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1. 发明授权

US09782484B2 Method for producing a composite organic compound powder for medical use 有权
公开(公告)号：US09782484B2
公开(公告)日：2017-10-10
申请号：US14010602
申请日：2013-08-27
申请人： ACTIVUS PHARMA CO., LTD.
发明人： Takashi Hirokawa , Takahiro Tada , Jun Nihira
IPC分类号： A61K47/34 , A61K9/10 , A61K9/14 , A61K31/4174 , A61K31/222 , A61K31/573 , A61K47/24 , A61K47/26 , A61K47/32 , A61K31/41 , A61K31/192 , A61K31/405
CPC分类号： A61K47/34 , A61K9/10 , A61K9/146 , A61K31/192 , A61K31/222 , A61K31/405 , A61K31/41 , A61K31/4174 , A61K31/573 , A61K47/24 , A61K47/26 , A61K47/32
摘要： The purpose of present invention is to provide a medicine which has low contamination with a fine-pulverizing medium, is safe and has improved bioavailability.A method for producing a composite organic compound powder for medical use is used which comprises: mixing a poorly water-soluble and crystalline organic compound powder, a physiologically acceptable salt, a physiologically acceptable polyol, and a carboxyvinyl polymer and fine-pulverizing the organic compound powder; and removing at least the salt and the polyol during or after fine-pulverizing.

2. 发明授权

US11376262B2 Method of treating an inflammatory or infectious disease 有权
公开(公告)号：US11376262B2
公开(公告)日：2022-07-05
申请号：US16732173
申请日：2019-12-31
申请人： Activus Pharma Co., Ltd.
发明人： Takahiro Tada , Kazuhiro Kagami , Kenta Kikuchi
IPC分类号： A61K31/573 , A61K47/10 , A61K47/12 , A61K47/24 , A61K47/32 , A61K47/34 , A61K47/38 , A61K31/57 , A61K31/58 , A61K9/10 , A61P31/04 , A61P29/00
摘要： A method of treating an inflammatory or infectious disease includes administering an effective amount of pharmaceutical composition to a subject in need of treatment of the inflammatory or infectious disease. The composition includes an aqueous suspension of nanoparticles of a glucocorticosteroid compound.

3. 发明授权

US10588913B2 Aqueous suspension agent containing glucocorticosteroid nanoparticles 有权
公开(公告)号：US10588913B2
公开(公告)日：2020-03-17
申请号：US15571986
申请日：2016-05-09
申请人： ACTIVUS PHARMA CO., LTD.
发明人： Takahiro Tada , Kazuhiro Kagami , Kenta Kikuchi
IPC分类号： A61K31/573 , A61K31/58 , A61K31/57 , A61K47/10 , A61K9/10 , A61K47/34 , A61K47/32 , A61K47/24 , A61K47/12 , A61K47/38 , A61P31/04 , A61P29/00
摘要： An aqueous suspension containing as an active component a glucocorticosteroid compound is described. The aqueous suspension contains nanoparticles of a glucocorticosteroid compound and a dispersion stabilizer. The nanoparticles have a mean particle diameter of 300 nm or less and a D90 particle diameter of 450 nm or less. The pharmaceutical compositions containing the aqueous suspension are for parenteral administrations, injections, eye drops or ear drops. More specifically the aqueous suspensions containing glucocorticosteroid nanoparticles are used as an eye drop for treating or preventing inflammatory diseases of the eye or an ear drop for treating or preventing inflammatory diseases of the ear.

