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    Bradykinin-inhibiting tripeptide derivatives
    1.
    发明授权
    Bradykinin-inhibiting tripeptide derivatives 失效
    缓激肽抑制三肽衍生物

    公开(公告)号：US4242329A

    公开(公告)日：1980-12-30

    申请号：US58333

    申请日：1979-07-17

    申请人： Karl G. Claeson ,  Leif R. Simonsson ,  Salo Arielly

    发明人： Karl G. Claeson ,  Leif R. Simonsson ,  Salo Arielly

    IPC分类号： A61K38/00 ,  A61K38/06 ,  C07K5/08 ,  C07K5/087 ,  C07K5/097 ,  C07K14/00 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K5/0823 ,  C07K5/0812

    摘要： Tripeptide derivatives of the formulaH-D-X-Phe-Arg-Yin whichX is selected from the group consisting of Pro and PheY is selected from the group consisting of O--R.sub.1 and NH--R.sub.2 in whichR.sub.1 is selected from the group consisting of straight, branched and cyclic alkyl group with 1-12 C atoms, andR.sub.2 is selected from the group consisting of H, straight, branched and cyclic alkyl group with 1-12 C atoms, and physiologically acceptable salts thereof.A process for producing said tripeptide derivatives by synthesis and purification methods which are known in the peptide chemistry.Pharmaceutical preparations comprising said tripeptide derivatives.

    摘要翻译： 其中X选自Pro和Phe Y的式HDX-Phe-Arg-Y的三肽衍生物选自O-R1和NH-R2，其中R1选自由以下组成的组： 具有1-12个C原子的直链，支链和环状烷基，R2选自H，具有1-12个C原子的直链，支链和环状烷基及其生理上可接受的盐。 通过肽化学中已知的合成和纯化方法制备所述三肽衍生物的方法。 包含所述三肽衍生物的药物制剂。

    New peptide derivatives
    2.
    发明授权
    New peptide derivatives 失效
    新肽衍生物

    公开(公告)号：US4797472A

    公开(公告)日：1989-01-10

    申请号：US27969

    申请日：1987-03-19

    申请人： Stig I. Gustavsson ,  Salo Arielly

    发明人： Stig I. Gustavsson ,  Salo Arielly

    IPC分类号： C07K5/09 ,  C07K5/08

    CPC分类号： C07K5/0817 ,  Y10S530/802

    摘要： Tripeptide derivatives, characterized by the general formula:R.sub.1 --X--D--Arg--A--Arg--NH--R.sub.2wherein R.sub.1 is hydrogen, .alpha.- or .beta.-naphtyl residue, lower alkyl residue which may be substituted with a carboxyl group, unsubstituted or substituted phenyl- or phenylalkyl residue. ##STR1## or a single bond with the proviso that when R.sub.1 is hydrogen then and only then X is a single bondA=Gly or SarR.sub.2 =an aromatic or heterocyclic residue which gives a compound R.sub.2 --NH.sub.2 by enzymatic hydrolysis, which can be determined quantitativelyor disalts and trisalts of inorganic or organic acids thereof, process for their preparation and method for determination of serine proteases, especially Factor X.sub.a,or components which can interact with serine proteases or zymogen forms thereof.

    摘要翻译： 三肽衍生物，其特征在于通式为：R1-XD-Arg-A-Arg-NH-R2，其中R1为氢，α-或β-萘基残基，可被羧基取代的未取代或取代的低级烷基残基 苯基或苯基烷基残基。 或单键，条件是当R 1是氢时，然后只有X是单键A = Gly或Sar R 2 =通过酶水解得到化合物R2-NH2的芳族或杂环残基，其可以是 确定其无机或有机酸的定量或三价，其制备方法和丝氨酸蛋白酶，特别是因子Xa的测定方法或可与丝氨酸蛋白酶或其酶原形式相互作用的组分。

    Chromogenic substrate
    4.
    发明授权
    Chromogenic substrate 失效
    显色底物

    公开(公告)号：US5334703A

    公开(公告)日：1994-08-02

    申请号：US859717

    申请日：1992-06-11

    申请人： Salo Arielly

    发明人： Salo Arielly

    IPC分类号： C07K1/02 ,  C07K1/113 ,  C07K5/08 ,  C07K5/083 ,  C07K5/093 ,  C07K5/10 ,  C07K5/103 ,  C07K11/00 ,  C12Q1/37 ,  C07K5/00

