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1. 发明授权

US5942521A Quinolinone derivative and anti-allergic agent with said quinolinone derivative as the active ingredient 失效
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.

2. 发明授权

US4525303A Process for preparation of steroids 失效
标题翻译：类固醇的制备方法
公开(公告)号：US4525303A
公开(公告)日：1985-06-25
申请号：US505292
申请日：1983-06-17
申请人： Hidetsugu Takagaki , Shigenori Nakanishi , Yasuyuki Tanaka , Michihiro Watanabe , Yoriko Yonehara
发明人： Hidetsugu Takagaki , Shigenori Nakanishi , Yasuyuki Tanaka , Michihiro Watanabe , Yoriko Yonehara
IPC分类号： C07J5/00 , C07J21/00 , C07J71/00
CPC分类号： C07J5/0053 , C07J21/006 , C07J71/001 , C07J71/0015
摘要： A novel process for preparing a steroid of the following formula (to be referred to as compound .circle.13 ) is provided. ##STR1## This compound is known to have marked anti-inflammatory and anti-rheumatoid arthritic activity with very much reduced side effects on humans, such as weight loss, sodium retention, potassium loss and adrenal and pituitary inhibition which are observed in many steroids. The process is characterized in that starting from hydrocortisone, it can produce the desired compound .circle.13 at low cost and that it goes through the following two novel compounds (I) and (II) as intermediates. ##STR2## In the above formulae, >W--X represents >C.dbd.O or >CH--OH, >Y--Z-- represents >C.dbd.CH-- or ##STR3## Q represents a hydrogen or bromine atom, and OR.sup.1 and OR.sup.2 are identical or different and each represents an acyloxy group or a sulfuric or phosphoric acid ester residue.
摘要翻译：提供了制备下式的类固醇的新方法（以下称为化合物＆Cir＆13）。已知这种化合物具有显着的抗炎和抗类风湿关节炎活性，对人类的副作用大大减少，例如在许多类固醇中观察到的体重减轻，钠滞留，钾损失以及肾上腺和垂体抑制。该方法的特征在于，从氢化可的松开始，它可以以低成本生产所需化合物＆lt; 13＆13，并且通过以下两种新化合物（I）和（II）作为中间体。（II）在上式中，WX表示C = O或> CH-OH，YZ-表示C = CH-或Q表示氢或溴原子 OR 1和OR 2相同或不同，各自表示酰氧基或硫酸或磷酸酯残基。

3. 发明授权

US06242425B1 Quinolinone glycoside, production process, and anti-allergic agent 失效
标题翻译：喹啉酮糖苷，生产过程和抗过敏剂
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）。

4. 发明授权

US6114352A Quinolinone derivative and anti-allergic agent with said quinolinone derivative as the active ingredient 有权
标题翻译：喹啉酮衍生物和抗过敏剂与所述喹啉酮衍生物作为活性成分
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。

5. 发明授权

US5981495A Benzopyran derivative and method for treating heart disease using this derivative 失效
标题翻译：苯并吡喃衍生物和使用该衍生物治疗心脏病的方法
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。

6. 发明授权

US5068364A Chalcone derivatives and process for producing the same 失效
标题翻译： CHALCONE衍生物及其生产方法
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.

7. 发明授权

US4874855A Steroid compounds and process of preparing the same 失效
标题翻译：类固醇化合物及其制备方法
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.

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