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1. 发明授权

US5952387A Photostable aqueous solution containing benzyl alcohol derivatives 失效
标题翻译：含有苯甲醇衍生物的光稳定水溶液
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

2. 发明授权

US6162833A Photostable aqueous solution comprising benzyl alcohol derivatives 有权
标题翻译：包含苯甲醇衍生物的光稳定水溶液
公开(公告)号：US6162833A
公开(公告)日：2000-12-19
申请号：US292664
申请日：1999-04-16
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
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：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：及其药理学上可接受的盐。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）基于一定体积的水溶液。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

3. 发明授权

US5126337A Thiazetoquinoline-3-carboxylic acid derivative and a pharmaceutical composition comprising the same 失效
标题翻译：噻唑烷-3-羧酸衍生物和包含其的药物组合物
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.

4. 发明授权

US5095022A Piperidine derivatives and pharmaceutical compositions comprising the same 失效
标题翻译：哌啶衍生物和包含其的药物组合物
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).

5. 发明授权

US5344828A Piperazinealkanoic acid and a pharmaceutical composition comprising the same 失效
标题翻译：哌嗪烷酸和包含其的药物组合物
公开(公告)号：US5344828A
公开(公告)日：1994-09-06
申请号：US663154
申请日：1991-03-01
申请人： Hiroyuki Sawanishi , Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Kouji Morikawa
发明人： Hiroyuki Sawanishi , Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Kouji Morikawa
IPC分类号： A61K31/55 , A61K31/00 , A61K31/554 , A61P1/00 , A61P1/08 , A61P9/06 , A61P9/12 , A61P25/00 , A61P25/04 , A61P37/08 , A61P43/00 , C07D223/20 , C07D267/20 , C07D281/16 , C07D487/04 , C07D403/04 , C07D413/04 , C07D417/04
CPC分类号： C07D487/04 , C07D223/20 , C07D267/20 , C07D281/16
摘要： Novel polycyclic compounds represented by the following formula: A--(CH.sub.2).sub.n --COOR.sup.1, wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; n represents an integer of from 0 to 5; and A is a group represented by the following formula: ##STR1## wherein X represents a hydrogen atom or a halogen atom; and Y represents a methylene group, an oxygen atom, or a sulfur atom, or A is a group represented by the following formula: ##STR2## and pharmacologically acceptable salts thereof are disclosed. Also disclosed are a method for preparing the same, a pharmaceutical composition comprising the same, an antiallergic agent and an agent for bronchial asthma comprising the same, and a method for treatment of an allergic disease or bronchial asthma comprising the step of administering the same.
摘要翻译：由下式表示的新型多环化合物：A-（CH 2）n -COOR 1，其中R 1表示氢原子或低级烷基; n表示0〜5的整数， A是由下式表示的基团：其中X表示氢原子或卤素原子; Y表示亚甲基，氧原子或硫原子，或A为下式表示的基团：其中，可以列举出其药理学上可接受的盐。还公开了其制备方法，包含其的药物组合物，抗过敏剂和包含其的支气管哮喘剂，以及治疗过敏性疾病或支气管哮喘的方法，包括施用该过敏性疾病或支气管哮喘的步骤。

6. 发明授权

US5153207A Piperidine derivative, method for preparation thereof, and a pharmaceutical composition comprising the same 失效
标题翻译：哌啶衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US5153207A
公开(公告)日：1992-10-06
申请号：US520064
申请日：1990-05-03
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： C07D211/46 , C07D211/54
CPC分类号： C07D211/54 , C07D211/46
摘要： A piperidine derivative represented by the following general formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each independently represents a hydrogen atom, a halogen atom, a lower alkyl group, or a lower alkoxy group; R.sub.3 represents a hydrogen atom or a lower alkyl group; X represents an oxygen atom or a sulfur atom; Y represents an alkylene group having 1 to 7 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 represents 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), 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).

7. 发明授权

US5432192A Tricyclic compounds and method for treating allergic diseases 失效
标题翻译：三环化合物和治疗过敏性疾病的方法
公开(公告)号：US5432192A
公开(公告)日：1995-07-11
申请号：US122603
申请日：1993-10-01
申请人： Hiroyuki Sawanishi , Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Kouji Morikawa
发明人： Hiroyuki Sawanishi , Yasuo Ito , Hideo Kato , Eiichi Koshinaka , Nobuo Ogawa , Kouji Morikawa
IPC分类号： A61K31/195 , A61K31/335 , A61K31/35 , A61K31/352 , A61P37/08 , A61P43/00 , C07C229/14 , C07D311/80 , C07D311/82 , C07D313/12 , C07D313/14
CPC分类号： C07D313/14 , C07C229/14 , C07D311/82 , C07D313/12 , C07C2103/32
摘要： Tricyclic compounds represented by the following formula: ##STR1## wherein X represents --CH.dbd.CH--, --CH.sub.2 O--, or --O--;R.sup.1 represents a lower alkyl group,R.sup.2 represents a hydrogen atom or a lower alkyl group; andn represents an integer of from 1 to 5, pharmacologically acceptable salts thereof, and a method for preparing the same. The present compounds have anti-allergic and anti-histaminic activities and reduced side effects, and are useful as anti-allergic agents and anti-histaminic agents.
摘要翻译： PCT No.PCT / JP92 / 00365 Sec。 371日期：1993年10月1日 102（e）日期1993年10月1日PCT 1991年3月26日PCT公布。第WO92 / 17440号公报日期：10月15日，1992.由下式表示的三环化合物：其中X表示-CH = CH-，-CH 2 O-或-O-; R1表示低级烷基，R2表示氢原子或低级烷基; 和n表示1〜5的整数，其药理学上可接受的盐及其制备方法。本发明化合物具有抗过敏和抗组胺活性并减少副作用，并且可用作抗过敏剂和抗组胺剂。

8. 发明授权

US4534980A Antiinflammatory and antipyretic cream 失效
标题翻译：抗炎和解热霜
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。

9. 发明授权

US4525356A N-substituted flavone-8-carboxamides 失效
标题翻译： N-取代的黄酮-8-甲酰胺
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。

10. 发明授权

US4115392A Monofumarate salt of 3-pyridylmethyl nicotinate 失效
标题翻译： 3-吡啶基甲基烟酸的单富马酸盐
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。

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