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1.发明公开LONG-ACTING STABLE PEPTIDE GHRELIN ANALOGS FOR THE TREATMENT OF CACHEXIA 审中-公开长效稳定肽GHRELIN类似物用于治疗CACHEXIA
公开(公告)号：EP3157948A1
公开(公告)日：2017-04-26
申请号：EP15739501.3
申请日：2015-06-22
申请人： Ustav organicke chemie a biochemie AV CR, v.v.i. , Fyziologicky Ústav Akademie VED Ceské Republiky, V.V.I.
IPC分类号： C07K14/435
CPC分类号： C07K14/575 , A61K38/00
摘要： The present invention provides long-acting stable peptide ghrelin analogs of general formulae (Sar)S(Dpr-X
1 )mLSPEHQKAQQRKESKKPPA(K-Z)LQPR (I), and/or (Sar)S(Dpr-X
2 )FLSPEHQKAQQR(K-Z)ES (II), wherein Dpr is diaminopropionic acid, Sar is sarcosin, X
1 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, X
2 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 aminogroup 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，X 1表示选自辛酰基，癸酰基，肉豆蔻酰基，9-癸酰基和通过酰胺键与Dpr结合的N-10-十一碳酰基的组中的脂肪酸残基，X 2表示癸酰基 或肉豆蔻酰基，m表示选自苯丙氨酸，萘基丙氨酸，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是棕榈酰基，其可以任选通过酰胺键与赖氨酸的第二氨基群键合或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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2.发明授权PREGNANOLONE DERIVATIVES SUBSTITUTED IN 3ALPHA-POSITION WITH THE CATIONIC GROUP, USAGE AND PHARMACEUTICAL PREPARATION INVOLVING THEM 有权在阳离子基团取代的孕烯醇酮衍生物，涉及它们的阳离子基团，用途和药物制剂
公开(公告)号：EP2675821B1
公开(公告)日：2018-04-18
申请号：EP12711108.6
申请日：2012-02-15
申请人： Ústav Organické Chemie A Biochemie Akademie Ved Ceské Republiky, v.v.i. , Fyziologicky Ústav Akademie VED Ceské Republiky, V.V.I.
发明人： CHODOUNSKÁ, Hana , KAPRAS, Vojtech , VYKLICKY, Ladislav , BOROVSKÁ, Jirina , VYKLICKY, Vojtech , VALES , Karel , STUCHLÍK, Ales , RAMBOUSEK, Lukás
CPC分类号： C07J41/0011 , C07J41/0005 , C07J41/005
摘要： Pregnanolone derivatives, substituted in 3 alpha-position with the cationic group, of general formula I, and a method of the production of these compounds and their utilization for treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post traumatic stress disorder, and other diseases related to stress, anxiety, schizophrenia, and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy, and gliomas. The compounds are also used for production of veterinary and human pharmaceutical preparation for treatment of above mentioned diseases and for production of pharmaceutical preparations containing these compounds.
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3.发明公开PREGNANOLONE DERIVATIVES SUBSTITUTED IN 3ALPHA-POSITION WITH THE CATIONIC GROUP, METHOD OF THEIR PRODUCTION, USAGE AND PHARMACEUTICAL PREPARATION INVOLVING THEM 有权在3ALPHA位取代PREGNANOLONDERIVATE用阳离子GROUP，方法制作，以便在使用和药物研制
公开(公告)号：EP2675821A1
公开(公告)日：2013-12-25
申请号：EP12711108.6
申请日：2012-02-15
申请人： Ústav Organické Chemie A Biochemie Akademie Ved Ceské Republiky, v.v.i. , Fyziologicky Ústav Akademie VED Ceské Republiky, V.V.I.
发明人： CHODOUNSKÁ, Hana , KAPRAS, Vojtech , VYKLICKY, Ladislav , BOROVSKÁ, Jirina , VYKLICKY, Vojtech , VALES , Karel , STUCHLÍK, Ales , RAMBOUSEK, Lukás
CPC分类号： C07J41/0011 , C07J41/0005 , C07J41/005
摘要： Pregnanolone derivatives, substituted in 3 alpha-position with the cationic group, of general formula I, and a method of the production of these compounds and their utilization for treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post traumatic stress disorder, and other diseases related to stress, anxiety, schizophrenia, and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy, and gliomas. The compounds are also used for production of veterinary and human pharmaceutical preparation for treatment of above mentioned diseases and for production of pharmaceutical preparations containing these compounds.
摘要翻译： 孕衍生物，substituiertem与阳离子基团3α-位中，通式I，和生产合成化合物的方法及其在治疗与谷氨酸能神经递质系统，颜色的不平衡神经精神障碍的利用：例如CNS的缺血性损伤 ，神经退行性变化和中枢神经系统的障碍，情感障碍，抑郁症，创伤后应激障碍，以及与应激，焦虑症，精神分裂症，和精神障碍，疼痛，成瘾，多发性硬化，癫痫，神经胶质瘤和其他疾病。 因此，该化合物用于制造用于治疗上述疾病的兽医和人类药物制剂和生产含有合成化合物的药物制剂。
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4.发明授权ANIONIC PREGNANE COMPOUNDS, METHOD FOR THEIR PRODUCING AND USE OF THEM 有权阴离子PREGNANVERBINDUNGEN，制造方法及其应用
公开(公告)号：EP2313424B1
公开(公告)日：2014-04-23
申请号：EP09775815.5
申请日：2009-07-09
申请人： Ústav organické chemie a biochemie Akademie ved Ceské republiky, v.v.i. , Fyziologicky ústav Akademie ved Ceské republiky, v.v.i.
发明人： STASTNA, Eva , CHODOUNSKA, Hana , POUZAR, Vladimir , KAPRAS, Vojtech , CAIS, Ondrich , VYKLICKY, Ladislav , KOHOUT, Ladislav
CPC分类号： C07J41/0077 , C07J7/002 , C07J31/006
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公开(公告)号：EP3094643A2
公开(公告)日：2016-11-23
申请号：EP15723290.1
申请日：2015-01-15
申请人： Fyziologicky Ústav Akademie VED Ceské Republiky, V.V.I. , Ustav Organicke Chemie A Biochemie Akademie Ved Cr, v.v.i.
IPC分类号： C07K14/575 , A61K31/00
CPC分类号： A61K47/48038 , A61K38/00 , A61K38/22 , A61K47/542 , A61K47/60 , C07K7/08 , C07K14/001 , C07K14/575
摘要： Lipidated analogs of prolactin-releasing peptides (PrRP) and their use in controlling and lowering blood glucose in mammals is disclosed. Useful compounds included lipidated analogs of PrRP20 and PrRP31. Pharmacological effects are demonstrated both in vitro and in vivo. Peripheral administration of the lipidated peptides lowers blood glucose levels. These treatments are applicable for treating impaired glucose tolerance (IGT), and glucose intolerance condition. The disclosed compounds have application in treating medical conditions including diabetes, pre-diabetes, eating disorders, and obesity.
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