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1. 发明申请

US20170051031A1 LIPIDATED PEPTIDES AS NEUROPROTECTIVE AGENTS 审中-公开
标题翻译：作为神经保护剂的疏水肽
公开(公告)号：US20170051031A1
公开(公告)日：2017-02-23
申请号：US15307262
申请日：2015-05-20
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I.
发明人： Lenka MALETINSKA , Blanka ZELEZNA , Miroslava BLECHOVA , Andrea SPOLCOVA , Barbora MIKULASKOVA , Jaroslav KUNES
IPC分类号： C07K14/575
CPC分类号： C07K14/575 , C07K14/57554
摘要： Lipidated neuropeptides based on PrRP31, PrRP20, containing C14 and/or C16 fatty acid, in which sequence of IRPVGRF-NH2 at the C-terminus is variable in the site of isoleucine, valine and phenylalanine; the fatty acid is bound in position 1 or 11 for PrRP31 or its analog and in position 1 or 7 for PrRP20 or its analog; the fatty acid is bound directly or through a hydrophilic linker X2, for use in the treatment and prevention of neurodegenerative diseases such as Alzheimer's disease (AD), Parkinson's disease (PD), cognitive impairment no dementia (CIND), brain trauma, and neurodegenerative changes and disorders.
摘要翻译：基于含有C14和/或C16脂肪酸的PrRP31 PrRP20的脂质化神经肽，其中C-末端的IRPVGRF-NH2的序列在异亮氨酸，缬氨酸和苯丙氨酸的位点是可变的; PrRP31或其类似物的脂肪酸结合位置1或11，PrRP20或其类似物的位置1或7; 脂肪酸直接或通过亲水接头X2结合，用于治疗和预防神经变性疾病如阿尔茨海默病（AD），帕金森病（PD），认知障碍无痴呆（CIND），脑创伤和神经变性变化和紊乱。

2. 发明申请

US20170044230A1 LONG-ACTING STABLE PEPTIDE GHRELIN ANALOGS FOR THE TREATMENT OF CACHEXIA 审中-公开
标题翻译：用于治疗慢性乙型肝炎的长效稳定肽GHRELIN模拟物
公开(公告)号：US20170044230A1
公开(公告)日：2017-02-16
申请号：US15305617
申请日：2015-06-22
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I. , FYZIOLOGICKY USTAV AV CR, V.V.I.
发明人： Lenka MALETINSKA , Blanka ZELEZNA , Jaroslav KUNES , Martina HOLUBOVA , Jana ZEMENOVA
IPC分类号： C07K14/575
CPC分类号： C07K14/575 , A61K38/00
摘要： The present invention provides long-acting stable peptide ghrelin analogs of general formulae (I) (Sar)S(Dpr-X1)mLSPEHQKAQQRKESKKPPA(K-Z)LQPR, and/or (II) (Sar)S(Dpr-X2)FLSPEHQKAQQR(K-Z)ES, in which Dpr is diaminopropionic acid, Sar is sarcosin, X1 represents a fatty acid residue selected from the group comprising octanoyl, decanoyl, myristoyl, 9-decenoyl and N-10-undecynoyl bound to Dpr through an amide bond, X2 represents decanoyl or myristoyl, m represents a non-coded amino acid selected from the group comprising phenylalanine, naphtylalanine, cyclohexylalanine, t-butylalanine and dichlorophenylalanine, Z is palmitoyl which can be optionally bound to the secondary amino group of lysine through an amide bond or Z is not present. The compounds of the invention are suitable for use in a method of treatment of cachexia and/or anorexia.
摘要翻译：本发明提供了通式（Sar）S（Dpr-X1）mLSPEHQKAQQRKESKKPPA（KZ）LQPR（I）和/或（Sar）S（Dpr-X2）FLSPEHQKAQQR（KZ）ES（）的长效稳定肽生长素释放肽类似物 II），其中Dpr是二氨基丙酸，Sar是肌氨酸，X1表示选自由酰基键连接到Dpr的辛酰基，癸酰基，肉豆蔻酰基，9-癸烯酰基和N-10-十一碳炔酰基的脂肪酸残基，X2表示癸酰基或肉豆蔻酰基，m表示选自苯丙氨酸，萘丙氨酸，环己基丙氨酸，叔丁基丙氨酸和二氯苯丙氨酸的非编码氨基酸，Z是可以任选地通过酰胺键与赖氨酸的次级氨基结合的棕榈酰基，或Z不是当下。本发明的化合物适用于治疗恶病质和/或厌食症的方法。

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