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1. 发明授权

US08022072B2 Azolylmethylidenehydrazine derivative and use thereof 失效
标题翻译：唑基亚甲基肼衍生物及其用途
公开(公告)号：US08022072B2
公开(公告)日：2011-09-20
申请号：US12664834
申请日：2008-06-17
申请人： Hironobu Ogura , Yoshiyuki Tatsumi , Yuji Fukamizu
发明人： Hironobu Ogura , Yoshiyuki Tatsumi , Yuji Fukamizu
IPC分类号： A61K31/4025 , C07D233/64 , C07D409/02 , C07D409/06
CPC分类号： C07D233/61 , C07D233/54 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D417/12 , C07D417/14
摘要： An azolylmethylidenehydrazine derivative represented by the formula (I) wherein Ar is an aryl group optionally having substituent(s) or a heteroaryl group optionally having substituent(s), R1 and R2 are the same or different and each is an alkyl group, a cycloalkyl group, an aralkyl group optionally having substituent(s), an aryl group optionally having substituent(s), a heteroarylalkyl group optionally having substituent(s), or R1 and R2 are bonded to each other to form a nitrogen-containing heterocyclic group optionally having substituent(s), and X is CH or a nitrogen atom, or a pharmacologically acceptable salt thereof is useful as a medicament, particularly as an antifungal agent, or an anti-inflammatory agent or an antiallergic agent.
摘要翻译：式（I）表示的唑基亚甲基肼衍生物，其中Ar为任选具有取代基的芳基或任选具有取代基的杂芳基，R1和R2相同或不同，分别为烷基，环烷基基团，任选具有取代基的芳烷基，任选具有取代基的芳基，任选具有取代基的杂芳基烷基，或R 1和R 2彼此键合以形成含氮杂环基，任选地具有取代基，X为CH或氮原子，或其药理学上可接受的盐可用作药物，特别是抗真菌剂，抗炎剂或抗过敏剂。

2. 发明申请

US20100190754A1 AZOLYLMETHYLIDENEHYDRAZINE DERIVATIVE AND USE THEREOF 失效
标题翻译：衍生物及其用途
公开(公告)号：US20100190754A1
公开(公告)日：2010-07-29
申请号：US12664834
申请日：2008-06-17
申请人： Hironobu Ogura , Yoshiyuki Tatsumi , Yuji Fukamizu
发明人： Hironobu Ogura , Yoshiyuki Tatsumi , Yuji Fukamizu
IPC分类号： A61K31/655 , C09B27/00 , A61P27/14 , A61P29/00
CPC分类号： C07D233/61 , C07D233/54 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D417/12 , C07D417/14
摘要： An azolylmethylidenehydrazine derivative represented by the formula (I) wherein Ar is an aryl group optionally having substituent(s) or a heteroaryl group optionally having substituent(s), R1 and R2 are the same or different and each is an alkyl group, a cycloalkyl group, an aralkyl group optionally having substituent(s), an aryl group optionally having substituent(s), a heteroarylalkyl group optionally having substituent(s), or R1 and R2 are bonded to each other to form a nitrogen-containing heterocyclic group optionally having substituent(s), and X is CH or a nitrogen atom, or a pharmacologically acceptable salt thereof is useful as a medicament, particularly as an antifungal agent, or an anti-inflammatory agent or an antiallergic agent.
摘要翻译：式（I）表示的唑基亚甲基肼衍生物，其中Ar为任选具有取代基的芳基或任选具有取代基的杂芳基，R1和R2相同或不同，分别为烷基，环烷基基团，任选具有取代基的芳烷基，任选具有取代基的芳基，任选具有取代基的杂芳基烷基，或R 1和R 2彼此键合以形成含氮杂环基，任选地具有取代基，X为CH或氮原子，或其药理学上可接受的盐可用作药物，特别是抗真菌剂，抗炎剂或抗过敏剂。

