公开(公告)号：US4115392A

公开(公告)日：1978-09-19

申请号：US734312

申请日：1976-10-20

申请人： Hideo Kato ,  Eiichi Koshinaka ,  Sakae Kurata ,  Ikuo Uesaka

发明人： Hideo Kato ,  Eiichi Koshinaka ,  Sakae Kurata ,  Ikuo Uesaka

IPC分类号： C07D213/80 ,  C07C57/15 ,  C07D213/55

CPC分类号： C07C57/15

摘要： The monofumarate of 3-pyridylmethyl nicotinate and the method of making same. The monofumaric acid addition salt of 3-pyridylmethyl nicotinate is prepared by reacting approximately equimolar amounts of fumaric acid and 3-pyridylmethyl nicotinate.

摘要翻译： 3-吡啶基甲基烟酸的单富马酸及其制备方法。 通过使大约等摩尔量的富马酸和3-吡啶基甲基烟酸酯反应制备烟酸3-吡啶基甲基甲基酮的单富马酸加成盐。

公开(公告)号：US4612329A

公开(公告)日：1986-09-16

申请号：US786742

申请日：1985-10-11

申请人： Yasuo Itoh ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Sakae Kurata ,  Hiroyuki Nishino ,  Toshihiko Yoshida

发明人： Yasuo Itoh ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Sakae Kurata ,  Hiroyuki Nishino ,  Toshihiko Yoshida

IPC分类号： A61K31/275 ,  A61K31/445 ,  C07C20060101 ,  C07C255/58 ,  C07D20060101 ,  C07D211/08 ,  C07D295/08 ,  C07C121/78

CPC分类号： C07C255/00

摘要： Novel alpha-aminoalkyl-alpha-alkylphenylacetonitrile derivatives useful for treatment of cartino vaso diseases, a peripheral circulatory insufficiency and cerebral circulation failure are disclosed.

摘要翻译： 公开了用于治疗纸浆血管疾病，外周循环功能不全和脑循环衰竭的新型α-氨基烷基-α-烷基苯基乙腈衍生物。

公开(公告)号：US4478838A

公开(公告)日：1984-10-23

申请号：US441635

申请日：1982-11-15

申请人： Yasuo Itho ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Sakae Kurata ,  Kagari Yamagishi

发明人： Yasuo Itho ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Sakae Kurata ,  Kagari Yamagishi

IPC分类号： C07D243/08 ,  A61K31/55 ,  A61P9/08 ,  C07D295/18 ,  C07D295/185 ,  A61K31/495 ,  C07D241/04

CPC分类号： C07D295/185 ,  Y10S514/929

摘要： 1-(3,4,5-Trimethoxycinnamoyl)-4-aminocarbonylethyl-substituted piperazine derivatives represented by general formula (I): ##STR1## wherein R is a straight- or branched-chain alkyl group having 1 to 6 carbon atoms or a cycloalkyl group having 5 to 7 carbon atoms, and pharmaceutically acceptable acid addition salts thereof are disclosed.The 1-(3,4,5-trimethoxycinnamoyl)-4-aminocarbonylethyl-substituted piperazine derivatives are useful as vasodilator agents.

摘要翻译： 由通式（I）表示的1-（3,4,5-三甲氧基肉桂酰基）-4-氨基羰基乙基取代的哌嗪衍生物：其中R是具有1至6个碳原子的直链或支链烷基或 公开了具有5至7个碳原子的环烷基基团及其药学上可接受的酸加成盐。 1-（3,4,5-三甲氧基肉桂酰基）-4-氨基羰基乙基取代的哌嗪衍生物可用作血管舒张剂。

公开(公告)号：US4205074A

公开(公告)日：1980-05-27

申请号：US16515

申请日：1979-03-01

申请人： Hideo Kato ,  Eiichi Koshinaka

发明人： Hideo Kato ,  Eiichi Koshinaka

IPC分类号： C07D455/02 ,  C07D471/04 ,  A61K31/445

CPC分类号： C07D471/04 ,  C07D455/02

摘要： Phenyl- or thienyl-substituted quinolizidines and indolizidines as well as quaternary salts thereof are disclosed. These compounds are useful as pharmaceutical agents exhibiting strong spasmolytic, anti-ulcer, anti-histaminic and antiemetic activities with minimized side effects such as thirst and dilation of the pupil.Phenyl- or thienyl-substituted quinolizidine-methanols and indolizidine-methanols which are starting materials of the aforementioned quinolizidine and indolizidine compounds are also useful as having spasmolytic, anti-ulcer, anti-histaminic and anti-emetic activities.

