公开(公告)号：US4377523A

公开(公告)日：1983-03-22

申请号：US243092

申请日：1981-03-12

申请人： Armin Walser ,  Rodney I. Fryer

发明人： Armin Walser ,  Rodney I. Fryer

IPC分类号： C07D243/16 ,  C07D243/20 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

CPC分类号： C07D487/04 ,  C07D243/16 ,  C07D243/20 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

摘要： Novel Imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. An especially preferred genus included within the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro and halogen, most preferably, chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof, R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably, halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety and R.sub.2 is hydrogen and lower alkyl.

摘要翻译： 新型咪唑并二氮杂类及其类似物可用作抗惊厥药，肌肉松弛剂，抗焦虑药和镇静剂。 该类的优选化合物属于可能具有非常多种有机取代基的咪唑并[1,5-a] [1,4]二氮杂类。 包括在本发明的范围内的特别优选的类包括式IMA的化合物，其中R 1是氢，低级烷基优选是甲基; R3和R5是氢; R4是氢，硝基和卤素，最优选氯，最优选的实施方案中，当位于咪唑并二氮杂的稠合苯并部分位于其8-位时，R 6是苯基或卤素，硝基或低级烷基取代的 苯基，优选卤素，氟是优选的卤素，取代的氟位于苯基部分的2-位，并且R 2是氢和低级烷基。

公开(公告)号：US4376075A

公开(公告)日：1983-03-08

申请号：US243025

申请日：1981-03-12

申请人： Armin Walser ,  Rodney I. Fryer

发明人： Armin Walser ,  Rodney I. Fryer

IPC分类号： C07D243/16 ,  C07D243/20 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

CPC分类号： C07D487/04 ,  C07D243/16 ,  C07D243/20 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

摘要： Novel Imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. An especially preferred genus included within the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro and halogen, most preferably, chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof, R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably, halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety and R.sub.2 is hydrogen and lower alkyl.

摘要翻译： 新型咪唑并二氮杂类及其类似物可用作抗惊厥药，肌肉松弛剂，抗焦虑药和镇静剂。 该类的优选化合物属于可能具有非常多种有机取代基的咪唑并[1,5-a] [1,4]二氮杂类。 包括在本发明的范围内的特别优选的类包括式IMA的化合物，其中R 1是氢，低级烷基优选是甲基; R3和R5是氢; R4是氢，硝基和卤素，最优选氯，最优选的实施方案中，当位于咪唑并二氮杂的稠合苯并部分位于其8-位时，R 6是苯基或卤素，硝基或低级烷基取代的 苯基，优选卤素，氟是优选的卤素，取代的氟位于苯基部分的2-位和R2

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：US4349477A

公开(公告)日：1982-09-14

申请号：US243026

申请日：1981-03-12

申请人： Armin Walser ,  Rodney I. Fryer

发明人： Armin Walser ,  Rodney I. Fryer

IPC分类号： C07D243/16 ,  C07D243/20 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

CPC分类号： C07D487/04 ,  C07D243/16 ,  C07D243/20 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

