PEPTIDES, METHOD OF THEIR SYNTHESIS, AGENT SHOWING BRADYKININ-ANTAGONISTIC ACTIVITY

FIELD: biologically active peptides. SUBSTANCE: product: peptides of the formula (I): Z-P-A-B-C-E-F-K-(D)Q-G-M- -Y where Z means 9-fluorenylmethyloxycarbonyl (Fmoc), dibenzyl acetate, cyclohexylcarbonyl, N,N-dibenzylglycyl, 2-(4-isobutylphenyl)- -propionyl, 2-R-(tert.-butylsulfonylmethyl)-3-(1-napht...

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Hauptverfasser:	KHERMANN GERKHARDS, BERNVARD SHEL'KENS, GERKHARD BRAJPOL, KLAUS VIRT, KHANS-GEORG AL'PERMANN, STEFAN KHENKE, JOKHEN KNOLLE
Format:	Patent
Sprache:	eng
Schlagworte:	CHEMISTRY HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEPTIDES PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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creator	KHERMANN GERKHARDS BERNVARD SHEL'KENS GERKHARD BRAJPOL KLAUS VIRT KHANS-GEORG AL'PERMANN STEFAN KHENKE JOKHEN KNOLLE
description	FIELD: biologically active peptides. SUBSTANCE: product: peptides of the formula (I): Z-P-A-B-C-E-F-K-(D)Q-G-M- -Y where Z means 9-fluorenylmethyloxycarbonyl (Fmoc), dibenzyl acetate, cyclohexylcarbonyl, N,N-dibenzylglycyl, 2-(4-isobutylphenyl)- -propionyl, 2-R-(tert.-butylsulfonylmethyl)-3-(1-naphthyl)- -propionyl-indole-3-yl-acetyl, 6-(4-benzoylbenzoylamino)-hexa- -noyl-1,8-naphthalimidoacetyl, 7-theophylline-acetyl or N-benzoyl; P means direct bond, Aoc, epsi-aminohexanoyl; D - Aoc, Aeq (Fmoc), 4-aminocyclohexylcarbonyl or Oic; A means (D)- or (L)-Arg, (D)- or (L)-Lys or bond; B means Arg; C means Pro-Hyp-Gly; E means Thia; F means Ser; K means direct bond; Q means Tic; M means direct bond; G means cis-endo, cis-exo, trans-octahydroindole-2-carboxylic acid; means Arg and Y means OH. Peptides (I) are synthesized by solid-phase method. Peptides are incorporated as an active component at effective amount to agent showing bradykinin-antagonistic activity and can be used in medicine. EFFECT: improved method of synthesis. 16 cl, 3 tbl
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SUBSTANCE: product: peptides of the formula (I): Z-P-A-B-C-E-F-K-(D)Q-G-M- -Y where Z means 9-fluorenylmethyloxycarbonyl (Fmoc), dibenzyl acetate, cyclohexylcarbonyl, N,N-dibenzylglycyl, 2-(4-isobutylphenyl)- -propionyl, 2-R-(tert.-butylsulfonylmethyl)-3-(1-naphthyl)- -propionyl-indole-3-yl-acetyl, 6-(4-benzoylbenzoylamino)-hexa- -noyl-1,8-naphthalimidoacetyl, 7-theophylline-acetyl or N-benzoyl; P means direct bond, Aoc, epsi-aminohexanoyl; D - Aoc, Aeq (Fmoc), 4-aminocyclohexylcarbonyl or Oic; A means (D)- or (L)-Arg, (D)- or (L)-Lys or bond; B means Arg; C means Pro-Hyp-Gly; E means Thia; F means Ser; K means direct bond; Q means Tic; M means direct bond; G means cis-endo, cis-exo, trans-octahydroindole-2-carboxylic acid; means Arg and Y means OH. Peptides (I) are synthesized by solid-phase method. Peptides are incorporated as an active component at effective amount to agent showing bradykinin-antagonistic activity and can be used in medicine. 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SUBSTANCE: product: peptides of the formula (I): Z-P-A-B-C-E-F-K-(D)Q-G-M- -Y where Z means 9-fluorenylmethyloxycarbonyl (Fmoc), dibenzyl acetate, cyclohexylcarbonyl, N,N-dibenzylglycyl, 2-(4-isobutylphenyl)- -propionyl, 2-R-(tert.-butylsulfonylmethyl)-3-(1-naphthyl)- -propionyl-indole-3-yl-acetyl, 6-(4-benzoylbenzoylamino)-hexa- -noyl-1,8-naphthalimidoacetyl, 7-theophylline-acetyl or N-benzoyl; P means direct bond, Aoc, epsi-aminohexanoyl; D - Aoc, Aeq (Fmoc), 4-aminocyclohexylcarbonyl or Oic; A means (D)- or (L)-Arg, (D)- or (L)-Lys or bond; B means Arg; C means Pro-Hyp-Gly; E means Thia; F means Ser; K means direct bond; Q means Tic; M means direct bond; G means cis-endo, cis-exo, trans-octahydroindole-2-carboxylic acid; means Arg and Y means OH. Peptides (I) are synthesized by solid-phase method. Peptides are incorporated as an active component at effective amount to agent showing bradykinin-antagonistic activity and can be used in medicine. 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SUBSTANCE: product: peptides of the formula (I): Z-P-A-B-C-E-F-K-(D)Q-G-M- -Y where Z means 9-fluorenylmethyloxycarbonyl (Fmoc), dibenzyl acetate, cyclohexylcarbonyl, N,N-dibenzylglycyl, 2-(4-isobutylphenyl)- -propionyl, 2-R-(tert.-butylsulfonylmethyl)-3-(1-naphthyl)- -propionyl-indole-3-yl-acetyl, 6-(4-benzoylbenzoylamino)-hexa- -noyl-1,8-naphthalimidoacetyl, 7-theophylline-acetyl or N-benzoyl; P means direct bond, Aoc, epsi-aminohexanoyl; D - Aoc, Aeq (Fmoc), 4-aminocyclohexylcarbonyl or Oic; A means (D)- or (L)-Arg, (D)- or (L)-Lys or bond; B means Arg; C means Pro-Hyp-Gly; E means Thia; F means Ser; K means direct bond; Q means Tic; M means direct bond; G means cis-endo, cis-exo, trans-octahydroindole-2-carboxylic acid; means Arg and Y means OH. Peptides (I) are synthesized by solid-phase method. Peptides are incorporated as an active component at effective amount to agent showing bradykinin-antagonistic activity and can be used in medicine. EFFECT: improved method of synthesis. 16 cl, 3 tbl</abstract><edition>6</edition><oa>free_for_read</oa></addata></record>
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subjects	CHEMISTRY HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEPTIDES PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title	PEPTIDES, METHOD OF THEIR SYNTHESIS, AGENT SHOWING BRADYKININ-ANTAGONISTIC ACTIVITY
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