公开(公告)号：US4548750A

公开(公告)日：1985-10-22

申请号：US542329

申请日：1983-10-17

申请人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

发明人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

IPC分类号： C07C45/63 ,  C07D209/48 ,  C07D223/16 ,  C07D487/04

CPC分类号： C07D209/48 ,  C07C45/63 ,  C07D223/16 ,  C07D487/04

摘要： There is presented a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, chloro, bromo, alkoxy, hydroxy, lower alkyl substituted thio and NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are hydrogen, lower alkyl and di-substituted lower alkylamino lower alkyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl and amino; R.sub.3 is selected from the group consisting of hydrogen, acyloxy and hydroxy; X is halogen and Y is hydrogen or halogen and the N-oxides thereof when R.sub.3 is hydrogenand the pharmaceutically acceptable salts thereof.The pyrimido[4,5-d][2]benzazepines are useful as anxiolytic and sedative agents.Also presented are processes and intermediates in the production of the above pyrimido[4,5-d][2]benzazepines.

摘要翻译： 存在下式的化合物，其中R 1选自氢，低级烷基，氯，溴，烷氧基，羟基，低级烷基取代的硫代和NR 4 R 5，其中R 4和R 5是氢，低级烷基和 二取代的低级烷基氨基低级烷基; R2选自氢，低级烷基和氨基; R3选自氢，酰氧基和羟基; X是卤素，Y是氢或卤素，当R 3是氢时，其N-氧化物及其可药用盐。 嘧啶并[4,5-d] [2]苯并氮杂可用作抗焦虑剂和镇静剂。 还提出了上述嘧啶并[4,5-d] [2]苯并氮杂的制备方法和中间体。

公开(公告)号：US4428878A

公开(公告)日：1984-01-31

申请号：US404664

申请日：1982-08-03

申请人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

发明人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

IPC分类号： C07C29/147 ,  C07C45/30 ,  C07C63/72 ,  C07D207/32 ,  C07D207/335 ,  C07D207/34 ,  C07D487/04

CPC分类号： C07D207/335 ,  C07C255/00 ,  C07C29/147 ,  C07C45/305 ,  C07C63/72 ,  C07D207/34 ,  C07D487/04

摘要： 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.

摘要翻译： 本发明涉及式IMA的化合物，其中R 1选自氢，低级烷基，C 3至C 7链烯基或炔基，羟甲基，其中R 11为氢，羟基，烷氧基，氨基 和单 - 或二 - 低级烷基氨基; R 3选自氢，低级烷基，C 3至C 7烯基或炔基，羟甲基，其中R 11为氢，羟基，三卤甲基，烷氧基，氨基和一或二低级烷基氨基; R2选自氢，低级烷基，C3至C7烯基或炔基，基团C2至C7羧酸及其酯和酰胺，羟基C2至C7烷基和氨基或单 - 或二 - 低级烷基氨基C2至C7烷基; R4选自氢，酰氧基，直链低级烷氧基和羟基; R5是卤素或氢; R6是卤素，条件是如果R 1或R 3中的一个是羟甲基或其中R 11如上所述的基团，则剩余的取代基选自氢，低级烷基和C 3至C 7烯基或炔基，以及 R2为氢，另外条件是（A）当R 4为酰氧基时，R 1和R 3为氢，低级烷基，C 3至C 7链烯基或C 3至C 7炔基，R 2为当R 4为羟基时的基团 那么R 1和R 3为氢，低级烷基，C 3至C 7链烯基或C 3至C 7炔基，R 2为氢或（C）当R 4为烷氧基时，R 1和R 3为氢，低级烷基，C 3至C 7链烯基或C 3至C 7 炔基及其药学上可接受的盐，其显示出作为镇静剂和抗焦虑药的活性。 还公开了吡咯并氮杂吖庚因的某些5,6二氢衍生物，N-氧化物和季铵盐。