摘要： This invention is directed toward pharmacologically active compound of the formula ##STR1## wherein A is ##STR2## R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, phenyl, alkoxy lower alkyl, halo lower alkyl, amino lower alkyl, substituted amino lower alkyl, substituted phenyl, pyridyl, aralkyl and the groups ##STR3## wherein R is hydrogen or lower alkyl and ROOC where R is lower alkyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, alkoxy lower alkyl, halo lower alkyl, amino or substituted amino lower alkyl, amino, cyano, cyano lower alkyl, substituted amino, chloro, bromo and iodo, the group --COOR where R is hydrogen or lower alkyl, the group ##STR4## where R is hydrogen or lower alkyl, or derivatives thereof, e.g., the group R--C.dbd.N--R' wherein R' is hydrogen, lower alkyl, hydroxy, phenyl, alkoxy, amino, mono or di-alkylamino and arylamino and R is hydrogen or lower alkyl, the group ##STR5## (where R and R' are individually hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl, aryl or together R and R' form a part of a heterocyclic ring and the group (CH.sub.2).sub.n NRR' where R and R' are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or together R and R' form a part of a heterocyclic ring and n is 1 to 4); the group ##STR6## where R.sup.10, R.sup.11, R.sup.12 are hydrogen or lower alkyl and the group (CH.sub.2).sub.n NR.sup.13 R.sup.14 where n is 1 to 4 and R.sup.13, R.sup.14 are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or R.sup.13 and R.sup.14 together form part of a heterocyclic ring, with the limitation that where R.sup.10, R.sup.11 or R.sup.12 is a basic side chain, then the remaining substituents are hydrogen or lower alkyl; R.sub.3 is selected from the group consisting of hydrogen and lower alkyl; R.sub.5 is selected from the group consisting of hydrogen, lower alkanoyloxy and hydroxy; R.sub.4 is selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl, substituted amino, amino, hydroxy lower alkyl and lower alkanoyl; R.sub.6 is selected from the group consisting of phenyl, mono-substituted phenyl, di-substituted phenyl, pyridyl and mono-substituted pyridyl; and ##STR7## is selected from the group consisting of ##STR8## and the pharmaceutically acceptable salts thereof. Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formulas illustrated above and their analogs are useful as anticonvulsants, muscle relaxants, anxiolytic and sedative agents.

公开(公告)号：US4349475A

公开(公告)日：1982-09-14

申请号：US242945

申请日：1981-03-12

申请人： Armin Walser ,  Rodney I. Fryer

发明人： Armin Walser ,  Rodney I. Fryer

IPC分类号： C07D243/16 ,  C07D243/20 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

CPC分类号： C07D487/04 ,  C07D243/16 ,  C07D243/20 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

摘要： This invention is directed toward pharmacologically active compound of the formula ##STR1## wherein A is ##STR2## R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, phenyl, alkoxy lower alkyl, halo lower alkyl, amino lower alkyl, substituted amino lower alkyl, substituted phenyl, pyridyl, aralkyl and the groups ##STR3## wherein R is hydrogen or lower alkyl and ROOC where R is lower alkyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, alkoxy lower alkyl, halo lower alkyl, amino or substituted amino lower alkyl, amino, cyano, cyano lower alkyl, substituted amino, chloro, bromo and iodo, the group --COOR where R is hydrogen or lower alkyl, the group ##STR4## where R is hydrogen or lower alkyl, or derivatives thereof, e.g., the group R--C.dbd.N--R' wherein R' is hydrogen, lower alkyl, hydroxy, phenyl, alkoxy, amino, mono or di-alkylamino and arylamino and R is hydrogen or lower alkyl, the group ##STR5## (where R and R' are individually hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl, aryl or together R and R' form a part of a heterocyclic ring and the group (CH.sub.2).sub.n NRR' where R and R' are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or together R and R' form a part of a heterocyclic ring and n is 1 to 4); the group ##STR6## where R.sup.10, R.sup.11, R.sup.12 are hydrogen or lower alkyl and the group (CH.sub.2).sub.n NR.sup.13 R.sup.14 where n is 1 to 4 and R.sup.13, R.sup.14 are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or R.sup.13 and R.sup.14 together form part of a heterocyclic ring, with the limitation that where R.sup.10, R.sup.11 or R.sup.12 is a basic side chain, then the remaining substituents are hydrogen or lower alkyl; R.sub.3 is selected from the group consisting of hydrogen and lower alkyl; R.sub.5 is selected from the group consisting of hydrogen, lower alkanoyloxy and hydroxy; R.sub.4 is selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl, substituted amino, amino, hydroxy lower alkyl and lower alkanoyl; R.sub.6 is selected from the group consisting of phenyl, mono-substituted phenyl, di-substituted phenyl, pyridyl and mono-substituted pyridyl; and ##STR7## is selected from the group consisting of ##STR8## and the pharmaceutically acceptable salts thereof. Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formulas illustrated above and their analogs are useful as anticonvulsants, muscle relaxants, anxiolytic and sedative agents.

