AR009422A1 - ANALOGS PEPTIDES LH-RH, THEIR EMPLOYMENT AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT - Google Patents

ANALOGS PEPTIDES LH-RH, THEIR EMPLOYMENT AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT

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Publication number
AR009422A1
AR009422A1 ARP970105288A AR009422A1 AR 009422 A1 AR009422 A1 AR 009422A1 AR P970105288 A ARP970105288 A AR P970105288A AR 009422 A1 AR009422 A1 AR 009422A1
Authority
AR
Argentina
Prior art keywords
amino acid
alkyl
substituted
pharmaceutical compositions
peptide
Prior art date
Application number
Other languages
Spanish (es)
Original Assignee
Theramex
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
Application filed by Theramex filed Critical Theramex
Publication of AR009422A1 publication Critical patent/AR009422A1/en

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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Análogos péptidos LH-RH con excelente afinidad con los receptores LH-RH, de la formula: V-W-X-SPL-Y-Pro-Z donde:*V es un péptido A1A2 donde: -A1 espGlu, Acsar o un D-aminoácido aromático y -A2 es un enlace directo, His, DFen, DpFFen o DpClFen; *W es un L- o D-aminoácido aromático; *X es eldipéptido A3A4 donde: -A3 es Ala, Thr, Ser, Dser, Ser(OBzl) o MeSer y -A4 es Tir, Fen, cPzACAIa, L- o D-PicLis, L- o D-NicLis o L- o D-IprLis; *SPL es elespirolactama de formula (I), *Y es el dipéptido A5A6 donde -A5 es un aminoácido con una cadena lateral (C1-C8)alquil o (C3-C6)cicloalquil y -A6es L- o D-(Arg, HArg, Lis, Hlis, Orn, Cit. HCit o Aph), donde L- o D-(Arg y Harg) pueden substituirse por uno o dos grupos (C1-C4)alquily L- o D-(Lis,Hlis, Orn, y Aph) pueden substituirse por un grupo isopropil, nocotinoil o picolinoil; y *Z es GliNH2, DalaNH2, AzaGliNH2 o -NHR1 donde R1 es un(C1-C4)alquil opcionalmente sustituido por un hidroxi o uno o más átomos de fluor,(C3-C6)cicloalquil o un radical heterocíclico seleccionado entremorfolinil, pirrolidinil y piperidil, y las sales farmacéuticamente aceptables de los mismos. Empleo de dichos análogos péptidos y composicionesfarmacéuticas que los contienen.LH-RH peptide analogs with excellent affinity for LH-RH receptors, of the formula: VWX-SPL-Y-Pro-Z where: * V is an A1A2 peptide where: -A1 espGlu, Acsar or an aromatic D-amino acid and -A2 is a direct bond, His, DFen, DpFFen or DpClFen; * W is an aromatic L- or D-amino acid; * X is the A3A4 dipeptide where: -A3 is Ala, Thr, Ser, Dser, Ser (OBzl) or MeSer and -A4 is Tir, Fen, cPzACAIa, L- or D-PicLis, L- or D-NicLis or L- or D-IprLis; * SPL is the spirolactam of formula (I), * Y is the A5A6 dipeptide where -A5 is an amino acid with a (C1-C8) alkyl or (C3-C6) cycloalkyl side chain and -A6 is L- or D- (Arg, HArg, Lis, Hlis, Orn, Cit. HCit or Aph), where L- or D- (Arg and Harg) can be substituted by one or two groups (C1-C4) alkyl and L- or D- (Lis, Hlis, Orn , and Aph) can be substituted by an isopropyl, nocotinoyl or picolinoyl group; and * Z is GliNH2, DalaNH2, AzaGliNH2 or -NHR1 where R1 is a (C1-C4) alkyl optionally substituted by a hydroxy or one or more fluorine atoms, (C3-C6) cycloalkyl or a heterocyclic radical selected from morpholinyl, pyrrolidinyl and piperidil, and the pharmaceutically acceptable salts thereof. Use of said peptide analogues and pharmaceutical compositions containing them.

ARP970105288 1996-11-14 1997-11-13 ANALOGS PEPTIDES LH-RH, THEIR EMPLOYMENT AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT AR009422A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP96404418 1996-11-14

Publications (1)

Publication Number Publication Date
AR009422A1 true AR009422A1 (en) 2000-04-12

Family

ID=45724553

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP970105288 AR009422A1 (en) 1996-11-14 1997-11-13 ANALOGS PEPTIDES LH-RH, THEIR EMPLOYMENT AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT

Country Status (1)

Country Link
AR (1) AR009422A1 (en)

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