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1. 发明授权

US08952044B2 Antimycotic pharmaceutical composition 有权
标题翻译：抗真菌药物组合物
公开(公告)号：US08952044B2
公开(公告)日：2015-02-10
申请号：US13389071
申请日：2010-07-29
申请人： Hirokazu Kobayashi , Nobuo Kubota
发明人： Hirokazu Kobayashi , Nobuo Kubota
IPC分类号： A01N43/10 , A01N25/00 , A61K31/4178 , A61K9/00 , A61K47/08
CPC分类号： A61K31/4178 , A61K9/0014 , A61K47/08 , A61P17/00 , A61P31/10
摘要： A pharmaceutical composition which comprises 1) a compound represented by the following general formula (1) and/or a salt thereof; and 2) a ketone such as methyl ethyl ketone. Preferably, the compound represented by the following general formula (1) is luliconazole, where R1═R2=a chlorine atom: where R1 and R2 each independently represents a hydrogen atom or a halogen atom, and at least one of R1 and R2 represents a halogen atom. The present invention provides a preparation excellent in solubilization stability for a compound represented by the general formula (1) and/or a salt thereof in low-temperature or high-temperature storage.
摘要翻译：一种药物组合物，其包含1）由以下通式（1）表示的化合物和/或其盐; 和2）酮如甲基乙基酮。优选地，由以下通式（1）表示的化合物是卢可康唑，其中R 1 = R 2 =氯原子：其中R 1和R 2各自独立地表示氢原子或卤素原子，并且R 1和R 2中的至少一个表示卤素原子。本发明提供了在低温或高温储存中对通式（1）表示的化合物和/或其盐的增溶稳定性优异的制剂。

2. 发明授权

US08420687B2 Pharmaceutical composition 有权
公开(公告)号：US08420687B2
公开(公告)日：2013-04-16
申请号：US13362545
申请日：2012-01-31
申请人： Yasushi Murakami , Naoko Kobayashi , Azuma Nishio , Nobuo Kubota
发明人： Yasushi Murakami , Naoko Kobayashi , Azuma Nishio , Nobuo Kubota
IPC分类号： A01N43/52 , A61K31/415 , C07D233/28 , C07D233/91
CPC分类号： A61K31/4168 , A61K9/0019 , A61K47/12 , A61K47/18 , A61K47/22
摘要： To provide a pharmaceutical composition which can enhance the storage stability of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole without impairing the effect of the compound.The pharmaceutical composition includes 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole, which is represented by formula (1): and a compound having chelating ability.

3. 发明申请

US20120129905A1 PHARMACEUTICAL COMPOSITION 有权
标题翻译：药物组合物
公开(公告)号：US20120129905A1
公开(公告)日：2012-05-24
申请号：US13362527
申请日：2012-01-31
申请人： Yasushi MURAKAMI , Naoko Kobayashi , Azuma Nishio , Nobuo Kubota
发明人： Yasushi MURAKAMI , Naoko Kobayashi , Azuma Nishio , Nobuo Kubota
IPC分类号： A61K31/4168 , A61P35/00
CPC分类号： A61K31/4168 , A61K9/0019 , A61K47/12 , A61K47/18 , A61K47/22
摘要： To provide a pharmaceutical composition which can enhance the storage stability of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole without impairing the effect of the compound.The pharmaceutical composition includes 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole, which is represented by formula (1): and a compound having chelating ability.
摘要翻译：提供能够提高1-（1-羟甲基-2,3-二羟基丙氧基甲基）-2-硝基咪唑的保存稳定性的药物组合物，而不损害化合物的作用。药物组合物包括由式（1）表示的1-（1-羟甲基-2,3-二羟基丙氧基甲基）-2-硝基咪唑：和具有螯合能力的化合物。

4. 发明授权

US10130610B2 Antimycotic pharmaceutical composition 有权
公开(公告)号：US10130610B2
公开(公告)日：2018-11-20
申请号：US13258114
申请日：2010-04-09
申请人： Hirokazu Kobayashi , Eiko Kosugi , Nobuo Kubota
发明人： Hirokazu Kobayashi , Eiko Kosugi , Nobuo Kubota
IPC分类号： A61K31/4178 , A61K9/00 , A61K9/08 , A61K9/70 , A61K47/08 , A61K47/10 , A61K47/14
摘要： In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof in an amount of 5% by mass or more, comprised is/are acetone, a polyoxyethylene alkyl (having 8 to 30 carbon atoms) ether, and/or a polyoxyethylene alkenyl (having 8 to 30 carbon atoms) ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrrolidone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60° C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20° C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5° C. for 2 weeks after manufacture.

