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11. 发明申请

US20160051640A1 SOLUBLE GLYCOSAMINOGLYCANASES AND METHODS OF PREPARING AND USING SOLUBLE GLYCOSAMINOGLYCANASES 有权
标题翻译：可溶性糖蛋白酶体及其制备和使用可溶性糖蛋白酶体的方法
公开(公告)号：US20160051640A1
公开(公告)日：2016-02-25
申请号：US14936290
申请日：2015-11-09
申请人： Halozyme, Inc.
发明人： Louis H. Bookbinder , Anirban Kundu , Gregory I. Frost
IPC分类号： A61K38/47 , A61K39/395
CPC分类号： A61K38/47 , A61K39/395 , A61K39/3955 , A61K45/06 , A61K2039/505 , C12N9/2408 , C12Y302/01035 , A61K2300/00
摘要： The invention relates to the discovery of novel soluble neutral active Hyaluronidase Glycoproteins (sHASEGPs), methods of manufacture, and their use to facilitate administration of other molecules or to alleviate glycosaminoglycan associated pathologies. Minimally active polypeptide domains of the soluble, neutral active sHASEGP domains are described that include asparagine-linked sugar moieties required for a functional neutral active hyaluronidase domain. Included are modified amino-terminal leader peptides that enhance secretion of sHASEGP. The invention further comprises sialated and pegylated form of a recombinant sHASEGP to enhance stability and serum pharmacokinetics over naturally occurring slaughterhouse enzymes. Further described are suitable formulations of a substantially purified recombinant sHASEGP glycoprotein derived from a eukaryotic cell that generate the proper glycosylation required for its optimal activity.
摘要翻译：本发明涉及新型可溶性中性活性透明质酸酶糖蛋白（sHASEGPs）的发现，其制备方法及其用于促进其它分子的施用或减轻糖胺聚糖相关病理学的用途。描述了可溶性中性活性sHASEGP结构域的微活性多肽结构域，其包括功能性中性活性透明质酸酶结构域所需的天冬酰胺连接的糖部分。包括改进的氨基末端前导肽，其增强sHASEGP的分泌。本发明还包含重组sHASEGP的唾液酸化和聚乙二醇化形式，以增强天然存在的屠宰酶的稳定性和血清药代动力学。进一步描述了衍生自真核细胞的基本上纯化的重组sHASEGP糖蛋白的合适制剂，其产生其最佳活性所需的适当糖基化。

12. 发明申请

US20140341875A1 Human chondroitinase glycoprotein (CHASEGP), process for preparing the same, and pharmaceutical compositions comprising thereof 审中-公开
标题翻译：人类软骨素酶糖蛋白（CHASEGP），其制备方法和由其组成的药物组合物
公开(公告)号：US20140341875A1
公开(公告)日：2014-11-20
申请号：US14120972
申请日：2014-07-16
申请人： Halozyme, Inc.
发明人： Gregory I. Frost , Anirban Kundu , Louis H. Bookbinder
IPC分类号： C12N9/88
CPC分类号： C12N9/88 , A61K38/47 , C12Y402/02004
摘要： The invention relates to the discovery of a novel Chondroitinase Glycoproteins (CHASEGPs), methods of manufacture, and potential uses in conditions where removal of chondroitin sulfates may be of therapeutic benefit. Chondroitinase Glycoproteins require both a substantial portion of the catalytic domain of the CHASEGP polypeptide and asparagine-linked glycosylation for optimal chondroitinase activity. The invention also includes carboxy-terminal deletion variants of CHASEGP that result in secreted variants of the protein to facilitate manufacture of a recombinant CHASEGP. Further described are suitable formulations of a substantially purified recombinant CHASEGP glycoprotein derived from a eukaryotic cell that generate the proper glycosylation required for its optimal activity. CHASEGP is useful for the degradation of glycosaminoglycans and chondroitin sulfate proteoglycans under clinical conditions where their removal is of therapeutic value.
摘要翻译：本发明涉及在去除硫酸软骨素可能具有治疗益处的条件下发现新型软骨素酶糖蛋白（CHASEGPs），制造方法和潜在用途。软骨素酶糖蛋白需要CHASEGP多肽的大部分催化结构域和天冬酰胺连接的糖基化以获得最佳的软骨素酶活性。本发明还包括CHASEGP的羧基末端缺失变体，其导致蛋白质的分泌型变体以促进重组CHASEGP的制备。进一步描述了衍生自真核细胞的基本上纯化的重组CHASEGP糖蛋白的合适制剂，其产生其最佳活性所需的适当糖基化。 CHASEGP可用于在其去除具有治疗价值的临床条件下降解糖胺聚糖和硫酸软骨素蛋白聚糖。

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