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1. 发明授权

US06949543B2 Amide derivative 失效
标题翻译：酰胺衍生物
公开(公告)号：US06949543B2
公开(公告)日：2005-09-27
申请号：US10416371
申请日：2001-11-08
申请人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Yoji Miyazaki , Hiroshi Suzuki , Eiichi Nakai , Shunji Kageyama
发明人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Yoji Miyazaki , Hiroshi Suzuki , Eiichi Nakai , Shunji Kageyama
IPC分类号： A61K8/42 , A61P31/22 , C07D277/40 , C07D277/62 , C07D277/64 , C07D277/74 , C07D417/12 , C07D417/14 , A61K31/426
CPC分类号： C07D277/74 , C07D277/40 , C07D277/62 , C07D277/64 , C07D417/12 , C07D417/14
摘要： The invention relates to a novel amide derivative which is an N-({[4-(substituted thiazol-4-yl)phenyl]carbamoyl}methyl)amide derivative having a characteristic in that an aryl or heteroaryl group as an aromatic ring group is directly substituted on the N atom of amido group. Since said amide derivative has excellent anti-herpesvirus action, it is useful as medicaments and antiviral agents, particularly as preventive or therapeutic agents for various diseases accompanied by Herpesviridae virus infections, illustratively, varicella (chickenpox) accompanied by varicella zoster virus infection, shingles accompanied by the recurrent infection of latent varicella zoster virus, labial herpes and herpes encephalitis accompanied by HSV-1 infection, genital herpes accompanied by HSV-2 and the like various herpesvirus infections.
摘要翻译：本发明涉及一种新颖的酰胺衍生物，其是具有芳基或杂芳基作为芳族环基的特征的N - （{[4-（取代的噻唑-4-基）苯基]氨基甲酰基}甲基）直接取代在氨基的N原子上。由于所述酰胺衍生物具有优异的抗疱疹病毒作用，因此可用作药物和抗病毒剂，特别是作为伴随疱疹病毒科病毒感染的各种疾病的预防或治疗剂，例如伴随水痘带状疱疹病毒感染的水痘（水痘），带状疱疹伴随由于潜伏性水痘带状疱疹病毒的复发感染，伴有HSV-1感染的唇疱疹和疱疹性脑炎，伴有HSV-2的生殖器疱疹等各种疱疹病毒感染。

2. 发明申请

US20050032855A1 Tetrahydro-2H-thiopyran-4-carboxamide derivative 有权
公开(公告)号：US20050032855A1
公开(公告)日：2005-02-10
申请号：US10912232
申请日：2004-08-06
申请人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Tomoaki Kawano , Akio Kamikawa , Hiroshi Suzuki , Kenji Sudo
发明人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Tomoaki Kawano , Akio Kamikawa , Hiroshi Suzuki , Kenji Sudo
IPC分类号： A61P31/22 , C07D335/02 , C07D413/12 , A61K31/4245 , A61K31/422 , C07D413/02
CPC分类号： C07D335/02 , C07D413/12
摘要： A pharmaceutical drug, particularly a novel compound useful for the prophylaxis or therapeutic treatment of various diseases involving infections with viruses of the Herpesviridae family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella zoster via recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis via HSV-1 and genital herpes via HSV-2 infection. N-{2-[(4-Substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide derivative where the phenyl group is substituted at position 4 with a specific five-membered or 6-membered heteroaryl group, has such great anti-virus activity that the oral dosing thereof at a low dose enabled the therapeutic treatment of the diseases.

3. 发明授权

US07465748B2 Amide derivative 有权
标题翻译：酰胺衍生物
公开(公告)号：US07465748B2
公开(公告)日：2008-12-16
申请号：US10567565
申请日：2004-08-05
申请人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Tomoaki Kawano , Akio Kamikawa , Hiroshi Suzuki , Kenji Sudo
发明人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Tomoaki Kawano , Akio Kamikawa , Hiroshi Suzuki , Kenji Sudo
IPC分类号： A61K31/41 , C07D271/06
CPC分类号： C07D335/02 , C07D413/12
摘要： There is provided a pharmaceutical drug, particularly a novel compound useful for prophylaxis or a therapeutic treatment of various diseases involving infections with viruses of the herpesvirus family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella zoster via recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis via HSV-1 and genital herpes via HSV-2 infection.An N-{2-[(4-substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide derivative, of which phenyl group is substituted at position 4 with a specific 5- or 6-membered heteroaryl group, and a salt thereof have an effective anti-virus activity, and the oral administration thereof at a low dose enabled the therapeutic treatment of the above diseases.
摘要翻译：提供药物，特别是可用于预防或治疗涉及疱疹病毒家族病毒感染的各种疾病的新型化合物，特别是各种疱疹病毒感染如通过水痘带状疱疹病毒的水痘（水痘），水痘带状疱疹经由复发通过HSV-1和生殖器疱疹通过HSV-2感染感染潜伏性水痘带状疱疹病毒，唇疱疹和疱疹脑炎。 N-（2 - [（4-取代苯基）氨基] -2-氧代乙基}四氢-2H-噻喃-4-甲酰胺衍生物，其苯基在4位被特定的5或6元杂芳基取代基团和其盐具有有效的抗病毒活性，并且以低剂量口服给药能够治疗上述疾病。

