摘要:
This invention relates to new peptide derivatives of the general formula (I) A-Xaa-Arg-H, wherein A represents a D- or L-isochroman-1-carbonyl, D- or L-isochroman-3-carbonyl group, furthermore an acyl group of the general formula: D- or DL-A'--CH(OH)--CO, wherein A' represents a phenyl, benzyl, 1-naphthyl, 1-naphthylmethyl, 2-naphthyl, 2-naphthylmethyl, 9-fluorenyl, benzhydryl, cyclohexyl, cyclohexylmethyl, 2-pyridyl, 3-pyridyl or 4-pyridyl group, and Xaa represents an L-prolyl or an L-pipecolinic acid residue, and Arg stands for an L-arginine residue, their acid addition salts formed with an organic or inorganic acid and pharmaceutical compositions containing the same. Furthermore the invention relates to a process for preparing them. The compounds of the invention have valuable therapeutic, particularly anticoagulant, properties.
摘要:
This invention relates to peptide aldehyde derivatives of formula (I): D-Xaa-Pro-Arg-H, wherein Xaa represent a 2-cycloheptyl-2-hydroxyacetyl or 2-cyclopentyl-2-hydroxyacetyl group, Pro represents an L-prolyl residue and Arg represents an L-arginyl residue, their acid-additon salts formed with an organic or inorganic acid and pharmaceutical compositions containing the same. The compounds of formula (I) of the invention have therapeutic, particularly anticoagulant, antiplatelet and antithrombotic properties.
摘要:
The invention relates to a new (3R)-3-amino-4-carboxybutyraldehyde derivatives of general formula(I) wherein X represents a C1-4 alkyloxycarbonyl, an optionally substituted phenyl-(C1-2 alkyloxy)-carbonyl, a C1-4 alkylcarbonyl or an optionally substituted phenyl-(C1-3 alkyl)-carbonyl group, n represents 1 or 0, Y represents, in the case when n=1, a tetrapeptide of general formula Y4-Y3-Y2-Y1, a tripeptide of general formula Y3-Y2-Y1 or a dipeptide of general formula Y2-Y1 or an amino acid residue of general formula Y1, or in the case when n=0, an &agr;-hydroxyacyl-tripeptide of general formula Q4-Y3-Y2-Y1, an &agr;-hydroxyacyl-dipeptide of general formula Q3-Y2-Y1 or an &agr;-hydroxyacyl-aminoacyl residue of general formula Q2-Y1; wherein Y1-Y4 represent a residue selected from the group of the following L- or D-amino acids: alanine, alloisoleucine, cyclohexyl-glycine, phenyl-alanine, glutamine, histidine, isoleucine, leucine, lysine, methionine, pipecolic acid, proline, tyrosine and valine; and Q2-Q4 represent an acyl group selected from the following &agr;-hydroxyacids of R or S configuration: 2-cycloheptyl-2-hydroxy-acetic acid, 2-cyclohexyl-2-hydroxyacetic acid, 3-cyclohexyllactic acid, 3-phenyllactic acid, 2-hydroxy-3-methylbutyric acid, 2-hydroxy-3-methylvaleric acid, mandelic acid or lactic acid, and salts thereof formed with organic or inorganic bases, and pharmaceutical compositions containing the same. The compounds of general formula (I) of the invention are valuable inhibitors of the interleukin-1&bgr; converting enzyme.
摘要:
The present invention deals with LHRH analogs which contain cytotoxic moieties, have influence on the release of gonadotropins from the pituitary in mammals (possess high agonistic or antagonistic activity) and have antineoplastic effect. The compounds of this invention are represented by Formula I: X-R1-R2-R3-Ser-R5-R6(Q)-Leu-Arg-Pro-R10-NH2, wherein R1 is pGlu or D-Nal(2), R2 is His or D-Phe(4Cl), R3 is Trp, D-Trp or D-Pal(3), R5 is Tyr or Arg, R6 is D-Lys or D-Orn, R10 is Gly or D-Ala, X is hydrogen or a lower alkanoyl group of 2-5 carbon atoms, Q is a cytotoxic moiety having the formula —Q4 or —A(Q3) or —B(Q1)2 or —B(AQ2)2, wherein A is —NH—(CH2)n—CO— or —OC—(CH2)n—CO— where n is 2-6, B is —NH—CH2—(CH2)m—CH(NH)—(CH2)n—CO— where m is 0 or 1, n is 0 or 1, the —CO moiety of A— and of B— being bonded to an amino group on R6, and in the group B(AQ2)2, the —CO moiety of A— and of B— being bonded to the episilon or delta amino group of R6 when R6 is Lys or Orn respectively, and in the group B(AQ2)2, the —CO moiety of A being bonded to an amino group on B, Q1 is D or L-Mel, cyclopropanealkanoyl, aziridine-2-carbonyl, epoxyalkyl or 1,4-naphthoquinone-5-oxy-carbonyl-ethyl, Q2 is Q1, 2-anthraquinonyl-methylenoxy or doxorubicinyl, Q3 is Q2, mitomicinyl, esperamycinyl or methotrexoyl, Q4 is Q1 or methotrexoyl and pharmaceutically acceptable salts thereof and methods of use pertaining these compounds.
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 idea of the present invention providing a solution for configuration problems of a node is based on the following components. A problem recognition system, which analyses performance indicators and identifies root causes, so that signatures can be attached to a found problems. Furthermore there is a signature based filtering system, which looks for transactions satisfying signatures. A customer identification system labels the transactions with the subscriber identify. A solution feedback system generates feedback event to the end node according to the rule of the signature.
摘要:
The idea of the present invention providing a solution for configuration problems of a node is based on the following components. A problem recognition system, which analyses performance indicators and identifies root causes, so that signatures can be attached to a found problems. Furthermore there is a signature based filtering system, which looks for transactions satisfying signatures. A customer identification system labels the transactions with the subscriber identify. A solution feedback system generates feedback event to the end node according to the rule of the signature.