RU97107089A - POLYEPEPTIDE COMPOUNDS CONTAINING D-2-ALKYLTRIPTOPHANE, STIMULATING THE RELEASE OF GROWTH HORMONE - Google Patents

POLYEPEPTIDE COMPOUNDS CONTAINING D-2-ALKYLTRIPTOPHANE, STIMULATING THE RELEASE OF GROWTH HORMONE

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Publication number
RU97107089A
RU97107089A RU97107089/04A RU97107089A RU97107089A RU 97107089 A RU97107089 A RU 97107089A RU 97107089/04 A RU97107089/04 A RU 97107089/04A RU 97107089 A RU97107089 A RU 97107089A RU 97107089 A RU97107089 A RU 97107089A
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RU
Russia
Prior art keywords
mrp
phe
lysnh
trp
ala
Prior art date
Application number
RU97107089/04A
Other languages
Russian (ru)
Other versions
RU2157378C2 (en
Inventor
Дегенги Романо
Original Assignee
Дегенги Романо
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from ITMI941954A external-priority patent/IT1270021B/en
Priority claimed from IT95MI001293A external-priority patent/IT1276734B1/en
Application filed by Дегенги Романо filed Critical Дегенги Романо
Publication of RU97107089A publication Critical patent/RU97107089A/en
Application granted granted Critical
Publication of RU2157378C2 publication Critical patent/RU2157378C2/en

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Claims (1)