摘要翻译： 公开了苯基或噻吩基取代的喹嗪基和吲哚嗪及其季盐。 这些化合物可用作具有强的解痉，抗溃疡，抗组胺和止吐活性的药物，其最小化的副作用如瞳孔的口渴和扩张。 作为上述喹嗪基和吲哚嗪化合物的起始原料的苯基或噻吩基取代的喹嗪基 - 甲醇和吲哚来啶 - 甲醇也可用作具有解痉，抗溃疡，抗组胺和抗呕吐活性。

公开(公告)号：US5126337A

公开(公告)日：1992-06-30

申请号：US505138

申请日：1990-04-05

申请人： Yasuo Ito ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Noriyuki Yagi ,  Toshihiko Yoshida ,  Tomio Suzuki

发明人： Yasuo Ito ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Noriyuki Yagi ,  Toshihiko Yoshida ,  Tomio Suzuki

IPC分类号： C07D513/04

CPC分类号： C07D513/04

摘要： A thiazetoquinoline-3-carboxylic acid derivative represented by the general formula (I) ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl group; R.sub.2 is a fluorine atom or a chlorine atom; R.sub.3 is a hydrogen atom, a lower alkyl group, a lower alkanoyl group, a halogenated lower alkanoyl, or alkoxycarbonyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, and a pharmacologically acceptable salt thereof, a process for preparation thereof, a pharmaceutical composition comprising the same, and a method for the treatment of an infectious disease by administering the same, are disclosed.

公开(公告)号：US5095022A

公开(公告)日：1992-03-10

申请号：US538085

申请日：1990-06-13

申请人： Yasuo Ito ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Hiroyuki Nishino ,  Jun Sakaguchi

发明人： Yasuo Ito ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Hiroyuki Nishino ,  Jun Sakaguchi

IPC分类号： C07D211/70 ,  C07D405/04

CPC分类号： C07D405/04 ,  C07D211/70

摘要： A piperidine derivative represented by the following general formula (I): ##STR1## wherein R represents a hydrogen atom or a lower alkyl group; X represents --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, or --CH.sub.2 O--; Y represents an alkylene group having 1 to 5 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an --A--O--B-- group wherein A and B are the same or different and each independently represented an alkylene group having 1 to 3 carbon atoms which may be optionally substituted with a lower alkyl group is disclosed. Also disclosed are a pharmacologically acceptable salt of a compound of formula (I), a method for preparation of a compound of formula (I), an antihistaminic and antiallergic agent comprising a compound of formula (I), a pharmaceutical composition comprising a compound of formula (I), and a method for the treatment of an allergic disease by administering a compound of formula (I).

公开(公告)号：US4534980A

公开(公告)日：1985-08-13

申请号：US633139

申请日：1984-07-23

申请人： Yasuo Itoh ,  Hideo Kato ,  Kugako Matsumura ,  Tomoyasu Nishikawa ,  Akira Hisano ,  Takehisa Yamada ,  Eiichi Koshinaka

发明人： Yasuo Itoh ,  Hideo Kato ,  Kugako Matsumura ,  Tomoyasu Nishikawa ,  Akira Hisano ,  Takehisa Yamada ,  Eiichi Koshinaka

IPC分类号： A61K9/06 ,  A61K9/00 ,  A61K31/165 ,  A61K31/19 ,  A61K47/00 ,  A61K47/16 ,  A61K47/18 ,  A61P17/00 ,  A61P25/04 ,  A61P29/00

CPC分类号： A61K9/0014 ,  A61K31/165 ,  A61K31/19 ,  A61K47/18 ,  Y10S514/871

摘要： Creams for external or topical use comprising ketoprofen as an effective component and crotamiton as an agent for preventing crystalline precipitation of the effective component. The creams possess an antiinflammatory and antipyretic effect and are excellent in permeation and absorption into the skin which enables the topical and external use of the creams.

摘要翻译： 用于外用或局部用途的霜剂，其包含酮洛芬作为有效成分，克罗他米通作为用于防止有效成分的结晶沉淀的试剂。 乳霜具有抗炎和解热作用，并且在皮肤中的渗透和吸收优异，能够局部和外部使用霜剂。

公开(公告)号：US4525356A

公开(公告)日：1985-06-25

申请号：US546481

申请日：1983-10-28

申请人： Yasuo Itho ,  Hideo Kato ,  Nobuo Ogawa ,  Kagari Yamagishi ,  Eiichi Koshinaka ,  Kazuya Mitani

发明人： Yasuo Itho ,  Hideo Kato ,  Nobuo Ogawa ,  Kagari Yamagishi ,  Eiichi Koshinaka ,  Kazuya Mitani

IPC分类号： C07D311/30 ,  C07D405/12 ,  A61K31/35 ,  C07D405/10

CPC分类号： C07D405/12 ,  C07D311/30

摘要： Derivatives of N-substituted flavone-8-carboxamides represented by general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group or an ethyl group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxyl group, a halogen atom or a nitro group, R.sub.3 represents a hydrogen atom or a lower alkyl group, k represents 0, 1, 2, or 3, m represents 0 or 1; X and Y, which must be different, represent a hydrogen atom or methyl group. A represents an amino group having the formula ##STR2## wherein, R.sub.4 and R.sub.5, which may be the same or different, represent a lower alkyl group or a cyclic amino group together with the nitrogen atom and with or without an oxygen atom, R.sub.6 represents a lower alkyl group and n represents 2 or 3, are disclosed, as well as pharmaceutical compositions thereof and method of treating therewith.The N-substituted flavone-8-carboxamides derivatives are useful as agents for treatment of dysurea.