公开(公告)号：US4427589A

公开(公告)日：1984-01-24

申请号：US286123

申请日：1981-07-23

申请人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

发明人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

IPC分类号： C07C45/63 ,  C07D209/48 ,  C07D223/16 ,  C07D487/04

CPC分类号： C07D209/48 ,  C07C45/63 ,  C07D223/16 ,  C07D487/04

摘要： There is presented a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, chloro, bromo, alkoxy, hydroxy, lower alkyl substituted thio and NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are hydrogen, lower alkyl and di-substituted lower alkylamino lower alkyl;R.sub.2 is selected from the group consisting of hydrogen, lower alkyl and amino;R.sub.3 is selected from the group consisting of hydrogen, acyloxy and hydroxy;X is halogen and Y is hydrogen or halogen and the N-oxides thereof when R.sub.3 is hydrogenand the pharmaceutically acceptable salts thereof.The pyrimido[4,5-d][2]benzazepines are useful as anxiolytic and sedative agents.Also presented are processes and intermediates in the production of the above pyrimido[4,5-d][2]benzazepines.

摘要翻译： 存在下式的化合物，其中R 1选自氢，低级烷基，氯，溴，烷氧基，羟基，低级烷基取代的硫代和NR 4 R 5，其中R 4和R 5是氢，低级烷基和 二取代的低级烷基氨基低级烷基; R2选自氢，低级烷基和氨基; R3选自氢，酰氧基和羟基; X是卤素，Y是氢或卤素，当R 3是氢时，其N-氧化物及其可药用盐。 嘧啶并[4,5-d] [2]苯并氮杂可用作抗焦虑剂和镇静剂。 还提出了上述嘧啶并[4,5-d] [2]苯并氮杂的制备方法和中间体。

公开(公告)号：US4354973A

公开(公告)日：1982-10-19

申请号：US286124

申请日：1981-07-23

申请人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

发明人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

IPC分类号： A61K31/55 ,  C07C29/147 ,  C07C45/30 ,  C07C63/72 ,  C07D207/32 ,  C07D207/335 ,  C07D207/34 ,  C07D487/04

CPC分类号： C07C29/147 ,  C07C255/00 ,  C07C45/305 ,  C07C63/72 ,  C07D207/335 ,  C07D207/34 ,  C07D487/04

摘要： 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 akyl, 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## lower alkyl, 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## lower alkoxy, (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.

摘要翻译： 本发明涉及式IMA的化合物，其中R 1选自氢，低级烷基，C 3至C 7链烯基或炔基，羟甲基，其中R 11为氢，羟基，烷氧基，氨基 和单 - 或二 - 低级烷基氨基; R 3选自氢，低级烷基，C 3至C 7链烯基或炔基，羟甲基，其中R 11为氢，羟基，三卤甲基，烷氧基，氨基和一或二低级烷基氨基; R2选自氢，低级烷基，C3至C7烯基或炔基，低级烷基，C2至C7羧酸及其酯和酰胺，羟基C2至C7烷基和氨基或单 - 或二低级烷基氨基C2至C7烷基; R4选自氢，酰氧基，直链低级烷氧基和羟基; R5是卤素或氢; R6是卤素，条件是如果R 1或R 3中的一个是羟甲基或其中R 11如上所述的基团，则剩余的取代基选自氢，低级烷基和C 3至C 7链烯基或炔基，以及 R2为氢，另外条件是（A）当R4为酰氧基时，R 1和R 3为氢，低级烷基，C 3至C 7链烯基或C 3至C 7炔基，R 2为低级烷氧基，（B） R 4为羟基，R 1和R 3为氢，低级烷基），C 3至C 7烯基或C 3至C 7炔基，R 2为氢或（C）当R 4为烷氧基时，R 1和R 3为氢，低级烷基，C 3至C 7链烯基 或C 3至C 7炔基，及其药学上可接受的盐。 还公开了吡咯并氮杂吖庚因的某些5,6二氢衍生物，N-氧化物和季铵盐。

公开(公告)号：US4243589A

公开(公告)日：1981-01-06

申请号：US99109

申请日：1979-11-30

申请人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

发明人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

IPC分类号： A61K31/55 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  C07C33/46 ,  C07C45/63 ,  C07C45/68 ,  C07C45/79 ,  C07D209/48 ,  C07D249/06 ,  C07D403/06 ,  C07D487/04 ,  C07D249/04

