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：US06407064B2

公开(公告)日：2002-06-18

申请号：US09729266

申请日：2000-12-05

申请人： Hiroyuki Masuda ,  Masayuki Jinbo ,  Keiichiro Sakai ,  Yuji Matsuzaki

发明人： Hiroyuki Masuda ,  Masayuki Jinbo ,  Keiichiro Sakai ,  Yuji Matsuzaki

IPC分类号： A61K31535

CPC分类号： C07D295/13

摘要： An aminoalcohol derivative which is a ceramide analogue, and a medicament, especially an agent for treating neuronal diseases and an agent for protecting brain, comprising the same.

摘要翻译： 作为神经酰胺类似物的氨基醇衍生物，以及药剂，特别是治疗神经元疾病的药剂和用于保护脑的药剂。

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：US20090018162A1

公开(公告)日：2009-01-15

申请号：US12162975

申请日：2007-02-01

申请人： Yuji Matsuzaki ,  Mitsuki Kano ,  Satoru Ikeda

发明人： Yuji Matsuzaki ,  Mitsuki Kano ,  Satoru Ikeda

IPC分类号： A61K31/47 ,  A61P31/18

CPC分类号： C07D215/56

摘要： The present invention provides 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 (herein referred to as Compound I) or a pharmaceutically acceptable salt thereof, for the production of an agent for the treatment in a patient. The invention further provides a use of Compound I or a salt thereof for an agent for inhibition of integrase activity. Compound I or a salt thereof is also effective in inhibiting the replication of a retrovirus resistant to at least one anti-retroviral drug. In the use of the invention, Compound I or a salt thereof may be administered alone or in combination with at least one anti-retroviral drug other than Compound I or a salt thereof. The present invention also provides kits comprising Compound I or a salt thereof.

摘要翻译： 本发明提供治疗有效量的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，用于制备患者治疗剂。 本发明还提供了化合物I或其盐作为抑制整合酶活性的药物的用途。 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。 在本发明的使用中，化合物I或其盐可以单独或与除化合物I以外的至少一种抗逆转录病毒药物或其盐组合施用。 本发明还提供了包含化合物I或其盐的试剂盒。

公开(公告)号：US07211572B2

公开(公告)日：2007-05-01

申请号：US11255605

申请日：2005-10-13

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： A01N43/00 ,  A01N43/58 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554

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. 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。 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：US20050288326A1

公开(公告)日：2005-12-29

申请号：US11133463

申请日：2005-05-20

申请人： Yuji Matsuzaki ,  Wataru Watanabe ,  Satoru Ikeda ,  Mitsuki Kano

发明人： Yuji Matsuzaki ,  Wataru Watanabe ,  Satoru Ikeda ,  Mitsuki Kano

IPC分类号： A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K31/506 ,  A61K31/52 ,  A61K31/536 ,  A61K31/7072

CPC分类号： A61K31/7072 ,  A61K31/39 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K31/506 ,  A61K31/52 ,  A61K31/536 ,  A61K31/675 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to a combination therapy for treating an HIV infection or inhibiting integrase comprising (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (“Compound A”) or a pharmaceutically acceptable solvate or salt thereof in combination with at least one other anti-HIV agent. In some embodiments of the present invention, the other anti-HIV agents are chosen from reverse transcriptase inhibitors and protease inhibitors. In certain embodiments of the present invention, the other anti-HIV agents are chosen from AZT, 3TC, PMPA, efavirenz, indinavir, nelfinavir, a combination of AZT/3TC, and a combination of PMPA/3TC. Since Compound A has a high inhibitory activity specific for integrases, when used in combinations with other anti-HIV agents it can provide a combination therapy with fewer side effects for humans.

摘要翻译： 本发明涉及用于治疗HIV感染或抑制整合酶的组合疗法，其包含（S）-6-（3-氯-2-氟苄基）-1-（1-羟甲基-2-甲基丙基）-7-甲氧基-4 - 氧代-1,4-二氢喹啉-3-羧酸（“化合物A”）或其药学上可接受的溶剂合物或其盐与至少一种其它抗HIV剂组合。 在本发明的一些实施方案中，其它抗HIV剂选自逆转录酶抑制剂和蛋白酶抑制剂。 在本发明的某些实施方案中，其它抗HIV剂选自AZT，3TC，PMPA，依法韦仑，茚地那韦，奈非那韦，AZT / 3TC的组合和PMPA / 3TC的组合。 由于化合物A对整合酶具有高的抑制活性，因此当与其它抗HIV剂组合使用时，可以提供对人类副作用较少的组合疗法。