3. 发明授权

US08889155B2 Gel composition for treating mycosis 有权
标题翻译：用于治疗真菌病的凝胶组合物
公开(公告)号：US08889155B2
公开(公告)日：2014-11-18
申请号：US12521483
申请日：2007-12-28
申请人： Tomohiro Okumura , Akiko Ochiai , Keizo Sakuda , Yoshiyuki Tatsumi
发明人： Tomohiro Okumura , Akiko Ochiai , Keizo Sakuda , Yoshiyuki Tatsumi
IPC分类号： A61K9/00 , A61K47/32 , A61K47/26 , A61K47/10 , A61K47/14 , A61K31/454 , A61K9/06
CPC分类号： A61K31/454 , A61K9/0014 , A61K9/06 , A61K47/10 , A61K47/14 , A61K47/26 , A61K47/32
摘要： The present invention provides a stable gel composition for mycosis treatment, with increased absorption and permeation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin -1-yl)-1-(1H-1,2,4-triazol-1-yl)-butan-2-ol into a target site (skin and nail). The gel composition for mycosis treatment, comprises (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl) -1-(1H-1,2,4-triazol-1-yl)-butan-2-ol or an acid addition salt thereof, a lower alcohol, a polyhydric alcohol and a gel-forming polymer. The gel composition of the present invention increases permeation of the above compound into a target site and into the nail. The gel composition of the present invention allows the drug to be directly and rapidly absorbed and permeated into a target site in a constant manner, for mycosis treatment, particularly onychomycosis treatment.
摘要翻译：本发明提供了用于真菌病治疗的稳定凝胶组合物，其中（2R，3R）-2-（2,4-二氟苯基）-3-（4-亚甲基哌啶-1-基）-1-（1H -1,2,4-三唑-1-基） - 丁-2-醇转化成靶位点（皮肤和指甲）。用于真菌病治疗的凝胶组合物包含（2R，3R）-2-（2,4-二氟苯基）-3-（4-亚甲基哌啶-1-基）-1-（1H-1,2,4-三唑-1-基） - 丁基） - 丁-2-醇或其酸加成盐，低级醇，多元醇和凝胶形成聚合物。本发明的凝胶组合物增加了上述化合物渗透到靶部位和钉子中。本发明的凝胶组合物允许药物以恒定的方式直接且快速地吸收并渗透到靶位点，用于真菌病治疗，特别是甲真菌病治疗。

4. 发明申请

US20100317695A1 GEL COMPOSITION FOR TREATING MYCOSIS 有权
标题翻译：用于治疗糖皮质激素的凝胶组合物
公开(公告)号：US20100317695A1
公开(公告)日：2010-12-16
申请号：US12521483
申请日：2007-12-28
申请人： Tomohiro Okumura , Akiko Ochiai , Keizo Sakuda , Yoshiyuki Tatsumi
发明人： Tomohiro Okumura , Akiko Ochiai , Keizo Sakuda , Yoshiyuki Tatsumi
IPC分类号： A61K31/454 , A61P31/10
CPC分类号： A61K31/454 , A61K9/0014 , A61K9/06 , A61K47/10 , A61K47/14 , A61K47/26 , A61K47/32
摘要： The present invention aims to provide a gel composition for mycosis treatment, which ensures good absorption and permeation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)-butan-2-ol into a target site (skin and nail). The present invention also aims to provide a gel composition for mycosis treatment, which is excellent in stability of this drug.It is a gel composition for mycosis treatment, which comprises (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)-butan-2-ol or an acid addition salt thereof, a lower alcohol, a polyhydric alcohol and a gel-forming polymer.The gel composition of the present invention is excellent in permeation of KP-103 into a target site and also excellent in permeation into the nail. Thus, the gel composition of the present invention allows the drug to be directly and rapidly absorbed and permeated into a target site in a constant manner, and thereby produces an excellent effect in mycosis treatment, particularly onychomycosis treatment.
摘要翻译：本发明旨在提供用于真菌病治疗的凝胶组合物，其确保（2R，3R）-2-（2,4-二氟苯基）-3-（4-亚甲基哌啶-1-基）-1- （1H-1,2,4-三唑-1-基） - 丁-2-醇转化成靶位点（皮肤和指甲）。本发明的目的还在于提供一种用于真菌病治疗的凝胶组合物，该药物的稳定性优异。它是用于真菌病治疗的凝胶组合物，其包含（2R，3R）-2-（2,4-二氟苯基）-3-（4-亚甲基哌啶-1-基）-1-（1H- 三唑-1-基） - 丁-2-醇或其酸加成盐，低级醇，多元醇和形成凝胶的聚合物。本发明的凝胶组合物的KP-103在目标部位的渗透性优异，对于指甲的渗透性优异。因此，本发明的凝胶组合物能够使药物以恒定的方式直接且快速地吸收并渗透到靶部位，从而在真菌病治疗，特别是甲真菌病治疗中产生优异的效果。

