公开(公告)号：US4960595A

公开(公告)日：1990-10-02

申请号：US222309

申请日：1987-11-16

申请人： Sadao Hirota ,  Hiroshi Kikuchi ,  Hitoshi Yamauchi ,  Munehiro Tomikawa

发明人： Sadao Hirota ,  Hiroshi Kikuchi ,  Hitoshi Yamauchi ,  Munehiro Tomikawa

IPC分类号： A61K31/70 ,  A61K9/00 ,  A61K9/127 ,  A61P1/16

CPC分类号： A61K9/1272 ,  Y10T428/249997

摘要： Lipid membrane structures containing a lactose monofatty acid ester or amide are disclosed. The lipid membrane structures are delivered preferentially to the liver parenchymal cells and are useful as carriers of drugs.

摘要翻译： 公开了含有乳糖单脂肪酸酯或酰胺的脂质膜结构。 脂质膜结构优先递送到肝实质细胞，并且可用作药物的载体。

公开(公告)号：US5141751A

公开(公告)日：1992-08-25

申请号：US663775

申请日：1991-03-04

申请人： Munehiro Tomikawa ,  Sadao Hirota ,  Hitoshi Yamauchi ,  Hiroshi Kikuchi ,  Yasuyoshi Kawato

发明人： Munehiro Tomikawa ,  Sadao Hirota ,  Hitoshi Yamauchi ,  Hiroshi Kikuchi ,  Yasuyoshi Kawato

IPC分类号： A61K9/107 ,  A61K9/127

CPC分类号： A61K9/1075 ,  A61K9/1272 ,  Y10S436/829 ,  Y10T428/2984

摘要： Lipid membrane structures containing, in the lipid membrane thereof, a compound represented by formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a fatty acid residue; R.sub.2 represents a hydrogen atom or an acyclic hydrocarbon residue; R.sub.3 represents an amino group, a guanidino group or an amidino group; and n represents an integer of from 1 to 6; provided that R.sub.1 and R.sub.2 do not represent hydrogen atoms at the same time, or a salt thereof. The lipid membrane structures exhibit excellent specific affinity for tumor cells and can be delivered preferentially to tumor cells.

摘要翻译： 脂质膜结构在其脂质膜中含有式（I）表示的化合物：其中R1表示氢原子或脂肪酸残基; R2表示氢原子或无环烃残基; R3表示氨基，胍基或脒基; n表示1〜6的整数， 条件是R1和R2不同时表示氢原子或其盐。 脂质膜结构对肿瘤细胞表现出优异的特异性亲和力，并可优先递送至肿瘤细胞。

公开(公告)号：US5096891A

公开(公告)日：1992-03-17

申请号：US330580

申请日：1989-03-30

申请人： Sadao Hirota ,  Hitoshi Yamauchi

发明人： Sadao Hirota ,  Hitoshi Yamauchi

IPC分类号： A61K9/00 ,  A61K47/02 ,  A61K47/10 ,  A61K47/36 ,  A61K47/40

CPC分类号： A61K31/70 ,  A61K47/02 ,  A61K47/10 ,  A61K47/36 ,  A61K47/40 ,  A61K9/0014 ,  Y10S514/925 ,  Y10S514/928 ,  Y10S514/969 ,  Y10S514/97

摘要： An ointment comprising an adenosine 3',5'-cyclic phosphate derivative as an active ingrediment, an ointment base having water-absorbing and drying properties, a saccharide and/or inorganic high polymer is disclosed. The ointment exhibits improved stability of the adenosine 3',5'-cyclic phosphate derivative.

公开(公告)号：US5376380A

公开(公告)日：1994-12-27

申请号：US79842

申请日：1993-06-22

申请人： Hiroshi Kikuchi ,  Kiyoto Yachi ,  Hiromi Morita ,  Sadao Hirota

发明人： Hiroshi Kikuchi ,  Kiyoto Yachi ,  Hiromi Morita ,  Sadao Hirota

IPC分类号： A61K9/127 ,  A61K9/107 ,  B01J13/02 ,  B01J13/20

CPC分类号： A61K9/1277

摘要： A method of producing liposomal products which comprises treating a positively or negatively charged, freeze- or spray-dried liposomal preparation with an aqueous solution of a drug charged oppositely to the charge of the liposomes.

摘要翻译： 一种生产脂质体产物的方法，其包括用与所述脂质体的电荷相反的药物的水溶液处理带正电荷或带负电荷的，冻干或喷雾干燥的脂质体制剂。

公开(公告)号：US4983725A

公开(公告)日：1991-01-08

申请号：US176329

申请日：1988-03-31

申请人： Hideki Miyaji ,  Shusaburo Hokukoku ,  Munehiro Tomikawa ,  Sadao Hirota ,  Hiroshi Kikuchi

发明人： Hideki Miyaji ,  Shusaburo Hokukoku ,  Munehiro Tomikawa ,  Sadao Hirota ,  Hiroshi Kikuchi

IPC分类号： A61K9/127 ,  C07H13/06

CPC分类号： A61K9/1271 ,  A61K9/1272 ,  C07H13/06 ,  Y10T428/2984

摘要： Novel mannobiose derivative represented by the general formula [I]: ##STR1## wherein groups of R.sub.1 to R.sub.5 each represents --OH, --OR.sub.6, --NHR.sub.6, (R.sub.6 represents an acyl group) or a group represented by the following formula (a), (b), (c), (d) or (e), provided that one of R.sub.1 to R.sub.5 represents --OR.sub.6 or --NHR.sub.6, one of the other 4 groups of R.sub.1 to R.sub.5 represents one of the groups represented by the formulae (a) to (e), and the remaining 3 groups of R.sub.1 to R.sub.5 represent --OH: ##STR2## wherein represents .alpha. or .beta. bond are provided by the invention.These compounds give liposomes a specific affinity for Kupffer cells of liver, and can be produced industrially.

公开(公告)号：US6060080A

公开(公告)日：2000-05-09

申请号：US409924

申请日：1995-03-23

申请人： Hiroshi Kikuchi ,  Kiyoto Yachi ,  Sadao Hirota

发明人： Hiroshi Kikuchi ,  Kiyoto Yachi ,  Sadao Hirota

IPC分类号： A61K9/127

CPC分类号： A61K9/127

摘要： A liposomal aqueous dispersion and method of making the liposomal aqueous dispersion is useful for encapsulation of drugs. The liposomal aqueous dispersion comprises: an aqueous suspension medium; multilamellar liposomes comprising an anionic phospholipid and cholesterol as essential components; neutral phospholipid in a mole ratio of 0 to 40% based on the total amount of said multilamellar liposomes; and a cation moiety-containing water-soluble drug, wherein the electrolyte concentration of said aqueous suspension medium is not more than 40 mM.

摘要翻译： 脂质体水分散体和制备脂质体水分散体的方法可用于药物的包封。 脂质体水性分散体包含：水性悬浮液; 包含阴离子磷脂和胆固醇作为必需组分的多层脂质体; 中性磷脂的摩尔比为0〜40％，基于所述多层脂质体的总量; 和含阳离子部分的水溶性药物，其中所述水性悬浮介质的电解质浓度不超过40mM。

公开(公告)号：US4923862A

公开(公告)日：1990-05-08

申请号：US133975

申请日：1987-12-17

申请人： Sadao Hirota

发明人： Sadao Hirota

IPC分类号： A61K9/06 ,  A61K31/535 ,  A61K47/38 ,  A61P17/00

CPC分类号： A61K31/535

摘要： A topical preparation containing, as an active ingredient, 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3][1,4]-benzoxazine-6-carboxylic acid or a salt thereof.