CPC分类号： C07D209/48 ,  A61K31/55 ,  C07C33/46 ,  C07C45/63 ,  C07C45/68 ,  C07C45/79 ,  C07D249/06 ,  C07D487/04 ,  Y10S514/906

摘要： There is presented triazolobenzazepines of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl and X and Y are hydrogen or halogenand the pharmaceutically acceptable salts thereof.Also disclosed are novel processes and intermediates leading to the triazolobenzazepines.The triazolobenzazepines are useful compounds having anxiolytic, sedative, muscle relaxant and anticonvulsant activity.

摘要翻译： 呈现式为“IMAGE”的三唑并苯并吖庚因，其中R 1是氢或低级烷基，X和Y是氢或卤素及其药物上可接受的盐。 还公开了导致三唑并苯并吖嗪的新方法和中间体。 三唑并苯并吖嗪是具有抗焦虑，镇静，肌肉松弛和抗惊厥活性的有用化合物。

公开(公告)号：US4546183A

公开(公告)日：1985-10-08

申请号：US643509

申请日：1984-08-23

申请人： Rodney I. Fryer ,  Norman W. Gilman ,  Eugene J. Trybulski ,  Armin Walser

发明人： Rodney I. Fryer ,  Norman W. Gilman ,  Eugene J. Trybulski ,  Armin Walser

IPC分类号： C07C45/63 ,  C07C45/71 ,  C07C65/34 ,  C07D209/48 ,  C07D223/16 ,  C07D239/42 ,  C07D317/16 ,  C07D317/30 ,  C07D487/04 ,  C07D211/70

CPC分类号： C07D209/48 ,  C07C45/63 ,  C07C45/71 ,  C07C65/34 ,  C07D223/16 ,  C07D239/42 ,  C07D317/16 ,  C07D317/30 ,  C07D487/04

摘要： There is presented compounds of the formula ##STR1## wherein A is selected from the group consisting of ##STR2## R.sub.1 is selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, the group NR.sub.4 R.sub.5, the group --CH.sub.2 --CO--R.sub.7, the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, hydroxy, lower alkoxy, mercapto and lower alkyl mercapto; R.sub.2 is selected from the group consisting of hydrogen, amino and di-lower alkyl amino; R.sub.3 is selected from the group consisting of hydrogen, lower acyloxy and hydroxy; X is selected from the group consisting of hydrogen, halogen, trifluoromethyl, ethyl, .alpha.-hydroxy ethyl and acetyl; Y is hydrogen or halogen; R.sub.4 and R.sub.5 are hydrogen or lower alkyl or together with their co-bonded nitrogen atom form a five to seven membered heterocyclic group; R.sub.7 is selected from the group consisting of hydroxy lower alkoxy and NR.sub.8 R.sub.9 ; R.sub.8 and R.sub.9 are hydrogen or lower alkyl; n is 0 or 1 and m is 1 to 7 with the limitations that (1) at least one of R.sub.1 and R.sub.2 are hydrogen, (2) when R.sub.3 is lower acyloxy or hydroxy, A is the group (a), X is hydrogen, halogen, trifluoromethyl, ethyl or acetyl and R.sub.1 is the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9, then R.sub.8 and R.sub.9 are lower alkyl, (3) when A is group (d) and R.sub.1 is the group --NH(CH.sub.2).sub.m NR.sub.8 R.sub.9 then R.sub.8 and R.sub.9 are lower alkyl and (4) when n is 1, R.sub.1 is hydrogen, lower alkyl, lower alkoxy, chlorine, bromine or the group --CH.sub.2 --CO--R.sub.7 with R.sub.7 as above then A is the group (a) or (b)and the pharmaceutically acceptable salts thereof.The compounds exhibit pharmacological activity as anxiolytics and sedatives.Also presented are various novel intermediates and processes to produce the above end products.

