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1. 发明申请

US20100166847A1 Method for coating fine particles with lipid membrane 审中-公开
标题翻译：用脂质膜包覆微粒的方法
公开(公告)号：US20100166847A1
公开(公告)日：2010-07-01
申请号：US12656487
申请日：2010-02-01
申请人： Yasuki Kato , Masahiro Yamauchi , Hiroko Kusano , Takeshi Iwata , Takaaki Uochi , Shiro Akinaga
发明人： Yasuki Kato , Masahiro Yamauchi , Hiroko Kusano , Takeshi Iwata , Takaaki Uochi , Shiro Akinaga
IPC分类号： A61K9/127 , A61K38/02 , A61K31/7088
CPC分类号： A61K9/5123 , A61K9/127 , A61K9/1271 , A61K9/1272 , A61K9/141 , A61K9/146 , A61K9/5015 , A61K9/5192 , A61K31/7088 , A61K47/6911 , B01J13/12
摘要： An object of the present invention is to provide a safe, convenient and efficient method for coating fine particles with lipid membrane.There is provided a method for coating fine particles with lipid membrane, characterized in that, the rate of a polar organic solvent in an aqueous solution containing the polar organic solvent where the fine particles are dispersed and lipid is dissolved, is decreased.
摘要翻译：本发明的目的是提供一种安全，方便和有效的用脂质膜涂覆微粒的方法。提供了一种用脂质膜包覆微粒的方法，其特征在于，含有分散有微粒的极性有机溶剂和溶解脂质的水溶液中的极性有机溶剂的比例降低。

2. 发明授权

US07678415B2 Method of coating fine particles with lipid film 有权
标题翻译：用脂质膜包覆微粒的方法
公开(公告)号：US07678415B2
公开(公告)日：2010-03-16
申请号：US10398222
申请日：2001-10-04
申请人： Yasuki Kato , Masahiro Yamauchi , Hiroko Kusano , Takeshi Iwata , Takaaki Uochi , Shiro Akinaga
发明人： Yasuki Kato , Masahiro Yamauchi , Hiroko Kusano , Takeshi Iwata , Takaaki Uochi , Shiro Akinaga
IPC分类号： B01J13/02 , B05D7/00
CPC分类号： A61K9/5123 , A61K9/127 , A61K9/1271 , A61K9/1272 , A61K9/141 , A61K9/146 , A61K9/5015 , A61K9/5192 , A61K31/7088 , A61K47/6911 , B01J13/12
摘要： An object of the present invention is to provide a safe, convenient and efficient method for coating fine particles with lipid membrane.There is provided a method for coating fine particles with lipid membrane, characterized in that, the rate of a polar organic solvent in an aqueous solution containing the polar organic solvent where the fine particles are dispersed and lipid is dissolved, is decreased.
摘要翻译：本发明的目的是提供一种安全，方便和有效的用脂质膜涂覆微粒的方法。提供了一种用脂质膜包覆微粒的方法，其特征在于，含有分散有微粒的极性有机溶剂和溶解脂质的水溶液中的极性有机溶剂的比例降低。

3. 发明授权

US09757344B2 Fine particles coated with lipid membrane 有权
公开(公告)号：US09757344B2
公开(公告)日：2017-09-12
申请号：US12656487
申请日：2010-02-01
申请人： Yasuki Kato , Masahiro Yamauchi , Hiroko Kusano , Takeshi Iwata , Takaaki Uochi , Shiro Akinaga
发明人： Yasuki Kato , Masahiro Yamauchi , Hiroko Kusano , Takeshi Iwata , Takaaki Uochi , Shiro Akinaga
IPC分类号： A61K9/19 , A61K9/64 , A61K9/51 , A61K9/14 , A61K9/127 , A61K9/50 , B01J13/12 , A61K31/7088 , A61K47/48
CPC分类号： A61K9/5123 , A61K9/127 , A61K9/1271 , A61K9/1272 , A61K9/141 , A61K9/146 , A61K9/5015 , A61K9/5192 , A61K31/7088 , A61K47/6911 , B01J13/12
摘要： A coated fine particle comprisisng: (i) a complex of a drug and a cationic lipid, wherein (a) the drug is a nucleic acid and the complex is obtained by mixing the drug and the cationic lipid in water, wherein the complex has a diameter of 10 nm to 1,000 nm, and (ii) a lipid layer formed of lipid(s), wherein the lipid(s) is selected from phospholipid, glyceroglycolipid, sphingoglycolipid, cholesterol and synthetic lipid, wherein the complex is coated with the lipid layer.

