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    Matrix for sustained-release preparation
    3.
    发明授权
    Matrix for sustained-release preparation 失效
    用于缓释制剂的基质

    公开(公告)号：US5665394A

    公开(公告)日：1997-09-09

    申请号：US723152

    申请日：1996-09-30

    申请人： Yasutaka Igari ,  Akira Saikawa ,  Kayoko Okamoto ,  Shigeru Kamei ,  Masahisa Oka ,  Atsunori Sano

    发明人： Yasutaka Igari ,  Akira Saikawa ,  Kayoko Okamoto ,  Shigeru Kamei ,  Masahisa Oka ,  Atsunori Sano

    IPC分类号： A61K9/16 ,  C08G63/06 ,  A61K9/50 ,  A61F2/02 ,  A61F9/02 ,  A61K9/48

    CPC分类号： C08G63/06 ,  A61K9/1647

    摘要： The present invention relates to a matrix for sustained-release preparation comprising an ester formed at a terminal carboxyl group of a straight-chain polyester which essentially consists of an .alpha.-hydroxymonocarboxylic acid. The matrix is stable to light, heat, moisture, coloring etc., and is of low toxicity. The sustained-release preparation produced by using the ester of the present invention offers stable drug release over an extended period of time, ensuring sustained stable effect. Furthermore, the sustained-release preparation does not show excess drug release just after administration.

    摘要翻译： 本发明涉及用于缓释制剂的基质，其包含在直链聚酯的末端羧基上形成的酯，其基本上由α-羟基单羧酸组成。 基质对光，热，水分，着色等均稳定，毒性低。 通过使用本发明的酯制备的缓释制剂在延长的时间内提供稳定的药物释放，确保持续的稳定的效果。 此外，缓释制剂在施用后不显示过量的药物释放。

    Sustained-release preparation
    5.
    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
    6.
    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
    7.
    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
    8.
    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.

    MEDICINAL PREPARATIONS FOR TREATING SEX HORMONE-DEPENDENT DISEASES
    9.
    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。

    Sustained-release preparation
    10.
    发明授权
    Sustained-release preparation 失效

    公开(公告)号：US5972891A

    公开(公告)日：1999-10-26

    申请号：US892315

    申请日：1997-07-14

    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 ,  A61K38/08 ,  C07K7/06

    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.