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1.发明专利6-(heterocycle-substituted benzyl)-4-oxoquinoline compound and use of the same as hiv integrase inhibitor 有权6-（杂环取代的苯甲基）-4-氧杂环丁烷化合物及其作为HIV整合酶抑制剂的用途
公开(公告)号：JP2008110960A
公开(公告)日：2008-05-15
申请号：JP2007164676
申请日：2007-06-22
申请人： Japan Tobacco Inc , 日本たばこ産業株式会社
发明人： SATO MOTOHIDE , ARAMAKI HISAAKI , YAMASHITA MASAKI , INOUE AKIFUMI , KAWAKAMI HIROSHI , SHINKAI HISASHI , NAKAMURA HIROSHI , MATSUZAKI YUJI , WAMAKI SHUICHI
IPC分类号： C07D215/56 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P31/18 , A61P43/00 , C07D401/10 , C07D413/10 , C07D417/10 , C12N9/99 , C12N15/09
CPC分类号： C07D215/56 , C07D401/10 , C07D413/10 , C07D417/10
摘要： PROBLEM TO BE SOLVED: To provide a new 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, or a solvate of the compound or the salt useful as an anti-HIV agent. SOLUTION: The invention relates to a compound represented by the general formula [I], a pharmaceutically acceptable salt thereof, or a solvate of the compound or the salt; and a pharmaceutical composition, an anti-HIV agent, and an HIV integrase inhibitor, each comprising the compound. The compound has an action of inhibiting the HIV integrase activity, and therefore is useful as an anti-HIV agent or a therapeutic or prophylactic agent for AIDS. By using in combination with other anti-HIV agent such as a protease inhibitor and a reverse transcriptase inhibitor, the compound can act as a more effective anti-HIV agent. Further, because of its high inhibitory activity specifically against an integrase, the compound can act as an agent which is safe for a human body and has few adverse side-effects. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译： 要解决的问题：提供新的4-氧代喹啉化合物或其药学上可接受的盐，或者可用作抗HIV剂的化合物或盐的溶剂合物。 解决方案：本发明涉及由通式[I]表示的化合物，其药学上可接受的盐或化合物或其盐的溶剂合物; 以及各自包含该化合物的药物组合物，抗HIV剂和HIV整合酶抑制剂。 该化合物具有抑制HIV整合酶活性的作用，因此可用作抗HIV剂或用于AIDS的治疗或预防剂。 通过与其他抗HIV剂如蛋白酶抑制剂和逆转录酶抑制剂组合使用，该化合物可以作为更有效的抗HIV剂。 此外，由于其对整合酶具有高的抑制活性，所以该化合物可以作为对人体安全并且几乎没有不良副作用的药剂。 版权所有（C）2008，JPO＆INPIT
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公开(公告)号：JP2005002092A
公开(公告)日：2005-01-06
申请号：JP2003391228
申请日：2003-11-20
申请人： Japan Tobacco Inc , 日本たばこ産業株式会社
发明人： SATO MOTOHIDE , KAWAKAMI HIROSHI , ITO YOSHIHARU , SHINKAI HISASHI , MOTOMURA TAKANAO , ARAMAKI HISAAKI , MATSUZAKI YUJI , WATANABE WATARU , WAMAKI SHUICHI
IPC分类号： C12N9/99 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/5377 , A61P31/12 , A61P31/18 , A61P37/04 , A61P43/00 , C07D215/56 , C07D215/58 , C07D401/06 , C07D409/06 , C07D417/06 , C07D471/04
摘要： PROBLEM TO BE SOLVED: To provide an anti-HIV agent that has the HIV integrase inhibitory activity. SOLUTION: This invention relates to an anti-HIV agent that includes 4-oxoquinoline compound represented by general formula [I] or its pharmaceutically acceptable salts and relates to the anti-HIV agent including these compounds. The compound according to this invention has the action to inhibit the HIV integrase activity and is used as an anti-HIV agent for treating or preventing AIDS. Further, this anti-HIV agent is combined with other anti-HIV agent, for example, a protease inhibitor or a reverse transcriptase inhibitor to give more effective anti-HIV agents. The fact that this inhibitor has specifically high inhibitory action to integrase means that this substance can become a medicine that is safe to human bodies with reduced side effects. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译： 待解决的问题：提供具有HIV整合酶抑制活性的抗HIV剂。 本发明涉及包含由通式[I]表示的4-氧代喹啉化合物或其药学上可接受的盐的抗HIV剂，涉及包括这些化合物在内的抗HIV剂。 根据本发明的化合物具有抑制HIV整合酶活性的作用，并且用作用于治疗或预防AIDS的抗HIV剂。 此外，该抗HIV剂与其它抗HIV剂例如蛋白酶抑制剂或逆转录酶抑制剂组合以产生更有效的抗HIV剂。 该抑制剂对整合酶具有特别高的抑制作用的事实意味着该物质可以成为对人体有安全作用的药物，副作用降低。 版权所有（C）2005，JPO＆NCIPI
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公开(公告)号：JPH0641174A
公开(公告)日：1994-02-15
申请号：JP19700792
申请日：1992-07-23
申请人： JAPAN TOBACCO INC
发明人： MATSUMOTO KATSUYA , EBATA TAKASHI , KOSEKI YUKIFUMI , OKANO KOJI , KAWAKAMI HIROSHI , MATSUSHITA HAJIME
摘要： PURPOSE:To provide a method to efficiently obtain the subject compound useful for medicines, agricultural chemicals, etc., in a high yield by reacting a compound obtained by adding an iodine group and an acyloxy group to a double bond of anhydrodideoxythreohexoenopyranose under specific conditions. CONSTITUTION:In a compound of formula II (R is an acyl) obtained by adding an iodine group at alpha configuration to 4-position of the double bond of 1,6- anhydro-3,4-dideoxy-beta-D-threo-hexo-3-enopyranose of formula I and adding an acyloxy ion at beta configuration to 3-position of the double bond of the compound of formula I to carry out trans-addition, the acyloxy group is hydrolyzed in the presence of a base to afford a compound of formula III having an oxirane ring at beta configuration. The ring of this compound is reductively opened and the hydroxyl group is protected to give a compound of formula IV (R is a protecting group of hydroxy group). The 1,6-anhydro bond and the protecting group of the hydroxy group of the compound of formula IV are hydrolyzed with an acid to provide the compound of formula V.
