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    Cyclodextrin complex of fumagillin derivative
    2.
    发明授权
    Cyclodextrin complex of fumagillin derivative 失效
    FUMAGILLIN衍生物的CYCLODEXTRIN复合物

    公开(公告)号：US5196406A

    公开(公告)日：1993-03-23

    申请号：US704347

    申请日：1991-05-23

    申请人： Shigeru Kamei ,  Hiroaki Okada ,  Katsuichi Sudo ,  Shoji Kishimoto

    发明人： Shigeru Kamei ,  Hiroaki Okada ,  Katsuichi Sudo ,  Shoji Kishimoto

    IPC分类号： A61K31/335 ,  A61K47/48

    CPC分类号： B82Y5/00 ,  A61K31/335 ,  A61K47/48969

    摘要： A complex of a fumagillin derivative represented by the general formula: ##STR1## wherein R.sup.1 is hydrogen; R.sup.2 is halogen, N(O)mR.sup.5 R.sup.6, N.sup.+ R.sup.5 R.sup.6 R.sup.7.X.sup.-, S(O)nR.sup.5 or S.sup.+ R.sup.5 R.sup.6.X.sup.- (wherein R.sup.5, R.sup.6 and R.sup.7 are independently an optionally substituted hydrocarbon or heterocyclic group; X.sup.- is a counter anion; m is an integer of 0 or 1; n is an integer from 0 to 2; and R.sup.5 and R.sup.6 together with the adjacent nitrogen or sulfur atom may form a nitrogen- or sulfur-containing heterocyclic group which may be substituted and form a condensed ring); or R.sup.1 and R.sup.2 together represent a bond; R.sup.3 is 2-methyl-1-propenyl group or isobutyl group; A is O or NR.sup.8 (wherein R.sup.8 is hydrogen or an optionally substituted lower alkyl or aryl group); R.sup.4 is hydrogen, an optionally substituted hydrocarbon group or an optionally substituted acyl group); or a salt thereof, with an optionally etherified cyclodextrin is disclosed. The present invention also provides an antineoplastic agent containing the complex.

    Sustained-release preparation
    3.
    发明授权
    Sustained-release preparation 有权
    缓释制剂

    公开(公告)号：US07048947B2

    公开(公告)日：2006-05-23

    申请号：US10127558

    申请日：2002-04-23

    申请人： Shigeru Kamei ,  Yasutaka Igari ,  Yasuaki Ogawa

    发明人： Shigeru Kamei ,  Yasutaka Igari ,  Yasuaki Ogawa

    IPC分类号： A61K9/14 ,  C07K7/23

    CPC分类号： C07K7/23 ,  A61K9/1647 ,  A61K38/00 ,  A61K38/09

    摘要： A sustained-release preparation which comprises a physiologically active peptide of general formula wherein X represents an acyl group; R1, R2 and R4 each represents an aromatic cyclic group; R3 represents a D-amino acid residue or a group of the formula wherein R3′ is a heterocyclic group; R5 represents a group of the formula —(CH2)n—R5′ wherein n is 2 or 3, and R5′ is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group; R6 represents a group of the formula —(CH2)n—R6′ wherein n is 2 or 3, and R6′ is an amino group which may optionally be substituted; R7 represents a D-amino acid residue or an azaglycyl residue; and Q represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group. The sustained-release preparation shows a constant release of the peptide over a long time and is substantially free from an initial burst.

    摘要翻译： 一种持续释放制剂，其包含通式的生理活性肽，其中X表示酰基; R 1，R 2和R 4各自表示芳族环状基团; R 3表示D-氨基酸残基或下式的基团其中R 3'是杂环基; R 5表示下式的基团 - （CH 2）n - n -R 5其中n为2 或3，并且R 5'是可任选被取代的氨基，芳族环状基团或O-糖基基团; R 6表示下式的基团 - （CH 2）n - 其中n为2 或3，并且R 6'是可任选被取代的氨基; R 7表示D-氨基酸残基或azaglycyl残基; Q表示氢或低级烷基，或其盐和具有末端羧基的生物降解性聚合物。 持续释放制剂显示长时间的肽的恒定释放并且基本上没有初始爆发。

    Sustained-release preparation
    4.
    发明授权
    Sustained-release preparation 失效
    缓释制剂

    公开(公告)号：US06528093B1

    公开(公告)日：2003-03-04

    申请号：US09386232

    申请日：1999-08-31

    申请人： Shigeru Kamei ,  Yasutaka Igari ,  Yasuaki Ogawa

    发明人： Shigeru Kamei ,  Yasutaka Igari ,  Yasuaki Ogawa

    IPC分类号： A61K914

    CPC分类号： C07K7/23 ,  A61K9/1647 ,  A61K38/00 ,  A61K38/09

    摘要： A sustained-release preparation which comprises a physiologically active peptide of general formula: wherein X represents an acyl group; R1, R2 and R4 each represents an aromatic cyclic group; R3 represents a D-amino acid residue or a group of the formula: wherein R3′ is a heterocyclic group; R5 represents a group of the formula —(CH2)n—R5′ wherein n is 2 or 3, and R5′ is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group; R6 represents a group of the formula —(CH2)n—R6′ wherein n is 2 or 3, and R6′ is an amino group which may optionally be substituted; R7 represents a D-amino acid residue or an azaglycyl residue; and Q represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group. The sustained-release preparation shows a constant release of the peptide over a long time and is substantially free from an initial burst.