5. 发明申请

US20130090365A1 ANTIMYCOTIC PHARMACEUTICAL COMPOSITION 有权
标题翻译：抗生物药物组合物
公开(公告)号：US20130090365A1
公开(公告)日：2013-04-11
申请号：US13703300
申请日：2011-06-10
申请人： Nobuo Kubota , Hirokazu Kobayashi , Takaaki Masuda
发明人： Nobuo Kubota , Hirokazu Kobayashi , Takaaki Masuda
IPC分类号： A61K31/4178 , A61K47/22 , A61K47/10 , A61K47/14
CPC分类号： A61K31/4178 , A61K9/0014 , A61K9/08 , A61K31/385 , A61K47/10 , A61K47/14 , A61K47/22
摘要： An object is to provide a medicament preparation which is excellent in the solubilization stability in relation to a compound represented by the general formula (1) during the storage in a low temperature region and a high temperature region. The present invention resides in a pharmaceutical composition comprising 1) the compound represented by the general formula (1) and/or a salt thereof and 2) a polyhydric alcohol derivative. General formula (1) (In the formula, R1, R2 independently represent hydrogen atom or halogen atom respectively, and at least one of R1, R2 is halogen atom.)
摘要翻译：本发明提供一种药物制剂，其在低温区域和高温区域的储存过程中，相对于由通式（1）表示的化合物的溶解稳定性优异。本发明涉及一种药物组合物，其包含1）由通式（1）表示的化合物和/或其盐和2）多元醇衍生物。通式（1）（式中，R 1，R 2分别独立地表示氢原子或卤原子，R 1，R 2中的至少一个为卤素原子）

6. 发明授权

US08258166B2 Pharmaceutical composition 有权
标题翻译：药物组成
公开(公告)号：US08258166B2
公开(公告)日：2012-09-04
申请号：US13365723
申请日：2012-02-03
申请人： Yasushi Murakami , Naoko Kobayashi , Azuma Nishio , Nobuo Kubota
发明人： Yasushi Murakami , Naoko Kobayashi , Azuma Nishio , Nobuo Kubota
IPC分类号： A01N43/52 , A61K31/415 , C07D233/28 , C07D233/91
CPC分类号： A61K9/08 , A61K9/0019 , A61K31/4168 , A61K41/0038 , C07D233/91
摘要： A Cancer radiotherapeutic method using 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole (compound (i), and creatinine in an amount of 0.001 to part by mass with respect to 1 part by mass of compound (1); and irradiation.
摘要翻译：相对于1质量份化合物，使用1-（1-羟甲基-2,3-二羟丙基）氧甲基-2-硝基咪唑（化合物（i））和肌酸酐0.001〜质量份的癌症放射治疗法 1）和照射。

7. 发明申请

US20120022120A1 ANTIMYCOTIC PHARMACEUTICAL COMPOSITION 有权
标题翻译：抗生物药物组合物
公开(公告)号：US20120022120A1
公开(公告)日：2012-01-26
申请号：US13258324
申请日：2010-04-09
申请人： Hirokazu Kobayashi , Eiko Kosugi , Nobuo Kubota
发明人： Hirokazu Kobayashi , Eiko Kosugi , Nobuo Kubota
IPC分类号： A61K31/427 , A61P31/10
CPC分类号： A61K9/7015 , A61K9/0014 , A61K9/08 , A61K31/4178
摘要： In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof, comprised are a higher alcohol which is in a liquid state at 1 atm and 25° C. and/or a diester of a dibasic acid, provided that a diester carbonate is excluded, and a polyoxyethylene alkyl ether and/or a polyoxyethylene alkenyl ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrroridone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60 degrees C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20° C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5° C. for 2 weeks after manufacture.
摘要翻译：在含有诸如卢可康唑和/或其盐的化合物的外用药物组合物中，包括在1大气压和25℃下处于液体状态的高级醇和/或二元酸的二酯，不包括碳酸二酯，聚氧乙烯烷基醚和/或聚氧乙烯烯基醚。本发明提供使用克罗他米通以外的溶剂，碳酸亚丙酯和N-甲基-2-吡咯烷酮作为增溶和空间稳定化的溶剂的制剂，具有以下性质：1）当由通式（1）表示的化合物和 /或其盐具有立体异构体，在60℃的保存条件下生产的化合物和/或其盐的立体异构体的量为3周时相对于总质量为1质量％化合物和/或其盐在保存开始时; 2）制备后立即在20°C的恒温下保存时，制剂处于透明液体状态; 和3）当制剂在制备后在5℃下保存2周后，不沉积晶体。

