AR034407A1 - Peptidos lineales selectivos con actividad agonista de receptor de melanocortina-4 (mc4-r) - Google Patents

Peptidos lineales selectivos con actividad agonista de receptor de melanocortina-4 (mc4-r)

Info

Publication number
AR034407A1
AR034407A1 ARP010101552A ARP010101552A AR034407A1 AR 034407 A1 AR034407 A1 AR 034407A1 AR P010101552 A ARP010101552 A AR P010101552A AR P010101552 A ARP010101552 A AR P010101552A AR 034407 A1 AR034407 A1 AR 034407A1
Authority
AR
Argentina
Prior art keywords
hydrogen
formula
branched
linear
compound
Prior art date
Application number
ARP010101552A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR034407A1 publication Critical patent/AR034407A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/665—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
    • C07K14/68—Melanocyte-stimulating hormone [MSH]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Endocrinology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Obesity (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Un compuesto de comprende la estructura de fórmula (1), en donde R1, R6, R7, R8, m, n, A y B son como se definen en (a) a (d), y en donde el compuesto se selecciona entre el grupo que consiste de: a) un compuesto de la fórmula (2) en donde: m es 0 ó 1; n es 0 ó 1; R1 es alquilo C1-8 lineal o ramificado, insustituido o monosustituido con fenilo o carboxilo, fenilo insustituido o monosustituido con flúor, cloro o alquilo C1-4 lineal o ramificado; X es un resto de fórmula (6), (7) u (8) en donde R2, R3 y R4 son independientemente hidrógeno o un alcoxi C1-4 lineal o ramificado, en donde cuando R3 es alcoxi, R2 y R4 son ambos hidrógeno; R9 es hidrógeno, alquilo C1-3 lineal o ramificado, alcoxi C1-3 lineal o ramificado o fenoxi insustituido; R11 es ciclohexilo, cicloheptilo, o un alquilo C3-8 ramificado; R6 es hidrógeno o metilo; R7 es un compuesto de fórmula (9), (11) u (11); Y es -CH2-, -CH2CH2-, ó >CH-CH3, y R8 es hidrógeno o metilo; o Y es un compuesto de fórmula (12), (13) ó (14) y R8 es hidrógeno; b) un compuesto de la fórmula (3) en donde: m, n y R1 son como se definen en (a); R2, R3 y R4 son independientemente hidrógeno, un alquilo C1-4 lineal o ramificado, hidroxi, alcoxi C1-4 lineal o ramificado, o cloro, en donde cuando R3 es alquilo, hidroxi, alcoxi o cloro, R2 y R4 son ambos hidrógeno; R6 es hidrógeno o metilo; R7 es un resto de fórmula (9) ó (10); Y es -CH2-, -CH2CH2-, ó >CH-CH3, y R8 es hidrógeno o metilo; o Y es un resto de fórmula (13) ó (14) y R8 es hidrógeno; c) un compuesto de la fórmula (4) en donde: m, n, R1, R7, R8 e Y son como se definen en (a); y R10 es hidrógeno, halo, alquilo C1-3 lineal o ramificado, alcoxi C1-3 lineal o ramificado, ó -NR12R13 en donde R12 y R13 son cada uno independientemente un alquilo C1-3 lienal o ramificado, o juntos son -(CH2)q- en donde q es 3, 4 ó 5; y d) un compuesto de la fórmula (5) en donde: R1 es alquilo C4-8 lineal o ramificado insustituido; R6 es hidrógeno o metilo; R8 es hidrógeno o metilo; p es 2, 3 ó 4 y R14 es un resto de fórmula (15), o p es 4 y R14 es un resto de fórmula (16), o p es 3 y R14 es un resto de fórmula (17). El uso de compuestos de acuerdo con la presente, para la preparación de medicamentos para el tratamiento y/o profilaxis de enfermedades que están asociadas con el receptor de melanocortina-4, tal como obesidad. Dichos compuestos activan selectivamente la actividad del receptor de melanocortina-4 (MC-4).
ARP010101552A 2000-04-04 2001-03-30 Peptidos lineales selectivos con actividad agonista de receptor de melanocortina-4 (mc4-r) AR034407A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US19445000P 2000-04-04 2000-04-04

Publications (1)

Publication Number Publication Date
AR034407A1 true AR034407A1 (es) 2004-02-25

Family

ID=22717646

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010101552A AR034407A1 (es) 2000-04-04 2001-03-30 Peptidos lineales selectivos con actividad agonista de receptor de melanocortina-4 (mc4-r)

Country Status (9)

Country Link
US (4) US6600015B2 (es)
EP (1) EP1272516B1 (es)
JP (1) JP3938690B2 (es)
AR (1) AR034407A1 (es)
AU (1) AU2001250407A1 (es)
CA (1) CA2402416A1 (es)
DE (1) DE60133730T2 (es)
ES (1) ES2304128T3 (es)
WO (1) WO2001074844A2 (es)

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Also Published As

Publication number Publication date
US6600015B2 (en) 2003-07-29
JP2003529607A (ja) 2003-10-07
ES2304128T3 (es) 2008-09-16
US20080177036A1 (en) 2008-07-24
US20030229200A1 (en) 2003-12-11
EP1272516A2 (en) 2003-01-08
DE60133730T2 (de) 2009-07-02
US20050239711A1 (en) 2005-10-27
US20010056179A1 (en) 2001-12-27
DE60133730D1 (de) 2008-06-05
WO2001074844A2 (en) 2001-10-11
CA2402416A1 (en) 2001-10-11
EP1272516B1 (en) 2008-04-23
WO2001074844A3 (en) 2002-06-13
JP3938690B2 (ja) 2007-06-27
AU2001250407A1 (en) 2001-10-15

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