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1. 发明授权

EP2771021B1 NMDA RECEPTOR MODULATORS AND USES THEREOF 有权
公开(公告)号：EP2771021B1
公开(公告)日：2018-08-29
申请号：EP12844456.9
申请日：2012-10-24
申请人： North Western University
发明人： KHAN, Amin, M. , MOSKAL, Joseph
IPC分类号： C07K5/103 , C07K5/078 , C07K5/097 , A61K38/07 , A61K38/00 , A61P25/24
CPC分类号： C07K5/1013 , A61K38/00 , A61K38/07 , C07D403/06 , C07K5/06165 , C07K5/0823
摘要： Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders, such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

2. 发明公开

EP3223613A4 4-FLUORO-THIO-CONTAINING INHIBITORS OF APP2, COMPOSITIONS THEREOF AND METHOD OF USE 有权
公开(公告)号：EP3223613A4
公开(公告)日：2018-07-18
申请号：EP15862635
申请日：2015-10-30
申请人： SIMMONS WILLIAM H
发明人： SIMMONS WILLIAM H
IPC分类号： C07K5/08 , A61K38/00
CPC分类号： C07K5/0823 , A61K38/00 , A61K38/06
摘要： The present invention has multiple aspects. In its first aspect, it is directed to a compound that is a 4(S)-fluoro-thio-tripeptide analog that has the unexpectedly superior property of specifically inhibiting the enzyme, membrane-bound aminopeptidase P2 (APP2), whose natural substrate is bradykinin, but not the enzyme angiotensin converting enzyme (ACE) which also cleaves bradykinin. In its second aspect, the present invention is directed to a pharmaceutical composition comprising the 4(S)-fluoro-thio-tripeptide analog and a pharmaceutically acceptable carrier. In its third aspect, the invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, comprising administering a therapeutically effective amount of the compound of the invention to a mammalian patient in need of inhibition of bradykinin degradation.

3. 发明公开

EP3331898A1 CHROMOGENIC AND FLUOROGENIC PEPTIDE SUBSTRATES FOR THE DETECTION OF SERINE PROTEASE ACTIVITY 审中-公开
公开(公告)号：EP3331898A1
公开(公告)日：2018-06-13
申请号：EP16756940.9
申请日：2016-08-03
申请人： Ruprecht-Karls-Universität Heidelberg
发明人： KRÄMER, Roland , ARIAN, Dumitru , HARENBERG, Job
IPC分类号： C07K5/087 , C07K5/09 , G01N33/68
CPC分类号： C07K5/0817 , C07K5/06026 , C07K5/06165 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0815 , C07K5/0819 , C07K5/0823 , C07K5/1008 , C07K5/101 , C12Q1/37
摘要： The present invention relates to chromogenic and fluorogenic substrates that can be used for the highly sensitive and selective detection of the activity of serine proteases. The present invention further relates to methods for the detection of the activity of serine proteases, said methods using the substrates of the present invention. Furthermore, the present invention relates to diagnostic kits and test strips using the above substrates, as well as uses of said substrates.

