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1. 发明专利

JP2008110960A 6-(heterocycle-substituted benzyl)-4-oxoquinoline compound and use of the same as hiv integrase inhibitor 有权
标题翻译： 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

2. 发明专利

JP2006232849A Nitrogenous fused-ring compound and use thereof as hiv integrase inhibitor 审中-公开
标题翻译：硝酸纤维素化合物及其作为HIV整合抑制剂的用途
公开(公告)号：JP2006232849A
公开(公告)日：2006-09-07
申请号：JP2006118260
申请日：2006-04-21
申请人： Japan Tobacco Inc , 日本たばこ産業株式会社
发明人： MIYAZAKI SUSUMU , KATO SUSUMU , ADACHI KAORU , ISOJIMA HIROTAKA , KOBAYASHI AKIRA , MATSUZAKI YUJI , WATANABE WATARU , YAMATAKA KAZUNAO , KIYONARI SHINICHI , WAMAKI SHUICHI
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/4985 , A61K31/499 , A61K31/5025 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/5377 , A61K31/551 , A61K45/00 , A61P31/12 , A61P31/18 , A61P43/00 , C07D471/10 , C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide a new nitrogen-containing fused-ring compound usable as an anti-HIV agent or a pharmaceutically acceptable salt. SOLUTION: The nitrogen-containing fused-ring compound represented by general formula [I], or the pharmaceutically acceptable salt thereof, and the anti-HIV agent containing such compound are provided. 2-(3,4-Dichlorobenzyl)-9-hydroxy-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,8-dione hydrochloride is cited as a concrete example. The compound has an HIV integrase inhibitory activity, and is useful as an agent for the prophylaxis or treatment of AIDS, or as an anti-HIV agent. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供可用作抗HIV剂或药学上可接受的盐的新的含氮稠环化合物。解决方案：提供由通式[I]表示的含氮稠环化合物或其药学上可接受的盐和含有该化合物的抗HIV剂。作为具体实例，举出2-（3,4-二氯苄基）-9-羟基-3,4-二氢-2H-吡啶并[1,2-a]吡嗪-1,8-二酮盐酸盐。该化合物具有HIV整合酶抑制活性，并且可用作预防或治疗AIDS或作为抗HIV剂的药剂。此外，通过与其它抗HIV剂如蛋白酶抑制剂，逆转录酶抑制剂等的组合使用，它可以是更有效的抗HIV剂。因为它显示出整合酶特异性的高抑制活性，所以化合物可以是对人体安全的药剂，其副作用较小。版权所有（C）2006，JPO＆NCIPI

3. 发明专利

JP2011037857A Use of 6-(3-chloro-2-fluorobenzyl)-1-[(2s)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or salt thereof for treating retrovirus infection 审中-公开
标题翻译：使用6-（3-氯-2-氟代甲基）-1 - [（2S）-1-羟基-3-甲基丁-2-炔基] -7-甲氧基-4-氧代-1,4-二氢喹啉-3-酮用于治疗逆转录病毒感染的羧酸或其盐
公开(公告)号：JP2011037857A
公开(公告)日：2011-02-24
申请号：JP2010182092
申请日：2010-08-17
申请人： Japan Tobacco Inc , 日本たばこ産業株式会社
发明人： MATSUZAKI YUJI , KANO MITSUKI , IKEDA SATORU
IPC分类号： A61K31/47 , A61K45/00 , A61P31/18 , A61P43/00 , C07D215/56
CPC分类号： C07D215/56
摘要： PROBLEM TO BE SOLVED: To provide a therapeutic agent, a therapeutic composition and kit production of retrovirus infection. SOLUTION: A use of a therapeutically effective amount of 6-(3-chloro-2-fluorobenzyl)-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid (hereinafter referred to as a compound I) or a pharmaceutically acceptable salt thereof is provided. Further, the use of the compound I or the salt thereof for an inhibitor of integrase activity is provided. The compound I or the salt thereof is also effective in inhibiting replication of a retrovirus resistant to at least one anti-retroviral drug. The compound I or the salt thereof is administered alone or in combination with at least one anti-retroviral drug other than the compound I or the salt thereof. Further, production of a kit containing the compound I or the salt thereof is provided. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供治疗剂，治疗组合物和试剂盒生产逆转录病毒感染。解决方案：使用治疗有效量的6-（3-氯-2-氟苄基）-1 - [（2S）-1-羟基-3-甲基丁-2-基] -7-甲氧基-4 - 氧代-1,4-二氢喹啉-3-羧酸（以下称为化合物I）或其药学上可接受的盐。此外，提供了化合物I或其盐作为整合酶活性抑制剂的用途。化合物I或其盐对于抑制对至少一种抗逆转录病毒药物具有抗性的逆转录病毒的复制也是有效的。化合物I或其盐单独或与除化合物I或其盐以外的至少一种抗逆转录病毒药物组合施用。此外，提供了含有化合物I或其盐的试剂盒的制备。版权所有（C）2011，JPO＆INPIT

