AR065948A1 - Antagonistas del receptor de la hormona liberadora de gonadotropina y procedimientos relacionados con los mismos - Google Patents

Antagonistas del receptor de la hormona liberadora de gonadotropina y procedimientos relacionados con los mismos

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Publication number
AR065948A1
AR065948A1 ARP080101411A ARP080101411A AR065948A1 AR 065948 A1 AR065948 A1 AR 065948A1 AR P080101411 A ARP080101411 A AR P080101411A AR P080101411 A ARP080101411 A AR P080101411A AR 065948 A1 AR065948 A1 AR 065948A1
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AR
Argentina
Prior art keywords
alkyl
independently
substituted
case
heterocycle
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ARP080101411A
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English (en)
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Neurocrine Biosciences Inc
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Application filed by Neurocrine Biosciences Inc filed Critical Neurocrine Biosciences Inc
Publication of AR065948A1 publication Critical patent/AR065948A1/es

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    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Quinoline Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Se describen antagonistas del receptor GnRH que tienen utilidad en el tratamiento de una diversidad de afecciones relacionadas con las hormonas sexuales tanto en hombres como en mujeres. También se describen composiciones que contienen un compuestode esta invencion junto con un vehículo farmacéuticamente aceptable, así como procedimientos para el uso de los mismos para antagonizar la hormona liberadora de gonadotropina en un sujeto que lo necesita. Reivindicacion 1: Un compuesto que tiene lasiguiente estructura (1) y estereoisomeros, ésteres, solvatos y sales farmacéuticamente aceptables del mismo, en la que: A es piridilo, fenilo, quinolinilo, naftiridinilo, tienopirimidinilo o 2-oxo-pirimidinilo, donde el piridilo, fenilo,quinolinilo, tienopirimidinilo o 2-oxo-pirimidinilo están sustituidos con 0-5 R4; R1a es H, halogeno, alquilo C1-4, alcoxi o trifluorometilo; R1b R1c son iguales o diferentes y son independientemente H, halogeno, hidroxi, haloalquilo C1-4, -alquilC1-6-(R5)p, -O-alquil C1-6-(R5)p, alquil C1-6-O-alquil C1-6-(R5)p, -NR7-alquil C1-6-(R5)p o -S(O)m-alquil C1-6-(R5)p; R1d es Cl, F, metilo, CF3 o ciano; R2 es -alquil C1-4-(R5)p; R2a es fenilo sustituido con 0-4 R3, heteroarilo sustituido con 0-4R3, alquilo C1-6 sustituido con 0-4 R3, aril-alquilo C1-4 sustituido con 0-4 R3, o heteroaril-alquilo C1-4 sustituido con 0-4 R3; R3 es, independientemente en cada caso, halogeno, ciano, halo-alquilo C1-4, R5, -alquil C1-6-(R5)p, -alquil C1-6-O-alquil C1-6-(R5)p, -O-alquil C1-6-(R5)p, -NR7-alquil C1-6-(R5)p, -S(O)m-alquil C1-6-(R5)p, -O-alquil C1-6-NR7-alquil C1-6-(R5)p, heterociclo-(R5)p; R4 es, independientemente en cada caso, halogeno, alquilo C1-6, haloalquilo C1-4, alcoxi C1-6,hidroxi, ciano, tioalquilo C1-6, -C(O)NR7R8 o heteroarilo de 5 miembros; R5 es independientemente en cada caso, H, hidroxi, -OC(O)-alquilo C1-6, -OC(O)O-alquilo C1-6, -OC(O)-alquil C1-6-NR7R8, -COOR6, -C(O)NR7R8, -NR7C(O)NR7R8, -S(O)2NR9R9, -S(O)m-alquilo C1-4, -NR7R8, alcoxi C1-6, -O-heterociclo, o heterociclo donde dicho heterociclo y dicho -O-heterociclo están sustituidos con 0-4 grupos seleccionados enter haoleno, alquilo C1-6, haloalquilo C1-4, hidroxi, oxo, tio, -NH2, -S(O)2-alquilo C1-4 y -COOH; R6 es, independientemente en cada caso, H, alquilo C1-4, alquil C1-4-O-C(O)-alquilo C1-6 o alquil C1-4-O-C(O)-O-alquilo C1-6; R7 es, independientemente en cada caso, H, alquilo C1-4, hidroxi o heterociclo donde dicho heterociclo estásustituido con 0-4 grupos seleccionados entre halogeno, alquilo C1-6, hidroxi, ceto, -NH2 y -COOH; R8 es, independientemente en cada caso, H, alquilo C1-4, haloalquilo C1-4, -C(O)-alquilo C1-4, -C(O)-haloalquilo C1-4, -S(O)m-haloalquilo C1-4 o -S(O)m-alquilo C1-4; R9 es, independientemente en cada caso, H, alquilo C1-4 o -C(O)alquilo C1-4; m es 0-2; y p es, independientemente en cada caso, 1-3.
ARP080101411A 2007-04-06 2008-04-04 Antagonistas del receptor de la hormona liberadora de gonadotropina y procedimientos relacionados con los mismos AR065948A1 (es)

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