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公开(公告)号：JPH0641107A
公开(公告)日：1994-02-15
申请号：JP19700892
申请日：1992-07-23
申请人： JAPAN TOBACCO INC
发明人： MATSUMOTO KATSUYA , EBATA TAKASHI , KOSEKI YUKIFUMI , OKANO KOJI , KAWAKAMI HIROSHI , MATSUSHITA HAJIME
IPC分类号： C07D307/33 , C07D493/04 , C07D493/08 , C07D493/18 , C07H3/10
摘要： PURPOSE:To easily and selectively produce the compound from an easily available raw material in a high yield. CONSTITUTION:The (3R,4R)-3-hydroxy-4-hydroxymethyl-4-butanolide of formula VI can be produced by reducing the 2-carbonyl group of a levoglucosenone of formula I easily available as a thermal decomposition product of cellulose to obtain a compound of formula II having beta-configuration hydroxyl group, adding a configuration iodine group to the 4-site and beta-configuration acyloxy ion to the 3-site of the double bond of the compound by trans-addition reaction, hydrolyzing the acyloxy group in the presence of a base, oxidizing the 2-hydroxyl group of the resultant compound of formula III having oxirane ring at beta-configuration, reductively opening the oxirane ring of the produced compound of formula IV to obtain the compound of formula V unsubstituted at 3-site and having beta-configuration hydroxyl group at 4-site and, finally, subjecting the compound of formula V to Baeyer-Villiger oxidization.
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公开(公告)号：JPH0525152A
公开(公告)日：1993-02-02
申请号：JP20460191
申请日：1991-07-22
申请人： JAPAN TOBACCO INC
IPC分类号： C07D307/33 , C07D307/60
摘要： PURPOSE:To easily and selectively obtain the subject compound known as an intrinsic feeding stimulant in short steps compared with conventional synthetic process by using gamma-ribonolactone as a raw material. CONSTITUTION:The objective (2S,4S)-2-hydroxy-4-hydroxymethyl-4-butanolide (3-DAP-lactone) of formula V can be produced by introducing protecting groups R (e.g. acetyl, pivaloyl or benzoyl) to the 2- and 5-hydroxyl groups of gamma- ribonolactone of formula I to obtain the compound of formula II, subjecting the product to beta-elimination with an elimination group (e.g. mesyl group or trifluoromethanesulfonyl group) in the presence of a basic compound to eliminate the 3-hydroxyl group and form a double bond between the 2- and 3-sites, reducing the double bond between the 2- and 3-sites of the obtained compound of formula III by catalytic hydrogenation and finally eliminating the protecting group of the resultant compound of formula IV.
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公开(公告)号：JPH03109383A
公开(公告)日：1991-05-09
申请号：JP24645589
申请日：1989-09-25
发明人： EBATA TAKASHI , KAWAKAMI HIROSHI , KOSEKI YUKIFUMI , MATSUSHITA HAJIME , ITO KAZUO , NAOI YOSHITAKA
IPC分类号： C07D307/20
摘要： PURPOSE:To obtain the title compound useful for AIDS-related researches by protecting hydroxyl group of tetrahydrofurfuryl alcohol, then oxidizing to give lactone and reducing. CONSTITUTION:Hydroxyl group of tetrahydrofurfuryl alcohol shown by formula I is protected to give a compound shown by formula II (R is OH-protecting group), which is oxidized with ruthenium oxide to give a lactone shown by formula III. Then the lactone is reduced with diisobutyl aluminum hydride to give the objective compound shown by formula IV.
