公开(公告)号：US4396773A

公开(公告)日：1983-08-02

申请号：US306012

申请日：1981-09-28

申请人： Dong H. Kim ,  Ronald J. McCaully

发明人： Dong H. Kim ,  Ronald J. McCaully

IPC分类号： C07D209/42 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07D209/42

摘要： Disclosed herein are N-(3-mercapto-2-alkyl-1-oxopropyl)-2,3-dihydro-1H-indole-2-carboxylic acids and derivatives thereof which act as inhibitors of angiotensin converting enzyme and as anti-hypertensive agents. Derivatives include those in which the 3-mercapto group is substituted with phosphate derivatives or is replaced by a variously substituted amino group. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is -SH, ##STR2## wherein L is O, NR.sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, SR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.10 are, independently, hydrogen, lower alkyl, or aryl);A is O, NR.sub.13 or S;R.sub.11 and R.sub.12 are, independently, hydrogen, alkyl, aralkyl or aryl;R.sub.13 is hydrogen or lower alkyl;m is 0, 1, 2, or 3;R.sub.20 is hydrogen or aryl; andR.sub.21 is hydroxy or lower alkoxy;or pharmaceutically acceptable salts thereof.

摘要翻译： 本文公开了作为血管紧张素转化酶抑制剂和作为抗高血压剂的N-（3-巯基-2-烷基-1-氧代丙基）-2,3-二氢-1H-吲哚-2-羧酸及其衍生物 。 衍生物包括其中3-巯基被磷酸酯衍生物取代或被不同取代的氨基取代的衍生物。 本发明的化合物（不包括所公开的中间体）具有以下通式：其中n为1或0; R1是氢，低级烷基，芳基或芳烷基; R2是氢或低级烷基; R3是氢，低级烷基或芳酰基; R5是羟基，氨基或低级烷氧基; X是氢，羟基，低级烷基，低级烷氧基或卤素; Y是氢，低级烷基或芳基; R4是-SH，其中L是O，NR7或S（其中R7是氢或低级烷基）; M是R 8，OR 8，SR 8或NR 9 R 10（其中R 8是氢，低级烷基，芳基或芳烷基;且R 9和R 10独立地是氢，低级烷基或芳基）。 A为O，NR 13或S; R 11和R 12独立地为氢，烷基，芳烷基或芳基; R 13是氢或低级烷基; m为0,1,2或3; R 20是氢或芳基; 和R 21是羟基或低级烷氧基; 或其药学上可接受的盐。

公开(公告)号：US4454291A

公开(公告)日：1984-06-12

申请号：US391080

申请日：1982-06-22

申请人： Dong H. Kim ,  Ronald J. McCaully

发明人： Dong H. Kim ,  Ronald J. McCaully

IPC分类号： C07D209/42 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07D209/42 ,  Y02P20/55

摘要： Disclosed herein are 2,3-dihydro-1H-indole-2-carboxylic acids substituted on the nitrogen with 3-mercapto-2-alkyl-1-oxoalkyl, 3-phosphoryl-2-alkyl-1-oxopropyl, or 2-amino-2-alkyl-1-oxoalkyl derivatives which act as inhibitors of angiotensin converting enzyme and as antihypertensive agents. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen;Y is hydrogen, lower alkyl, or aryl;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is ##STR2## wherein: L is O, NR.sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, SR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.10 are, independently, hydrogen, lower alkyl, or aryl);A is O, NR.sub.13 or S;R.sub.11 and R.sub.12 are, independently, hydrogen, alkyl, aralkylor aryl;R.sub.13 is hydrogen or lower alkyl;m is 0, 1, 2, or 3;R.sub.20 is hydrogen or aryl; andR.sub.21 is hydroxy or lower alkoxy; or pharmaceutically acceptable salts thereof.Claimed compounds are intermediates of the formula: ##STR3## wherein R.sub.13 is hydrogen or lower alkyl; R.sub.14 is R.sub.5 or OZ, where R.sub.5 is hydroxy, amino, or lower alkoxy, and Z is a carboxylic acid protecting group.