8. 发明授权

US09491933B2 Infected nail of animal infected with fungus 有权
标题翻译：感染真菌感染的指甲
公开(公告)号：US09491933B2
公开(公告)日：2016-11-15
申请号：US12810202
申请日：2008-12-25
申请人： Nobuo Kubota , Tsuyoshi Shimamura , Saori Nagasaka
发明人： Nobuo Kubota , Tsuyoshi Shimamura , Saori Nagasaka
IPC分类号： A61K48/00 , A01K67/00 , C12Q1/02 , C12Q1/18
CPC分类号： A01K67/00 , A01K2207/10 , A01K2227/107 , A01K2267/0337 , C12Q1/025 , C12Q1/18
摘要： The invention can produce an infected nail of an animal and an infected animal model in which the nail plate and nail bed of the nail are sufficiently infected with a superficial fungus which were difficult to be produced in the past, and provides an evaluation method useful for development of a therapeutic agent for intractable infectious diseases such as tinea unguium using the nail and the infected animal model. For producing the infected nail of an animal and the infected animal model infected with a superficial fungus, an immunosuppressive component is administered to an animal in advance to decrease immunocompetence, and then, a superficial fungus is inoculated into the animal, whereby the infected nail of an animal and the infected animal model reflecting clinical manifestation in which the nail plate and nail bed of the nail are sufficiently infected with the superficial fungus can be produced with good reproducibility in a short period of time.
摘要翻译：本发明可以产生感染的动物指甲和感染的动物模型，其中钉子的甲板和甲板被过去难以产生的浅表真菌充分感染，并且提供了用于使用指甲和感染动物模型开发难治性感染性疾病如癣菌的治疗剂。为了产生受感染的动物指甲和感染表皮真菌的受感染动物模型，预先向动物施用免疫抑制成分以降低免疫能力，然后将表面真菌接种到动物中，由此将受感染的指甲可以在短时间内以良好的再现性产生反映临床表现的动物和感染的动物模型，其中甲板的指甲板和甲床被表面真菌充分感染。

9. 发明授权

US09050271B2 Antimycotic pharmaceutical composition 有权
标题翻译：抗真菌药物组合物
公开(公告)号：US09050271B2
公开(公告)日：2015-06-09
申请号：US13258324
申请日：2010-04-09
申请人： Hirokazu Kobayashi , Eiko Kosugi , Nobuo Kubota
发明人： Hirokazu Kobayashi , Eiko Kosugi , Nobuo Kubota
IPC分类号： A61K31/4178 , A61K9/70 , A61K9/00 , A61K9/08
CPC分类号： A61K9/7015 , A61K9/0014 , A61K9/08 , A61K31/4178
摘要： In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof, comprised are a higher alcohol which is in a liquid state at 1 atm and 25° C. and/or a diester of a dibasic acid, provided that a diester carbonate is excluded, and a polyoxyethylene alkyl ether and/or a polyoxyethylene alkenyl ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrroridone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60 degrees C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20° C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5° C. for 2 weeks after manufacture.
摘要翻译：在含有诸如卢可康唑和/或其盐的化合物的外用药物组合物中，包括在1大气压和25℃下处于液体状态的高级醇和/或二元酸的二酯，不包括碳酸二酯，聚氧乙烯烷基醚和/或聚氧乙烯烯基醚。本发明提供使用克罗他米通以外的溶剂，碳酸亚丙酯和N-甲基-2-吡咯烷酮作为增溶和空间稳定化的溶剂的制剂，具有以下性质：1）当由通式（1）表示的化合物和 /或其盐具有立体异构体，在60℃的保存条件下生产的化合物和/或其盐的立体异构体的量为3周时相对于总质量为1质量％化合物和/或其盐在保存开始时; 2）制备后立即在20°C的恒温下保存时，制剂处于透明液体状态; 和3）当制剂在制备后在5℃下保存2周后，不沉积晶体。

10. 发明申请

US20090030059A1 PHARMACEUTICAL COMPOSITION FOR EXTERNAL USE 有权
标题翻译：用于外用的药物组合物
公开(公告)号：US20090030059A1
公开(公告)日：2009-01-29
申请号：US12281969
申请日：2006-10-02
申请人： Toyohiko Miki , Akira Nozawa , Nobuo Kubota , Susumu Tomiyama , Hirokazu Kobayashi
发明人： Toyohiko Miki , Akira Nozawa , Nobuo Kubota , Susumu Tomiyama , Hirokazu Kobayashi
IPC分类号： A61K31/4178
CPC分类号： A61K31/4178 , A61K31/19 , A61K2300/00
摘要： Provided is a pharmaceutical composition for external use, including: (i) luliconazole represented by the following structural formula (1) and/or a salt thereof; and (ii) α-hydroxycarboxylic acid and/or a salt thereof.
摘要翻译：本发明提供一种外用药物组合物，其包括：（i）由以下结构式（1）表示的联利康唑和/或其盐; 和（ii）α-羟基羧酸和/或其盐。

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