摘要翻译： 提供式IMA的化合物，其中A选自由下列组成的组：R 1选自氢，氯，溴，低级烷基，基团NR 4 R 5，基团-CH 2 -CO-R7，基团-NH（CH2）mNR8R9，羟基，低级烷氧基，巯基和低级烷基巯基; R2选自氢，氨基和二低级烷基氨基; R3选自氢，低级酰氧基和羟基; X选自氢，卤素，三氟甲基，乙基，α-羟基乙基和乙酰基; Y是氢或卤素; R4和R5是氢或低级烷基，或与它们的共键键合的氮原子一起形成5至7元杂环基; R7选自羟基低级烷氧基和NR8R9; R8和R9是氢或低级烷基; n为0或1，m为1至7，限制为（1）R 1和R 2中的至少一个为氢，（2）当R3为酰氧基或羟基时，A为（a），X为氢 ，卤素，三氟甲基，乙基或乙酰基，R 1为基团-NH（CH 2）m NR 8 R 9，则R 8和R 9为低级烷基，（3）当A为基团（d）且R 1为基团-NH（CH 2）m NR 8 R 9时 R8和R9为低级烷基，（4）当n为1时，R1为氢，低级烷基，低级烷氧基，氯，溴，或基团为-CH2-CO-R7，R7为上述，则A为（a）或 （b）及其药学上可接受的盐。 该化合物显示出作为抗焦虑药和镇静剂的药理活性。 还提出了生产上述最终产品的各种新型中间体和方法。

公开(公告)号：US4431823A

公开(公告)日：1984-02-14

申请号：US404788

申请日：1982-08-03

申请人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

发明人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

IPC分类号： C07C29/147 ,  C07C45/30 ,  C07C63/72 ,  C07D207/32 ,  C07D207/335 ,  C07D207/34 ,  C07D487/04

CPC分类号： C07D207/335 ,  C07C255/00 ,  C07C29/147 ,  C07C45/305 ,  C07C63/72 ,  C07D207/34 ,  C07D487/04

摘要： 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.

摘要翻译： 本发明涉及式IMA的化合物，其为下式化合物的中间体：其中R 1选自氢，低级烷基，C 3至C 7链烯基或炔基，羟甲基， 其中R 11是氢，羟基，烷氧基，氨基和一或二低级烷基氨基; R 3选自氢，低级烷基，C 3至C 7烯基或炔基，羟甲基，其中R 11为氢，羟基，三卤甲基，烷氧基，氨基和一或二低级烷基氨基; R2选自氢，低级烷基，C3至C7烯基或炔基，C2至C7羧酸及其酯和酰胺，羟基C2至C7烷基和氨基或单或二低级 烷基氨基C2至C7烷基; R4选自氢，酰氧基，直链低级烷氧基和羟基; R5是卤素或氢; R6是卤素，条件是如果R1或R3中的一个是羟甲基或其中R11如上所述，则剩余的取代基选自氢，低级烷基和C 3至C 7烯基或炔基，R 2 另外条件是（A）当R 4为酰氧基时，R 1和R 3为氢，低级烷基，C 3至C 7烯基或C 3 -C 7炔基，R 2为当R 4为羟基时R 1和 R3为氢，低级烷基，C3至C7烯基或C3至C7炔基，R2为氢或（C）当R4为烷氧基时，R1和R3为氢，低级烷基，C3至C7烯基或C3至C7炔基，以及 其药学上可接受的盐。 还公开了吡咯并氮杂吖庚因的某些5,6二氢衍生物，N-氧化物和季铵盐。

公开(公告)号：US4405518A

公开(公告)日：1983-09-20

申请号：US404936

申请日：1982-08-02

申请人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

发明人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

IPC分类号： C07C29/147 ,  C07C45/30 ,  C07C63/72 ,  C07D207/32 ,  C07D207/335 ,  C07D207/34 ,  C07D487/04

CPC分类号： C07D207/335 ,  C07C255/00 ,  C07C29/147 ,  C07C45/305 ,  C07C63/72 ,  C07D207/34 ,  C07D487/04

摘要： 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.