摘要翻译： 本文公开了在氮上与3-巯基-2-烷基-1-氧代烷基，3-磷酰基-2-烷基-1-氧代丙基或2-氨基取代的2,3-二氢-1H-吲哚-2-羧酸 -2-烷基-1-氧代烷基衍生物，其作为血管紧张素转化酶的抑制剂和抗高血压药。 本发明的化合物（不包括所公开的中间体）具有以下通式：其中n为1或0; R1是氢，低级烷基，芳基或芳烷基; R2是氢或低级烷基; R3是氢，低级烷基或芳酰基; R5是羟基，氨基或低级烷氧基; X是氢，羟基，低级烷基，低级烷氧基或卤素; Y是氢，低级烷基或芳基; Y是氢，低级烷基或芳基; R 4是O，NR 7或S（其中R 7是氢或低级烷基）; M是R 8，OR 8，SR 8或NR 9 R 10（其中R 8是氢，低级烷基，芳基或芳烷基;且R 9和R 10独立地是氢，低级烷基或芳基）。 A为O，NR 13或S; R 11和R 12独立地为氢，烷基，芳烷基或芳基; R 13是氢或低级烷基; m为0,1,2或3; R 20是氢或芳基; 和R 21是羟基或低级烷氧基; 或其药学上可接受的盐。 所要求的化合物是下式的中间体：其中R 13是氢或低级烷基; R14是R5或OZ，其中R5是羟基，氨基或低级烷氧基，Z是羧酸保护基。

公开(公告)号：US4350633A

公开(公告)日：1982-09-21

申请号：US284433

申请日：1981-07-20

申请人： Dong H. Kim ,  Ronald J. McCaully

发明人： Dong H. Kim ,  Ronald J. McCaully

IPC分类号： C07D209/42 ,  C07D513/04 ,  C07D209/04

CPC分类号： C07D513/04 ,  C07D209/42

摘要： Disclosed herein are 2,3-dihydro-1H-indole-2-carboxylic acids substituted on the nitrogen with 3-mercapto-2-alkyl-1-oxoalkyl, 3-phosphoryl-2-alkyl-1-oxopropyl, or 2-amino-2-alkyl-1-oxoalkyl derivatives which act as inhibitors of angiotensin converting enzyme and as antihypertensive agents. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen;Y is hydrogen, lower alkyl, or aryl;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is ##STR2## wherein: L is O, NR.sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, SR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.10 are, independently, hydrogen, lower alkyl, or aryl);A is O, NR.sub.13 or S;R.sub.11 and R.sub.12 are, independently, hydrogen, alkyl, aralkyl or aryl;R.sub.13 is hydrogen or lower alkyl;m is 0, 1, 2, or 3;R.sub.20 is hydrogen or aryl; andR.sub.21 is hydroxy or lower alkoxy;or pharmaceutically acceptable salts thereof.

摘要翻译： 本文公开了在氮上与3-巯基-2-烷基-1-氧代烷基，3-磷酰基-2-烷基-1-氧代丙基或2-氨基取代的2,3-二氢-1H-吲哚-2-羧酸 -2-烷基-1-氧代烷基衍生物，其作为血管紧张素转化酶的抑制剂和抗高血压药。 本发明的化合物（不包括所公开的中间体）具有以下通式：其中n为1或0; R1是氢，低级烷基，芳基或芳烷基; R2是氢或低级烷基; R3是氢，低级烷基或芳酰基; R5是羟基，氨基或低级烷氧基; X是氢，羟基，低级烷基，低级烷氧基或卤素; Y是氢，低级烷基或芳基; Y是氢，低级烷基或芳基; R 4是O，NR 7或S（其中R 7是氢或低级烷基）; M是R 8，OR 8，SR 8或NR 9 R 10（其中R 8是氢，低级烷基，芳基或芳烷基;且R 9和R 10独立地是氢，低级烷基或芳基）。 A为O，NR 13或S; R 11和R 12独立地为氢，烷基，芳烷基或芳基; R 13是氢或低级烷基; m为0,1,2或3; R 20是氢或芳基; 和R 21是羟基或低级烷氧基; 或其药学上可接受的盐。

公开(公告)号：US4506077A

公开(公告)日：1985-03-19

申请号：US463428

申请日：1983-02-03

申请人： Ronald J. McCaully ,  Dong H. Kim

发明人： Ronald J. McCaully ,  Dong H. Kim

IPC分类号： C07D209/42 ,  C07D209/18

CPC分类号： C07D209/42

摘要： Disclosed herein is a process for obtaining indoline-2-carboxylic acid ester tin complexes directly from o-nitropyruvic acids using metallic tin and dry hydrogen chloride gas in a lower alkanol solvent, at atmospheric pressures.

