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1. 发明授权

US11559490B2 Pharmaceutical formulation 有权
公开(公告)号：US11559490B2
公开(公告)日：2023-01-24
申请号：US16498943
申请日：2018-03-28
申请人： Merck Patent GmbH
发明人： Simon Geissler , Martina Jeschke , Patrizia Boniforte , Markus Weigandt
IPC分类号： A61K9/20 , A61K9/00 , A61K9/10 , A61K9/14 , A61K9/16 , A61K9/28 , A61K9/48 , A61K31/5377 , A61P35/00 , C07D413/14
摘要： A pharmaceutical formulation has (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol or pharmaceutically acceptable salt thereof.

2. 发明申请

US20230119567A1 PHARMACEUTICAL FORMULATION 有权
公开(公告)号：US20230119567A1
公开(公告)日：2023-04-20
申请号：US18060929
申请日：2022-12-01
申请人： Merck Patent GmbH
发明人： Simon Geissler , Martina Jeschke , Patrizia Boniforte , Markus Weigandt
IPC分类号： A61K9/20 , A61K9/00 , A61K9/10 , A61K9/14 , A61K9/48 , A61K31/5377 , A61P35/00 , A61K9/28 , A61K9/16
摘要： A pharmaceutical formulation has (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol or pharmaceutically acceptable salt thereof.

3. 发明申请

US20210085611A1 Pharmaceutical formulation 有权
公开(公告)号：US20210085611A1
公开(公告)日：2021-03-25
申请号：US16498943
申请日：2018-03-28
申请人： Merck Patent GmbH
发明人： Simon GEISSLER , Martina Jeschke , Patrizia Boniforte , Markus Weigandt
IPC分类号： A61K9/20 , A61K9/14 , A61K9/48 , A61K31/5377
摘要： A pharmaceutical formulation has (S)-[2-chloro-4-fluoro-5-(7-tnorpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol or pharmaceutically acceptable salt thereof.

4. 发明申请

US20160279213A1 Survivin-Directed Cancer Vaccine Therapy 审中-公开
标题翻译：存活蛋白导向癌症疫苗治疗
公开(公告)号：US20160279213A1
公开(公告)日：2016-09-29
申请号：US15036629
申请日：2014-12-16
申请人： MERCK PATENT GMBH
发明人： Simon Geissler , Patrizia Boniforte , Joerg Plaschke , Markus Weigandt , Stefan Jaekel , Roland Kellner , Thomas Rysiok , Dirk Mueller-Pompalla , Kenneth Hance
IPC分类号： A61K39/00 , A61K39/39 , A61K45/06 , C07K14/47
CPC分类号： A61K39/0011 , A61K39/39 , A61K45/06 , A61K2039/55511 , A61K2039/55555 , A61K2039/572 , C07K14/4747 , C07K14/4748
摘要： The invention relates to a therapeutically effective truncated survivin and its therapeutic use as vaccine in a liposomal preparation, wherein the survivin fragment is preferably gluconoylated, and said liposomal preparation elicits in-vivo anti-tumor activity. The invention is directed, in more detail, to a cancer vaccine comprising a fragment of human survivin that is specifically effective in conjunction with an lipid adjuvant. The invention relates in more detail to a liposomal vaccine delivery system comprising an active truncated survivin molecule as tumor antigen and a chiral cationic lipid, for example R-DOTAP acting as adjuvant, which is part of the liposome preparation, wherein the liposomal drug delivery system is optimized with regard to its lipid and adjuvant components, physical or physicochemical parameters, and the final therapeutic efficacy of the released truncated survivin molecules. The invention is finally related to a method of increasing CD4+/CD8+ T-cell responses in-vivo, thus resulting in an increased anti-tumor activity by providing a liposome preparation comprising said truncated preferably gluconoylated survivin.
摘要翻译：本发明涉及治疗有效的截短的存活蛋白及其作为脂质体制剂中的疫苗的治疗用途，其中存活蛋白片段优选葡萄糖酰化，并且所述脂质体制剂引起体内抗肿瘤活性。本发明更详细地涉及包含与脂质佐剂特异有效的人存活素片段的癌症疫苗。本发明更详细地涉及包含作为肿瘤抗原的活性截短的存活蛋白分子和手性阳离子脂质的脂质体疫苗递送系统，例如作为佐剂的R-DOTAP，其是脂质体制剂的一部分，其中脂质体药物递送系统针对其脂质和佐剂组分，物理或物理化学参数以及释放的截短的存活蛋白分子的最终治疗功效进行了优化。本发明最终涉及在体内增加CD4 + / CD8 + T细胞应答的方法，从而通过提供包含所述截短的优选葡萄糖酰化的存活蛋白的脂质体制剂来增加抗肿瘤活性。

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