4. 发明授权

US08226983B2 Method for producing pulverized organic compound particle 有权
标题翻译：粉碎有机化合物颗粒的制造方法
公开(公告)号：US08226983B2
公开(公告)日：2012-07-24
申请号：US12585786
申请日：2009-09-24
申请人： Takashi Hirokawa , Takahiro Tada
发明人： Takashi Hirokawa , Takahiro Tada
IPC分类号： A61K9/14
CPC分类号： A61K31/015 , A61K9/0019 , A61K9/0073 , A61K9/14 , A61K31/192 , A61K31/216 , A61K31/404 , A61K31/41 , A61K31/4174 , A61K31/4422 , A61K31/4704 , A61K31/56 , A61K31/57 , A61K31/573 , Y10T428/2982
摘要： Disclosed is a method for producing pulverized particles of a crystalline organic compound which is poorly water-soluble. Also disclosed is a pulverized organic compound particle produced by such a method. Specifically disclosed is a method for producing a poor water solubility organic compound particle for medical use, which is characterized in that a poor water solubility organic compound for medical use is mixed with a physiologically acceptable salt and a physiologically acceptable polyol, and subjected to wet milling. Also specifically disclosed is a poor water solubility organic compound particle for medical use, which is produced by such a production method.
摘要翻译：公开了一种水溶性差的结晶有机化合物的粉碎微粒的制造方法。还公开了通过这种方法制造的粉碎的有机化合物颗粒。具体公开了一种生产用于医疗用途的差的水溶性有机化合物颗粒的方法，其特征在于将用于医疗用途的难溶性有机化合物与生理上可接受的盐和生理上可接受的多元醇混合，并进行湿磨。还具体公开了通过这种制造方法制造的用于医疗用途的差的水溶性有机化合物颗粒。

5. 发明申请

US20110021621A1 Drug for treating circulatory insufficiency 审中-公开
标题翻译：用于治疗循环功能不全的药物
公开(公告)号：US20110021621A1
公开(公告)日：2011-01-27
申请号：US12923589
申请日：2010-09-29
申请人： Hidetsugu Takagaki , Yasuo Aoki , Mitsuteru Ishiwara
发明人： Hidetsugu Takagaki , Yasuo Aoki , Mitsuteru Ishiwara
IPC分类号： A61K31/353 , C07D311/56 , A61P7/00 , A61P9/00
CPC分类号： C07D311/56 , A61K31/37
摘要： The present invention relate to a drug for treating circulatory insufficiency containing a benzopyran derivative represented by the following general formula (I): and/or a physiologically acceptable salt thereof as an active ingredient, wherein R1 is an alkyl group having 1 to 10 carbon atoms, or an alkenyl group having 2 to 10 carbon atoms; and any one of R2, R3, R4 and R5 is a hydroxyl group, an alkoxy group, an alkenyloxy group, an alkoxy group substituted with a hydroxyl group, or an alkoxy group substituted with a carboxy group, and the others are hydrogen atoms.
摘要翻译：本发明涉及含有下列通式（I）表示的苯并吡喃衍生物的循环功能不全药物：和/或其生理学上可接受的盐作为有效成分，其中R1为碳原子数1〜10的烷基，或具有2〜10个碳原子的烯基; R 2，R 3，R 4和R 5中的任一个是羟基，烷氧基，烯氧基，被羟基取代的烷氧基或被羧基取代的烷氧基，其它是氢原子。

6. 发明授权

US10792248B2 Aqueous suspension preparation comprising nanoparticles of macrolide antibacterial agent 有权
公开(公告)号：US10792248B2
公开(公告)日：2020-10-06
申请号：US15034437
申请日：2014-11-07
申请人： ACTIVUS PHARMA CO., LTD.
发明人： Takahiro Tada , Kazuhiro Kagami , Shiro Yokota , Kenta Kikuchi
IPC分类号： A61K9/10 , A61K47/32 , A61K47/38 , A61K31/7048 , A61K9/00 , A61K9/14 , A61K47/10 , A61K47/26 , A61K31/7052 , A61K47/44
摘要： An aqueous suspension preparation that comprises a macrolide antibacterial agent as an active component.The aqueous suspension preparation is characterized by comprising nanoparticles of a macrolide antibacterial agent and a dispersion stabilizer; an aqueous suspension in which the average particle size of nanoparticles is 500 nm or less and the D90 particle size is 1,500 nm or less; a parenterally administered pharmaceutical composition that comprises this aqueous suspension preparation; an injection preparation; and eye drops or ear drops, more specifically, eye drops for the treatment or prevention of inflammatory diseases of the eye or ear drops for the treatment or prevention of inflammatory diseases of the ear.