    CPC分类号： C07K11/00 ,  C07K5/101 ,  Y02P20/55

    摘要： The invention relates to, novel peptide derivatives with the formula: R.sub.1 -A.sub.1 -A.sub.2 -A.sub.3 -A.sub.4 -R.sub.2 or its salt, wherein R.sub.1 =H or a protective group, A.sub.1 =H, Ile, Leu or Val, A.sub.2 =Glu, Asp, Ser, Thr; A.sub.3 =Gly or Glyc; A.sub.4 =Arg or Lys; R.sub.2 =4-nitroaniline with the proviso that A.sub.3 is Gly when A.sub.4 is Lys and that A.sub.3 is Glyc when A.sub.4 is Arg. The invention also discloses the process for the preparation of the peptide derivatives, the method for the determination of the bacterial endotoxins by the use of the invented peptide derivatives and the use of these derivatives for determination of bacterial endotoxins.

    摘要翻译： PCT No.PCT / SE90 / 00797 Sec。 371日期：1992年6月11日 102（e）日期1992年6月11日PCT 1990年12月3日PCT PCT。 第WO91 / 09052号公报 日期：1991年6月27日本发明涉及具有下式的新型肽衍生物：R1-A1-A2-A3-A4-R2或其盐，其中R1 = H或保护基，A1 = H，Ile，Leu 或Val，A2 = Glu，Asp，Ser，Thr; A3 = Gly或Glyc; A4 = Arg或Lys; R2 = 4-硝基苯胺，条件是当A4为Lys时A3为Gly，当A4为Arg时，A3为Glyc。 本发明还公开了制备肽衍生物的方法，通过使用本发明的肽衍生物测定细菌内毒素的方法以及这些衍生物用于测定细菌内毒素的用途。

    Peptide substrates for determination of protease activity
    5.
    发明授权
    Peptide substrates for determination of protease activity 失效

    公开(公告)号：US4748116A

    公开(公告)日：1988-05-31

    申请号：US53569

    申请日：1987-05-21

    申请人： Leif R. Simonsson ,  Salo Arielly ,  Leif E. Aurell ,  Karl G. Claeson

    发明人： Leif R. Simonsson ,  Salo Arielly ,  Leif E. Aurell ,  Karl G. Claeson

    IPC分类号： C07D237/32 ,  C07K5/08 ,  C07K14/00 ,  C12Q1/37 ,  G01N33/52 ,  C12Q1/38 ,  C07K5/06 ,  C07K5/10

    CPC分类号： C12Q1/37 ,  C07D237/32 ,  C07K5/08 ,  C12Q2337/00 ,  Y10S530/802 ,  Y10S930/28

    摘要： Peptide sequences consisting of 2-4 amino acids with high affinity and comparatively high specificity to a number of various, physiologically important proteases are known to have been synthetized before. Such sequences with an added C-terminal marker have been widely used as substrates for the quantitative determination of the kind of proteases mentioned above. The method is based on the fact that the marker is split off under influence of the enzyme and that the liberated marker possesses an easily measurable, for instance, optic property which differs from that of the original substrate. The type of markers used until today have mainly been chromophores or fluorophores which can be quantified by photometry or fluorometry.The present invention relates to a new type of markers coupled to known peptide sequences. These markers are luminol or isoluminol which in their free state can be brought to luminate intensely, but lose considerably in luminescence when they are amide-bound to a peptide sequence.The peptide derivatives consist of acyl derivates of luminol (5-amino-2,3-dihydro-1,4-phthalazinedione) or isoluminol (6-amino-2,3-dihydro-1,4-phthalazinedione) where the acyl residue consists of an amide-bound amino acid or amino acid sequence with 2-4 amino acid residues and where the .alpha.-amino group is either free of acylated.The greatest advantages of the luminogenic substrates according to the invention are that theyare considerably more sensitive than the previously use chromogenic or fluorogenic substrates and can be used for measuring even extremely low protease concentration;permit measurement of minute final volumes in standard luminometers which also are technically less complicated and, therefore, cheaper than both spectrophotometers and fluorometers; as a result, costs for both analysis reagents and devices can be cut down;permit linear response measurements within a much wider concentration range than is the case with the usual chromogenic and fluorogenic methods;generate markers less sensitive to deactivating interference as, for instance, chemical quenching; this distinguishes them from, for instance, fluorogenic substrates.