公开(公告)号：US4528299A

公开(公告)日：1985-07-09

申请号：US530096

申请日：1983-09-07

申请人： Hitoshi Uno ,  Tadahiko Karasawa ,  Tatsuya Kon ,  Tsugutaka Ito

发明人： Hitoshi Uno ,  Tadahiko Karasawa ,  Tatsuya Kon ,  Tsugutaka Ito

IPC分类号： C07D295/10 ,  A61K31/40 ,  A61P25/00 ,  A61P25/08 ,  C07D295/108 ,  C07D207/04

CPC分类号： C07D295/108

摘要： 1-(2,3-Dimethyl-4-methoxyphenyl)-2-methyl-3-(1-pyrrolidinyl)-1-propanone and its pharmaceutically acceptable acid addition salts, which are useful as centrally acting muscle relaxants in the treatment of spasticity in mammals including humans, process for the preparation thereof, and pharmaceutical composition containing said compound as an active ingredient.

摘要翻译： 1-（2,3-二甲基-4-甲氧基苯基）-2-甲基-3-（1-吡咯烷基）-1-丙酮及其药学上可接受的酸加成盐，其用作中枢作用的肌肉松弛剂用于治疗痉挛状态 在包括人的哺乳动物中，其制备方法和含有所述化合物作为活性成分的药物组合物。

公开(公告)号：US4870074A

公开(公告)日：1989-09-26

申请号：US42474

申请日：1987-04-24

申请人： Tatsuya Kon ,  Shiro Kato ,  Toshiya Morie ,  Kazunori Ohno ,  Katsuhiko Hino ,  Tadahiko Karasawa ,  Naoyuki Yoshida

发明人： Tatsuya Kon ,  Shiro Kato ,  Toshiya Morie ,  Kazunori Ohno ,  Katsuhiko Hino ,  Tadahiko Karasawa ,  Naoyuki Yoshida

IPC分类号： A61K31/535 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  C07D265/30 ,  C07D267/08 ,  C07D267/10 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12

CPC分类号： C07D265/30 ,  C07D267/10 ,  C07D413/06 ,  C07D413/12

摘要： Compounds of the formula: ##STR1## wherein R is hydrogen, alkoxycarbonyl, benzyloxycarbonyl, heteroarylalkyl, phenylalkenyl, or --T--(Y).sub.p --R.sub.6 (wherein T is single bond or alkylene, Y is oxygen, sulfur or carbonyl, R.sub.6 is phenyl, substituted phenyl, naphthyl, or diphenylmethyl, and p is 0 or 1, provided that when T is single bond, p is 0); R.sub.1 is halogen, hydroxy, alkoxy, cycloalkyloxy, alkenyloxy, alkynyloxy, alkoxy interrupted by oxygen or carbonyl, alkylthio, amino, monosubstituted amino, or a substituted alkoxy; R.sub.2 is hydrogen; R.sub.3 is hydrogen, halogen, amino, alkylamino, dialkylamino, alkanoylamino, or nitro; R.sub.4 is hydrogen, halogen, nitro, sulfamoyl, alkylsulfamoyl, or dialkylsulfamoyl; or any two adjacent groups of the R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may combine to form alkylenedioxy, and the remaining two groups are each hydrogen; R.sub.5 is hydrogen or alkyl; X is alkylene; m and n are each 1 or 2; provided that at least one of the groups R.sub.2, R.sub.3 and R.sub.4 is other than hydrogen, and acid addition salts, quaternary ammonium salts and N-oxide derivatives thereof, processes for preparation thereof, and pharmaceutical composition containing the same. Said compounds, salts and N-oxide derivatives thereof show excellent gastrointestinal motility enhancing activity.

