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 PRESENTInfo
- 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
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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.
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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1997
- 1997-11-13 AR ARP970105288 patent/AR009422A1/en unknown
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |