摘要:
The present invention relates to a process for the preparation of high purity crystalline peptides Arg Lys Asp hydrate acetate and Arg Lys Asp Val from crude, amorphous peptides Arg Lys Asp and Arg Lys Asp Val hydrate acetate.The process is characterized in thatthe crude, amorphous peptide Arg Lys Asp or Arg Lys Asp Val is let stand at room temperature in 5 to 20 unit volume of ethanol containing 0.5 to 4.0% by volume of acetic acid and 5 to 25% by volume of water, wherein the volume unit is calculated for the mass unit of the material and mass unit relates to volume unit as g relates to ml,then the crystallized peptide is separated from the crystalline suspension, preferably after cooling.
摘要:
Peptides are disclosed which inhibit the immune system. The peptides are selected from the group consisting of:Arg-Lys(Chc)-Asp-ValArg-Lys(Chc)-AspArg-Sar-Asp-ValArg-Sar-AspOrn-Lys-Asp-ValOrn-Lys-AspArg-Lys-Aad-ValArg-Lys-Aad[Arg-Lys-Asp-NH-CH.sub.2 -].sub.2 ##STR1##Lys-Ser-Lys-LeuSer-Lys-LeuSer-Ser-Ser-ThrLys-Glu-ThrLys-Thr-Glu-ThrPro-Lys-Leu-ThrLys-Lys-Thr-Glu andLys-His-Leu-NH.sub.2,and pharmaceutically acceptable acid addition salts thereof.
摘要:
The invention relates to novel peptides of formula (I),A-Try-B-Asp-Phg-NH.sub. 2 (I)whereinA is tert.-butoxycarbonyl-aminooxy-acyl, benzyloxycarbonyl-aminooxy-acyl, (aminooxy)-acyl or E-aminooxy-acyl, wherein E is benzoyl or straight-chained or branched C.sub.1-5 aliphatic acyl, andB represents methionyl, leucyl, norleucyl, norvalyl or 2-amino-decanoyl,or acid addition salts or complexes thereof. The novel compounds according to the invention exert gastrin effects and can be applied to advantage in the diagnostics and therapy. The novel compounds of formula (I) are prepared according to the invention by reacting a tetrapeptideamide of formula (II),H-Try-B-Asp-Phg-NH.sub. 2 (II)wherein B is as defined above, with an (aminooxy)-acyl containing compound of the general formula A.sub.1 -X, whereinA.sub.1 has the same meanings as A with the exception of the (aminooxy)-acyl, andX is hydroxy group, halogen, pivaloyloxy, a group of the formula R--O--CO.sub.2 -- (wherein R is lower alkyl, phenoxy which can have a nitro substituent or one or more halogen or N-succinimidoxy.
摘要:
Peptides of the formula:A--Trp--B--Asp--Phe--NH--Ywherein A is tert.-butoxycarbonyl-aminooxy-acyl, benzyloxycarbonyl-aminooxy-acyl, (aminooxy)-acyl, or E-aminooxy-acyl, wherein E is benzoyl or straight-chain or branched C.sub.1-5 aliphatic acyl, B is methionyl, leucyl, norleucyl, norvalyl or 2-amino-decanoyl, and Y is hydrogen or carboxymethoxy, and pharmaceutically acceptable acid-addition salts or complexes thereof have gastric-acid secretion increasing effects.
摘要:
The invention relates to the preparation of biologically active polypeptides containing the aspartyl group, particularly an aspartyl-glycine moiety, using the active-ester technique.According to the method of the invention, human adrenocorticotropic hormone and its fragments characteristic to the individual species, as well as the blocked derivatives of such compounds are prepared by the pentafluorophenol method, i.e., the carboxy group of the acylating component is activated by converting it into pentafluorophenyl ester in the coupling reaction carried out with blocked peptides containing the aspartyl group or an aspartylglycine moiety. The acylation is carried out preferably using equimolar quantities of the respective reactants. The free peptides obtained after removing the blocking groups can be converted into their acid addition salts or pharmaceutically acceptable complexes or condensates.Human adrenocorticotropic hormone and its derivatives are valuable substances of therapeutical activity.
摘要:
The present invention relates to novel peptides of formulaeXaa Glu Asp Cys Lys (SEQ I.D. No: 1),andGlu Asp Cys Lys (SEQ I.D. No: 2)wherein the Cys sulfur is bonded to an acetamidomethyl group, and Xaa is pyro-Glu, the acid addition salts thereof, the pharmaceutical compositions comprising the same and a process for the preparation of the novel peptides and compositions.The novel peptides selectively inhibit the proliferation of hemopoietic cells.The invention also covers the treatment of mammals (including human beings) with the said peptides and compositions for selectively inhibiting the proliferation of hemopoietic cells.The advantage of the novel compounds is that they are almost completely harmless, they do not have any side-effect in therapeutic dose-range, in addition they significantly inhibit the damaging effects of drugs and radiation used for the therapy of tumorous diseases or the dose of drug or radiation can be increased when they are administered.
摘要翻译:本发明涉及式Xaa Glu Asp Cys Lys(SEQ ID No:1)和Glu Asp Cys Lys(SEQ ID No:2)的新型肽,其中Cys硫与乙酰氨基甲基结合,Xaa是热解 - Glu,其酸加成盐,包含其的药物组合物和制备新肽和组合物的方法。 新型肽选择性抑制造血细胞的增殖。 本发明还涵盖用所述肽和用于选择性抑制造血细胞增殖的组合物治疗哺乳动物(包括人)。 新化合物的优点是它们几乎完全无害,它们在治疗剂量范围内没有任何副作用,此外它们显着抑制用于治疗肿瘤疾病或剂量的药物和辐射的破坏作用 药物或放射线在施用时可以增加。
摘要:
Peptides affecting the immune regulation selected from the following group:Arg-Lys-AspArg-Lys-Asp-ValArg-Lys-Asn-ValArg-Lys-Asu-ValArg-Lys-Ala-ValArg-Lys-Asp-AlaArg-Lys-Asp-IleArg-Lys-Glu-ValArg-Ala-Asp-ValArg-Asp-Lys-ValAla-Lys-Asp-ValLys-Arg-Asp-ValGlp-Arg-Lys-AspGlp-Arg-Lys-Asp-ValGlp-Arg-Lys-Asp-Val-Tyr and salts, amides lower alkyl esters and protected derivatives thereof.
摘要:
The invention relates to novel pyridine derivatives of formula (I), ##STR1## wherein Q stand for a nitro or cyano group; andX.sup.1 and X.sup.2, independently from each other, represent hydrogen or halogen or a trifluoromethyl, a lower alkyl or alkoxy or nitro group bound to any of the carbon atoms of the phenyl ring.The invention further relates to pharmaceutical compositions containing these compounds and a process for their preparation.The compounds of formula (I) possess gastric acid secretion inhibiting, tissue-protecting, analgetic and mild antiinflammatory effects and are useful for therapeutical purposes.
摘要:
The invention relates to novel peptides and their acid addition salts, suppressing the function of the immune system, pharmaceutical compositions containing these peptides as well as to a process for preparing these peptides and compositions. The peptides are represented by formulae (1) to (16): ##STR1## The novel peptides are useful for the therapy of diseases where a decrease in the activity of the immune system is desirable.