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    Pyrimido-2-benzazepines
    3.
    发明授权
    Pyrimido-2-benzazepines 失效
    嘧啶-2-苯并吖庚因

    公开(公告)号：US4481142A

    公开(公告)日：1984-11-06

    申请号：US437047

    申请日：1982-10-27

    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 ,  C07C45/68 ,  C07C45/71 ,  C07C65/34 ,  C07C291/04 ,  C07C309/66 ,  C07D209/48 ,  C07D223/16 ,  C07D239/42 ,  C07D317/16 ,  C07D317/30 ,  C07D487/04

    CPC分类号： C07D209/48 ,  C07C291/04 ,  C07C309/66 ,  C07C45/63 ,  C07C45/68 ,  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 dilower 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，NR 4 R 5基团，基团 -CH 2 -CO-R 7，基团-NH（CH 2）m NR 8 R 9，羟基，低级烷氧基，巯基和低级烷基巯基; R2选自氢，氨基和二元烷基氨基; 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-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。 还提出了各种新型中间体和方法来生产上述最终产品。

    Pyrrolo[3,4-d][2]benzazepinones
    4.
    发明授权
    Pyrrolo[3,4-d][2]benzazepinones 失效
    吡咯并[3,4-d] [2]苯并氮杂

    公开(公告)号：US4436662A

    公开(公告)日：1984-03-13

    申请号：US481021

    申请日：1983-03-31

    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 ,  C07C51/347 ,  C07D207/34 ,  C07D209/94 ,  C07D487/04 ,  C07D487/02

    CPC分类号： C07D487/04 ,  C07C255/00 ,  C07C29/147 ,  C07C45/305 ,  C07C51/347 ,  C07D207/34 ,  C07D209/94

    摘要： The present invention relates to compounds of the formula ##STR1## wherein R.sub.1 and R.sub.3 are selected from the group consisting of hydrogen, lower alkyl, hydroxy, lower alkoxy or acyloxy and R.sub.2 and R.sub.4 are hydrogen or R.sub.1 and R.sub.2 and/or R.sub.3 and R.sub.4 taken together are oxo groups with the proviso that at least one oxo group is present; R is selected from the group consisting of hydrogen, 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 C.sub.2 to C.sub.7 alkyl or mono- or di-lower alkyl amino C.sub.2 to C.sub.7 alkyl; R.sub.5 is halogen or hydrogen; and R.sub.6 is halogen with the proviso that when R.sub.1 or R.sub.3 is hydroxy, lower alkoxy or acyloxy, then R is lower alkyl or hydrogen and the N-oxides and the pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及下式化合物：其中R1和R3选自氢，低级烷基，羟基，低级烷氧基或酰氧基，R2和R4是氢或R1，R2和/或R3和R4 一起是氧基，条件是存在至少一个氧代基团; R选自氢，低级烷基，C 2至C 7羧酸及其酯和酰胺，羟基C 2至C 7烷基和氨基C 2至C 7烷基或单 - 或二 - 低级烷基氨基C 2至C 7烷基; R5是卤素或氢; 并且R 6为卤素，条件是当R 1或R 3为羟基，低级烷氧基或酰氧基时，则R为低级烷基或氢，以及其N-氧化物及其药学上可接受的盐。

    Pyrimido-2-benzazepines and intermediates in their preparation
    5.
    发明授权
    Pyrimido-2-benzazepines and intermediates in their preparation 失效
    嘧啶-2-苯并吖庚因及其制备中间体

    公开(公告)号：US4547581A

    公开(公告)日：1985-10-15

    申请号：US643563

    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 ,  C07C45/68 ,  C07C291/04 ,  C07C309/66 ,  C07D209/48 ,  C07D223/16 ,  C07D317/00

    CPC分类号： C07D209/48 ,  C07C291/04 ,  C07C309/66 ,  C07C45/63 ,  C07C45/68 ,  C07D223/16

    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（a）（b）（c）和（d）R1选自组 由氢，氯，溴，低级烷基，基团NR4R5，基团-CH2-CO-R7，基团-NH（CH2）mNR8R9，羟基，低级烷氧基，巯基和低级烷基巯基组成; 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。

    Pyrrolo[3,4,-d][2]benzazepines
    6.
    发明授权
    Pyrrolo[3,4,-d][2]benzazepines 失效
    吡咯并[3,4，d] [2]苯并吖庚因

    公开(公告)号：US4428879A

    公开(公告)日：1984-01-31

    申请号：US404787

    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。

    Pyrrolo[3,4-D][2]Benzazepines
    7.
    发明授权
    Pyrrolo[3,4-D][2]Benzazepines 失效
    吡咯并[3,4-D] [2]苯并氮杂

    公开(公告)号：US4409390A

    公开(公告)日：1983-10-11

    申请号：US404935

    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 ,  C07D207/333

    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; 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。 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。

    3H-2-Benzazepines
    10.
    发明授权
    3H-2-Benzazepines 失效
    3H-2-苯并氮杂

    公开(公告)号：US4549988A

    公开(公告)日：1985-10-29

    申请号：US509256

    申请日：1983-06-29

    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

    CPC分类号： C07D209/48 ,  C07C45/63 ,  C07D223/16 ,  Y10S514/906

    摘要： There is presented 3H-2-benzazepines and 4,5-dihydro-3H-2-benzazepines of the formula ##STR1## wherein X is hydrogen, chloro or bromo, Y is hydrogen, fluoro or chloro with the proviso that X and Y cannot both be hydrogen and R.sub.1 is selected from the group consisting of hydrogen, bromo, chloro, iodo, a radical of the formula ##STR2## and a radical of the formula ##STR3## wherein R.sub.2 is hydrogen, phthalimido, lower alkyl, hydroxy, amino, monoalkylamino and dialkylamino and R.sub.3 is hydroxy, phthalimido or amino with the proviso that where R.sub.1 is other than hydrogen then the bonding at the 4,5-position is unsaturated,and the pharmaceutically acceptable salts thereof.

    摘要翻译： 提出了具有式“IMAGE”的3H-2-苯并吖庚因和4,5-二氢-3H-2-苯并吖庚因，其中X是氢，氯或溴，Y是氢，氟或氯，条件是X和Y不能 二者均为氢，R 1选自氢，溴，氯，碘，式“IMAGE”基团和式“IMAGE”基团，其中R 2为氢，苯二甲酰亚氨基，低级烷基，羟基，氨基 ，单烷基氨基和二烷基氨基，并且R 3是羟基，苯二甲酰亚氨基或氨基，条件是其中R 1不是氢，则4位的键合是不饱和的，及其药学上可接受的盐。