4. 发明公开

EP3145943A1 PEPTIDES, COMPOSITIONS COMPRISING THEM AND USES IN PARTICULAR COSMETIC USES 审中-实审转让
标题翻译：肽，ZUSAMMENSETZUNGEN DAMIT UND SPEERIZEN KOSMETISCHEN ANWENDUNGEN VERWENDUNGEN
公开(公告)号：EP3145943A1
公开(公告)日：2017-03-29
申请号：EP15732391.6
申请日：2015-05-21
申请人： Sederma
发明人： PESCHARD, Olivier , DOUCET, Anne , LE ROUX, Richard , MONDON, Philippe
IPC分类号： C07K5/097 , A61K8/64 , A61Q19/08
CPC分类号： A61K8/64 , A61K38/00 , A61K2800/74 , A61Q19/08 , C07K5/0823
摘要： The peptides have the general following formula: X-Pro*-Pro*-Xaa-Y in which: —Xaa is selected from Leucine (Leu, L), Arginine (Arg, R), Lysine (Lys, K), Alanine (Ala, A), Serine (Ser, S), and Aspartic acid (Asp, D); —At the N terminal end of the peptide, X is selected from H, —CO—R1 and —SO2—R1; —At the C terminal end of the peptide, Y is selected from OH, OR1, NH2, NHR1 and NR1R2; —R1 and R2 are, independently from each other, selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy and aryloxy group, that can be linear, branched, cyclic, poly-cyclic, non-saturated, hydroxylated, carbonylated, phosphorylated and/or sulfured, and which skeletum can comprise an heteroatom, in particular an O, S and/or N atom; —Pro* correspond to a Proline, an analogue or derivative thereof; —if X is H then Y is selected from OR1, NH2, NHR1 and NR1R2, and if Y is OH then X is —CO— or —SO2—R1; and the peptide hypoxanthine-Pro-Pro-Arg being excluded. The invention provides the use of the peptides of above formula I to stimulate the synthesis of the molecules constituting the dermal extracellular matrix, including collagen I and IV and elastin. A cosmetic treatment according to the invention includes anti-aging, anti-wrinkles, improving mechanical properties of the skin, firmness/tone/elasticity/suppleness/flexibility, increasing density and volume of the skin, restructuring effect, fighting stretch marks, improving skin barrier and/or skin hydration.
摘要翻译：肽具有以下通式：X-Pro * -Pro * -Xaa-Y，其中：-Xaa选自亮氨酸（Leu，L），精氨酸（Arg，R），赖氨酸（Lys，K），丙氨酸 Ala，A），丝氨酸（Ser，S）和天冬氨酸（Asp，D）; - 在肽的N末端，X选自H，-CO-R 1和-SO 2 -R 1; - 肽的C末端，Y选自OH，OR1，NH2，NHR1和NR1R2; -R1和R2彼此独立地选自烷基，芳基，芳烷基，烷基芳基，烷氧基和芳氧基，其可以是直链，支链，环状，多环，非饱和，羟基化，羰基化，磷酸化和 /或硫化，哪些骨架可以包含杂原子，特别是O，S和/或N原子; -Pro *对应于脯氨酸，其类似物或衍生物; - 如果X是H，那么Y选自OR1，NH2，NHR1和NR1R2，如果Y是OH，则X是-CO-或-SO2-R1; 并排除了次黄嘌呤-Pro-Pro-Arg。本发明提供上述式I的肽刺激构成真皮细胞外基质（包括胶原I和IV和弹性蛋白）的分子的合成。根据本发明的美容处理包括抗老化，抗皱纹，改善皮肤的机械性能，坚固性/色调/弹性/柔软性/柔韧性，增加皮肤的密度和体积，重组效果，抗妊娠纹，改善皮肤屏障和/或皮肤水合。

5. 发明公开

EP3066112A1 SELECTIVE INHIBITORS OF PROTEINASE 3 审中-公开
标题翻译：蛋白酶3的选择性抑制剂
公开(公告)号：EP3066112A1
公开(公告)日：2016-09-14
申请号：EP14793149.7
申请日：2014-11-04
申请人： INSERM - Institut National de la Santé et de la Recherche Médicale , Université de Tours Francois Rabelais , Uniwersytet Gdanski
发明人： GAUTHIER, Francis , KORKMAZ, Brice , LESNER, Adam
IPC分类号： C07K5/093 , A61K38/06 , C07K5/097 , C07K5/103 , C07K5/117 , C07K5/083 , A61P35/00 , A61P37/00 , A61P29/00
CPC分类号： C07K5/1021 , A61K38/00 , A61K47/545 , A61K47/60 , C07K5/0808 , C07K5/0819 , C07K5/0823 , C07K5/101 , C07K5/1024 , G01N33/573
摘要： The present invention relates to peptidyl phosphonate esters compounds and their use selective inhibitors of proteinase 3, in particular for treating or diagnosing inflammator autoimmune and cancer disorders. More specifically, the invention concerns nov peptidyl phosphonate esters compounds, including without limitation, compounds wi Asp-Tyr-Asp-Ala or Pro-Tyr-Asp-Ala, Pro-Tyr-Asp-Avl, Val-Tyr-Asp-Avl peptide structu or their derivatives.