    摘要翻译： 一种持续释放制剂，其包含通式如下的生理活性肽：其中X表示酰基; R 1，R 2和R 4各自表示芳族环状基团; R 3表示D-氨基酸残基或下式基团：其中 R 3'是杂环基; R 5表示式 - （CH 2）n -R 5'的基团，其中n是2或3，R5'是可以被取代的氨基，芳族环基或O- 糖基; R 6表示式 - （CH 2）n -R 6'的基团，其中n为2或3，并且R 6'为可任选被取代的氨基; R 7表示D-氨基酸残基或偶氮缩水甘油基 ; 并且Q表示氢或低级烷基，或其盐和具有末端羧基的生物可降解聚合物。持续释放制剂长时间显示出肽的恒定释放并且基本上没有初始爆发。

    Sustained-release preparation
    5.
    发明授权
    Sustained-release preparation 失效
    缓释制剂

    公开(公告)号：US5480868A

    公开(公告)日：1996-01-02

    申请号：US162698

    申请日：1993-12-07

    申请人： Shigeru Kamei ,  Yasutaka Igari ,  Yasuaki Ogawa

    发明人： Shigeru Kamei ,  Yasutaka Igari ,  Yasuaki Ogawa

    IPC分类号： A61K9/52 ,  A61K20060101 ,  A61K9/16 ,  A61K9/22 ,  A61K9/50 ,  A61K38/04 ,  A61K38/09 ,  A61K38/12 ,  A61K47/34 ,  A61K47/42 ,  C07K7/23 ,  A61K38/00 ,  C08G63/08 ,  C08G63/91 ,  C08L67/00

    CPC分类号： C07K7/23 ,  A61K38/09 ,  A61K9/1647 ,  A61K38/00

    摘要： A sustained-release preparation which comprises a physiologically active peptide of general formula ##STR1## wherein X represents an acyl group; R.sub.1, R.sub.2 and R.sub.4 each represents an aromatic cyclic group; R.sub.3 represents a D-amino acid residue or a group of the formula ##STR2## wherein R.sub.3 ' is a heterocyclic group; R.sub.5 represents a group of the formula --(CH.sub.2).sub.n --R.sub.5 ' wherein n is 2 or 3, and R.sub.5 ' is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group;R.sub.6 represents a group of the formula --(CH.sub.2).sub.n --R.sub.6 ' wherein n is 2 or 3, and R.sub.6 ' is an amino group which may optionally be substituted;R.sub.7 represents a D-amino acid residue or an azaglycyl residue; andQ represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group.The sustained-release preparation shows a constant release of the peptide over a long time and is substantially free from an initial burst.

    摘要翻译： 包含通式的生理活性肽的缓释制剂含有酰基; R1，R2和R4各自表示芳族环状基团; R3表示D-氨基酸残基或式“IMAGE”的基团，其中R3'为杂环基; R5表示式 - （CH2）n-R5'的基团，其中n为2或3，R5'为任选取代的氨基，芳族环基或O-糖基; R6表示式 - （CH2）n-R6'的基团，其中n为2或3，R6'为可任意取代的氨基; R7表示D-氨基酸残基或氮杂十八烷基残基; Q表示氢或低级烷基，或其盐和具有末端羧基的生物降解性聚合物。 持续释放制剂显示长时间的肽的恒定释放并且基本上没有初始爆发。

    Sustained-release preparation
    6.
    发明申请
    Sustained-release preparation 审中-公开

    公开(公告)号：US20090048180A1

    公开(公告)日：2009-02-19

    申请号：US12285494

    申请日：2008-10-07

    申请人： Shigeru Kamei ,  Yasutaka Igari ,  Yasuaki Ogawa

    发明人： Shigeru Kamei ,  Yasutaka Igari ,  Yasuaki Ogawa

    IPC分类号： A61K38/08 ,  C07K7/00

    CPC分类号： C07K7/23 ,  A61K9/1647 ,  A61K38/00 ,  A61K38/09

    摘要： A sustained-release preparation which comprises a physiologically active peptide of general formula wherein X represents an acyl group; R1, R2 and R4 each represents an aromatic cyclic group; R3 represents a D-amino acid residue or a group of the formula wherein R3′ is a heterocyclic group; R5 represents a group of the formula —(CH2)n—R5′ wherein n is 2 or 3, and R5′ is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group; R6 represents a group of the formula —(CH2)n—R6′ wherein n is 2 or 3, and R6′ is an amino group which may optionally be substituted; R7 represents a D-amino acid residue or an azaglycyl residue; and Q represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group. The sustained-release preparation shows a constant release of the peptide over a long time and is substantially free from an initial burst.