1. Пептид, имеющий формулу
A-D-Mrp(Ala)n-B-C
в которой A представляет любую природную L-аминокислоту или ее D-изомер, при условии, что A не является His, если B представляет Trp, и C представляет D-Lys-NH2; или A представляет имидазолацетил, изонипекотил, 4-аминобутирил, 4-(аминометил)циклогексанкарбонил, Glu-Tyr-Ala-His, Tyr-Ala-His, Tyr-His, D-Thr-His, D относится к декстроизомеру, Mrp представляет собой 2-(C1-C3-алкил)триптофан; n представляет 0 или 1; B является L- или D-Trp, Phe или D-β-Nal; C представляет собой NH2; D-Trp-Lys-NH2; D-Phe-LysNH2, Phe-LysNH2, D-Phe-Lys-ThrNH2, D-Phe-Lys-D-ThrNH2, OR, в которой R представляет алкильную группу C1-C3 и аддитивные соли фармацевтически приемлемых органических или неорганических кислот любого из указанных полипептидов.1. The peptide having the formula
AD-Mrp (Ala) n -BC
in which A represents any natural L-amino acid or its D-isomer, provided that A is not His if B is Trp and C is D-Lys-NH 2 ; or A represents imidazole acetyl, isonipecotyl, 4-aminobutyryl, 4- (aminomethyl) cyclohexanecarbonyl, Glu-Tyr-Ala-His, Tyr-Ala-His, Tyr-His, D-Thr-His, D refers to the dextroisomer, Mrp represents 2- (C 1 -C 3 -alkyl) tryptophan; n represents 0 or 1; B is L- or D-Trp, Phe or D-β-Nal; C represents NH 2 ; D-Trp-Lys-NH 2 ; D-Phe-LysNH 2 , Phe-LysNH 2 , D-Phe-Lys-ThrNH 2 , D-Phe-Lys-D-ThrNH 2 , OR, in which R represents a C 1 -C 3 alkyl group and pharmaceutically acceptable addition salts organic or inorganic acids of any of these polypeptides. 2. Пептид по п. 1, в котором Mrp выбирают из 2-метилтриптофана, 2-этилтриптофана, 2-пропилтриптофана, 2-изопропилтриптофана. 2. The peptide according to claim 1, wherein Mrp is selected from 2-methyltryptophan, 2-ethyltryptophan, 2-propyltryptophan, 2-isopropyltryptophan. 3. Пептид по п. 1, в котором Mrp представляет 2-метилтриптофан. 3. The peptide of claim 1, wherein Mrp is 2-methyltryptophan. 4. Пептид по п.1, в котором A представляет имидазолацетил, изонипекотил, 4-аминобутирил, D-Ala, D-Thr, Tyr. 4. The peptide according to claim 1, in which A is imidazole acetyl, isonipecotyl, 4-aminobutyryl, D-Ala, D-Thr, Tyr. 5. Пептид по п. 1, в котором C представляет Phe-LysNH2, D-Trp-LysNH2, NH2, или, в котором R представляет алкильную группу C1-C3.5. The peptide according to claim 1, in which C represents Phe-LysNH 2 , D-Trp-LysNH 2 , NH 2 , or, in which R represents an alkyl group C 1 -C 3 . 6. Пептид по п. 1, выбранный из группы, включающей в себя:
IMA-D-Mrp-D-Trp-Phe-LysNH2;
IMA-D-Mrp-D-β-Nal-Phe-LysNH2;
INIP-D-Mrp-D-Trp-Phe-LysNH2;
INIP-D-Mrp-D-β-Nal-Phe-LysNH2;
GAB-D-Mrp-D-Trp-Phe-LysNH2;
GAB-D-Mrp-D-β-Nal-Phe-LysNH2;
GAB-D-Mrp-D-β-Nal-NH2;
GAB-D-Mrp-D-β-Nal-OC2H5;
4-(аминометил)циклогексанкарбонил-D-Mrp-D-Trp-Phe-Lys-NH2;
4-(аминометил)циклогексанкарбонил-D-Mrp-D-β-Nal-Phe-LysNH2;
7. Пептид по п. 1, выбранный из группы, включающей:
Имидазолацетил-D-Mrp-Ala-Trp-D-Phe-LysNH2;
D-Ala-D-Mrp-Ala-Trp-D-Phe-LysNH2;
D-Thr-D-Mrp-Ala-Trp-D-Phe-LysNH2;
His-D-Mrp-Ala-TrpNH2;
D-Thr-D-Mrp-Ala-TrpNH2;
His-D-Mrp-Ala-Phe-D-Trp-LysNH2;
D-Thr-D-Mrp-Ala-Trp-D-Phe-Lys-D-ThrNH2;
D-Thr-His-D-Mrp-Ala-Trp-D-Phe-LysNH2;
His-D-Mrp-Ala-Trp-D-Phe-Lys-ThrNH2;
His-D-Mrp-Ala-Trp-D-Phe-Lys-D-ThrNH2;
8. Пептид по п.6 или 7, в котором Mrp представляет 2-метилтриптофан.6. The peptide according to claim 1, selected from the group including:
IMA-D-Mrp-D-Trp-Phe-LysNH 2 ;
IMA-D-Mrp-D-β-Nal-Phe-LysNH 2 ;
INIP-D-Mrp-D-Trp-Phe-LysNH 2 ;
INIP-D-Mrp-D-β-Nal-Phe-LysNH 2 ;
GAB-D-Mrp-D-Trp-Phe-LysNH 2 ;
GAB-D-Mrp-D-β-Nal-Phe-LysNH 2 ;
GAB-D-Mrp-D-β-Nal-NH 2 ;
GAB-D-Mrp-D-β-Nal-OC 2 H 5 ;
4- (aminomethyl) cyclohexanecarbonyl-D-Mrp-D-Trp-Phe-Lys-NH 2 ;
4- (aminomethyl) cyclohexanecarbonyl-D-Mrp-D-β-Nal-Phe-LysNH 2 ;
7. The peptide according to claim 1, selected from the group including:
Imidazoleacetyl-D-Mrp-Ala-Trp-D-Phe-LysNH 2 ;
D-Ala-D-Mrp-Ala-Trp-D-Phe-LysNH 2 ;
D-Thr-D-Mrp-Ala-Trp-D-Phe-LysNH 2 ;
His-D-Mrp-Ala-TrpNH 2 ;
D-Thr-D-Mrp-Ala-TrpNH 2 ;
His-D-Mrp-Ala-Phe-D-Trp-LysNH 2 ;
D-Thr-D-Mrp-Ala-Trp-D-Phe-Lys-D-ThrNH 2 ;
D-Thr-His-D-Mrp-Ala-Trp-D-Phe-LysNH 2 ;
His-D-Mrp-Ala-Trp-D-Phe-Lys-ThrNH 2 ;
His-D-Mrp-Ala-Trp-D-Phe-Lys-D-ThrNH 2 ;
8. The peptide according to claim 6 or 7, in which Mrp is 2-methyltryptophan. 9. Применение пептидов по пп. 1-8 для получения лекарственного средства, стимулирующего высвобождение ростового гормона у животных
10. Применение по п. 9, в котором данный медикамент пригоден для лечения человека.9. The use of peptides in paragraphs. 1-8 to obtain a drug that stimulates the release of growth hormone in animals
10. The use of claim 9, wherein the medicament is suitable for treating a person. 11. Применение пептидов из п. 7 для получения лекарственного средства, стимулирующего повышение внутриклеточной активности аденилциклазы. 11. The use of the peptides of claim 7 for the manufacture of a medicament that stimulates an increase in the intracellular activity of adenylcyclase. 12. Фармацевтические композиции, включающие эффективное количество по крайней мере пептида по пп. 1-8, в качестве активного ингредиента, необязательно в смеси с носителями и наполнителями. 12. Pharmaceutical compositions comprising an effective amount of at least a peptide according to claims. 1-8, as an active ingredient, optionally in a mixture with carriers and excipients. 13. Композиции по п. 12 в форме для парентерального, интраназального, орального введения, с контролируемым высвобождением, для подкожного имплантирования. 13. The composition according to p. 12 in the form for parenteral, intranasal, oral administration, with controlled release, for subcutaneous implantation.
RU97107089/04A 1994-09-27 1995-09-13 Polypeptide compounds containing d-2-alkyltryptophan that stimulates growth hormone release RU2157378C2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
ITMI941954A IT1270021B (en) 1994-09-27 1994-09-27 Polypeptide compounds containing D-2-methyltryptophan having activity increasing intracellular cAMP
ITMI94A001954 1994-09-27
ITMI95A001293 1995-06-16
IT95MI001293A IT1276734B1 (en) 1995-06-16 1995-06-16 Polypeptide compounds containing D-2-alkyl tryptophane capable of promoting the release of growth hormone

Publications (2)

Publication Number Publication Date
RU97107089A true RU97107089A (en) 1999-05-20
RU2157378C2 RU2157378C2 (en) 2000-10-10

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US (1) US5795957A (en)
EP (1) EP0783521B8 (en)
JP (1) JP3810083B2 (en)
KR (1) KR100369105B1 (en)
CN (1) CN1121413C (en)
AT (1) ATE225806T1 (en)
AU (1) AU700066B2 (en)
CA (1) CA2201122A1 (en)
CZ (1) CZ291798B6 (en)
DE (1) DE69528531T2 (en)
DK (1) DK0783521T3 (en)
ES (1) ES2186730T3 (en)
HK (1) HK1001207A1 (en)
HU (1) HU221481B (en)
IL (1) IL115381A (en)
MX (1) MX9702275A (en)
PL (1) PL181588B1 (en)
PT (1) PT783521E (en)
RU (1) RU2157378C2 (en)
SK (1) SK284550B6 (en)
WO (1) WO1996010040A1 (en)

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