公开(公告)号：US07872004B2

公开(公告)日：2011-01-18

申请号：US11767021

申请日：2007-06-22

申请人： Motohide Satoh ,  Hisateru Aramaki ,  Masaki Yamashita ,  Masafumi Inoue ,  Hiroshi Kawakami ,  Hisashi Shinkai ,  Hiroshi Nakamura ,  Yuji Matsuzaki ,  Shuichi Wamaki

发明人： Motohide Satoh ,  Hisateru Aramaki ,  Masaki Yamashita ,  Masafumi Inoue ,  Hiroshi Kawakami ,  Hisashi Shinkai ,  Hiroshi Nakamura ,  Yuji Matsuzaki ,  Shuichi Wamaki

IPC分类号： A61K31/5377 ,  A61K31/4709 ,  C07D413/02 ,  C07D215/00

CPC分类号： C07D215/56 ,  C07D401/10 ,  C07D413/10 ,  C07D417/10

摘要： The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical composition, an anti-HIV agent and an HIV integrase inhibitor containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an anti-HIV agent, or as an agent for the prophylaxis or treatment of AIDS. 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.

摘要翻译： 本发明涉及由下式[I]表示的化合物，其中每个符号如说明书中所定义，或其药学上可接受的盐，或其溶剂合物，药物组合物，抗HIV剂和HIV 含有这种化合物的整合酶抑制剂。 本发明的化合物具有HIV整合酶抑制活性，可用作抗HIV剂，或用作预防或治疗AIDS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。

公开(公告)号：US20080207618A1

公开(公告)日：2008-08-28

申请号：US11767021

申请日：2007-06-22

申请人： Motohide SATOH ,  Hisateru Aramaki ,  Masaki Yamashita ,  Masafumi Inoue ,  Hiroshi Kawakami ,  Hisashi Shinkai ,  Hiroshi Nakamura ,  Yuji Matsuzaki ,  Shuichi Wamaki

发明人： Motohide SATOH ,  Hisateru Aramaki ,  Masaki Yamashita ,  Masafumi Inoue ,  Hiroshi Kawakami ,  Hisashi Shinkai ,  Hiroshi Nakamura ,  Yuji Matsuzaki ,  Shuichi Wamaki

IPC分类号： A61K31/5377 ,  C07D413/08 ,  C07D403/08 ,  A61K31/4709 ,  A61P31/18

CPC分类号： C07D215/56 ,  C07D401/10 ,  C07D413/10 ,  C07D417/10

摘要： The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical composition, an anti-HIV agent and an HIV integrase inhibitor containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an anti-HIV agent, or as an agent for the prophylaxis or treatment of AIDS. 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.

摘要翻译： 本发明涉及由下式[I]表示的化合物，其中每个符号如说明书中所定义，或其药学上可接受的盐，或其溶剂合物，药物组合物，抗HIV剂和HIV 含有该化合物的整合酶抑制剂。 本发明的化合物具有HIV整合酶抑制活性，可用作抗HIV剂，或用作预防或治疗AIDS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。

公开(公告)号：US20050239819A1

公开(公告)日：2005-10-27

申请号：US10492833

申请日：2003-11-20

申请人： Motohide Satoh ,  Hiroshi Kawakami ,  Yoshiharu Itoh ,  Hisashi Shinkai ,  Takahisa Motomura ,  Hisateru Aramaki ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Shuichi Wamaki

发明人： Motohide Satoh ,  Hiroshi Kawakami ,  Yoshiharu Itoh ,  Hisashi Shinkai ,  Takahisa Motomura ,  Hisateru Aramaki ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Shuichi Wamaki

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 ,  A61K31/4745 ,  C07D215/16 ,  C07D471/02

CPC分类号： A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/5377 ,  A61K45/06 ,  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.

摘要翻译： 作为活性成分的含有下式[I]表示的4-氧代喹啉化合物的抗HIV剂，其中各符号如说明书中所述，或其药学上可接受的盐。 本发明的化合物具有HIV整合酶抑制作用，可用作预防或治疗AIDS的抗HIV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，化合物可以变成更有效的抗HIV剂。 由于该化合物对整合酶具有高的抑制活性，因此可提供对人体副作用较小的安全药剂。

公开(公告)号：US07531554B2

公开(公告)日：2009-05-12

申请号：US11133470

申请日：2005-05-20

申请人： Motohide Satoh ,  Takashi Matsuda ,  Satoshi Okuda ,  Hiroshi Kawakami ,  Hisateru Aramaki ,  Hisashi Shinkai ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Kazunobu Yamataka ,  Shinichi Kiyonari ,  Shuichi Wamaki ,  Mitsuru Takahashi ,  Naohito Yamada ,  Akemi Nagao

发明人： Motohide Satoh ,  Takashi Matsuda ,  Satoshi Okuda ,  Hiroshi Kawakami ,  Hisateru Aramaki ,  Hisashi Shinkai ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Kazunobu Yamataka ,  Shinichi Kiyonari ,  Shuichi Wamaki ,  Mitsuru Takahashi ,  Naohito Yamada ,  Akemi Nagao