6. 发明公开

EP2648735A2 GRANZYME B INHIBITOR COMPOSITIONS, METHODS AND USES FOR PROMOTING WOUND HEALING 审中-公开
标题翻译：酶B性组合物，方法和用途用于促进伤口愈合
公开(公告)号：EP2648735A2
公开(公告)日：2013-10-16
申请号：EP11846821.4
申请日：2011-12-06
申请人： The University of British Columbia
发明人： HIEBERT, Paul, R. , KNIGHT, Darryl, A. , GRANVILLE, David, J. , BOIVIN, Wendy, A. , COOPER, Dawn, M.
IPC分类号： A61K31/55 , A61K31/365 , A61K31/4025 , A61K31/675 , A61K38/05 , A61K38/57 , A61K39/395 , A61P17/00 , A61P17/02 , C07C237/22 , C07D307/88 , C07D487/06 , C07F9/6561 , C07K5/00 , C07K14/82 , C07K16/40 , C12N9/64
CPC分类号： A61K38/005 , A61K31/167 , A61K31/365 , A61K31/55 , A61K38/06 , A61K38/07 , A61K38/55 , A61K45/05 , A61K45/06 , C07D307/33 , C07D307/83 , C07D487/04 , C07K5/0823 , C07K5/1005 , C07K5/1024 , G01N2333/96436 , G01N2500/02
摘要： Methods of promoting wound healing in a subject is disclosed. The method include applying a Granzyme B (Granzyme B) inhibitor to the wound. The wound may be a skin wound. The Granzyme B inhibitor may be comprised of nucleic acids, or peptides, including but not limited to antibodies, or small molecules.

7. 发明公开

EP2607373A1 Liquid phase synthesis of self-assembling peptides to be linked to polymers or to other bioactive and/or self-assembling peptides 审中-公开
标题翻译：自组装肽的液相合成链接到聚合物或与其它生物活性和/或自组装肽
公开(公告)号：EP2607373A1
公开(公告)日：2013-06-26
申请号：EP11195626.4
申请日：2011-12-23
申请人： SOLVAY SA
发明人： Moussa, Wafa , Jeannin, Laurent , Callens, Roland , Bousmanne, Martin
IPC分类号： C07K5/10 , C07K1/02
CPC分类号： C07K1/02 , C07K1/026 , C07K5/06078 , C07K5/0806 , C07K5/0815 , C07K5/0823 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K5/1019 , C07K5/1021
摘要： The present invention relates to a process for preparing a peptide moiety comprising an amino acid sequence (I)

R-Xaa1-Xaa5-Xaa3-Xaa6-R1 (I),

wherein R1 is selected from OH and NH 2
and a peptide moiety comprising an amino acid sequence (II)

H-Xaa1-Xaa2-Xaa3-Xaa4-Xaal-Xaa5-Xaa3-Xaa6-R1 (II),

wherein R1 is selected from OH and NH 2
whereby Xaa1 and Xaa3 are residues of hydrophobic amino acids and are preferably selected from the group consisting of phenylalanine, tryptophan, histidine, tyrosine, isoleucine, alanine, leucine, norleucine and valine ; and Xaa2, Xaa4, Xaa5 and Xaa6 are residues of charged amino acids and are preferably selected from the group consisting of arginine, aspartic acid, glutamic acid and lysine.
The invention further relates to a process for synthesis of a polymer covalently linked with at least one peptide, wherein the peptide comprises said peptide moiety.
摘要翻译：本发明涉及一种用于制备的肽部分，其包含氨基酸序列（I）€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒR-的Xaa 1的Xaa 5-Xaa3-的Xaa 6-R1€ƒ€的 ƒƒ€€€ƒƒ（I）中，R1 worin选自OH和NH 2和包含氨基酸序列（II）€€ƒƒƒ€€€ƒƒƒ€€€ƒƒh的肽部分选择 Xaa1-Xaa2-Xaa3-的Xaa 4的Xaa1-的Xaa 5-Xaa3-的Xaa 6-R1€ƒ€ƒ€ƒ€ƒ€ƒ（II），worin R 1选自OH和NH 2中选择，由此Xaa1并且Xaa3是疏水性氨基酸残基并且优选选自苯丙氨酸，色氨酸，组氨酸，酪氨酸，异亮氨酸，丙氨酸，亮氨酸，正亮氨酸和缬氨酸的选择; 和Xaa2，4的Xaa，5的Xaa和6的Xaa是带电荷的氨基酸残基，且优选选自精氨酸，天冬氨酸，谷氨酸和赖氨酸组成的组。本发明还涉及一种用于具有至少一个肽共价连接的聚合物，worin肽包括所述肽部分的合成的方法。

