公开(公告)号：US5525595A

公开(公告)日：1996-06-11

申请号：US312192

申请日：1994-09-26

申请人： Hidetsugu Takagaki ,  Masayoshi Abe ,  Yasuo Aoki ,  Yoshiyuki Sano ,  Mitsuru Sakai ,  Nobuyuki Kimura

发明人： Hidetsugu Takagaki ,  Masayoshi Abe ,  Yasuo Aoki ,  Yoshiyuki Sano ,  Mitsuru Sakai ,  Nobuyuki Kimura

IPC分类号： C07H17/075 ,  A61K31/70

CPC分类号： C07H17/075 ,  Y10S514/826 ,  Y10S514/829 ,  Y10S514/885

摘要： There are provided novel compounds of the formulae I and II: ##STR1## and their physiologically acceptable salts. The compounds according to the present invention and their physiologically acceptable salts exhibit an antiallergic activity and are useful for treating allergic diseases.

摘要翻译： 提供式I和II的新化合物：其中（I）和（II）化合物及其生理上可接受的盐。 根据本发明的化合物及其生理上可接受的盐表现出抗过敏​​活性，并且可用于治疗过敏性疾病。

公开(公告)号：US6114352A

公开(公告)日：2000-09-05

申请号：US223271

申请日：1998-12-30

申请人： Hidetsugu Takagaki ,  Masayoshi Abe ,  Mitsuru Sakai ,  Yasuo Aoki ,  Shigenori Nakanishi ,  Nobuyuki Kimura ,  Akihide Koda

发明人： Hidetsugu Takagaki ,  Masayoshi Abe ,  Mitsuru Sakai ,  Yasuo Aoki ,  Shigenori Nakanishi ,  Nobuyuki Kimura ,  Akihide Koda

IPC分类号： A61K31/00 ,  A61K31/47 ,  A61K31/4704 ,  A61P11/00 ,  A61P11/06 ,  A61P37/00 ,  A61P37/08 ,  C07D215/22 ,  C07D215/38

CPC分类号： C07D215/22 ,  C07D215/38

摘要： The present invention offers 7-aminoquinolinone derivatives, physiologically acceptable salts thereof, anti-allergic agents having as an active ingredient a 7-aminoquinolinone derivative or physiologically acceptable salt thereof, and 7-nitroquinolinone derivatives, wherein the 7-aminoquinolinone derivative is expressed by the following general formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl group;R.sub.2 and R.sub.3 are mutually different groups, each of which is selected from among hydrogen atoms, acyl groups, alkyl groups or alkenyl groups; andR.sub.4 and R.sub.5 are mutually different or identical groups, each of which is selected from among hydrogen atoms, acyl groups, alkyl groups, alkenyl groups or aralkyl groups;and physiologically acceptable salts thereof.

摘要翻译： 本发明提供了7-氨基喹啉酮衍生物，其生理上可接受的盐，作为活性成分的7-氨基喹啉酮衍生物或其生理学上可接受的盐的抗过敏剂和7-硝基喹啉酮衍生物，其中7-氨基喹啉酮衍生物由 通式（I）：其中R 1是氢原子或烷基; R2和R3是相互不同的基团，其各自选自氢原子，酰基，烷基或烯基; 并且R 4和R 5是相互不同或相同的基团，其各自选自氢原子，酰基，烷基，烯基或芳烷基; 及其生理上可接受的盐。

公开(公告)号：US5942521A

公开(公告)日：1999-08-24

申请号：US784915

申请日：1997-01-16

申请人： Hidetsugu Takagaki ,  Masayoshi Abe ,  Mitsuru Sakai ,  Yasuo Aoki ,  Shigenori Nakanishi ,  Nobuyuki Kimura ,  Akihide Koda

发明人： Hidetsugu Takagaki ,  Masayoshi Abe ,  Mitsuru Sakai ,  Yasuo Aoki ,  Shigenori Nakanishi ,  Nobuyuki Kimura ,  Akihide Koda

IPC分类号： A61K31/00 ,  A61K31/47 ,  A61K31/4704 ,  A61P11/00 ,  A61P11/06 ,  A61P37/00 ,  A61P37/08 ,  C07D215/22 ,  C07D215/38