公开(公告)号：US07745459B2

公开(公告)日：2010-06-29

申请号：US11230330

申请日：2005-09-20

申请人： Motohide Satoh ,  Hisateru Aramaki ,  Hiroshi Nakamura ,  Masafumi Inoue ,  Hiroshi Kawakami ,  Hisashi Shinkai ,  Yuji Matsuzaki ,  Kazunobu Yamataka

发明人： Motohide Satoh ,  Hisateru Aramaki ,  Hiroshi Nakamura ,  Masafumi Inoue ,  Hiroshi Kawakami ,  Hisashi Shinkai ,  Yuji Matsuzaki ,  Kazunobu Yamataka

IPC分类号： A01N43/90 ,  A61K31/44 ,  C07D455/02

CPC分类号： C07D471/04 ,  A61K31/4745 ,  A61K31/519 ,  C07D455/02

摘要： A pharmaceutical agent having an anti-HIV action, particularly, a pharmaceutical agent having an integrase inhibitory action, is provided.The present invention relates to a quinolizinone compound represented by the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing same as an active ingredient. The compound of the present invention has an 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 compounds can become a more effective anti-HIV agent. Since the compound has a high inhibitory activity specific for integrases, the compound can provide a safe pharmaceutical agent for human with a fewer side effects.

摘要翻译： 提供具有抗HIV作用的药剂，特别是具有整合酶抑制作用的药剂。 本发明涉及由下式[I]表示的喹嗪酮化合物，其中各符号如说明书中所定义，其药学上可接受的盐和含有作为活性成分的抗HIV剂。 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。 由于化合物对整合酶具有高的抑制活性，所以化合物可以为人体提供安全的药剂，副作用较少。

公开(公告)号：US20090087584A1

公开(公告)日：2009-04-02

申请号：US12280521

申请日：2006-02-22

申请人： Koki Taguchi ,  Akiyoshi Mizuta ,  Katsuhiko Ishida ,  Yuji Matsuzaki ,  Seiichi Nagatome ,  Hideo Nakajima ,  Soong-Keun Hyun

发明人： Koki Taguchi ,  Akiyoshi Mizuta ,  Katsuhiko Ishida ,  Yuji Matsuzaki ,  Seiichi Nagatome ,  Hideo Nakajima ,  Soong-Keun Hyun

IPC分类号： B05D1/04

CPC分类号： C23C4/134 ,  C23C4/073 ,  Y02T50/67

摘要： The pore size, porosity, and pore distribution of a porous metal is controlled by applying a plasma spraying to the surface of the porous metal.

摘要翻译： 通过对多孔金属的表面施加等离子体喷涂来控制多孔金属的孔径，孔隙率和孔分布。

公开(公告)号：US07281054B2

公开(公告)日：2007-10-09

申请号：US10095083

申请日：2002-03-12

申请人： Taisuke Ishioka ,  Yuji Matsuzaki ,  Atsushi Nishide ,  Yu Minakuchi ,  Shigeki Moride ,  Takayuki Yamamoto

发明人： Taisuke Ishioka ,  Yuji Matsuzaki ,  Atsushi Nishide ,  Yu Minakuchi ,  Shigeki Moride ,  Takayuki Yamamoto

IPC分类号： G06F15/16

CPC分类号： H04L67/306 ,  H04L29/06 ,  H04L29/06027 ,  H04L65/4092 ,  H04L69/329 ,  H04N7/165 ,  H04N7/17318 ,  H04N7/17336 ,  H04N21/23109 ,  H04N21/233 ,  H04N21/23418 ,  H04N21/25891 ,  H04N21/26603 ,  H04N21/2668 ,  H04N21/4622 ,  H04N21/4782 ,  H04N21/658 ,  H04N21/812 ,  H04N21/84 ,  H04N21/8456

摘要： A system of the present invention is structured based on a connection between an information distributing unit that processes distributed contents information and a client unit of a user via a network such that they can communicate with each other. The contents information selected based on profile information of the user is transmitted from the information distributing unit to the client unit. The system makes the user input evaluation information relating to the evaluation of the transmitted contents information. The contents information to be distributed to the user is changed based on the input evaluation information.

摘要翻译： 基于通过网络处理分发的内容信息的信息分发单元和用户的客户端单元之间的连接，使得它们可以彼此通信来构造本发明的系统。 基于用户的简档信息选择的内容信息从信息分发单元发送到客户单元。 该系统使得用户输入与所发送的内容信息的评估有关的评估信息。 基于输入的评价信息来改变要分配给用户的内容信息。

公开(公告)号：US20060052361A1

公开(公告)日：2006-03-09

申请号：US11255605

申请日：2005-10-13

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： A61K31/55 ,  A61K31/503 ,  A61K31/553 ,  A61K31/519

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，