IPC分类号： C07D215/04 ,  A61K31/44

CPC分类号： C07D215/56 ,  C07D401/04 ,  C07D401/06 ,  C07D405/06 ,  C07D491/04

摘要： Provision of a compound having an anti-HIV activity, particularly an integrase inhibitory activity.A 4-oxoquinoline compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof: wherein each symbol is as defined in the specification. The present invention also relates to a pharmaceutical composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier; an integrase inhibitor, an antiviral agent, anti-HIV agent, and the like, which contains the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient; an anti-HIV composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and one or more other kinds of anti-HIV activity substances as active ingredients; an anti-HIV agent containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient, which is used for a multiple drug therapy with other anti-HIV agent(s), and the like.

摘要翻译： 提供具有抗HIV活性的化合物，特别是整合酶抑制活性。 由下式[I]表示的4-氧代喹啉化合物或其药学上可接受的盐：其中每个符号如说明书中所定义。 本发明还涉及含有4-氧代喹啉化合物或其药学上可接受的盐和药学上可接受的载体的药物组合物; 含有4-氧代喹啉化合物或其药学上可接受的盐作为活性成分的整合酶抑制剂，抗病毒剂，抗HIV剂等; 含有4-氧代喹啉化合物或其药学上可接受的盐的抗HIV组合物和一种或多种其它类型的抗HIV活性物质作为活性成分; 含有4-氧代喹啉化合物或其药学上可接受的盐作为活性成分的抗HIV剂，其用于与其它抗HIV剂的多重药物治疗等。

公开(公告)号：US07176220B2

公开(公告)日：2007-02-13

申请号：US10492833

申请日：2003-11-20

申请人： Motohide Satoh ,  Hiroshi Kawakami ,  Yoshiharu Itoh ,  Hisashi Shinkai ,  Takahisa Motomura ,  Hisateru Aramaki ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Shuichi Wamaki

发明人： Motohide Satoh ,  Hiroshi Kawakami ,  Yoshiharu Itoh ,  Hisashi Shinkai ,  Takahisa Motomura ,  Hisateru Aramaki ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Shuichi Wamaki

IPC分类号： A61K31/47 ,  C07D215/16

CPC分类号： A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/5377 ,  A61K45/06 ,  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.

摘要翻译： 作为活性成分的含有下式[I]表示的4-氧代喹啉化合物的抗HIV剂，其中各符号如说明书中所述，或其药学上可接受的盐。 本发明的化合物具有HIV整合酶抑制作用，可用作预防或治疗AIDS的抗HIV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，化合物可以成为更有效的抗HIV剂。 由于该化合物对整合酶具有高的抑制活性，因此可提供对人体副作用较小的安全药剂。

公开(公告)号：US20130172344A1

公开(公告)日：2013-07-04

申请号：US13528688

申请日：2012-06-20

申请人： Motohide SATOH ,  Hiroshi Kawakami ,  Yoshiharu Itoh ,  Hisashi Shinkai ,  Takahisa Motomura ,  Hisateru Aramaki ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Shuichi Wamaki

发明人： Motohide SATOH ,  Hiroshi Kawakami ,  Yoshiharu Itoh ,  Hisashi Shinkai ,  Takahisa Motomura ,  Hisateru Aramaki ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Shuichi Wamaki

IPC分类号： C07D471/04 ,  C07D215/58 ,  C07D417/06 ,  C07D401/06 ,  C07D215/56 ,  C07D409/06

CPC分类号： A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/5377 ,  A61K45/06 ,  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.

摘要翻译： 作为活性成分的含有下式[I]表示的4-氧代喹啉化合物的抗HIV剂，其中各符号如说明书中所述，或其药学上可接受的盐。 本发明的化合物具有HIV整合酶抑制作用，可用作预防或治疗AIDS的抗HIV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，化合物可以成为更有效的抗HIV剂。 由于该化合物对整合酶具有高的抑制活性，因此可提供对人体副作用较小的安全药剂。

公开(公告)号：US08232401B2

公开(公告)日：2012-07-31

申请号：US11446128

申请日：2006-06-05

申请人： Motohide Satoh ,  Hiroshi Kawakami ,  Yoshiharu Itoh ,  Hisashi Shinkai ,  Takahisa Motomura ,  Hisateru Aramaki ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Shuichi Wamaki

发明人： Motohide Satoh ,  Hiroshi Kawakami ,  Yoshiharu Itoh ,  Hisashi Shinkai ,  Takahisa Motomura ,  Hisateru Aramaki ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Shuichi Wamaki

IPC分类号： C07D215/38

CPC分类号： A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/5377 ,  A61K45/06 ,  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.