4. 发明授权

US07547675B2 Chemically modified polypeptides 失效
标题翻译：化学修饰的多肽
公开(公告)号：US07547675B2
公开(公告)日：2009-06-16
申请号：US10365418
申请日：2003-02-13
申请人： Motoo Yamasaki , Toshiyuki Suzawa , Ken Kobayashi , Noboru Konishi , Shiro Akinaga , Kumiko Maruyama
发明人： Motoo Yamasaki , Toshiyuki Suzawa , Ken Kobayashi , Noboru Konishi , Shiro Akinaga , Kumiko Maruyama
IPC分类号： A68K38/16 , C07K1/107
CPC分类号： C07K1/1077 , A61K38/00 , C07K14/535
摘要： The present invention relates to a chemically modified polypeptide in which at least one of hydroxyl groups in the polypeptide molecule is modified with a polyalkylene glycol derivative; a method for producing the modified polypeptide; a method of treatment using the modified polypeptide; use of the modified polypeptide; a pharmaceutical preparation comprising the modified polypeptide; and a composition for treatment comprising the modified polypeptide.
摘要翻译：本发明涉及化学修饰的多肽，其中所述多肽分子中的至少一个羟基用聚亚烷基二醇衍生物修饰; 生产修饰多肽的方法; 使用经修饰的多肽的治疗方法; 使用经修饰的多肽; 包含所述经修饰的多肽的药物制剂; 以及包含所述经修饰的多肽的治疗用组合物。

5. 发明授权

US06635662B2 Radicicol derivatives 失效
标题翻译：蓝霉素衍生物
公开(公告)号：US06635662B2
公开(公告)日：2003-10-21
申请号：US09791602
申请日：2001-02-26
申请人： Yoji Ino , Nobuyoshi Amishiro , Mayumi Miyata , Chikara Murakata , Harumi Ogawa , Tadakazu Akiyama , Shiro Akinaga , Shiro Soga , Yukimasa Shiotsu
发明人： Yoji Ino , Nobuyoshi Amishiro , Mayumi Miyata , Chikara Murakata , Harumi Ogawa , Tadakazu Akiyama , Shiro Akinaga , Shiro Soga , Yukimasa Shiotsu
IPC分类号： A61K3144
CPC分类号： C07D493/04 , C07D313/00
摘要： Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: wherein R1 and R2 are the same or different, and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl or tert-butyldimethylsilyl; R3 represents Y—R5 {wherein Y represents substituted or unsubstituted alkylene; and R5 represents CONR5R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl, and the like; R7 represents hydroxyl, substituted lower alkyl, and the like), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, and the like), and the like} and the like; X represents halogen or is combined together with R4 to represent a single bond; and R4 is combined together with X to represent a single bond, or represents hydrogen, alkanoyl, and the like.
摘要翻译：由下式（I）表示的具有酪氨酸激酶抑制活性的衍生物衍生物或其药理学上可接受的盐：其中R 1和R 2相同或不同，各自表示氢，链烷酰基，烯酰基，叔丁基二苯基甲硅烷基或叔丁基二甲基甲硅烷基; R 3表示Y-R 5 {其中Y表示取代或未取代的亚烷基; 并且R 5表示CONR 5 R 7（其中R 6表示氢，羟基，取代或未取代的低级烷基，取代或未取代的高级烷基等; R 7表示羟基，取代的低级烷基等），CO 2 R 12（其中R 12表示取代的低级烷基，取代或未取代的高级烷基等）等}等; X表示卤素或与R 4结合以表示单键;并且R 4与X一起组合以表示单键，或表示氢，烷酰基等。