公开(公告)号：US5017573A

公开(公告)日：1991-05-21

申请号：US384766

申请日：1989-07-25

申请人： Tatsuya Kon ,  Shiro Kato ,  Toshiya Morie ,  Tadahiko Karasawa ,  Naoyuki Yoshida

发明人： Tatsuya Kon ,  Shiro Kato ,  Toshiya Morie ,  Tadahiko Karasawa ,  Naoyuki Yoshida

IPC分类号： A61K31/55 ,  A61P1/00 ,  A61P1/08 ,  A61P9/00 ,  A61P25/00 ,  A61P25/04 ,  A61P43/00 ,  C07D243/08 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

CPC分类号： C07D401/14 ,  C07D243/08 ,  C07D403/12 ,  C07D405/14

摘要： An indazole-3-carboxylic acid derivative represented by the following general formula (I) or its physiologically acceptable acid addition salt or quaternary ammonium salt, ##STR1## wherein Y represents --NH-- or --O--; R.sub.1 and R.sub.2 are identical or different and each represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group, or R.sub.1 and R.sub.2, taken together, form a lower alkylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, or a phenyl group; R.sub.4 represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group; R.sub.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a trifluoromethyl group, a nitro group, an amino group or an acylamino group; m represents a number of 1, 2, 3 or 4; n represents a number of 1, 2 or 3; and p represents a number of 1, 2, 3 or 4.This compound is useful as a potent and selective antagonist of serotonin 3 (5--HT.sub.3) receptor.

公开(公告)号：US5166341A

公开(公告)日：1992-11-24

申请号：US670443

申请日：1991-03-11

申请人： Tatsuya Kon ,  Shiro Kato ,  Toshiya Morie ,  Tadahiko Karasawa ,  Naoyuki Yoshida

发明人： Tatsuya Kon ,  Shiro Kato ,  Toshiya Morie ,  Tadahiko Karasawa ,  Naoyuki Yoshida

IPC分类号： C07D243/08 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14

CPC分类号： C07D401/14 ,  C07D243/08 ,  C07D403/12 ,  C07D405/14

摘要： Indazole-3-carboxylic acid derivatives represented by the following general formula (I) and their physiologically acceptable acid addition salts or quaternary ammonium salts, ##STR1## are useful as a potent and selective antagonist of serotonin 3 (5-HT.sub.3) receptor. Also disclosed are compounds of the formula ##STR2## which are useful as intermediates in the production of the disclosed final product compounds.

摘要翻译： 由下列通式（I）表示的吲唑-3-羧酸衍生物及其生理上可接受的酸加成盐或季铵盐可用作5-羟色胺3（5-HT 3）受体的有效和选择性拮抗剂。 还公开了式（IMAGE）的化合物，其可用作制备所公开的最终产品化合物的中间体。

公开(公告)号：US4237135A

公开(公告)日：1980-12-02

申请号：US022779

申请日：1979-03-22

申请人： Hitoshi Uno ,  Yasutaka Nagai ,  Tadahiko Karasawa ,  Kiyoshi Furukawa

发明人： Hitoshi Uno ,  Yasutaka Nagai ,  Tadahiko Karasawa ,  Kiyoshi Furukawa

IPC分类号： A61K31/38 ,  A61K31/495 ,  A61P25/24 ,  A61P25/26 ,  C07D215/38 ,  C07D401/04

CPC分类号： C07D215/38

摘要： 2-(4-Ethyl-1-piperazinyl)-4-phenylquinoline and its pharmaceutically acceptable acid addition salts, which are useful as antidepressant agents in the treatment of depression or depressive state in mammals including humans, and processes for the preparation thereof.

摘要翻译： 2-（4-乙基-1-哌嗪基）-4-苯基喹啉及其药学上可接受的酸加成盐，其可用作抗抑郁药用于治疗包括人在内的哺乳动物的抑郁或抑郁状态及其制备方法。

公开(公告)号：US3983239A

公开(公告)日：1976-09-28

申请号：US557642

申请日：1975-03-12

申请人： Yasutaka Nagai ,  Hitoshi Uno ,  Masanao Shimizu ,  Tadahiko Karasawa

发明人： Yasutaka Nagai ,  Hitoshi Uno ,  Masanao Shimizu ,  Tadahiko Karasawa

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： Hexahydro-.gamma.-carboline derivatives of the formula: ##SPC1##Wherein R.sub.1 is methyl or ethyl, and R.sub.2 is hydrogen, methyl or ethyl, with proviso that when R.sub.1 is ethyl, R.sub.2 is hydrogen, and their pharmaceutically acceptable acid addition salts, which exhibit excellent psychotropic effect, and a process for the preparation thereof.

摘要翻译： 下式的六氢-γ-咔啉衍生物：