公开(公告)号：US4347364A

公开(公告)日：1982-08-31

申请号：US242860

申请日：1981-03-12

申请人： Armin Walser ,  Rodney I. Fryer

发明人： Armin Walser ,  Rodney I. Fryer

IPC分类号： C07D233/66 ,  C07D243/16 ,  C07D243/20 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561 ,  C07D403/04 ,  C07D409/04

CPC分类号： C07D487/04 ,  C07D243/16 ,  C07D243/20 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

摘要： This invention is directed toward pharmacologically active compound of the formula ##STR1## R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, phenyl, alkoxy lower alkyl, halo lower alkyl, amino lower alkyl, substituted amino lower alkyl, substituted phenyl, pyridyl, aralkyl and the groups ##STR2## wherein R is hydrogen or lower alkyl and ROOC where R is lower alkyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, alkoxy lower alkyl, halo lower alkyl, amino or substituted amino lower alkyl, amino, cyano, cyano lower alkyl, substituted amino, chloro, bromo and iodo, the group--COOR where R is hydrogen or lower alkyl, the group ##STR3## where R is hydrogen or lower alkyl, or derivatives thereof, e.g., the group R--C.dbd.N--R' wherein R' is hydrogen, lower alkyl, hydroxy, phenyl, alkoxy, amino, mono or di-alkylamino and arylamino and R is hydrogen or lower alkyl, the group ##STR4## (where R and R' are individually hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl, aryl or together R and R' form a part of a heterocyclic ring and the group (CH.sub.2).sub.n NRR' where R and R' are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or together R and R' form a part of a heterocyclic ring and n is 1 to 4); the group ##STR5## where R.sup.10, R.sup.11, R.sup.12 are hydrogen or lower alkyl and the group (CH.sub.2).sub.n NR.sup.13 R.sup.14 where n is 1 to 4 and R.sup.13, R.sup.14 are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or R.sup.13 and R.sup.14 together form part of a heterocyclic ring, with the limitation that where R.sup.10, R.sup.11 or R.sup.12 is a basic side chain, then the remaining substituents are hydrogen or lower alkyl; X is a leaving group selected from the group consisting of halogen and alkyl or aryl sulfonate. R.sub.4 is selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl, substituted amino, amino, hydroxy lower alkyl and lower alkanoyl; R.sub.6 is selected from the group consisting of phenyl, mono-substituted phenyl, di-substituted phenyl, pyridyl and mono-substituted pyridyl; and ##STR6## is selected from the group consisting of ##STR7## and the pharmaceutically acceptable salts thereof. Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formulas illustrated above and their analogs are useful as anticonvulsants, muscle relaxants, anxiolytic and sedative agents.

公开(公告)号：US4307237A

公开(公告)日：1981-12-22

申请号：US178208

申请日：1980-08-14

申请人： Armin Walser ,  Rodney I. Fryer

发明人： Armin Walser ,  Rodney I. Fryer

IPC分类号： C07D233/54 ,  C07D487/14 ,  C07D495/14 ,  C07F9/6561 ,  C07D401/10 ,  C07D405/10 ,  C07D413/10

CPC分类号： C07D233/64 ,  C07D487/14 ,  C07D495/14 ,  C07F9/6561

摘要： This invention is directed toward pharmacologically active compound of the formula ##STR1## wherein A is ##STR2## R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, phenyl, alkoxy lower alkyl, halo lower alkyl, amino lower alkyl, substituted amino lower alkyl, substituted phenyl, pyridyl, aralkyl and the groups ##STR3## wherein R is hydrogen or lower alkyl and ROOC where R is lower alkyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, alkoxy lower alkyl, halo lower alkyl, amino or substituted amino lower alkyl, amino, cyano, cyano lower alkyl, substituted amino, chloro, bromo and iodo, the group --COOR where R is hydrogen or lower alkyl, the group ##STR4## where R is hydrogen or lower alkyl, or derivatives thereof, e.g., the group R--C.dbd.N--R' wherein R' is hydrogen, lower alkyl, hydroxy, phenyl, alkoxy, amino, mono or di-alkylamino and arylamino and R is hydrogen or lower alkyl, the group ##STR5## (where R and R' are individually hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl, aryl or together R and R' form a part of a heterocyclic ring and the group (CH.sub.2).sub.n NRR' where R and R' are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or together R and R' form a part of a heterocyclic ring and n is 1 to 4); the group ##STR6## where R.sup.10, R.sup.11, R.sup.12 are hydrogen or lower alkyl and the group (CH.sub.2).sub.n NR.sup.13 R.sup.14 where n is 1 to 4 and R.sup.13, R.sup.14 are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or R.sup.13 and R.sup.14 together form part of a heterocyclic ring, with the limitation that where R.sup.10, R.sup.11 or R.sup.12 is a basic side chain, then the remaining substituents are hydrogen or lower alkyl; R.sub.3 is selected from the group consisting of hydrogen and lower alkyl; R.sub.5 is selected from the group consisting of hydrogen, lower alkanoyloxy and hydroxy; R.sub.4 is selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl, substituted amino, amino, hydroxy lower alkyl and lower alkanoyl; R.sub.6 is selected from the group consisting of phenyl, mono-substituted phenyl, di-substituted phenyl, pyridyl and mono-substituted pyridyl; and ##STR7## is selected from the group consisting of ##STR8## and the pharmaceutically acceptable salts thereof. Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formulas illustrated above and their analogs are useful as anticonvulsants, muscle relaxants, anxiolytic and sedative agents.

