AR043434A1 - Derivados de piperizacina acilados como agonistas del receptor de melanocortina-4. composiciones farmaceuticas y usos - Google Patents

Derivados de piperizacina acilados como agonistas del receptor de melanocortina-4. composiciones farmaceuticas y usos

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Publication number
AR043434A1
AR043434A1 ARP040100637A ARP040100637A AR043434A1 AR 043434 A1 AR043434 A1 AR 043434A1 AR P040100637 A ARP040100637 A AR P040100637A AR P040100637 A ARP040100637 A AR P040100637A AR 043434 A1 AR043434 A1 AR 043434A1
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AR
Argentina
Prior art keywords
independently selected
alkyl
substituted
unsubstituted
halogen
Prior art date
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ARP040100637A
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English (en)
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Merck & Co Inc
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Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR043434A1 publication Critical patent/AR043434A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Ciertos derivados de piperazina N-acilados son agonistas del receptor o receptores de melanocortina, en particular, son agonistas selectivos del receptor de melanocortina-4 humano (MC-4R). Por lo tanto, son útiles para el tratamiento, control o prevención de la diabetes y enfermedades sensibles a la activación de MC-4R, tales como obesidad, diabetes, disfunción sexual, incluyendo disfunción eréctil y disfunción sexual femenina. Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable de los mismos; donde X se selecciona entre el grupo compuesto por (1) -(CH2)n-fenilo, y (2) -(CH2)nC(R5)(R6)(R7), donde el fenilo esta no sustituido o sustituido con de una a tres grupos seleccionados independientemente entre R3 y donde cualquier metileno (CH2) en X está no sustituido o sustituido con de uno a dos grupos seleccionados independientemente entre halógeno, hidroxi y alquilo C1-4; R1 es alquilo C1-6; R2 es fenilo opcionalmente sustituido con uno a tres grupos seleccionados independientemente entre R3; cada R3 se selecciona independientemente entre el grupo compuesto por (1) alquilo C1-8; (2) halógeno, (3) -(CH2)n-heteroarilo, (4) -(CH2)nC(O)R9, (5) -(CH2)nC(O)OR9, y (6) -(CH2)nNR9C(O)R9, donde el heteroarilo está no sustituido o sustituido con uno a tres sustituyentes seleccionados independientemente entre halógeno, hidroxi, alquilo C1-4, trifluorometilo y alcoxi C1-4 y donde cualquier alquilo y átomo de C del metileno (CH2) en R3 está no sustituido o sustituido con uno a dos grupos seleccionados independientemente entre halógeno, hidroxi, oxo, alquilo C1-4, trifluorometilo y alcoxi C1-4, o dos sustituyentes R3 sobre el mismo átomo de C se toman junto con el átomo de C para formar un grupo ciclopropilo; R5 se selecciona independientemente entre el grupo compuesto por (1) -(CH2)n-cicloalquilo C3-7, y (2) -(CH2)n-fenilo, donde el fenilo está no sustituido o sustituido con uno a tres grupos seleccionados independientemente entre R3 y el cicloalquilo está no sustituido o sustituido con uno a tres grupos seleccionados independientemente entre R3 y oxo y donde cualquier metileno (CH2) en R5 está no sustituido o sustituido con uno a dos grupos seleccionados independientemente entre halógeno, hidroxi y alquilo C1-4; R4 y R6 son H; R7 se selecciona entre el grupo compuesto por (1) -(CH2)nN(R8)2, (2) -(CH2)nNR8C(O)R8, y (3) -(CH2)nNR8S(O)2R8, donde cualquier metileno (CH2) en R7 está no sustituido o sustituido con uno a dos grupos seleccionados independientemente entre halógeno, hidroxi y alquilo C1-4, o dos sustituyentes R8 junto con el átomo de C, N o S al que están unidos forman un anillo de 5, 6, o 7miembros saturado o insaturado que contiene N opcionalmente sustituido con uno a tres grupos seleccionados independientemente entre alquilo C1-8 y oxo; cada R8 se selecciona independientemente entre el grupo compuesto por (1) H, y (2) alquilo C1-8, cada R9 se selecciona independientemente entre el grupo compuesto por (1) H, (2) alquilo C1-8, y (3) cicloalquilo C3-6, donde el alquilo y el cicloalquilo están no sustituidos o sustituidos con uno a tres grupos seleccionados independientemente entre halógeno, alquilo C1-4, hidroxi y alcoxi C1-4, o dos grupos R9 junto con el átomo al que están unidos forman un sistema de anillo mono- o bicíclico de 4 a 8 miembros que contiene opcionalmente un heteroátomo adicional seleccionado entre O, S y N-alquilo C1-4; m es 0; n es 0, 1, 2, 3, o 4; r es 1 o 2; y s es 1.
ARP040100637A 2003-03-03 2004-02-27 Derivados de piperizacina acilados como agonistas del receptor de melanocortina-4. composiciones farmaceuticas y usos AR043434A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US45150203P 2003-03-03 2003-03-03
US51594303P 2003-10-30 2003-10-30

Publications (1)

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AR043434A1 true AR043434A1 (es) 2005-07-27

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Country Status (5)

Country Link
US (1) US7160886B2 (es)
AR (1) AR043434A1 (es)
PE (1) PE20040960A1 (es)
TW (1) TW200508223A (es)
WO (2) WO2004078716A1 (es)

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PE20040960A1 (es) 2004-12-14
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