摘要翻译： 由通式（I）表示的N-取代的黄酮-8-甲酰胺的衍生物其中R1表示氢原子，甲基或乙基，R2表示氢原子，低级烷基，低级烷氧基 卤素原子或硝基，R3表示氢原子或低级烷基，k表示0,1,2或3，m表示0或1; X和Y必须不同，表示氢原子或甲基。 A表示具有式“IMAGE”的氨基，其中可以相同或不同的R 4和R 5与氮原子一起表示低级烷基或环状氨基，并且具有或不具有氧原子，R6表示 低级烷基和n代表2或3，以及其药物组合物和其处理方法。 N-取代的黄酮-8-甲酰胺衍生物可用作治疗尿素的药剂。

公开(公告)号：US5952387A

公开(公告)日：1999-09-14

申请号：US983329

申请日：1998-01-27

申请人： Yasuo Ito ,  Hideo Kato ,  Eiichi Koshinaka ,  Masahiro Yamazaki ,  Kazuya Matsuo

发明人： Yasuo Ito ,  Hideo Kato ,  Eiichi Koshinaka ,  Masahiro Yamazaki ,  Kazuya Matsuo

IPC分类号： A61K31/137 ,  A61K47/10 ,  A61K47/26 ,  C07C215/60 ,  A61K31/135 ,  A61K33/023

CPC分类号： C07C215/60 ,  A61K31/137 ,  A61K47/10 ,  A61K47/26 ,  C07B2200/07 ,  Y10S514/935

摘要： Aqueous solution, including at least one of optically active (-)-(R)-.alpha.-((tert-butylamino)methyl)-2-chloro-4-hydroxybenzyl alcohol represented by the following formula: ##STR1## and pharmacologically acceptable salt thereof. The aqueous solution also includes at least one photostabilizer selected from the group consisting of saccharide, sugar alcohol, and polyalcohol. A content of the at least one of optically active (-)-(R)-.alpha.-((tert-butylamino)methyl)-2-chloro-4-hydroxybenzyl alcohol and pharmacologically acceptable salt thereof is 0.01 to 10% (w/v) based on a volume of the aqueous solution. A content of the at least one photostabilizer is 1 to 50% (w/v) based on the volume of the aqueous solution. The content of the at least one photostabilizer is at least 10% (w/w) based on a total weight of the at least one of optically active (-)-(R)-.alpha.-((tert-butylamino)methyl)-2-chloro-4-hydroxybenzyl alcohol and pharmacologically acceptable salt thereof. Method of making a stabilized aqueous solution.

摘要翻译： PCT No.PCT / JP96 / 01950 Sec。 371日期：1998年1月27日 102（e）日期1998年1月27日PCT提交1996年7月12日PCT公布。 公开号WO97 / 05860 日期：1997年2月20日水溶液，包括由下式表示的光学活性（ - ） - （R）-α-（（叔丁基氨基）甲基）-2-氯-4-羟基苄醇中的至少一种： 其可接受的盐。 水溶液还包括至少一种选自糖，糖醇和多元醇的光稳定剂。 光学活性（ - ） - （R）-α-（（叔丁基氨基）甲基）-2-氯-4-羟基苄醇及其药学上可接受的盐中的至少一种的含量为0.01〜10％（w / v）基于水溶液的体积。 基于水溶液的体积，至少一种光稳定剂的含量为1至50％（w / v）。 至少一种光稳定剂的含量基于光学活性（ - ） - （R）-α-（（叔丁基氨基）甲基） - 2-氯-4-羟基苄醇及其药理学上可接受的盐。 制备稳定水溶液的方法

公开(公告)号：US4971990A

公开(公告)日：1990-11-20

申请号：US301354

申请日：1989-01-24

申请人： Yasuo Itoh ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Kazuya Mitani ,  Shunichiro Sakurai

发明人： Yasuo Itoh ,  Hideo Kato ,  Eiichi Koshinaka ,  Nobuo Ogawa ,  Kazuya Mitani ,  Shunichiro Sakurai

IPC分类号： C07C311/27 ,  C07D295/26

CPC分类号： C07D295/26 ,  C07C311/27

摘要： Phenoxyethylamine derivatives represented by the general formula (I): ##STR1## wherein R.sub.1 and R.sub.5 represent lower-alkyl, R.sub.2 and R.sub.3, which may be the same or different, each represents hydrogen or lower-alkyl, or ##STR2## represents a 5- or 6-membered ring system which may include nitrogen, oxygen or sulfur as a ring membered atom, R.sub.4 represents hydrogen or lower-alkyl, and n represents an integer selected from 1 to 3, their optical isomers and pharmacologically-acceptable acid addition salts, which exhibit excellent .alpha..sub.1 -blocking activity, a process for their preparation, pharmaceutical compositions thereof, and a method for the treatment of a subject afflicted with hypertension or dysuria by administrating such a compound, are all disclosed.