公开(公告)号：US4080453A

公开(公告)日：1978-03-21

申请号：US663158

申请日：1976-03-02

申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

IPC分类号： C07D295/02 ,  C07D295/03 ,  C07D295/096 ,  C07D295/14 ,  A61K31/495

CPC分类号： C07D295/03 ,  C07D295/096

摘要： 1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##STR1## wherein X is 2- or 3-hydroxy, 2-methoxy, 3-methyl, 3-alkoxy having 1 to 4 carbon atoms, or 2- or 3-alkanoyloxy having 2 to 5 carbon atoms; R is allyl, 3-hydroxyisoamyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, propyl, an unsubstituted monocycloalkyl having 5 to 8 carbon atoms, 2-chlorophenyl, or a phenyl substituted by hydroxy or methoxy; with proviso that when X is a substituent at position 2, R is cyclohexyl and when X is 3-methyl, R is 2-methoxyphenyl or an unsubstituted monocycloalkyl having 6 to 8 carbon atoms, and their pharmaceutically acceptable salts, and the preparation thereof, and analgesic or antitussive compositions containing the same as the essentially active ingredient.

摘要翻译： 1-取代的4-（1,2-二苯基乙基）哌嗪衍生物，其结构式如下：其中X是2-或3-羟基，2-甲氧基，3-甲基，具有1至4个碳原子的3-烷氧基， 或具有2至5个碳原子的2-或3-烷酰氧基; R是烯丙基，3-羟基异戊基，3-甲基-2-丁烯基，3-甲基-3-丁烯基，丙基，未取代的具有5-8个碳原子的单环烷基，2-氯苯基或被羟基或甲氧基取代的苯基; 条件是当X是位置2的取代基时，R是环己基，当X是3-甲基时，R是2-甲氧基苯基或未取代的具有6-8个碳原子的单环烷基及其药学上可接受的盐及其制备方法， 以及含有与基本上活性成分相同的镇痛或镇咳药物。

公开(公告)号：US3988456A

公开(公告)日：1976-10-26

申请号：US561336

申请日：1975-03-24

申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

IPC分类号： C07D295/08 ,  A61K31/495 ,  A61P9/12 ,  A61P11/14 ,  A61P25/00 ,  A61P25/04 ,  C07D213/74 ,  C07D295/084 ,  C07D295/10

CPC分类号： C07D295/092 ,  Y10S514/849

摘要： 1,2-Diphenylethanolamine derivatives of the formula: ##SPC1##Wherein R.sub.1 and R.sub.2 are each hydrogen, a halogen, nitro, hydroxy, an alkyl or methoxy; R.sub.3 is a group of the formula: ##SPC2##Wherein R.sub.4, R.sub.5 and R.sub.6 are each hydrogen, a halogen or methoxy and n is an integer of 0 to 3, or a pyridyl; and Z is hydroxy or an acyloxy; with proviso that when R.sub.1 and/or R.sub.2 are hydroxy, Z is hydroxy, and their pharmaceutically acceptable salts, which have excellent analgesic and anti-tussive activities, and a process for the preparation thereof.

摘要翻译： 下式的1,2-二苯乙醇胺衍生物：

公开(公告)号：US3957788A

公开(公告)日：1976-05-18

申请号：US541351

申请日：1975-01-15

申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

IPC分类号： C07D295/02 ,  C07D295/03 ,  C07D295/096 ,  C07D295/145 ,  C07D295/08

CPC分类号： C07D295/03 ,  C07D295/096 ,  C07D295/145 ,  Y10S514/849

摘要： 1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##SPC1##Wherein X is hydroxy, methoxy, methyl or trifluoromethyl; and R is an unsubstituted monocycloalkyl group having 6 to 8 carbon atoms or 2-methoxyphenyl; provided that when X is hydroxy, R is cyclohexyl, and when X is trifluoromethyl, R is 2-methoxyphenyl,And their pharmaceutically acceptable salts, which have excellent analgesic, anti-tussive and anti-inflammatory activities, without undesirable side effect such as narcotic activity, and a process for the preparation thereof.

公开(公告)号：US4162316A

公开(公告)日：1979-07-24

申请号：US821918

申请日：1977-08-04

申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

IPC分类号： C07D295/02 ,  C07D295/03 ,  C07D295/096 ,  C07D241/04 ,  A61K31/495

CPC分类号： C07D295/03 ,  C07D295/096

摘要： 1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##STR1## wherein X is 2- or 3-hydroxy, 2-methoxy, 3-methyl, 3-alkoxy having 1 to 4 carbon atoms, or 2- or 3-alkanoyloxy having 2 to 5 carbon atoms; R is allyl, 3-hydroxyisoamyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, propyl, an unsubstituted monocycloalkyl having 5 to 8 carbon atoms, 2-chlorophenyl, or a phenyl substituted by hydroxy or methoxy; with proviso that when X is a substituent at position 2, R is cyclohexyl and when X is 3-methyl, R is 2-methoxyphenyl or an unsubstituted monocycloalkyl having 6 to 8 carbon atoms, and their pharmaceutically acceptable salts, and the preparation thereof, and analgesic or antitussive compositions containing the same as the essentially active ingredient.