4. 发明专利

JP2005002092A 4-oxoquinoline compound and its use as hiv integrase inhibitor 有权
标题翻译： 4-氧杂喹啉化合物及其作为HIV整合抑制剂使用
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

5. 发明专利

MY136173A 4-OXOQUINOLINE COMPOUND AND USE THEREOF AS HIV INTEGRASE INHIBITOR 未知
公开(公告)号：MY136173A
公开(公告)日：2008-08-29
申请号：MYPI20034478
申请日：2003-11-20
申请人： JAPAN TOBACCO INC
发明人： SATOH MOTOHIDE , KAWAKAMI HIROSHI , ITOH YOSHIHARU , SHINKAI HISASHI , MOTOMURA TAKAHISA , ARAMAKI HISATERU , MATSUZAKI YUJI , WATANABE WATARU , WAMAKI SHUICHI
IPC分类号： C07D215/56 , A61K20060101 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/5377 , A61K45/06 , A61P20060101 , A61P31/12 , A61P31/18 , A61P43/00 , C07D20060101 , C07D215/58 , C07D401/06 , C07D409/06 , C07D417/06 , C07D471/04
摘要： AN ANTI-HIV AGENT CONTAINING, AS AN ACTIVE INGREDIENT, A 4-OXOQUINOLINE COMPOUND REPRESENTED BY THE FOLLOWING FORMULA [ I ] WHEREIN EACH SYMBOL IS AS DEFINED IN THE SPECIFICATION, OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF. THE COMPOUND OF THE PRESENT INVENTION HAS HIV INTEGRASE INHIBITORY ACTION AND IS USEFUL AS AN ANTI-HIV AGENT FOR THE PROPHYLAXIS OR THERAPY OF AIDS. MOREOVER, BY A COMBINED USE WITH OTHER ANTI-HIV AGENTS SUCH AS PROTEASE INHIBITORS, REVERSE TRANSCRIPTASE INHIBITORS AND THE LIKE, THE COMPOUND CAN BECOME A MORE EFFECTIVE ANTI-HIV AGENT. SINCE THE COMPOUND HAS HIGH INHIBITORY ACTIVITY SPECIFIC FOR INTEGRASES, IT CAN PROVIDE A SAFE PHARMACEUTICAL AGENT WITH A FEWER SIDE EFFECTS FOR HUMAN.