6. 发明授权

US06376687B1 Steroid sulfatase inhibitors and methods for making and using the same 失效
标题翻译：类固醇硫酸酯酶抑制剂及其制备和使用方法
公开(公告)号：US06376687B1
公开(公告)日：2002-04-23
申请号：US09490302
申请日：2000-01-24
申请人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
发明人： Pui-Kai Li , Chikara Murakata , Shiro Akinaga
IPC分类号： C07J300
CPC分类号： C07J41/0072 , C07J41/0005 , C07J41/0011 , C07J41/0066 , C07J71/0094
摘要： Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.
摘要翻译：公开了用于治疗雌激素依赖性疾病的新型硫酸酯酶抑制剂化合物。这些化合物通常包含在C17位置取代的类固醇核。还公开了合成这些化合物并将其用于治疗和/或预防性治疗患者的方法。

7. 发明授权

US5798379A UCS1025 compounds 失效
标题翻译： UCS1025化合物
公开(公告)号：US5798379A
公开(公告)日：1998-08-25
申请号：US994029
申请日：1997-12-18
申请人： Tamio Mizukami , Harumi Ogawa , Ryuichiro Nakai , Akira Asai , Yoshinori Yamashita , Katsuhiko Ando , Tsutomu Agatsuma , Shiro Akinaga , Kozo Ouchi , Hideki Kawasaki
发明人： Tamio Mizukami , Harumi Ogawa , Ryuichiro Nakai , Akira Asai , Yoshinori Yamashita , Katsuhiko Ando , Tsutomu Agatsuma , Shiro Akinaga , Kozo Ouchi , Hideki Kawasaki
IPC分类号： C07D487/04 , C07D491/16 , C12P17/14 , A61K31/40 , C07D487/02
CPC分类号： C07D487/04 , C12P17/14
摘要： UCS1025 compounds represented by the following formula (I): ##STR1## wherein R represents hydrogen or hydroxyl group, or tautomers or pharmacologically acceptable salts thereof.
摘要翻译：由下式（I）表示的UCS1025化合物：其中R表示氢或羟基，或互变异构体或其药理学上可接受的盐。

8. 发明授权

US5604219A Indolocarbazole derivatives that stimulate platelet production 失效
标题翻译：刺激血小板生成的吲哚咔唑衍生物
公开(公告)号：US5604219A
公开(公告)日：1997-02-18
申请号：US404961
申请日：1995-03-16
申请人： Chikara Murakata , Junichi Watanabe , Yutaka Saitoh , Yukimasa Shiotsu , Takako Shiraki , Fumihiko Kanai , Tatsuya Tamaoki , Shiro Akinaga , Masami Okabe
发明人： Chikara Murakata , Junichi Watanabe , Yutaka Saitoh , Yukimasa Shiotsu , Takako Shiraki , Fumihiko Kanai , Tatsuya Tamaoki , Shiro Akinaga , Masami Okabe
IPC分类号： C07D498/22 , C07H9/06 , A61K31/55
CPC分类号： C07D498/22 , C07H9/06
摘要： Disclosed is an indolocarbazole derivative represented by the following formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## [wherein R.sup.1 represents substituted or unsubstituted lower alkyl, R.sup.2 represents hydrogen, substituted or unsubstituted lower alkyl, R.sup.3 and R.sup.4 are the same or different, and represent hydrogen, nitro, NR.sup.5 R.sup.6, OR.sup.9, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, or CH.dbd.NNR.sup.10 R.sup.11, W represents two hydrogen atoms or oxygen, and Me represents methyl, provided that when R.sup.1 is unsubstituted lower alkyl, R.sup.3 and R.sup.4 are not simultaneously hydrogen.
摘要翻译：公开了下式（I）表示的吲哚咔唑衍生物或其药学上可接受的盐：其中R 1表示取代或未取代的低级烷基，R 2表示氢，取代或未取代的低级烷基，R 3和R 4 代表氢，硝基，NR5R6，OR9，取代或未取代的低级烷基，取代或未取代的低级链烯基或CH = NNR10R11，W代表两个氢原子或氧，Me代表甲基，条件是当R 1 未取代的低级烷基，R3和R4不同时为氢。