摘要翻译： 作为活性成分的含有下式[I]表示的4-氧代喹啉化合物的抗HIV剂，其中各符号如说明书中所述，或其药学上可接受的盐。 本发明的化合物具有HIV整合酶抑制作用，可用作预防或治疗AIDS的抗HIV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，化合物可以成为更有效的抗HIV剂。 由于该化合物对整合酶具有高的抑制活性，因此可提供对人体副作用较小的安全药剂。

公开(公告)号：US20060217413A1

公开(公告)日：2006-09-28

申请号：US11446128

申请日：2006-06-05

申请人： Motohide Satoh ,  Hiroshi Kawakami ,  Yoshiharu Itoh ,  Hisashi Shinkai ,  Takahisa Motomura ,  Hisateru Aramaki ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Shuichi Wamaki

发明人： Motohide Satoh ,  Hiroshi Kawakami ,  Yoshiharu Itoh ,  Hisashi Shinkai ,  Takahisa Motomura ,  Hisateru Aramaki ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Shuichi Wamaki

IPC分类号： C07D471/02 ,  A61K31/4745 ,  A61K31/4709 ,  A61K31/4704 ,  C07D401/02

CPC分类号： A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/5377 ,  A61K45/06 ,  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.

摘要翻译： 作为活性成分的含有下式[I]表示的4-氧代喹啉化合物的抗HIV剂，其中各符号如说明书中所述，或其药学上可接受的盐。 本发明的化合物具有HIV整合酶抑制作用，可用作预防或治疗AIDS的抗HIV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，化合物可以成为更有效的抗HIV剂。 由于该化合物对整合酶具有高的抑制活性，因此可提供对人体副作用较小的安全药剂。

公开(公告)号：US20060019906A1

公开(公告)日：2006-01-26

申请号：US11133470

申请日：2005-05-20

申请人： Motohide Satoh ,  Takashi Matsuda ,  Satoshi Okuda ,  Hiroshi Kawakami ,  Hisateru Aramaki ,  Hisashi Shinkai ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Kazunobu Yamataka ,  Shinichi Kiyonari ,  Shuichi Wamaki ,  Mitsuru Takahashi ,  Naohito Yamada ,  Akemi Nagao

发明人： Motohide Satoh ,  Takashi Matsuda ,  Satoshi Okuda ,  Hiroshi Kawakami ,  Hisateru Aramaki ,  Hisashi Shinkai ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Kazunobu Yamataka ,  Shinichi Kiyonari ,  Shuichi Wamaki ,  Mitsuru Takahashi ,  Naohito Yamada ,  Akemi Nagao

IPC分类号： A61K31/4704 ,  C07H17/02 ,  C07D215/36

CPC分类号： C07D215/56 ,  C07D401/04 ,  C07D401/06 ,  C07D405/06 ,  C07D491/04

摘要： Provision of a compound having an anti-HIV activity, particularly an integrase inhibitory activity. A 4-oxoquinoline compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof: wherein each symbol is as defined in the specification. The present invention also relates to a pharmaceutical composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier; an integrase inhibitor, an antiviral agent, anti-HIV agent, and the like, which contains the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient; an anti-HIV composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and one or more other kinds of anti-HIV activity substances as active ingredients; an anti-HIV agent containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient, which is used for a multiple drug therapy with other anti-HIV agent(s), and the like.

摘要翻译： 提供具有抗HIV活性的化合物，特别是整合酶抑制活性。 由下式[I]表示的4-氧代喹啉化合物或其药学上可接受的盐：其中每个符号如说明书中所定义。 本发明还涉及含有4-氧代喹啉化合物或其药学上可接受的盐和药学上可接受的载体的药物组合物; 含有4-氧代喹啉化合物或其药学上可接受的盐作为活性成分的整合酶抑制剂，抗病毒剂，抗HIV剂等; 含有4-氧代喹啉化合物或其药学上可接受的盐的抗HIV组合物和一种或多种其它类型的抗HIV活性物质作为活性成分; 含有4-氧代喹啉化合物或其药学上可接受的盐作为活性成分的抗HIV剂，其用于与其它抗HIV剂的多重药物治疗等。

公开(公告)号：US20050054645A1

公开(公告)日：2005-03-10

申请号：US10958225

申请日：2004-10-05

申请人： Susumu Miyazaki ,  Susumu Katoh ,  Kaoru Adachi ,  Hirotaka Isoshima ,  Satoru Kobayashi ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Kazunobu Yamataka ,  Shinichi Kiyonari ,  Shuichi Wamaki

发明人： Susumu Miyazaki ,  Susumu Katoh ,  Kaoru Adachi ,  Hirotaka Isoshima ,  Satoru Kobayashi ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Kazunobu Yamataka ,  Shinichi Kiyonari ,  Shuichi Wamaki

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： The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing such compound. The compound of the present invention 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. Becuae 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.

摘要翻译： 本发明涉及由下式[I]表示的含氮稠环化合物，其中每个符号如说明书中所定义，或其药学上可接受的盐和含有该化合物的抗HIV剂。 本发明的化合物具有HIV整合酶抑制活性，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。 它表现出整合酶特异性的高抑制活性，该化合物可以作为人体安全的药物，这只会减少副作用。