7. 发明申请

US20120237768A1 METHOD FOR PRODUCING PULVERIZED ORGANIC COMPOUND PARTICLE 审中-公开
标题翻译：生产有机有机化合物颗粒的方法
公开(公告)号：US20120237768A1
公开(公告)日：2012-09-20
申请号：US13484460
申请日：2012-05-31
申请人： Takashi HIROKAWA , Takahiro Tada
发明人： Takashi HIROKAWA , Takahiro Tada
IPC分类号： B32B5/16
CPC分类号： A61K31/015 , A61K9/0019 , A61K9/0073 , A61K9/14 , A61K31/192 , A61K31/216 , A61K31/404 , A61K31/41 , A61K31/4174 , A61K31/4422 , A61K31/4704 , A61K31/56 , A61K31/57 , A61K31/573 , Y10T428/2982
摘要： Disclosed is a method for producing pulverized particles of a crystalline organic compound which is poorly water-soluble. Also disclosed is a pulverized organic compound particle produced by such a method. Specifically disclosed is a method for producing a poor water solubility organic compound particle for medical use, which is characterized in that a poor water solubility organic compound for medical use is mixed with a physiologically acceptable salt and a physiologically acceptable polyol, and subjected to wet milling. Also specifically disclosed is a poor water solubility organic compound particle for medical use, which is produced by such a production method.
摘要翻译：公开了一种水溶性差的结晶有机化合物的粉碎微粒的制造方法。还公开了通过这种方法制造的粉碎的有机化合物颗粒。具体公开了一种生产用于医疗用途的差的水溶性有机化合物颗粒的方法，其特征在于将用于医疗用途的难溶性有机化合物与生理上可接受的盐和生理上可接受的多元醇混合，并进行湿磨。还具体公开了通过这种制造方法制造的用于医疗用途的差的水溶性有机化合物颗粒。

8. 发明授权

US07687546B2 Quaternary ammonium compound, process for producing the same, therapeutic agent for cerebrovascular disorder, and therapeutic agent for heart disease 失效
标题翻译：第四季铵化合物，其制备方法，脑血管障碍治疗剂和心脏病治疗剂
公开(公告)号：US07687546B2
公开(公告)日：2010-03-30
申请号：US10594545
申请日：2005-03-29
申请人： Hidetsugu Takagaki , Yoshiyuki Sano , Yasuyuki Katakami , Masanori Miyamoto
发明人： Hidetsugu Takagaki , Yoshiyuki Sano , Yasuyuki Katakami , Masanori Miyamoto
IPC分类号： A01N33/12 , A61K31/14
CPC分类号： C07C217/22 , A61K31/205 , C07C309/42
摘要： A quaternary ammonium compound of the present invention is a quaternary ammonium compound represented by general formula (I) or (I′) (wherein, A represents a linear alkyl group having 1 to 4 carbon atoms, a branched alkyl group having 2 to 4 carbon atoms, a linear alkyl group having 1 to 4 carbon atoms and a hydroxyl group, or a branched alkyl group having 2 to 4 carbon atoms and a hydroxyl group, R1 to R3 may be the same or different and represent a linear or branched alkyl group having 1 to 12 carbon atoms, one of R4 to R8 represents CO2− or SO3−, while no more than three of the remaining R4 to R8 represent a group selected from the group consisting of a hydroxyl group and an alkoxy group having 1 to 4 carbon atoms, and other R4 to R8 represent a hydrogen atom, one of R′4 to R′8 represents CO2H or SO3H, no more than three of the remaining R′4 to R′8 represent a group selected from a protected hydroxyl group and an alkoxy group having 1 to 4 carbon atoms, while other R′4 to R′8 represent a hydrogen atom, and X− represents an anion capable of forming a salt with a quaternary ammonium group).
摘要翻译：本发明的季铵化合物是由通式（I）或（I'）（表示的季铵化合物，其中，A表示具有1至4个碳原子，具有2-4个碳支链烷基的直链烷基原子，碳原子数为1〜4的直链烷基和羟基的基团，或具有2至4个碳原子和羟基基团的支链烷基，R1至R3可以相同或不同，表示直链或支链的烷基具有1至12个碳原子，R4中的一个来R8表示CO 2 - 或SO 3 - ，而不超过三个剩余的R 4至R 8中的表示选自羟基的基团和具有1至4的烷氧基中的基团碳原子，并且另一个R 4至R 8表示氢原子，R'4中的一个来表示R 18 CO 2 H或SO 3 H，不超过三个剩余的R'4至R'8的表示从受保护的羟基中的基团和具有1至4个碳原子的烷氧基，而其它R 4至R'8表示氢原子，X - 表示能够形成与季铵基团的盐）的阴离子。