6. 发明专利

PE03612005A1 COMPUESTO DE ANILLO FUSIONADO CONTENIENDO NITROGENO REFERIDO A LA INHIBICION DE INTEGRASA VIH 未知
公开(公告)号：PE03612005A1
公开(公告)日：2005-06-27
申请号：PE0007872004
申请日：2004-08-13
申请人： JAPAN TOBACCO INC
发明人： MIYAZAKI SUSUMU , KATOH SUSUMU , ADACHI KAORU , ISOSHIMA HIROTAKA , KOBAYASHI SATORU , MATSUZAKI YUJI , WATANABE WATARU , YAMATAKA KAZUNOBU , KIYONARI SHINICHI , WAMAKI SHUICHI
IPC分类号： A61K31/4985 , A61K31/519 , A61K31/53 , A61K31/551 , A61P31/12 , A61P31/18 , A61P43/00 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： REFERIDA A UN COMPUESTO DE ANILLO FUSIONADO DE FORMULA I DONDE R1 ES ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; X ES -C(RX1)(RX2)-#, -C(RX10)=N-#, ENTRE OTROS; RX1 A RX10 SON CADA UNO C, O TAMBIEN RX1 Y RX2 FORMAN CADA UNO UN CICLOALQUILO C3-C8 CON EL CARBONO ADYANCENTE; Y1---Y2---Y3 DEL ANILLO B ES C=C(RY1)-N(RY2), N-C(RY1)=N, ENTRE OTROS; RY1 Y RY2 SON CADA UNO C; R2 ES H O UNA SAL. TAMBIEN REFERIDA A UNA COMPOSICION FARMACEUTICA QUE COMPRENDE DICHO COMPUESTO CUYOS PREFERIDOS SON: CLORHIDRATO DE 2-(3,4-DICLOROBENCIL)-9-HIDROXI-3,4-DIHIDRO-2H-PIRIDO[1,2-a]PIRAZINA-1,8-DIONA; ACIDO 2-(3,4-DICLOROBENCIL-9-HIDROXI-1,8-DIOXO-1,3,4,8-TETRAHIDRO-2H-PIRIDO[1,2-a]PIRAZINA-6-CARBOXILICO Y SAL SODICA DE 7-(2,2-DIMETILPROPIONIL)-2-(4-FLUOROBENCIL)-9-HIDROXI-2H-PIRIDO[1,2-a]PIRAZINA-1,8-DIONA; ENTRE OTROS. DICHOS COMPUESTOS SON UTILES COMO AGENTES ANTI-VIH E INHIBIDORES DE INTEGRASA

7. 发明专利

SK2662004A3 4-Oxoquinoline compound and its utilisation as integrase inhibitor 未知
公开(公告)号：SK2662004A3
公开(公告)日：2005-06-02
申请号：SK2662004
申请日：2003-11-20
申请人： JAPAN TOBACCO INC
发明人： SATOH MOTOHIDE , KAWAKAMI HIROSHI , ITOH YOSHIAHARU , SHINKAI HISASHI , MOTOMURA TAKAHISA , ARAMAKI HISATERU , MATSUZAKI YUJI , WATANABE WATARU , WAMAKI SHIUCHI
IPC分类号： A61K20060101 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/5377 , A61K45/06 , A61P20060101 , A61P31/12 , A61P31/18 , A61P43/00 , C07D20060101 , C07D215/56 , C07D215/58 , C07D401/06 , C07D409/06 , C07D417/06 , C07D471/04
摘要： An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.

8. 发明专利

CA2470365A1 4-OXOQUINOLINE COMPOUND AND USE THEREOF AS HIV INTEGRASE INHIBITOR 未知
公开(公告)号：CA2470365A1
公开(公告)日：2004-06-03
申请号：CA2470365
申请日：2003-11-20
申请人： JAPAN TOBACCO INC
发明人： ARAMAKI HISATERU , ITOH YOSHIHARU , KAWAKAMI HIROSHI , SHINKAI HISASHI , WAMAKI SHUICHI , SATOH MOTOHIDE , MOTOMURA TAKAHISA , MATSUZAKI YUJI , WATANABE WATARU
IPC分类号： A61K20060101 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/5377 , A61K45/06 , A61P20060101 , A61P31/12 , A61P31/18 , A61P43/00 , C07D20060101 , C07D215/56 , C07D215/58 , C07D401/06 , C07D409/06 , C07D417/06 , C07D471/04
摘要： 4-Oxoquinoline compounds represented by the following general formula [I]: [I] wherein each symbol has the meaning as defined in the description; or pharmaceutically acceptable salts thereof and anti-HIV agents containing these compounds. Because of having an activity of inhibiting HIV integrase, the above compounds are useful as anti-HIV agents in remedies or preventives for AIDS. By using together with other anti-HIV agents such as a protease inhibitor and a reverse transcriptase inhibitor, the above compounds can be used as more efficacious anti-HIV agents. Because of having a high inhibitory activity specific to the integrase, furthermore, these compounds are usable as drugs which are safe to the human body with little side effect.