CPC分类号： C07D215/22 ,  C07D215/38

摘要： The present invention offers 7-aminoquinolinone derivatives, physiologically acceptable salts thereof, anti-allergic agents having as an active ingredient a 7-aminoquinolinone derivative or physiologically acceptable salt thereof, and 7-nitroquinolinone derivatives, wherein the 7-aminoquinolinone derivative is expressed by the following general formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl group;R.sub.2 and R.sub.3 are mutually different groups, each of which is selected from among hydrogen atoms, acyl groups, alkyl groups or alkenyl groups; andR.sub.4 and R.sub.5 are mutually different or identical groups, each of which is selected from among hydrogen atoms, acyl groups, alkyl groups, alkenyl groups or aralkyl groups; and physiologically acceptable salts thereof.

公开(公告)号：US5580552A

公开(公告)日：1996-12-03

申请号：US446115

申请日：1995-05-19

申请人： Hidetsugu Takagaki ,  Masayoshi Abe ,  Yasuo Aoki ,  Mitsuru Sakai ,  Nobuyuki Kimura

发明人： Hidetsugu Takagaki ,  Masayoshi Abe ,  Yasuo Aoki ,  Mitsuru Sakai ,  Nobuyuki Kimura

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P37/08 ,  C07H17/075 ,  A01N43/04

CPC分类号： C07H17/075 ,  Y02P20/55

摘要： A 7-glycosyloxybenzopyran derivative represented by the following formula (I) ##STR1## wherein, R is a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an alkenyl group or an aralkyl group, R.sub.2 is a hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group or an aralkyl group and R.sub.3 is a glycosyl group whose hydroxyl group is protected or not protected, selected from the group consisting of glucosyl, mannosyl and galactosyl groups, and physiologically acceptable salts thereof.

摘要翻译： 由下式（I）表示的7-糖氧基苯并吡喃衍生物其中，R为氢原子，酰基，烷基，环烷基，链烯基或芳烷基，R2为 氢原子，烷基，环烷基，烯基或芳烷基，R3是羟基被保护或未被保护的糖基，选自葡糖基，甘露糖基和半乳糖基，以及生理上可接受的盐 其中。

公开(公告)号：US5428059A

公开(公告)日：1995-06-27

申请号：US938132

申请日：1992-11-20

申请人： Hidetsugu Takagaki ,  Mitsuru Sakai ,  Hiromu Takahashi ,  Kazuhiko Inazawa ,  Masayoshi Abe ,  Nobuyuki Kimura

发明人： Hidetsugu Takagaki ,  Mitsuru Sakai ,  Hiromu Takahashi ,  Kazuhiko Inazawa ,  Masayoshi Abe ,  Nobuyuki Kimura

IPC分类号： C07D311/56 ,  A61K31/35

CPC分类号： C07D311/56

摘要： The present invention relates to an extremely effective anti-allergic agent with a low toxicity, which possesses as its active ingredient a benzopyran derivative described by the general formula below (in the formula, R.sup.1 and R.sup.2 are each respectively a hydrogen atom, an acyl group, an alkyl group having 1.about.12 carbon atoms, or an alkenyl group having 2.about.10 carbon atoms; and R.sup.3 is a hydroxyl group, an acyloxy group, an alkoxy group having 1.about.10 carbon atoms, or an alkenyloxy group having 2.about.10 carbon atoms).General Formula ##STR1##

摘要翻译： PCT No.PCT / JP92 / 00095 Sec。 371日期：1992年11月20日 102（e）1992年11月20日PCT PCT 1992年1月31日PCT公布。 第WO92 / 13852号公报 本发明涉及一种毒性低的极有效的抗过敏剂，它具有下列通式所示的苯并吡喃衍生物作为其活性成分（式中，R1和R2各自分别为 氢原子，酰基，具有1个碳原子的烷基或具有2个碳原子的烯基; R3是羟基，酰氧基，具有1-10个碳原子的烷氧基， 或具有2个碳原子的烯氧基）。 通用公式