摘要翻译： 本文公开的是在大气压下使用金属锡和干氯化氢气体在低级链烷醇溶剂中直接从邻硝基丙酸得到二氢吲哚-2-羧酸酯锡络合物的方法。

公开(公告)号：US4385180A

公开(公告)日：1983-05-24

申请号：US306014

申请日：1981-09-28

申请人： Dong H. Kim ,  Ronald J. McCaully

发明人： Dong H. Kim ,  Ronald J. McCaully

IPC分类号： C07D209/42 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07D209/42

摘要： Disclosed herein are N-(3-mercapto-2-alkyl-1-oxopropyl)-2,5-dihydro-1H-indole-2-carboxylic acids and derivatives thereof which act as inhibitors of angiotensin converting enzyme and as anti-hypertensive agents. Derivatives include those in which the 5-mercapto group is substituted with phosphate derivatives or is replaced by a variously substituted amino group. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is --SH, ##STR2## wherein L is O, NR.sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, SR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.10 are, independently, hydrogen, lower alkyl, or aryl);A is O, NR.sub.15 or S;R.sub.11 and R.sub.12 are, independently, hydrogen, alkyl, aralkyl or aryl;R.sub.13 is hydrogen or lower alkyl;m is 0, 1, 2, or 3;R.sub.20 is hydrogen or aryl; andR.sub.21 is hydroxy or lower alkoxy;or pharmaceutically acceptable salts thereof.

摘要翻译： 本文公开了作为血管紧张素转化酶抑制剂和作为抗高血压剂的N-（3-巯基-2-烷基-1-氧代丙基）-2,5-二氢-1H-吲哚-2-羧酸及其衍生物 。 衍生物包括其中5-巯基被磷酸酯衍生物取代或被不同取代的氨基取代的衍生物。 本发明的化合物（不包括所公开的中间体）具有以下通式：其中n为1或0; R1是氢，低级烷基，芳基或芳烷基; R2是氢或低级烷基; R3是氢，低级烷基或芳酰基; R5是羟基，氨基或低级烷氧基; X是氢，羟基，低级烷基，低级烷氧基或卤素; Y是氢，低级烷基或芳基; R4是-SH，其中L是O，NR7或S（其中R7是氢或低级烷基）; M是R 8，OR 8，SR 8或NR 9 R 10（其中R 8是氢，低级烷基，芳基或芳烷基;且R 9和R 10独立地是氢，低级烷基或芳基）。 A为O，NR15或S; R 11和R 12独立地为氢，烷基，芳烷基或芳基; R 13是氢或低级烷基; m为0,1,2或3; R 20是氢或芳基; 和R 21是羟基或低级烷氧基; 或其药学上可接受的盐。

公开(公告)号：US4352753A

公开(公告)日：1982-10-05

申请号：US220652

申请日：1980-12-29

申请人： Dong H. Kim ,  Ronald J. McCaully

发明人： Dong H. Kim ,  Ronald J. McCaully

IPC分类号： C07D209/42 ,  C07D209/12 ,  C07D209/18

CPC分类号： C07D209/42

摘要： Disclosed herein are 3[[(2,3-dihydro-1H-indole-2-yl)carbonyl]thio]propanoic (and acetic) acids of the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl, or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen; andY is hydrogen, lower alkyl, or aryl; or salts thereof.These compounds are intermediates for the production of 1H,3H-[1,4]thiazepino[4,3-a]indoles and 1H-[1,4]thiazino[4,3-a]indoles which possess Angiotensin Converting Enzyme inhibition activity and anti-hypertensive activity.

