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：US08980914B2

公开(公告)日：2015-03-17

申请号：US10565828

申请日：2004-07-27

申请人： Hidetsugu Takagaki ,  Yasuo Aoki ,  Mitsuteru Ishiwara ,  Nobuaki Mizutani

发明人： Hidetsugu Takagaki ,  Yasuo Aoki ,  Mitsuteru Ishiwara ,  Nobuaki Mizutani

IPC分类号： A61K31/00 ,  A61K31/4704 ,  C07D215/38

CPC分类号： A61K31/4704 ,  C07D215/38

摘要： This therapeutic agent for chronic obstructive pulmonary disease comprises, an active ingredient, at least one of a 7-aminoquinolinone derivative represented by the general formula (I): wherein R1 represents a hydrogen atom or an alkyl group; R2 and R3 each represents a group selected from a hydrogen atom, an acyl group, an alkyl group and an alkenyl group; and R4 and R5 each represents a group selected from a hydrogen atom, an acyl group, an alkyl group, an alkenyl group and an aralkyl group, and its physiologically acceptable salt.

摘要翻译： 该慢性阻塞性肺疾病治疗剂包含活性成分，由通式（I）表示的7-氨基喹啉酮衍生物中的至少一种：其中R1表示氢原子或烷基; R2和R3各自表示选自氢原子，酰基，烷基和烯基的基团; R 4和R 5各自表示选自氢原子，酰基，烷基，烯基和芳烷基的基团及其生理学上可接受的盐。

公开(公告)号：US20090099256A1

公开(公告)日：2009-04-16

申请号：US12084052

申请日：2006-10-23

申请人： Hidetsugu Takagaki ,  Yasuo Aoki ,  Mitsuteru Ishiwara

发明人： Hidetsugu Takagaki ,  Yasuo Aoki ,  Mitsuteru Ishiwara

IPC分类号： A61K31/353 ,  C07D311/56 ,  A61P9/00

CPC分类号： C07D311/56 ,  A61K31/37

摘要： The present invention relate to a drug for treating circulatory insufficiency containing a benzopyran derivative represented by the following general formula (I): and/or a physiologically acceptable salt thereof as an active ingredient, wherein R1 is an alkyl group having 1 to 10 carbon atoms, or an alkenyl group having 2 to 10 carbon atoms; and any one of R2, R3, R4 and R5 is a hydroxyl group, an alkoxy group, an alkenyloxy group, an alkoxy group substituted with a hydroxyl group, or an alkoxy group substituted with a carboxy group, and the others are hydrogen atoms.

摘要翻译： 本发明涉及含有下列通式（I）表示的苯并吡喃衍生物的循环功能不全药物：和/或其生理学上可接受的盐作为有效成分，其中R1为碳原子数1〜10的烷基 ，或具有2〜10个碳原子的烯基; R 2，R 3，R 4和R 5中的任一个是羟基，烷氧基，烯氧基，被羟基取代的烷氧基或被羧基取代的烷氧基，其它是氢原子。

公开(公告)号：US20080269345A1

公开(公告)日：2008-10-30

申请号：US10594545

申请日：2005-03-29

申请人： Hidetsugu Takagaki ,  Yoshiyuki Sano ,  Yasuyuki Katakami ,  Masanori Miyamoto

发明人： Hidetsugu Takagaki ,  Yoshiyuki Sano ,  Yasuyuki Katakami ,  Masanori Miyamoto

IPC分类号： A61K31/14 ,  C07C217/54 ,  A61P7/00 ,  A61P9/00

CPC分类号： C07C217/22 ,  A61K31/205 ,  C07C309/42

摘要： A quaternary ammonium compound of the present invention is a quaternary ammonium compound represented by general formula (I) or (I′) (wherein, A represents a linear alkyl group having 1 to 4 carbon atoms, a branched alkyl group having 2 to 4 carbon atoms, a linear alkyl group having 1 to 4 carbon atoms and a hydroxyl group, or a branched alkyl group having 2 to 4 carbon atoms and a hydroxyl group, R1 to R3 may be the same or different and represent a linear or branched alkyl group having 1 to 12 carbon atoms, one of R4 to R8 represents CO2− or SO3−, while no more than three of the remaining R4 to R8 represent a group selected from the group consisting of a hydroxyl group and an alkoxy group having 1 to 4 carbon atoms, and other R4 to R8 represent a hydrogen atom, one of R′4 to R′8 represents CO2H or SO3H, no more than three of the remaining R′4 to R′8 represent a group selected from a protected hydroxyl group and an alkoxy group having 1 to 4 carbon atoms, while other R′4 to R′8 represent a hydrogen atom, and X− represents an anion capable of forming a salt with a quaternary ammonium group).