5. 发明授权

US07214506B2 Method for treating onychomycosis 有权
公开(公告)号：US07214506B2
公开(公告)日：2007-05-08
申请号：US10685266
申请日：2003-10-14
申请人： Yoshiyuki Tatsumi , Mamoru Yokoo , Kosho Nakamura , Tadashi Arika
发明人： Yoshiyuki Tatsumi , Mamoru Yokoo , Kosho Nakamura , Tadashi Arika
IPC分类号： C12Q1/18 , A01N43/26 , A01N43/34 , A61K31/445
CPC分类号： C07D231/12 , A61K31/4196 , A61K31/454 , C07D233/56 , C07D249/08 , C07D401/12 , C12Q1/04 , C12Q1/18 , G01N33/56911 , G01N33/56961 , G01N2500/00
摘要： A novel method for evaluating an effect of an antimicrobial agent which comprises removing the antimicrobial agent remaining in a biological sample or the like to thereby accurately evaluate the effect of the antimicrobial agent without being affected by the remaining antimicrobial agent. A therapeutic agent for onychomycosis which can be obtained according to the evaluation method of the drug effect.

6. 发明申请

US20070082375A1 Method for treating onychomycosis 有权
标题翻译：治疗甲真菌病的方法
公开(公告)号：US20070082375A1
公开(公告)日：2007-04-12
申请号：US10685266
申请日：2003-10-14
申请人： Yoshiyuki Tatsumi , Mamoru Yokoo , Kosho Nakamura , Tadashi Arika
发明人： Yoshiyuki Tatsumi , Mamoru Yokoo , Kosho Nakamura , Tadashi Arika
IPC分类号： C12Q1/18 , C12Q1/04
CPC分类号： C07D231/12 , A61K31/4196 , A61K31/454 , C07D233/56 , C07D249/08 , C07D401/12 , C12Q1/04 , C12Q1/18 , G01N33/56911 , G01N33/56961 , G01N2500/00
摘要： A novel method for evaluating an effect of an antimicrobial agent which comprises removing the antimicrobial agent remaining in a biological sample or the like to thereby accurately evaluate the effect of the antimicrobial agent without being affected by the remaining antimicrobial agent. A therapeutic agent for onychomycosis which can be obtained according to the evaluation method of the drug effect.
摘要翻译：一种用于评估抗微生物剂效果的新方法，其包括除去残留在生物样品等中的抗微生物剂，从而准确地评估抗微生物剂的效果而不受剩余的抗微生物剂的影响。根据药物作用的评价方法可以得到甲癣治疗剂。

7. 发明申请

US20080003636A1 Method for detecting pathogenic microorganism and antimicrobial agent, method for evaluating effect of antimicrobial agent, and antimicrobial agent 审中-公开
标题翻译：检测病原微生物和抗微生物剂的方法，评价抗菌剂效果的方法和抗菌剂
公开(公告)号：US20080003636A1
公开(公告)日：2008-01-03
申请号：US11728766
申请日：2007-03-27
申请人： Yoshiyuki Tatsumi , Mamoru Yokoo , Kosho Nakamura , Tadashi Arika
发明人： Yoshiyuki Tatsumi , Mamoru Yokoo , Kosho Nakamura , Tadashi Arika
IPC分类号： C12Q1/18 , C12Q1/04
CPC分类号： C07D231/12 , A61K31/4196 , A61K31/454 , C07D233/56 , C07D249/08 , C07D401/12 , C12Q1/04 , C12Q1/18 , G01N33/56911 , G01N33/56961 , G01N2500/00
摘要： A novel method for evaluating an effect of an antimicrobial agent which comprises removing the antimicrobial agent remaining in a biological sample or the like to thereby accurately evaluate the effect of the antimicrobial agent without being affected by the remaining antimicrobial agent. A therapeutic agent for onychomycosis which can be obtained according to the evaluation method of the drug effect.
摘要翻译：一种用于评估抗微生物剂效果的新方法，其包括除去残留在生物样品等中的抗微生物剂，从而准确地评估抗微生物剂的效果而不受剩余的抗微生物剂的影响。根据药物作用的评价方法可以得到甲癣治疗剂。

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