摘要翻译： 本发明涉及式IMA的化合物，其中R 1选自氢，低级烷基，C 3至C 7链烯基或炔基，羟甲基，其中R 11为氢，羟基，烷氧基，氨基 和单 - 或二 - 低级烷基氨基; R 3选自氢，低级烷基，C 3至C 7烯基或炔基，羟甲基，其中R 11为氢，羟基，三卤甲基，烷氧基，氨基和一或二低级烷基氨基; R2选自氢，低级烷基，C3至C7烯基或炔基，基团C2至C7羧酸及其酯和酰胺，羟基C2至C7烷基和氨基或单 - 或二 - 低级烷基氨基C2至C7烷基; R4选自氢，酰氧基，直链低级烷氧基和羟基; R5是卤素或氢; R 6是卤素，条件是如果R 1或R 3中的一个是羟甲基或基团 - 其中R 11如上所述，则剩余取代基选自氢，低级烷基和C 3至C 7烯基或炔基， 另外条件是（A）当R 4为酰氧基时，R 1和R 3为氢，低级烷基，C 3至C 7烯基或C 3至C 7炔基，R 2为当R 4为 羟基，则R 1和R 3为氢，低级烷基，C 3至C 7链烯基或C 3至C 7炔基，且R 2为氢或（C）当R 4为烷氧基时，R 1和R 3为氢，低级烷基，C 3至C 7链烯基或C 3至 C7炔基及其药学上可接受的盐。 还公开了吡咯并氮杂吖庚因的某些5,6二氢衍生物，N-氧化物和季铵盐。

公开(公告)号：US4299971A

公开(公告)日：1981-11-10

申请号：US173576

申请日：1980-07-30

申请人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

发明人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

IPC分类号： A61K31/55 ,  C07C45/63 ,  C07C45/68 ,  C07D209/48 ,  C07D249/06 ,  C07D487/04 ,  C07C69/76

CPC分类号： C07D209/48 ,  A61K31/55 ,  C07C45/63 ,  C07C45/68 ,  C07D249/06 ,  C07D487/04

摘要： There is presented triazolobenzazepines of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl and X and Y are hydrogen or halogenand the pharmaceutically acceptable salts thereof.Also disclosed are novel processes and intermediates leading to the triazolobenzazepines.The triazolobenzazepines are useful compounds having anxiolytic, sedative, muscle relaxant and anticonvulsant activity.

摘要翻译： 呈现式为“IMAGE”的三唑并苯并吖庚因，其中R 1是氢或低级烷基，X和Y是氢或卤素及其药物上可接受的盐。 还公开了导致三唑并苯并吖嗪的新方法和中间体。 三唑并苯并吖嗪是具有抗焦虑，镇静，肌肉松弛和抗惊厥活性的有用化合物。

公开(公告)号：US4260773A

公开(公告)日：1981-04-07

申请号：US173581

申请日：1980-07-30

申请人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

发明人： Rodney I. Fryer ,  Eugene J. Trybulski ,  Armin Walser

IPC分类号： A61K31/55 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  C07C33/46 ,  C07C45/63 ,  C07C45/68 ,  C07C45/79 ,  C07D209/48 ,  C07D249/06 ,  C07D403/06 ,  C07D487/04

CPC分类号： C07D209/48 ,  A61K31/55 ,  C07C33/46 ,  C07C45/63 ,  C07C45/68 ,  C07C45/79 ,  C07D249/06 ,  C07D487/04 ,  Y10S514/906

摘要： There is presented triazolobenzazepines of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl and X and Y are hydrogen or halogen and the pharmaceutically acceptable salts thereof.Also disclosed are novel processes and intermediates leading to the triazolobenzazepines.The triazolobenzazepines are useful compounds having anxiolytic, sedative, muscle relaxant and anticonvulsant activity.

摘要翻译： 呈现式为“IMAGE”的三唑并苯并吖庚因，其中R 1是氢或低级烷基，X和Y是氢或卤素及其药物上可接受的盐。 还公开了导致三唑并苯并吖嗪的新方法和中间体。 三唑并苯并吖嗪是具有抗焦虑，镇静，肌肉松弛和抗惊厥活性的有用化合物。