摘要翻译： 本发明的季铵化合物是通式（I）或（I'）表示的季铵化合物（其中，A表示碳原子数1〜4的直链烷基，碳原子数2〜4的支链烷基 原子，具有1至4个碳原子和羟基的直链烷基或具有2至4个碳原子和羟基的支链烷基，R 1至R 3， SUB>可以相同或不同，表示具有1至12个碳原子的直链或支链烷基，R 4至R 8中的一个表示CO 2 ^{- 或SO 3 - ，而不超过三个剩余的R 4至R 8表示选自羟基和碳原子数1〜4的烷氧基的基团，以及其它R 4〜R 8， SUB>表示氢原子，R'4'至R'8之一表示CO 2 H或SO 3}

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：

公开(公告)号：US06627642B1

公开(公告)日：2003-09-30

申请号：US09830584

申请日：2001-05-08

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： A61K31/4704 ,  C07D215/38

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：

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：US6136822A

公开(公告)日：2000-10-24

申请号：US201662

申请日：1998-12-01

申请人： Hidetsugu Takagaki ,  Shinobu Yamaguchi ,  Masayoshi Abe ,  Mitsuru Sakai ,  Osamu Misumi

发明人： Hidetsugu Takagaki ,  Shinobu Yamaguchi ,  Masayoshi Abe ,  Mitsuru Sakai ,  Osamu Misumi

IPC分类号： C07D215/22 ,  A61K31/00 ,  A61K31/47 ,  A61K31/4704 ,  A61P37/00 ,  A61P37/08 ,  C07C235/16 ,  C07D215/38 ,  C07D215/40 ,  C07D215/48 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D215/16 ,  C07D215/20 ,  C07D215/36

CPC分类号： C07D215/22 ,  C07C235/16 ,  C07D215/38 ,  C07D215/40 ,  C07D215/48 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06

摘要： The present invention relates to a simple method for preparing a quinolinone derivative, which is effective as a medicine, e.g., as an agent for treating allergic diseases and the like; novel amide derivatives effective as an intermediate in the method; novel quinolinone derivatives obtained according to the method; and an anti-allergic agent containing a quinolinone derivative and/or physiological salt of the same as the active ingredients. The quinolinone derivative is expressed by the following general formula (II); and the method is characterized in that an amide derivative, expressed by the following formula (I), is reacted with a basic agent, followed by intramolecular ring formation: ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkyl group containing a hydroxyl group an alkenyl group, or an aryl group; R.sub.2 represents an alkyl group, an alkenyl group, an aryl group, or an aralkyl group; R.sub.3 represents a reactive carboxyl group; and R.sub.4 to R.sub.7 represent, respectively and independently, a hydrogen atom; a hydroxyl group; an alkyl group; an alkoxy group; an alkenyl group; an alkenyloxy group; an aryl group; an aryloxy group; an aralkyloxy group; a R.sub.8 R.sub.9 N group wherein R.sub.8 and R.sub.9 represent, respectively and independently, a hydrogen atom, an alkyl group, an alkenyl group an aralkyl group, or an acyl group; a nitro group; or a R.sub.10 OOC group wherein R.sub.10 represents a hydrogen atom, an alkyl group, an alkenyl group, an aryl group, or an aralkyl group; ##STR2## wherein R.sub.1, R.sub.2 and R.sub.4 to R.sub.7 represent, respectively, the same constituents as described in formula (I).

摘要翻译： 本发明涉及一种制备喹啉酮衍生物的简单方法，其作为药物是有效的，例如用作治疗过敏性疾病等的药剂; 在该方法中作为中间体有效的新型酰胺衍生物; 按照该方法得到的新型喹啉酮衍生物; 以及含有与活性成分相同的喹啉酮衍生物和/或其生理盐的抗过敏剂。 喹啉酮衍生物由以下通式（II）表示; 该方法的特征在于将由下式（I）表示的酰胺衍生物与碱性试剂反应，然后分子内环形成：其中R 1表示氢原子，烷基，含有羟基的烷基 烯基或芳基; R2表示烷基，烯基，芳基或芳烷基; R3代表活性羧基; 和R 4至R 7分别独立地表示氢原子; 羟基; 烷基; 烷氧基 烯基; 烯氧基; 芳基; 芳氧基; 芳烷氧基; R8R9N基，其中R8和R9分别独立地表示氢原子，烷基，烯基，芳烷基或酰基; 硝基; 或R10OOC基，其中R10表示氢原子，烷基，烯基，芳基或芳烷基; 其中R1，R2和R4至R7分别表示与式（I）中所述相同的组分。

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。