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1. 发明授权

US5665394A Matrix for sustained-release preparation 失效
标题翻译：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。

2. 发明授权

US5594091A Matrix for sustained-release preparation 失效
公开(公告)号：US5594091A
公开(公告)日：1997-01-14
申请号：US391699
申请日：1995-02-21
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 , A61K47/32 , C08G63/08 , C08G63/66
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.

3. 发明授权

US07294344B2 Sustained-release preparation for AII antagonist, production and use thereof 失效
标题翻译： AII拮抗剂的缓释制剂，其制备和使用
公开(公告)号：US07294344B2
公开(公告)日：2007-11-13
申请号：US10443308
申请日：2003-05-22
申请人： Yasutaka Igari , Akira Saikawa , Yoshiyuki Inada , Shigeru Kamei
发明人： Yasutaka Igari , Akira Saikawa , Yoshiyuki Inada , Shigeru Kamei
IPC分类号： A61F2/00 , A61K9/14 , A61K9/50
CPC分类号： A61K31/00 , A61K9/1611 , A61K9/1647 , A61K31/4178 , A61K31/4184 , Y10S514/965
摘要： The present invention is to provide a sustained-release preparation which comprises a compound having angiotensin II antagonistic activity, its pro-drug or their salt, and a biodegradable polymer, and if necessary, a polyvalent metal, and which is highly stable and active and shows angiotensin II antagonistic activity while maintaining circadian rhythm of blood pressure for a long time.
摘要翻译：本发明提供一种缓释制剂，其包含具有血管紧张素II拮抗作用的化合物，其前药或其盐，以及可生物降解的聚合物，如果需要，提供多价金属，并且其具有高度稳定和活性的显示血管紧张素II拮抗活性，同时保持血压的昼夜节律长时间。

4. 发明授权

US06589547B1 Sustained-release preparation for AII antagonist, production and use thereof 失效
标题翻译： AII拮抗剂的缓释制剂，其制备和使用
公开(公告)号：US06589547B1
公开(公告)日：2003-07-08
申请号：US09601986
申请日：2000-08-09
申请人： Yasutaka Igari , Akira Saikawa , Yoshiyuki Inada , Shigeru Kamei
发明人： Yasutaka Igari , Akira Saikawa , Yoshiyuki Inada , Shigeru Kamei
IPC分类号： A61K916
CPC分类号： A61K31/00 , A61K9/1611 , A61K9/1647 , A61K31/4178 , A61K31/4184 , Y10S514/965
摘要： The present invention is to provide a sustained-release preparation which comprises a compound having angiotensin II antagonistic activity, its pro-drug or their salt, and a biodegradable polymer, and if necessary, a polyvalent metal, and which is highly stable and active and shows angiotensin II antagonistic activity while maintaining circadian rhythm of blood pressure for a long time.
摘要翻译：本发明提供一种缓释制剂，其包含具有血管紧张素II拮抗作用的化合物，其前药或其盐，以及可生物降解的聚合物，如果需要，提供多价金属，并且其具有高度稳定和活性的显示血管紧张素II拮抗活性，同时保持血压的昼夜节律长时间。

5. 发明授权

US07048947B2 Sustained-release preparation 有权
标题翻译：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。

6. 发明授权

US06528093B1 Sustained-release preparation 失效
标题翻译：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。

7. 发明授权

US5480868A Sustained-release preparation 失效
标题翻译：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。

8. 发明申请

US20090048180A1 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.

9. 发明授权

US5668111A Sustained-release preparation 失效
标题翻译：缓释制剂
公开(公告)号：US5668111A
公开(公告)日：1997-09-16
申请号：US471382
申请日：1995-06-06
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
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; R 3表示D-氨基酸残基或式（D）的基团，其中R 3'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。

10. 发明申请

US20080207524A1 MEDICINAL PREPARATIONS FOR TREATING SEX HORMONE-DEPENDENT DISEASES 审中-公开
标题翻译：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。

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