8. 发明公开

EP2598517A1 MODULATORS OF PROTEASE ACTIVATED RECEPTORS 有权
标题翻译：蛋白酶激活受体调节剂
公开(公告)号：EP2598517A1
公开(公告)日：2013-06-05
申请号：EP11811656.5
申请日：2011-07-28
申请人： The University of Queensland
发明人： FAIRLIE, David Paul , LIU, Ligong , YAU, Mei Kwan , SUEN, Jacky Yung
IPC分类号： C07K5/065 , A61K38/05 , A61K38/06 , A61P1/00 , A61P3/00 , A61P7/00 , A61P9/00 , A61P11/00 , A61P13/00 , A61P17/00 , A61P19/00 , A61P21/00 , A61P25/00 , A61P29/00 , A61P37/00 , C07K5/062 , C07K5/078 , C07K5/083
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/00 , C07K5/06034 , C07K5/06078 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0823 , C07K5/0825
摘要： The present invention provides novel compounds of the Formula (1), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for modulating Protease Activated Receptor-2 (PAR2) and for treating a subject at risk of—or susceptible to—a disease or disorder, or having a disease or disorder associated with undesirable PAR2 activity.

9. 发明授权

EP1506172B1 HEPATITIS C VIRUS INHIBITORS 有权
标题翻译：丙型肝炎病毒抑制剂
公开(公告)号：EP1506172B1
公开(公告)日：2011-03-30
申请号：EP03799806.9
申请日：2003-05-20
申请人： Bristol-Myers Squibb Company
发明人： RIPKA, Amy , CAMPBELL, Jeffrey, Allen , GOOD, Andrew, Charles , SCOLA, Paul, Michael , SIN, Ny , VENABLES, Brian
IPC分类号： C07K5/08 , A61K38/06 , C07D207/04 , A61K31/40 , C07K5/06
CPC分类号： A61K38/06 , A61K31/40 , C07D207/16 , C07K5/06165 , C07K5/0823
摘要： The present invention relates to tripeptide compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. In particular, the present invention provides novel tripeptide analogs, pharmaceutical compositions containing such analogs and methods for using these analogs in the treatment of HCV infection.
摘要翻译：本发明涉及用于治疗丙型肝炎病毒（HCV）感染的三肽化合物，组合物和方法。特别地，本发明提供了新的三肽类似物，含有这些类似物的药物组合物以及使用这些类似物治疗HCV感染的方法。

10. 发明公开

EP1893192A4 METHODS OF FACILITATING NEURAL CELL SURVIVAL USING NON-PEPTIDE AND PEPTIDE BDNF NEUROTROPHIN MIMETICS 审中-公开
标题翻译：基于METHOD FOR ENABLING神经细胞的存活非肽和肽SCHER BDNF神经营养蛋白模拟物
公开(公告)号：EP1893192A4
公开(公告)日：2010-03-31
申请号：EP06784665
申请日：2006-06-08
申请人： UNIV NORTH CAROLINA , UNIV CALIFORNIA , U S GOVERMENT REPRESENTED BY T
发明人： LONGO FRANK M , MASSA STEPHEN M
IPC分类号： C12N5/16
CPC分类号： C07C215/68 , A61K31/40 , A61K31/401 , A61K31/4178 , A61K38/185 , C07K5/0823 , C07K5/1016

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