9. 发明申请

US20100016597A1 Method for producing pulverized organic compound particle 有权
标题翻译：粉碎有机化合物颗粒的制造方法
公开(公告)号：US20100016597A1
公开(公告)日：2010-01-21
申请号：US12585786
申请日：2009-09-24
申请人： Takashi Hirokawa , Takahiro Tada
发明人： Takashi Hirokawa , Takahiro Tada
IPC分类号： C07D215/00 , C07D209/26 , C07D213/80 , C07J5/00 , C07C69/66 , C07J7/00 , C07D233/54 , C07C59/76 , C07D257/04 , B02C23/18
CPC分类号： A61K31/015 , A61K9/0019 , A61K9/0073 , A61K9/14 , A61K31/192 , A61K31/216 , A61K31/404 , A61K31/41 , A61K31/4174 , A61K31/4422 , A61K31/4704 , A61K31/56 , A61K31/57 , A61K31/573 , Y10T428/2982
摘要： Disclosed is a method for producing pulverized particles of a crystalline organic compound which is poorly water-soluble. Also disclosed is a pulverized organic compound particle produced by such a method. Specifically disclosed is a method for producing a poor water solubility organic compound particle for medical use, which is characterized in that a poor water solubility organic compound for medical use is mixed with a physiologically acceptable salt and a physiologically acceptable polyol, and subjected to wet milling. Also specifically disclosed is a poor water solubility organic compound particle for medical use, which is produced by such a production method.
摘要翻译：公开了一种水溶性差的结晶有机化合物的粉碎微粒的制造方法。还公开了通过这种方法制造的粉碎的有机化合物颗粒。具体公开了一种生产用于医疗用途的差的水溶性有机化合物颗粒的方法，其特征在于将用于医疗用途的难溶性有机化合物与生理上可接受的盐和生理上可接受的多元醇混合，并进行湿磨。还具体公开了通过这种制造方法制造的用于医疗用途的差的水溶性有机化合物颗粒。

10. 发明授权

US09278071B2 Organic compound nano-powder, method for producing the same and suspension 有权
标题翻译：有机复合纳米粉，其制备方法及悬浮液
公开(公告)号：US09278071B2
公开(公告)日：2016-03-08
申请号：US14001645
申请日：2013-05-11
申请人： Activus Pharma Co., Ltd.
发明人： Takahiro Tada , Kazuhiro Kagami , Shiro Yokota
IPC分类号： A61K9/50 , A61K9/14 , B02C1/00 , A61K9/16 , A61K31/12 , A61K31/167 , A61K31/192 , A61K31/196 , A61K31/405 , A61K31/41 , A61K31/445 , A61K31/57 , A61K31/573 , A61K31/7048 , B02C23/18 , A61K9/10 , A61K31/216 , A61K9/00
CPC分类号： A61K9/1682 , A61K9/0048 , A61K9/10 , A61K9/145 , A61K9/146 , A61K31/12 , A61K31/167 , A61K31/192 , A61K31/196 , A61K31/216 , A61K31/405 , A61K31/41 , A61K31/445 , A61K31/57 , A61K31/573 , A61K31/7048 , B02C23/18
摘要： An organic compound nano-powder comprising a granular organic compound with an average particle diameter of 500 nm or less and a 90%-diameter of less than 1500 nm and a carbohydrate compound comprising at least any one of a sugar and a sugar alcohol and with amount of 0.3 times or more by mass relative to amount of the organic compound, a method for producing the same, and a suspension having the organic compound dispersed in a liquid dispersion medium in which the organic compound is insoluble or poorly soluble.
摘要翻译：一种有机化合物纳米粉末，其包含平均粒径为500nm以下且90％直径小于1500nm的粒状有机化合物，以及包含糖和糖醇中的至少任一种的碳水化合物，相对于有机化合物的量为0.3倍以上的量，其制造方法和分散在有机化合物不溶或难溶性的液体分散介质中的有机化合物的悬浮液。

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