C7-炔基，且 R2 为氢，并有进一步的但书 (A) 当 R4 为酰氧基时，R1 和 R3 为氢、(B) 当 R4 表示羟基时，R1 和 R3 表示氢、低级烷基、C3-至 C7-烯基或 C3-至 C7-炔基，R2 表示氢、(C) 当 R4 为直链低级烷氧基时，R 和 R3 表示氢、低级烷基、C3-至 C7 烯基或 C3-至 C7 烷炔基， (D) 当 A 为上述基团(b)、(c)、(d)或(e)时，R4 表示氢，以及 (E) 当 A 为上述基团(b)或(e)时、R2 具有除氨基或单或双低烷基氨基-C2 至 C7 烷基以外的含义，以及式 I 化合物的药学上可接受的酸加成盐（其中 A 为(a)基团）是新型化合物。它们是有用的活性成分，具有镇静和抗焦虑特性，可以常规药物剂型的形式使用，也可以由部分新的起始原料制备。