摘要翻译： 本文公开了具有以下通式的3 [[（2,3-二氢-1H-吲哚-2-基）羰基]硫代]丙酸（和乙酸），其中：n为1或0; R 1是氢，低级烷基，芳基或芳烷基; R2是氢或低级烷基; R3是氢，低级烷基或芳酰基; X是氢，羟基，低级烷基，低级烷氧基或卤素; Y为氢，低级烷基或芳基; 或其盐。 这些化合物是生产具有血管紧张素转化酶抑制活性的1H，3H- [1,4]噻吩并[4,3-a]吲哚和1H- [1,4]噻嗪并[4,3-a]吲哚的中间体 和抗高血压活动。

公开(公告)号：US4454292A

公开(公告)日：1984-06-12

申请号：US391081

申请日：1982-06-22

申请人： Dong H. Kim ,  Ronald J. McCaully

发明人： Dong H. Kim ,  Ronald J. McCaully

IPC分类号： C07D209/42 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07D209/42

摘要： Disclosed herein are 2,3-dihydro-1H-indole-2-carboxylic acids substitued on the nitrogen with 3-mercapto-2-alkyl-1-oxoalkyl, 3-phosphoryl-2-alkyl-1-oxopropyl, or 2-amino-2-alkyl-1-oxoalkyl derivatives which act as inhibitors of angiotensin converting enzyme and as antihypertensive agents. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen; Y is hydrogen, lower alkyl, or aryl;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is ##STR2## wherein: L is O, NR.sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, SR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.10 are, independently, hydrogen, lower alkyl, or aryl);A is O, NR.sub.13 or S;R.sub.11 and R.sub.12 are, independently, hydrogen, alkyl, aralkylor aryl;R.sub.13 is hydrogen or lower alkyl;m is 0, 1, 2, or 3;R.sub.20 is hydrogen or aryl; andR.sub.21 is hydroxy or lower alkoxy; or pharmaceutically acceptable salts thereof.Claimed compounds are intermediates of the formula: ##STR3## wherein R.sub.15 is hydrogen or lower alkyl.

摘要翻译： 本文公开的是在氮上取代有3-巯基-2-烷基-1-氧代烷基，3-磷酰基-2-烷基-1-氧代丙基或2-氨基的2,3-二氢-1H-吲哚-2-羧酸 -2-烷基-1-氧代烷基衍生物，其作为血管紧张素转化酶的抑制剂和抗高血压药。 本发明的化合物（不包括所公开的中间体）具有以下通式：其中n为1或0; R1是氢，低级烷基，芳基或芳烷基; R2是氢或低级烷基; R3是氢，低级烷基或芳酰基; R5是羟基，氨基或低级烷氧基; X是氢，羟基，低级烷基，低级烷氧基或卤素; Y是氢，低级烷基或芳基; Y是氢，低级烷基或芳基; R 4是O，NR 7或S（其中R 7是氢或低级烷基）; M是R 8，OR 8，SR 8或NR 9 R 10（其中R 8是氢，低级烷基，芳基或芳烷基;且R 9和R 10独立地是氢，低级烷基或芳基）。 A为O，NR 13或S; R 11和R 12独立地为氢，烷基，芳烷基或芳基; R 13是氢或低级烷基; m为0,1,2或3; R 20是氢或芳基; 和R 21是羟基或低级烷氧基; 或其药学上可接受的盐。 所要求的化合物是下式的中间体：其中R 15是氢或低级烷基。

公开(公告)号：US4303583A

公开(公告)日：1981-12-01

申请号：US164992

申请日：1980-07-01

申请人： Dong H. Kim ,  Ronald J. McCaully

发明人： Dong H. Kim ,  Ronald J. McCaully

IPC分类号： C07D209/26 ,  C07D209/42 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07C327/00 ,  C07D209/42

摘要： Disclosed herein are N-(3-mercapto-2-alkyl-1-oxopropyl)-2,3-dihydro-1H-indole-2-carboxylic acids and derivatives thereof which act as inhibitors of angiotensin converting enzyme and as anti-hypertensive agents. Derivatives include those in which the 3-mercapto group is substituted with phosphate derivatives or is replaced by a variously substituted amino group. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is --SH, ##STR2## wherein L is O, NR.sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.10 are, independently, hydrogen, lower alkyl, or aryl);A is O, NR.sub.13 or S;R.sub.11 and R.sub.12 are, independently, hydrogen, alkyl, aralkyl or aryl;R.sub.13 is hydrogen or lower alkyl;m is 0, 1, 2, or 3;R.sub.20 is hydrogen or aryl; andR.sub.21 is hydroxy or lower alkoxy;or pharmaceutically acceptable salts thereof.