4. 发明申请

US20060229295A1 Amide derivatives 有权
标题翻译：酰胺衍生物
公开(公告)号：US20060229295A1
公开(公告)日：2006-10-12
申请号：US10567565
申请日：2004-08-05
申请人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Tomoaki Kawano , Akio Kamikawa , Hiroshi Suzuki , Kenji Sudo
发明人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Tomoaki Kawano , Akio Kamikawa , Hiroshi Suzuki , Kenji Sudo
IPC分类号： A61K31/55 , A61K31/551 , A61K31/506 , A61K31/5377 , A61K31/4545 , A61K31/4709 , A61K31/4439 , A61K31/433 , A61K31/428 , A61K31/422
CPC分类号： C07D335/02 , C07D413/12
摘要： There is provided a pharmaceutical drug, particularly a novel compound useful for prophylaxis or a therapeutic treatment of various diseases involving infections with viruses of the herpesvirus family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella zoster via recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis via HSV-1 and genital herpes via HSV-2 infection. An N-{2-[(4-substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide derivative, of which phenyl group is substituted at position 4 with a specific 5- or 6-membered heteroaryl group, and a salt thereof have an effective anti-virus activity, and the oral administration thereof at a low dose enabled the therapeutic treatment of the above diseases.
摘要翻译：提供药物，特别是可用于预防或治疗涉及疱疹病毒家族病毒感染的各种疾病的新型化合物，特别是各种疱疹病毒感染如通过水痘带状疱疹病毒的水痘（水痘），水痘带状疱疹经由复发通过HSV-1和生殖器疱疹通过HSV-2感染感染潜伏性水痘带状疱疹病毒，唇疱疹和疱疹脑炎。 N-（2 - [（4-取代苯基）氨基] -2-氧代乙基}四氢-2H-噻喃-4-甲酰胺衍生物，其苯基在4位被特定的5或6元杂芳基取代基团和其盐具有有效的抗病毒活性，并且以低剂量口服给药能够治疗上述疾病。

5. 发明授权

US06903125B2 Tetrahydro-2H-thiopyran-4-carboxamide derivative 有权
标题翻译：四氢-2H-噻喃-4-甲酰胺衍生物
公开(公告)号：US06903125B2
公开(公告)日：2005-06-07
申请号：US10912232
申请日：2004-08-06
申请人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Tomoaki Kawano , Akio Kamikawa , Hiroshi Suzuki , Kenji Sudo
发明人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Tomoaki Kawano , Akio Kamikawa , Hiroshi Suzuki , Kenji Sudo
IPC分类号： A61P31/22 , C07D335/02 , C07D413/12 , A61K31/41 , C07D271/06
CPC分类号： C07D335/02 , C07D413/12
摘要： A pharmaceutical drug, particularly a novel compound useful for the prophylaxis or therapeutic treatment of various diseases involving infections with viruses of the Herpesviridae family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella zoster via recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis via HSV-1 and genital herpes via HSV-2 infection. N-{2-[(4-Substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide derivative where the phenyl group is substituted at position 4 with a specific five-membered or 6-membered heteroaryl group, has such great anti-virus activity that the oral dosing thereof at a low dose enabled the therapeutic treatment of the diseases.
摘要翻译：一种药物，特别是可用于预防或治疗涉及疱疹病毒科家族病毒感染的各种疾病的新型化合物，特别是各种疱疹病毒感染如通过水痘带状疱疹病毒的水痘（水痘），水痘带状疱疹通过潜在的复发性感染水痘带状疱疹病毒，通过HSV-1和生殖器疱疹通过HSV-2感染的唇疱疹和疱疹脑炎。 N- {2 - [（4-取代的苯基）氨基] -2-氧代乙基}四氢-2H-噻喃-4-甲酰胺衍生物，其中苯基在4位被特定的5元或6元杂芳基取代具有如此巨大的抗病毒活性，以低剂量的口服给药能够治疗疾病。