公开(公告)号：US5981495A

公开(公告)日：1999-11-09

申请号：US821569

申请日：1997-03-19

申请人： Hidetsugu Takagaki ,  Nobuyuki Kimura ,  Yasuo Aoki ,  Shigenori Nakanishi ,  Masayoshi Abe ,  Osamu Misumi

发明人： Hidetsugu Takagaki ,  Nobuyuki Kimura ,  Yasuo Aoki ,  Shigenori Nakanishi ,  Masayoshi Abe ,  Osamu Misumi

IPC分类号： A61K31/37 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/76 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07D311/56 ,  C07H17/075 ,  A61K31/35 ,  C07D311/08

CPC分类号： C07H17/075 ,  A61K31/37 ,  C07D311/56

摘要： The present invention offers a safe and effective drug for heart diseases and a safe and effective method for treating heart diseases such as ischemic heart disease and cardiac arrhythmia. The method comprises administering a pathologically effective amount of a benzopyran derivative expressed by the following general formula (I): ##STR1## wherein R.sup.1 is an alkyl group or an alkenyl group, R.sup.2 is a hydrogen atom, an alkyl group, an alkyl group having at least one hydroxyl group, an alkenyl group, an acyl group or a glycosyl group; or physiologically acceptable salts thereof.

摘要翻译： 本发明提供一种安全有效的心脏病药物，以及治疗缺血性心脏病和心律失常等心脏病的安全有效的方法。 该方法包括施用病理有效量的由以下通式（I）表示的苯并吡喃衍生物：其中R1是烷基或烯基，R2是氢原子，烷基，具有至少一个 羟基，烯基，酰基或糖基; 或其生理上可接受的盐。

公开(公告)号：US06242425B1

公开(公告)日：2001-06-05

申请号：US09231492

申请日：1999-01-14

申请人： Hidetsugu Takagaki ,  Shigenori Nakanishi ,  Nobuyuki Kimura ,  Shinobu Yamaguchi ,  Yasuo Aoki

发明人： Hidetsugu Takagaki ,  Shigenori Nakanishi ,  Nobuyuki Kimura ,  Shinobu Yamaguchi ,  Yasuo Aoki

IPC分类号： A01N4304

CPC分类号： C07H17/02 ,  C07H15/26

摘要： An object is to provide: novel quinolinone glycosides which are useful as medicines; processes for producing the quinolinone glycosides; intermediates for synthesis; and medicines, and particularly anti-allergic agents, which comprise the quinolinone glycoside as an active ingredient. The object is achieved by: a quinolinone glycoside or a physiologically acceptable salt thereof; processes for producing this quinolinone glycosides; intermediates for synthesis; and medicines, and particularly anti-allergic agents, which comprise the quinolinone glycoside as an active ingredient; the quinolinone glycoside being expressed by general formula (I): (wherein, in the formula, each of R1 and R2 is a hydrogen atom or a glycosyl group selected from the group consisting of a glucuronyl group, a glucosyl group, a galactosyl group and a mannosyl group, and at least one of R1 and R2 is a glycosyl group in which a hydroxyl group in the glycosyl group is unprotected or protected with an acyl group having a carbon number of 2 to 7 or a benzyl group).

摘要翻译： 目的是提供：作为药物有用的新型喹啉酮糖苷; 制备喹啉酮糖苷的方法; 合成中间体; 以及包含喹啉酮糖苷作为活性成分的药物，特别是抗过敏剂。 该目的通过以下方法实现：喹啉酮糖苷或其生理上可接受的盐; 制备该喹啉酮糖苷的方法; 合成中间体; 以及包含喹啉酮糖苷作为活性成分的药物，特别是抗过敏剂; 喹啉酮糖苷由通式（I）表示:(式中，R 1和R 2各自为氢原子或选自葡糖醛酸基，葡糖基，半乳糖基和 甘油基，并且R1和R2中的至少一个是其中糖基中的羟基被未被保护或用碳数为2至7的酰基或苄基保护的糖基）。