9. 发明授权

US4992570A UCN-1028A and UCN-1028C and process for the production thereof 失效
标题翻译： UCN-1028A和UCN-1028C及其生产方法
公开(公告)号：US4992570A
公开(公告)日：1991-02-12
申请号：US173174
申请日：1988-03-24
申请人： Hirofumi Nakano , Eiji Kobayashi , Isami Takahashi , Katsuhiko Ando , Mayumi Yoshida , Shiro Akinaga , Takao Iida
发明人： Hirofumi Nakano , Eiji Kobayashi , Isami Takahashi , Katsuhiko Ando , Mayumi Yoshida , Shiro Akinaga , Takao Iida
IPC分类号： C12P15/00
CPC分类号： C12P15/00 , Y10S435/911
摘要： UCN-1028A and UCN-1028C having an anti-tumor activity and a protein kinase C inhibitory activity are produced by culturing a microorganism belonging to the genus Cladosporium.

10. 发明申请

US20100098690A1 PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：药物组合物
公开(公告)号：US20100098690A1
公开(公告)日：2010-04-22
申请号：US12529380
申请日：2008-03-05
申请人： Shiro Soga , Toshihiko Ishii , Takayuki Nakashima , Yukimasa Shiotsu , Shiro Akinaga
发明人： Shiro Soga , Toshihiko Ishii , Takayuki Nakashima , Yukimasa Shiotsu , Shiro Akinaga
IPC分类号： A61K31/122 , A61K31/216 , A61K31/135 , A61K31/495 , A61K31/445 , A61K31/47 , A61K31/5375 , A61K31/44 , A61K31/075 , A61K31/165 , A61K31/05 , A61K31/5377 , A61K39/395 , A61K31/4965 , A61P35/00
CPC分类号： A61K31/5375 , A61K31/198 , A61K31/337 , A61K31/5377 , A61K39/39558 , A61K45/06 , A61K2300/00
摘要： The present invention provides a pharmaceutical composition comprising a combination of an Hsp 90 family protein inhibitor and at least one compound, the said pharmaceutical composition wherein the Hsp 90 family protein inhibitor is a benozoyl compound represented by formula (I): [wherein n represents an integer of 1 to 5; R1 represents substituted or unsubstituted lower alkyl, CONR7R8 (wherein R7 and R8, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like), or the like; R2 represents substituted or unsubstituted aryl, or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R4 represents a hydrogen atom, hydroxy or halogen; and R6 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like], or a prodrug thereof; or a pharmaceutically acceptable salt thereof, and the like.
摘要翻译：本发明提供了包含Hsp90家族蛋白抑制剂和至少一种化合物的组合的药物组合物，所述药物组合物，其中Hsp 90家族蛋白抑制剂是由式（I）表示的新戊酰化合物：[其中n表示 1〜5的整数; R1表示取代或未取代的低级烷基CONR7R8（其中R7和R8可相同或不同，各自表示氢原子，取代或未取代的低级烷基等）等; R2表示取代或未取代的芳基等; R 3和R 5可以相同或不同，各自表示氢原子，取代或未取代的低级烷基等; R4表示氢原子，羟基或卤素; R6代表氢原子，卤素，取代或未取代的低级烷基等]或其前药; 或其药学上可接受的盐等。

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