6. 发明授权

US07034047B2 Triazole derivative 失效
标题翻译：三唑衍生物
公开(公告)号：US07034047B2
公开(公告)日：2006-04-25
申请号：US10848386
申请日：2004-05-19
申请人： Takahiko Tobe , Takashi Sugane , Wataru Hamaguchi , Itsuro Shimada , Kyoichi Maeno , Junji Miyata , Tetsuya Kimizuka , Takeshi Suzuki , Atsuyuki Kohara , Takuma Morita , Michael Arlt , Hartmut Greiner
发明人： Takahiko Tobe , Takashi Sugane , Wataru Hamaguchi , Itsuro Shimada , Kyoichi Maeno , Junji Miyata , Tetsuya Kimizuka , Takeshi Suzuki , Atsuyuki Kohara , Takuma Morita , Michael Arlt , Hartmut Greiner
IPC分类号： C07D239/08 , A61K31/4196
CPC分类号： C07D249/08 , A61K31/41 , A61K31/4155 , A61K31/416 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , C07D249/10 , C07D249/12 , C07D249/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/10 , C07D495/04
摘要： The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.
摘要翻译：本发明涉及具有活性抑制甘氨酸转运体并用作药物的三唑衍生物和新的三唑衍生物。本发明的三唑衍生物具有优异的抑制甘氨酸转运蛋白的活性，可用作痴呆，精神分裂症，认知障碍或参与各种疾病如阿尔茨海默病，帕金森病或亨廷顿病等的认知障碍或痉挛的治疗剂涉及诸如神经退行性疾病和脑血管障碍等疾病。特别地，药物对于改善痴呆等的学习障碍是有用的。

7. 发明申请

US20060025461A1 Triazole derivative 失效
公开(公告)号：US20060025461A1
公开(公告)日：2006-02-02
申请号：US11232011
申请日：2005-09-22
申请人： Takahiko Tobe , Takashi Sugane , Wataru Hamaguchi , Itsuro Shimada , Kyoichi Maeno , Junji Miyata , Tetsuya Kimizuka , Takeshi Suzuki , Atsuyuki Kohara , Takuma Morita , Michael Arlt , Hartmut Greiner
发明人： Takahiko Tobe , Takashi Sugane , Wataru Hamaguchi , Itsuro Shimada , Kyoichi Maeno , Junji Miyata , Tetsuya Kimizuka , Takeshi Suzuki , Atsuyuki Kohara , Takuma Morita , Michael Arlt , Hartmut Greiner
IPC分类号： A61K31/4196 , C07D403/02
CPC分类号： C07D249/08 , A61K31/41 , A61K31/4155 , A61K31/416 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , C07D249/10 , C07D249/12 , C07D249/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/10 , C07D495/04
摘要： The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

8. 发明授权

US07084164B2 Triazole derivative 失效
公开(公告)号：US07084164B2
公开(公告)日：2006-08-01
申请号：US11232011
申请日：2005-09-22
申请人： Takahiko Tobe , Takashi Sugane , Wataru Hamaguchi , Itsuro Shimada , Kyoichi Maeno , Junji Miyata , Tetsuya Kimizuka , Takeshi Suzuki , Atsuyuki Kohara , Takuma Morita , Michael Arlt , Hartmut Greiner
发明人： Takahiko Tobe , Takashi Sugane , Wataru Hamaguchi , Itsuro Shimada , Kyoichi Maeno , Junji Miyata , Tetsuya Kimizuka , Takeshi Suzuki , Atsuyuki Kohara , Takuma Morita , Michael Arlt , Hartmut Greiner
IPC分类号： A61K31/41 , C07D249/08
CPC分类号： C07D249/08 , A61K31/41 , A61K31/4155 , A61K31/416 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , C07D249/10 , C07D249/12 , C07D249/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/10 , C07D495/04
摘要： The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