摘要翻译： 本文公开了作为血管紧张素转化酶抑制剂和作为抗高血压剂的N-（3-巯基-2-烷基-1-氧代丙基）-2,3-二氢-1H-吲哚-2-羧酸及其衍生物 。 衍生物包括其中3-巯基被磷酸酯衍生物取代或被不同取代的氨基取代的衍生物。 本发明的化合物（不包括所公开的中间体）具有以下通式：其中n为1或0; R1是氢，低级烷基，芳基或芳烷基; R2是氢或低级烷基; R3是氢，低级烷基或芳酰基; R5是羟基，氨基或低级烷氧基; X是氢，羟基，低级烷基，低级烷氧基或卤素; Y是氢，低级烷基或芳基; R4是-SH，其中L是O，NR7或S（其中R7是氢或低级烷基）; M为R 8，OR 8或NR 9 R 10（其中R 8为氢，低级烷基，芳基或芳烷基;且R 9和R 10独立地为氢，低级烷基或芳基）; A为O，NR 13或S; R 11和R 12独立地为氢，烷基，芳烷基或芳基; R 13是氢或低级烷基; m为0,1,2或3; R 20是氢或芳基; 和R 21是羟基或低级烷氧基; 或其药学上可接受的盐。

公开(公告)号：US5635991A

公开(公告)日：1997-06-03

申请号：US399096

申请日：1995-03-03

申请人： Dong H. Kim

发明人： Dong H. Kim

IPC分类号： H04N9/64 ,  H04N9/77 ,  H04N5/14

CPC分类号： H04N9/77

摘要： A color signal processing system for a color television receiver which can improve the transition characteristic of a color difference signal, using the transition region of a luminance signal. The system includes a differentiator for differentiating the transition region of an input luminance signal, and a color difference signal processor for processing an input color difference signal by controlling the transition region of the color difference signal in accordance with the differentiated luminance signal. Thus, the transition characteristic of the color difference signal is compensated for in proportion to the transition characteristic of a luminance signal.

摘要翻译： 一种用于彩色电视接收机的彩色信号处理系统，其可以使用亮度信号的转变区域来改善色差信号的转换特性。 该系统包括用于区分输入亮度信号的过渡区域的微分器和通过根据微分亮度信号控制色差信号的过渡区域来处理输入色差信号的色差信号处理器。 因此，与亮度信号的转变特性成比例地补偿色差信号的转变特性。

公开(公告)号：US4849420A

公开(公告)日：1989-07-18

申请号：US148471

申请日：1988-01-26

申请人： Dong H. Kim

发明人： Dong H. Kim

IPC分类号： A61K31/55

CPC分类号： A61K31/55

摘要： This disclosure concerns antihypertensive isoquinobenzazepines of the formula ##STR1## wherein A and B may be, independently, hydrogen, hydroxy or C.sub.1 -C.sub.6 alkoxy, or A and B together may be --O--(CH.sub.2).sub.n --O-- wherein n may be 1,2 or 3;R.sup.1 and R.sup.2 may be, independently, hydrogen, hydroxy or C.sub.1 -C.sub.6 alkoxy;R.sup.3 may be hydrogen or C.sub.1 -C.sub.4 ; andX may be chlorine, bromine or iodine.

摘要翻译： 本公开涉及式XV的抗高血压异喹苯并氮平，其中A和B可以独立地是氢，羟基或C 1 -C 6烷氧基，或者A和B可以是-O-（CH 2）n O-，其中n可以是1 ，2或3; R 1和R 2可以独立地是氢，羟基或C 1 -C 6烷氧基; R3可以是氢或C1-C4; X可以是氯，溴或碘。