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AR044824A1 - Agonistas del receptor de melanocortina 4 (mc4), composicion farmaceutica y sus usos - Google Patents

Agonistas del receptor de melanocortina 4 (mc4), composicion farmaceutica y sus usos

Info

Publication number
AR044824A1
AR044824A1 ARP040102134A ARP040102134A AR044824A1 AR 044824 A1 AR044824 A1 AR 044824A1 AR P040102134 A ARP040102134 A AR P040102134A AR P040102134 A ARP040102134 A AR P040102134A AR 044824 A1 AR044824 A1 AR 044824A1
Authority
AR
Argentina
Prior art keywords
tyr
arg
ser
pro
phenyl
Prior art date
Application number
ARP040102134A
Other languages
English (en)
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of AR044824A1 publication Critical patent/AR044824A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/665Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
    • C07K14/68Melanocyte-stimulating hormone [MSH]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones

Landscapes

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

Abstract

La presente se refiere a agonistas del receptor MC4 y, como tales, son de utilidad en el tratamiento de trastornos que responden a la activación de este receptor, tales como obesidad, diabetes mellitus y disfunción sexual masculina y/o femenina. Reivindicación 1: Un compuesto de la fórmula (1) y sus sales farmacéuticamente aceptables, en el que W es Glu, Gln, Asp, Asn, Ala, Gly, Thr, Ser, Pro, Met, Ile, Val, Arg, His, Tyr, Trp, Phe, Lys, Leu, Cya o está ausente; R1 es -H, -C(O)CH3, -C(O)(CH2)1-4CH3, -C(O)(CH2)1-4NHC(NH)NH2, Tyr-betaArg-, Ac-Tyr-beta-hArg-, gluconoil-Tyr-Arg-, Ac-diaminobutiril-, Ac-diaminopropionil-, N-propionil-, N-butiril-, N-valeril-, N-metil-Tyr-Arg-, N-glutaril-Tyr-Arg-, N-succinil-Tyr-Arg-, R6-SO2-NHC(O)CH2CH2C(O)-, R6-SO2NHC(O)CH2CH2C(O)Arg-, R6-SO2NHCH2CH2CH2C(O)-, (cicloalquil C3-7)carbonilo, fenilsulfonilo, arilsulfonilo bicíclico C8-14, fenil(CH2)qC(O)-, (arilo bicíclico C8-14)(CH2)qC(O)-,como se muestra en los compuesto de fórmula (2) en el que R2 es -H, -NH2, -NHC(O)CH3, -NHC(O)(CH2)1-4CH3, -NH-TyrC(O)CH3, R6SO2NH-, Ac-Cya-NH-, Tyr-NH-, HO-(C6-H5)-CH2CH2C(O)NH-, o CH3-(C6H5)-C(O)CH2CH2C(O)NH-; R3 es alquilo C1-4 lineal o ramificado, NH2-CH2-(CH2)q-, HO-CH2-(CH3)2CHNH(CH2)4-, R6(CH2)q-, R6SO2NH-, Ser, Ile, como se muestra en los restos de fórmulas (3), q es 0, 1, 2 o 3; R6 es un fenilo o un arilo bicíclico C8-14; m es 1 o 2; n es 1, 2, 3 o 4; R9 es (CH2)p o (CH3)2C-; p es 1 o 2; R10 es NH- o está ausente; R7 es un heteroarilo de 5 o 6 miembros o un anillo heteroarilo de 5 o 6 miembros opcionalmente sustituido con R4; R4 es H, alquilo C1-4 lineal o ramificado, fenilo, bencilo o (C6H5)-CH2-O-CH2-; R8 es fenilo, un anillo fenilo opcionalmente sustituido con X o ciclohexilo; X es H, Cl, F, Br, metilo o metoxi; R11 es -C(O) o -CH2; R5 es -NH2, -OH, glicinol, NH2-Pro-Ser-, NH2-Pro-Lys-, HO-Ser-, HO-Pro-Ser-, HO-Lys-, alcohol de -Ser, alcohol de -Ser-Pro, alcohol de -Lys-Pro, HOCH2CH2-O-CH2CH2NH-, NH2-Phe-Arg-, NH2-Glu-, NH2CH2RCH2NH-, RNH-, o RO- donde R es un alquilo C1-4 lineal o ramificado; y L es -S-S o -S-CH2-S-.
ARP040102134A 2003-06-19 2004-06-18 Agonistas del receptor de melanocortina 4 (mc4), composicion farmaceutica y sus usos AR044824A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US47974003P 2003-06-19 2003-06-19
US55734704P 2004-03-29 2004-03-29
US57067604P 2004-05-13 2004-05-13
US57073704P 2004-05-13 2004-05-13

Publications (1)

Publication Number Publication Date
AR044824A1 true AR044824A1 (es) 2005-10-05

Family

ID=33556652

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040102134A AR044824A1 (es) 2003-06-19 2004-06-18 Agonistas del receptor de melanocortina 4 (mc4), composicion farmaceutica y sus usos

Country Status (17)

Country Link
US (1) US20070105759A1 (es)
EP (1) EP1644023A2 (es)
JP (1) JP2006527773A (es)
KR (1) KR20060014444A (es)
AR (1) AR044824A1 (es)
AU (1) AU2004251616A1 (es)
BR (1) BRPI0410731A (es)
CA (1) CA2530024A1 (es)
CR (1) CR8159A (es)
EA (1) EA200600055A1 (es)
EC (1) ECSP056236A (es)
IL (1) IL171931A0 (es)
MX (1) MXPA05013951A (es)
NO (1) NO20060259L (es)
PE (1) PE20050284A1 (es)
TW (1) TW200514791A (es)
WO (1) WO2005000339A2 (es)

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EP1658273B1 (en) 2003-08-20 2007-01-03 Eli Lilly And Company Compounds, methods and formulations for the oral delivery of a glucagon like peptide (glp)-1 compound or an melanocortin 4 receptor (mc4) agonist peptide
WO2006073772A1 (en) * 2005-01-05 2006-07-13 Eli Lilly And Company Polyethylene glycol linked mc4r or mc3r agonist peptides
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Also Published As

Publication number Publication date
IL171931A0 (en) 2006-04-10
BRPI0410731A (pt) 2006-06-20
US20070105759A1 (en) 2007-05-10
ECSP056236A (es) 2006-04-19
AU2004251616A1 (en) 2005-01-06
TW200514791A (en) 2005-05-01
EP1644023A2 (en) 2006-04-12
MXPA05013951A (es) 2006-02-24
NO20060259L (no) 2006-03-14
WO2005000339A2 (en) 2005-01-06
CR8159A (es) 2006-02-09
CA2530024A1 (en) 2005-01-06
JP2006527773A (ja) 2006-12-07
WO2005000339A8 (en) 2005-04-21
EA200600055A1 (ru) 2006-08-25
WO2005000339A3 (en) 2005-02-03
PE20050284A1 (es) 2005-05-20
KR20060014444A (ko) 2006-02-15

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