    Printed circuit board apparatus
    9.
    发明授权
    Printed circuit board apparatus 失效
    印刷电路板装置

    公开(公告)号：US5281770A

    公开(公告)日：1994-01-25

    申请号：US707041

    申请日：1991-05-29

    申请人： Shigeru Kamei ,  Yoshimi Watanabe

    发明人： Shigeru Kamei ,  Yoshimi Watanabe

    IPC分类号： H05K1/18 ,  H01R4/02 ,  H05K1/02 ,  H05K1/11 ,  H05K3/34 ,  H05K3/40 ,  H05K1/00

    CPC分类号： H05K3/4046 ,  H01R12/58 ,  H05K3/3447 ,  H01R4/02 ,  H05K2201/10401 ,  H05K2201/10916 ,  H05K3/3468

    摘要： A printed circuit board apparatus comprises a printed circuit board. The printed circuit board includes a first and a second surface and a hole portion. A printed pattern is formed on the first surface, and a parts having a lead is mounted on the second surface. The printed circuit board apparatus also includes an eyelet and plural solder entering portions. The eyelet includes a curling portion and a head portion positioned on the first and second surfaces of the printed circuit board, respectively, and a cylindrical portion, connecting the head and curling portion, inserted into the hole of the printed circuit board. A plurality of solder entering portions are formed at equal intervals on the curling portion. From the solder entering portions, solder enters into space between the curling portion and the first surface face of the printed pattern surrounding the hole of the printed circuit board and the eyelet.

    摘要翻译： 印刷电路板装置包括印刷电路板。 印刷电路板包括第一和第二表面和孔部分。 印刷图案形成在第一表面上，具有引线的部分安装在第二表面上。 印刷电路板装置还包括孔眼和多个焊料进入部分。 孔眼分别包括位于印刷电路板的第一和第二表面上的卷曲部分和头部，以及连接头部和卷曲部分的插入印刷电路板的孔中的圆柱形部分。 多个焊料进入部分以相等的间隔形成在卷曲部分上。 从焊料进入部分，焊料进入位于印刷电路板和孔眼的孔周围的印刷图案的卷曲部分和第一表面之间的空间中。

    MEDICINAL PREPARATIONS FOR TREATING SEX HORMONE-DEPENDENT DISEASES
    10.
    发明申请
    MEDICINAL PREPARATIONS FOR TREATING SEX HORMONE-DEPENDENT DISEASES 审中-公开
    用于治疗性交激素依赖性疾病的药物制剂

    公开(公告)号：US20080207524A1

    公开(公告)日：2008-08-28

    申请号：US11941356

    申请日：2007-11-16

    申请人： Yasutaka Igari ,  Shigeru Kamei

    发明人： Yasutaka Igari ,  Shigeru Kamei

    IPC分类号： A61K38/08 ,  A61K38/02 ,  A61K31/519 ,  A61K31/4365 ,  A61P5/24

    CPC分类号： A61K45/06 ,  A61K38/08 ,  A61K38/09 ,  A61K2300/00

    摘要： Medicinal preparations for treating sex hormone-dependent diseases which comprise a combination of a compound having a luteinizing hormone-releasing hormone agonistic effect or its salt with a compound having a luteinizing hormone-releasing hormone antagonistic effect or its salt for administering the compound having a luteinizing hormone-releasing hormone agonistic effect or its salt followed by the compound having a luteinizing hormone-releasing hormone antagonistic effect or its salt. By using these preparations, the concentration of a sex hormone (for example, testosterone, LH, FSH, estrogen) can be quickly recovered after the medicable period of a compound having a luteinizing hormone-releasing hormone antagonistic effect or its salt or a preparation containing the same (preferably a sustained-release preparation), which makes it possible to definitely determine the drug cessation period in an intermittent treatment.

    摘要翻译： 用于治疗性激素依赖性疾病的药物制剂，其包含具有促黄体激素释放激素激动作用的化合物或其盐与具有黄体生成激素释放激素拮抗作用的化合物的组合或其盐，用于给予具有黄体生成 激素释放激素激动作用或其盐，随后是具有黄体生成激素释放激素拮抗作用的化合物或其盐。 通过使用这些制剂，可以在具有促黄体生成激素释放激素拮抗作用的化合物或其盐或其制剂含有的药物治疗期后迅速恢复性激素（例如睾酮，LH，FSH，雌激素）的浓度 相同（优选缓释制剂），这使得可以在间歇处理中确定药物停止期。