9. 发明专利

CY1110690T1 ΕΝΩΣΕΙΣ 4-ΟΞΟΚΙΝΟΛΙΝΗΣ ΚΑΙ ΧΡΗΣΙΜΟΠΟΙΗΣΗ ΑΥΤΩΝ ΩΣ ΑΝΑΣΤΟΛΕΙΣ ΤΗΣ ΕΝΣΩΜΑΤΑΣΗΣ ΤΟΥ HIV 未知
公开(公告)号：CY1110690T1
公开(公告)日：2015-06-10
申请号：CY091101301
申请日：2009-12-11
申请人： JAPAN TOBACCO INC
发明人： SATOH MOTOHIDE , KAWAKAMI HIROSHI , ITOH YOSHIHARU , SHINKAI HISASHI , MOTOMURA TAKAHISA , ARAMAKI HISATERU , MATSUZAKI YUJI , WATANABE WATARU , WAMAKI SHUICHI
IPC分类号： C07D215/56 , A61K20060101 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/5377 , A61K45/06 , A61P20060101 , A61P31/12 , A61P31/18 , A61P43/00 , C07D20060101 , C07D215/58 , C07D401/06 , C07D409/06 , C07D417/06 , C07D471/04
摘要： Εδώπεριγράφεταιέναςαντι-HIV παράγονταςπουπεριέχει, ωςέναδραστικόσυστατικό, μιαένωση 4-οξοκινολίνηςπουπαριστάνεταιμετονακόλουθοτύπο (I) όπουκάθεσύμβολοέχειόπωςορίζεταιστηλεπτομερήπεριγραφήτηςευρεσιτεχνίας, ήέναφαρμακευτικώςαποδεκτόάλαςαυτής. Ηένωσητηςπαρούσαςεφεύρεσηςέχειανασταλτικήτηςενσωμάτωσηςτου HIV δράσηκαιείναιχρήσιμηωςέναςαντι-HIV παράγονταςγιατηνπροφύλαξηαπόή τηθεραπείατου AIDS. Επιπλέον, μετησυνδυασμένηχρήσημεάλλουςαντι-HIV παράγοντεςόπωςαναστολείςπρωτέασης, αναστολείςαντίστροφηςτρανσκριπτάσηςκαιταπαρόμοια, ηένωσημπορείνακαταστείέναςπιοαποτελεσματικόςαντι-HIV παράγοντας. Εφόσονη ένωσηέχειυψηλήανασταλτικήδραστικότηταειδικήγιατιςενσωματάσες, μπορείναπροσφέρειένανασφαλήφαρμακευτικόπαράγονταμελιγότερεςπαρενέργειεςγιατονάνθρωπο.

10. 发明专利

AT443048T 未知
公开(公告)号：AT443048T
公开(公告)日：2009-10-15
申请号：AT03811532
申请日：2003-11-20
申请人： JAPAN TOBACCO INC
发明人： SATOH MOTOHIDE , KAWAKAMI HIROSHI , ITOH YOSHIHARU , SHINKAI HISASHI , MOTOMURA TAKAHISA , ARAMAKI HISATERU , MATSUZAKI YUJI , WATANABE WATARU , WAMAKI SHUICHI
IPC分类号： C07D215/56 , A61K20060101 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/5377 , A61K45/06 , A61P20060101 , A61P31/12 , A61P31/18 , A61P43/00 , C07D20060101 , C07D215/58 , C07D401/06 , C07D409/06 , C07D417/06 , C07D471/04
摘要： An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.

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