9. 发明授权

US08853242B2 Nitrogenous-ring acylguanidine derivative 有权
标题翻译：氮环酰基胍衍生物
公开(公告)号：US08853242B2
公开(公告)日：2014-10-07
申请号：US13388872
申请日：2010-08-05
申请人： Isao Kinoyama , Takehiro Miyazaki , Yohei Koganemaru , Takuya Washio , Wataru Hamaguchi
发明人： Isao Kinoyama , Takehiro Miyazaki , Yohei Koganemaru , Takuya Washio , Wataru Hamaguchi
IPC分类号： A61K31/472 , A61K31/47 , A61K31/4709 , A61P25/00 , A61P25/18 , A61P25/28 , C07D215/48 , C07D215/60 , C07D217/14 , C07D215/54 , C07D217/02 , C07D217/22 , C07D217/16 , C07D401/04
CPC分类号： C07D215/48 , C07D215/54 , C07D215/60 , C07D217/02 , C07D217/14 , C07D217/16 , C07D217/22 , C07D401/04
摘要： [Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HT5A receptor modulating action, is provided.[Means for Solution] It was confirmed that acylguanidine derivatives (the following formula I; any one of Z1, Z2, Z3, Z4 and Z5 is nitrogen atom, and the others are carbon atoms) which have the characteristic structure in which the guanidine is bonded to one ring of the quinoline or isoquinoline via a carbonyl group, and a cyclic group is bonded to the other ring, exhibit potent 5-HT5A receptor modulating actions and excellent pharmacological actions based on the 5-HT5A receptor modulating action, and thus can be excellent agents for preventing or treating dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder. Thus, the present invention has been completed.
摘要翻译：提供了一种基于5-羟色胺5-HT5A受体调节作用预防或治疗痴呆，精神分裂症等的优异剂。 [解决方案]确认酰基胍衍生物（下式I，Z 1，Z 2，Z 3，Z 4和Z 5中的任一个为氮原子，其余为碳原子），其特征在于胍通过羰基键合到喹啉或异喹啉的一个环上，并且环状基团与另一个环键合，表现出基于5-HT5A受体调节作用的有效的5-HT5A受体调节作用和优异的药理作用，因此可以是预防或治疗痴呆，精神分裂症，双相情感障碍或注意缺陷多动障碍的优良药剂。因此，本发明已经完成。

10. 发明申请

US20120142727A1 NITROGENOUS-RING ACYLGUANIDINE DERIVATIVE 有权
标题翻译：硝基环丙酰胺衍生物
公开(公告)号：US20120142727A1
公开(公告)日：2012-06-07
申请号：US13388872
申请日：2010-08-05
申请人： Isao Kinoyama , Takehiro Miyazaki , Yohei Koganemaru , Takuya Washio , Wataru Hamaguchi
发明人： Isao Kinoyama , Takehiro Miyazaki , Yohei Koganemaru , Takuya Washio , Wataru Hamaguchi
IPC分类号： A61K31/472 , C07D217/14 , C07D215/60 , A61P25/00 , A61K31/4709 , A61P25/28 , A61P25/18 , C07D215/48 , A61K31/47
CPC分类号： C07D215/48 , C07D215/54 , C07D215/60 , C07D217/02 , C07D217/14 , C07D217/16 , C07D217/22 , C07D401/04
摘要： [Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HT5A receptor modulating action, is provided.[Means for Solution] It was confirmed that acylguanidine derivatives (the following formula I; any one of Z1, Z2, Z3, Z4 and Z5 is nitrogen atom, and the others are carbon atoms) which have the characteristic structure in which the guanidine is bonded to one ring of the quinoline or isoquinoline via a carbonyl group, and a cyclic group is bonded to the other ring, exhibit potent 5-HT5A receptor modulating actions and excellent pharmacological actions based on the 5-HT5A receptor modulating action, and thus can be excellent agents for preventing or treating dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder. Thus, the present invention has been completed.
摘要翻译：提供了一种基于5-羟色胺5-HT5A受体调节作用预防或治疗痴呆，精神分裂症等的优异剂。 [解决方案]确认酰基胍衍生物（下式I，Z 1，Z 2，Z 3，Z 4和Z 5中的任一个为氮原子，其余为碳原子），其特征在于胍通过羰基与喹啉或异喹啉的一个环键合，并且环状基团与另一个环键合，表现出基于5-HT5A受体调节作用的有效的5-HT5A受体调节作用和优异的药理作用，因此可以是预防或治疗痴呆，精神分裂症，双相情感障碍或注意缺陷多动障碍的优良药剂。因此，本发明已经完成。

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