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1. 发明申请

US20060172927A1 Analogs of human growth hormone-releasing hormone, their preparation and use 有权
标题翻译：人类生长激素释放激素的类似物，其制备和用途
公开(公告)号：US20060172927A1
公开(公告)日：2006-08-03
申请号：US10494218
申请日：2002-10-30
申请人： Jan Izdebski , Danuta Kunce , Alicja Orlowska , Ewa Witkowska , Wieslaw Szelejewski , Andrzej Kutner , Krzysztof Bankowski , Elzbieta Frackiewicz
发明人： Jan Izdebski , Danuta Kunce , Alicja Orlowska , Ewa Witkowska , Wieslaw Szelejewski , Andrzej Kutner , Krzysztof Bankowski , Elzbieta Frackiewicz
IPC分类号： C07K14/61
CPC分类号： C07K14/60 , A61K38/00 , Y02P20/55
摘要： Growth hormone-releasing hormone analogs having the amino acid sequence of the formula: Dat-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr10-R11-R12-VAL-Leu-Ala-Gln-Leu-Ser-Ala-R20-R2-Leu-Leu-Gln-Asp-Ile-Nle-Asp-R29-NH2 (I), wherein R11 is hArg, Gab or Gap; R12 is hArg, Orn, Gab or Gap; R20 is hArg, hArg, Gab or Gap; R21 is hArg, Orn, Gab or Gap; R29 is D-Arg, hArg, Gab or Gap; and their pharmaceutically acceptable salts. Said peptides are potent and selective stimulators of GH release and they are highly resistant to enzymatic degradation. Said peptides are prepared using the solid phase synthesis method, by introducing suitable derivatives of lysine, 2,4-diaminobutyric acid or 2,3-diaminopropionic acid at appropriate positions in the peptide chain attached to a polymeric support, deprotecting side-chain amino gorups and reacting free amino groups with a guanidinating agent, removing all remaining t-butyloxycarbonyl protective groups, and cleaving the synthesized peptide from the support, followed by purification and optionally, converting the peptide into a pharmaceutically acceptable salt.
摘要翻译：具有下式的氨基酸序列的生长激素释放激素类似物：Dat-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr 10 -R 11， -VAL-Leu-Ala-Gln-Leu-Ser-Ala-R-20-Leu-Leu-Leu-Leu-Ala-R -Gln-Asp-Ile-Nle-Asp-R 29 -NH 2（I）其中R 11是hArg，Gab或Gap ; R 12是hArg，Orn，Gab或Gap; R 20是hArg，hArg，Gab或Gap; R 21是hArg，Orn，Gab或Gap; R 29是D-Arg，hArg，Gab或Gap; 及其药学上可接受的盐。所述肽是GH释放的有效和选择性刺激物，并且它们对酶降解具有高度抗性。所述肽是使用固相合成法，通过在连接于聚合物载体的肽链的适当位置引入赖氨酸，2,4-二氨基丁酸或2,3-二氨基丙酸的适当衍生物，将侧链氨基酸并使游离氨基与胍基化剂反应，除去所有剩余的叔丁氧基羰基保护基团，并从载体上切割合成的肽，然后纯化并任选地将肽转化为药学上可接受的盐。

2. 发明授权

US07928063B2 Analogs of human growth hormone-releasing hormone, their preparation and use 有权
标题翻译：人类生长激素释放激素的类似物，其制备和用途
公开(公告)号：US07928063B2
公开(公告)日：2011-04-19
申请号：US10494218
申请日：2002-10-30
申请人： Jan Izdebski , Danuta Kunce , Alicja Orlowska , Ewa Witkowska , Wieslaw Szelejewski , Andrzej Kutner , Krzysztof Bankowski , Elzbieta Frackiewicz
发明人： Jan Izdebski , Danuta Kunce , Alicja Orlowska , Ewa Witkowska , Wieslaw Szelejewski , Andrzej Kutner , Krzysztof Bankowski , Elzbieta Frackiewicz
IPC分类号： A61K38/25
CPC分类号： C07K14/60 , A61K38/00 , Y02P20/55
摘要： Growth hormone-releasing hormone analogs having the amino acid sequence of the formula: Dat-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr10-R11-R12-VAL-Leu-Ala-Gln-Leu-Ser-Ala-R20-R21-Leu-Leu-Gln-Asp-Ile-Nle-Asp-R29-NH2 (I), wherein R11 is hArg, Gab or Gap; R12 is hArg, Orn, Gab or Gap; R20 is hArg, hArg, Gab or Gap; R21 is hArg, Orn, Gab or Gap; R29 is D-Arg, hArg, Gab or Gap; and their pharmaceutically acceptable salts. Said peptides are potent and selective stimulators of GH release and they are highly resistant to enzymatic degradation. Said peptides are prepared using the solid phase synthesis method, by introducing suitable derivatives of lysine, 2,4-diaminobutyric acid or 2,3-diaminopropionic acid at appropriate positions in the peptide chain attached to a polymeric support, deprotecting side-chain amino groups and reacting free amino groups with a guanidinating agent, removing all remaining t-butyloxycarbonyl protective groups, and cleaving the synthesized peptide from the support, followed by purification and optionally, converting the peptide into a pharmaceutically acceptable salt.
摘要翻译：具有下式的氨基酸序列的生长激素释放激素类似物：Dat-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr10-R11-R12-VAL-Leu-Ala-Gln-Leu-Ser -Ala-R20-R21-Leu-Leu-Gln-Asp-Ile-Nle-Asp-R29-NH2（I），其中R11为hArg，Gab或Gap; R12是hArg，Orn，Gab或Gap; R20是hArg，hArg，Gab或Gap; R21是hArg，Orn，Gab或Gap; R29是D-Arg，hArg，Gab或Gap; 及其药学上可接受的盐。所述肽是GH释放的有效和选择性刺激物，并且它们对酶降解具有高度抗性。所述肽通过使用固相合成方法，通过在连接于聚合物载体的肽链的适当位置引入赖氨酸，2,4-二氨基丁酸或2,3-二氨基丙酸的合适衍生物，将侧链氨基脱保护并使游离氨基与胍基化剂反应，除去所有剩余的叔丁氧基羰基保护基团，并从载体上切割合成的肽，然后纯化并任选地将肽转化为药学上可接受的盐。

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