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：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：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：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：US5068364A

公开(公告)日：1991-11-26

申请号：US439435

申请日：1989-11-21

申请人： Hidetsugu Takagaki ,  Shigenori Nakanishi ,  Masayoshi Abe ,  Hiromi Ohki ,  Yoshiyuki Sano

发明人： Hidetsugu Takagaki ,  Shigenori Nakanishi ,  Masayoshi Abe ,  Hiromi Ohki ,  Yoshiyuki Sano

IPC分类号： C07C45/67 ,  C07C49/835 ,  C07C49/84 ,  C07D309/12

CPC分类号： C07D309/12 ,  C07C45/673 ,  C07C49/835 ,  C07C49/84

摘要： Chalcone derivatives having at least one tetrahydropyranyloxy group is disclosed. Typically, the compounds are represented by general formula (I) ##STR1## wherein X and X' each represent a tetrahydropyranyl group, R and R', which are then same or different, each represent an alkyl group or a hydrogen atom, n and n' each are an integer of from 0 to 5, m and m' each are integers of from 0 to 5, provided that n+n' is 1 or more, and that n+m is an integer of from 0 to 5 and n'+m' is an integer of from 0 to 5. Also, disclosed are processes for producing the chalcone derivatives starting from acetophenone or its derivative and benzaldehyde or its derivative at least one of which has at least one tetrahydropyranyloxy group. Further, disclosed is 2,3,4,2',4'-pentahydroxychalcone.

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：US06271416B1

公开(公告)日：2001-08-07

申请号：US09595909

申请日：2000-06-20

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： C07C22900

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 general formula (I), is reacted with a basic agent, followed by intramolecular ring formation: General Formula (I) [wherein, R1 represents a hydrogen atom, an alkyl group, an alkyl group containing a hydroxyl group, an alkenyl group, or an aryl group; R2 represents an alkyl group, an alkenyl group, an aryl group, or an aralkyl group; R3 represents a reactive carboxyl group; and R4 to R7 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 R8R9N group (wherein, R8 and R9 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 R10OOC group (wherein, R10 represents a hydrogen atom, an alkyl group, an alkenyl group, an aryl group, or an aralkyl group)]. General Formula (II) [wherein, R1, R2 and R4 to R7 represent, respectively, the same constituents as described in general 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; 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以下通式（I）表示的酰胺衍生物与碱性试剂反应，然后分子内环形成：通式（I）[其中，R 1表示氢原子，烷基 基团，含有羟基，烯基或芳基的烷基; R2表示烷基，烯基，芳基或芳烷基; R3代表活性羧基; R 4〜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）]通式（II）[其中，R1，R2和R4至R7分别表示与通式（I）中所述相同的组分] 。

公开(公告)号：US4874855A

公开(公告)日：1989-10-17

申请号：US189849

申请日：1988-05-03

申请人： Hidetsugu Takagaki ,  Masayoshi Abe ,  Michihiro Watanabe ,  Kazuyuki Takeuchi ,  Shigenori Nakanishi ,  Yuuko Nakata ,  Keiji Yamazaki

发明人： Hidetsugu Takagaki ,  Masayoshi Abe ,  Michihiro Watanabe ,  Kazuyuki Takeuchi ,  Shigenori Nakanishi ,  Yuuko Nakata ,  Keiji Yamazaki

IPC分类号： C07J5/00 ,  C07J51/00

CPC分类号： C07J5/0053 ,  C07J51/00

摘要： Disclosed are steroid compounds represented by general formula (I) ##STR1## wherein X and W together as >W-X represent a carbonyl group (>C.dbd.O) or a hydroxymethylene group (>CH(OH)), the hydroxy moiety of the hydroxymethylene group being of .beta.-arrangement, and OR.sup.1 and OR.sup.2 independently represent an ester residue, and Y and Z together as --Y--Z-- represent a --(PpSe)CH--CH.sub.2 -- group where Pp represent a phenyl group or a 2-pyridyl group, or Y and Z each represent an ethenylene group or a 1-bromoethylene group.Also disclosed is a process of preparing the compound (I) includes reacting 6.beta., 9.alpha.-difluoro-5.alpha.,17.alpha.,21-trihydroxypregna-3,11,20-trione-17,21-diesters or 6.beta.,9.alpha.-difluoro-5.alpha.,11.beta.,17.alpha.,21-tetrahydroxypregna-3,20-dione-17,21-diesters as starting compound with an organic selenenyl halide selected from the group consisting of 2-pyridylselenenyl chloride, 2-pyridylselenenyl bromide, phenylselenenyl chlolride and phenylselenenyl bromide.Further disclosed is a process of preparing 2-bromo-6.beta.,9.alpha.-difluoro-11.beta.,17.alpha.,21-trihydroxy-1,4-pregnadien-3,20-di-one-17,21-diester represented by general formula (VII) ##STR2## wherein OR.sup.1 and OR.sup.2 independently represent an ester residue, which comprises reacting with hydrogen chloride, or with thionyl chloride in the presence of a basic substance, the compound (V), and optionally reducing with a reducing agent when >W-X represents a carbonyl group.