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公开(公告)号：JPH0352880A
公开(公告)日：1991-03-07
申请号：JP18481789
申请日：1989-07-19
发明人： KOSEKI YUKIFUMI , EBATA TAKASHI , KAWAKAMI HIROSHI , MATSUSHITA HAJIME , ITO KAZUO , NAOI YOSHITAKA
IPC分类号： C07D307/58
摘要： PURPOSE:To obtain the title compound useful as a synthetic raw material for drugs such as prostaglandin and anti-leukemic lignan inexpensively and in high yield by oxidizing levoglucosenone as a starting raw material with a peracid in an organic solvent. CONSTITUTION:Levoglucosenone as a raw material is oxidized with a peracid in an organic solvent at room temperature while stirring to give the objective compound. Peracetic acid, m-chloroperbenzoic acid, magnesium monoperoxyphthalate.6 hydrate, etc., may be cited as the peracid. The amount of the peracid used is 1.0-3.0mols based on 1mol levoglucosenone. Acetic acid, methylene chloride, methanol, etc., are properly used as the organic solvent. Levoglucosenone can be inexpensively and readily obtained by thermally decomposing cellulose.
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公开(公告)号：JPH0217198A
公开(公告)日：1990-01-22
申请号：JP16606288
申请日：1988-07-05
发明人： KAWAKAMI HIROSHI , MATSUSHITA HAJIME , MIZUTANI NOBUHIRO , TAKIGUCHI TOSHIMI , ITO KAZUO , NAOI YOSHITAKA
IPC分类号： C07H19/073 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61P31/12 , C07H19/06
摘要： PURPOSE:To industrially and readily obtain the subject derivative useful as an antiviral agent, etc., in high yield by subjecting a ribose derivative and a cytosine derivative to condensation reaction in the absence of a catalyst in an aprotic solvent. CONSTITUTION:(A) A 1-alpha-halogeno-2-deoxyribose derivative expressed by formula I (R and R represent hydroxyl group having protecting group; Y is halogen) and (B) a cytosine derivative expressed by formula II (R represents protecting group of hydroxyl group; X is H, halogen atom or alkyl or alkenyl which may be substituted by the above-mentioned atom) are subjected to condensation reaction to provide a 3',5'-di-substituted-2'-deoxy-beta-cytidine derivative expressed by formula III, which is then subjected to eliminating reaction of the protecting groups to afford the objective derivative expressed by formula IV. Furthermore, the components (A) and (B) are preferably subjected to the condensation reaction in the presence of amines.
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公开(公告)号：JPH06256334A
公开(公告)日：1994-09-13
申请号：JP40764890
申请日：1990-12-27
发明人： EBATA TAKASHI , MATSUMOTO KATSUYA , KOSEKI KOSHI , KAWAKAMI HIROSHI , MATSUSHITA HAJIME , YOSHIKOSHI HAJIME , OKANIWA MASAKAZU
IPC分类号： C07D307/33 , C07D315/00
摘要： PURPOSE:To easily and selectively synthesize a natural-type ciswhiskey lactone having high utility by inverting the steric configuration of the 4-butyl group of 4-trans-whiskey lactone via three steps. CONSTITUTION:The lactone part of 3,4-trans-whiskey lactone of formula I is hydrolyzed and an alkyl is added thereto to obtain a 3,4-trans compound of formula II (R is alkyl). The compound is made to react with an acyl compound in the presence of triphenylphosphine and an azodicarboxylic acid ester. Finally, the obtained 3,4-cis-compound of formula III (R' is acyl) is hydrolyzed and then lactonized to obtain the 3,4-cis-whiskey lactone of formula IV. (3R,4 S)-3-methyl-4-octanolide can be converted into (3R,4R)-3-methyl-4-octanolide by the process similar to the above reactions. The fragrance of a natural-type whiskey lactone existing in whiskey, wine, etc., is superior to that of other whiskey lactones.
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公开(公告)号：JPH04368382A
公开(公告)日：1992-12-21
申请号：JP14344691
申请日：1991-06-14
发明人： KAWAKAMI HIROSHI , MATSUMOTO KATSUYA , KOSEKI YUKIFUMI , EBATA TAKASHI , MATSUSHITA HAJIME , ITO KAZUO , NAOI YOSHITAKA
IPC分类号： C07D405/04 , C07F7/18 , C07H19/06
摘要： PURPOSE:To produce the subject compound having a high AIDS virus-resistant activity and useful as an anti-AIDS drug or a synthetic intermediate therefor by condensing a specific furanose derivative with a 5-saturated pyrimidine derivative. and subsequently subjecting the produced compound to a reductive desulfurization reaction and further to a protecting group-removing reaction. CONSTITUTION:A compound of formula II [R is (substituted) alkyl, (substituted) phenyl; Z is halogeno, alkoxy, etc.,] is derived from a compound of formula I (R is an OH-protecting group). The compound of formula II is condensed with a 5-substituted pyrimidine derivative of formula III [R -R are alkyl, phenyl; X is O, N; Y is H, halogen, (halogenated) alkyl, (halogenated) alkenyl]. The obtained compound of formula IV is subjected to a reductive desulfurization reaction to produce a compound of formula V, which is subjected to a protecting group-removing reaction to provide the objective compound of formula VI.
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