公开(公告)号：US06670391B2

公开(公告)日：2003-12-30

申请号：US10178238

申请日：2002-06-25

申请人： Hidetsugu Takagaki ,  Shingo Tanabe ,  Nobuyuki Kimura ,  Yasuo Aoki

发明人： Hidetsugu Takagaki ,  Shingo Tanabe ,  Nobuyuki Kimura ,  Yasuo Aoki

IPC分类号： A61K3135

CPC分类号： A61K31/37 ,  C07D311/56

摘要： The present invention provides a compound which is highly safe in terms of toxicity and has a stronger antiallergic action, and particularly has an action of inhibiting both immediate and delayed type allergic reactions. A benzopyran derivative represented by the general formula (I): wherein R1 is an alkyl group having 1-10 carbon atoms or an alkenyl group having 2-10 carbon atoms, and one of R2, R3, R4, and R5 is an alkoxy group substituted with a hydroxy group or an alkoxy group substituted with a carboxy group, and the others are hydrogen atoms or physiologically acceptable salts thereof are superior as the active ingredient of an antiallergic agent.

摘要翻译： 本发明提供了一种在毒性方面高度安全并且具有更强的抗过敏作用的化合物，特别是具有抑制立即和延迟型过敏反应的作用。 由通式（I）表示的苯并吡喃衍生物：其中R 1是具有1-10个碳原子的烷基或具有2-10个碳原子的烯基，R 2，R 3， R 4，R 5为被羟基或被羧基取代的烷氧基取代的烷氧基，其余为氢原子或其生理学上可接受的盐作为抗过敏剂的活性成分优异 。

公开(公告)号：US07081256B2

公开(公告)日：2006-07-25

申请号：US10171982

申请日：2002-06-17

申请人： Ryuji Kubota ,  Hiroshi Araya ,  Kouki Obata ,  Nobuyuki Kimura ,  Hiroyuki Fukui ,  Hidetsugu Takagaki

发明人： Ryuji Kubota ,  Hiroshi Araya ,  Kouki Obata ,  Nobuyuki Kimura ,  Hiroyuki Fukui ,  Hidetsugu Takagaki

IPC分类号： A61K9/14 ,  A61K9/16 ,  A61K31/47

CPC分类号： A61K31/4704 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/205 ,  A61K9/2054

摘要： A quinolinone derivative pharmaceutical composition comprising a quinolinone derivative represented by the structural formula (I): wherein the quinolinone derivative is in the form of particles, which have an average particle diameter of 0.5 to 10 μm and such a particle size distribution that particles having a particle diameter of 15 μm or less account for 90% or more of the totality of the particles, and also have a fusion enthalpy of 30 J/g or more, and the surface of the particles are coated with a water-soluble composition containing a water-soluble polymer, can quickly dissolve an active ingredient in the digestive tract and is also superior in long-term storage stability.

公开(公告)号：US06706733B2

公开(公告)日：2004-03-16

申请号：US10177137

申请日：2002-06-24

申请人： Nobuyuki Kimura ,  Hiroyuki Fukui ,  Hidetsugu Takagaki ,  Nahoko Muratake

发明人： Nobuyuki Kimura ,  Hiroyuki Fukui ,  Hidetsugu Takagaki ,  Nahoko Muratake

IPC分类号： A61K3147

CPC分类号： C07D215/227

摘要： The problem to be solved by the present invention is to provide a quinolinone derivative formulation, and its production method, having for its active ingredient the &bgr; crystal form and/or &ggr; crystal form of the quinolinone derivative represented with chemical formula (I), which is useful as a pharmaceutical, and particularly as an antiallergic, which has superior bioabsorption and stability. The present invention provides a quinolinone derivative, and its production method, having for its active ingredient the &bgr; crystal form and/or &ggr; crystal form of the quinolinone derivative represented with chemical formula (I):

摘要翻译： 本发明要解决的问题是提供一种喹啉酮衍生物制剂及其制备方法，其具有由化学式（I）表示的喹啉酮衍生物的β晶型和/或γ晶形式的活性成分，其中 可用作药物，特别是作为抗过敏药物，其具有优异的生物吸收和稳定性。 本发明提供了一种喹啉酮衍生物及其制备方法，其具有化学式（I）表示的喹啉酮衍生物的β晶型和/或γ晶形式的活性成分：