公开(公告)号：US4257946A

公开(公告)日：1981-03-24

申请号：US123525

申请日：1980-02-21

申请人： Armin Walser

发明人： Armin Walser

IPC分类号： C07D243/16 ,  C07D487/04 ,  C07D401/06 ,  C07D403/06

CPC分类号： C07D487/04 ,  C07D243/16

摘要： A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl; Y is selected from the group consisting of hydrogen, halogen or trifluoromethyl; R.sub.1 is hydrogen or lower alkyl and R.sub.2 is disubstituted amine.Also presented are novel intermediates utilized in the process.The end products and intermediates are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.

摘要翻译： 提出了一种用于制备下式的咪唑并二氮杂的多步骤方法，其中X选自氢，卤素，硝基和三氟甲基; Y选自氢，卤素或三氟甲基; R1是氢或低级烷基，R2是二取代的胺。 还提出了在该方法中使用的新型中间体。 终产物和中间体可用作镇静剂，抗焦虑药，肌肉松弛剂和抗惊厥药。 最终产品在用于术前麻醉的静脉内组合物中特别有用。

公开(公告)号：US4250095A

公开(公告)日：1981-02-10

申请号：US139531

申请日：1980-04-11

申请人： Armin Walser

发明人： Armin Walser

IPC分类号： C07D243/16 ,  C07D487/04 ,  C07D498/04

CPC分类号： C07D487/04 ,  C07D243/16 ,  Y10S514/906

摘要： A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl, Y is selected from the group consisting of hydrogen, halogen and trifluoromethyl and R.sub.1 is selected from the group consisting of hydrogen, lower alkyl and aryl.Also presented are novel intermediates utilized in the process.The end products are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.

摘要翻译： 提出了一种多步骤方法，用于制备下式的咪唑并二氮杂其中X选自氢，卤素，硝基和三氟甲基，Y选自氢，卤素和三氟甲基，R 1选自 由氢，低级烷基和芳基组成的组。 还提出了在该方法中使用的新型中间体。 最终产品可用作镇静剂，抗焦虑药，肌肉松弛剂和抗惊厥药。 最终产品在用于术前麻醉的静脉内组合物中特别有用。

公开(公告)号：US4247463A

公开(公告)日：1981-01-27

申请号：US139533

申请日：1980-04-11

申请人： Armin Walser

发明人： Armin Walser

IPC分类号： C07D243/16 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D243/16

摘要： A multistep process is presented for the preparation of imidazobenzodiazepines of the formula wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl, Y is selected from the group consisting of hydrogen, halogen and trifluoromethyl and R.sub.1 is selected from the group consisting of hydrogen, lower alkyl and arylAlso presented are novel intermediates utilized in the process.The end products are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.

摘要翻译： 提出了一种多步骤方法，用于制备下式的咪唑并二氮杂其中X选自氢，卤素，硝基和三氟甲基，Y选自氢，卤素和三氟甲基，R 1选自 由氢，低级烷基和芳基组成的组还介绍了在该过程中使用的新型中间体。 最终产品可用作镇静剂，抗焦虑药，肌肉松弛剂和抗惊厥药。 最终产品在用于术前麻醉的静脉内组合物中特别有用。