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AR056879A1 - Antagonistas del receptor 3 de la histamina - Google Patents

Antagonistas del receptor 3 de la histamina

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Publication number
AR056879A1
AR056879A1 ARP060104658A ARP060104658A AR056879A1 AR 056879 A1 AR056879 A1 AR 056879A1 AR P060104658 A ARP060104658 A AR P060104658A AR P060104658 A ARP060104658 A AR P060104658A AR 056879 A1 AR056879 A1 AR 056879A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
alkyls
group
halogens
Prior art date
Application number
ARP060104658A
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English (en)
Original Assignee
Pfizer Prod Inc
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Filing date
Publication date
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of AR056879A1 publication Critical patent/AR056879A1/es

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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
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    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/58—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Neurosurgery (AREA)
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  • Heart & Thoracic Surgery (AREA)
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  • Pain & Pain Management (AREA)
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  • Hematology (AREA)
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  • Immunology (AREA)
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  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Una composicion farmacéutica que contiene el compuesto de formula (1), para tratar un trastorno o enfermedad seleccionado del grupo que consiste en depresion, trastornos del humor, esquizofrenia, trastornos de ansiedad, enfermedad de Alzheimer, trastorno de hiperactividad con déficit de atencion (ADHD), trastornos psicoticos, trastornos cognitivos, trastornos del sueno, obesidad, vértigo, epilepsia, mareo, enfermedades respiratorias, alergias, reacciones de las vías respiratorias inducidas por alergia, rinitis alérgica, congestion nasal, congestion alérgica, congestion, hipotension, dolencias cardiovasculares, enfermedades del tracto gastrointestinal, hiper e hipo motilidad y secrecion ácida del tracto gastrointestinal. Reivindicacion 1: Un compuesto de formula (1), o una de sus sales farmacéuticamente aceptables, en la que R1 y R2 se seleccionan independientemente cada uno del grupo que consiste en hidrogeno; alquilo C1-8 opcionalmente sustituido con de 1 a 4 halogenos; un grupo alquilo C1-4 opcionalmente sustituido con un sustituyente seleccionado del grupo que consiste en OH, de uno a cuatro alquilos C1-4, cicloalquilo C3-7, dialquilamino C1-4, arilo C6-14 opcionalmente sustituido con un halogeno y opcionalmente sustituido con ariloxi C6-10 opcionalmente sustituido con de uno a dos halogenos, y heteroarilo de 5-10 miembros opcionalmente sustituido con un grupo arilo C6-10 y opcionalmente sustituido con de uno a tres grupos alquilo C2-4; cicloalquilo C3-7; arilo C6-14; -alquil C0-3-O-alquilo C1-3 opcionalmente sustituido con alquilo C1-3; -alquil C1-3-C(=O)O-alquilo C1-3; heterocicloalquilo de 3-8 miembros opcionalmente sustituido con uno o más grupos alquil-carbonilo C1-4; arilsulfonilo C6-19 opcionalmente sustituido con uno o más alquilos C1-2; heteroarilo de 5-10 miembros; y aril C6-14-alquilen C0-4-O-alquilo C0-4, en el que cada alquilo C0-4 y cada alquileno C0-4 están opcionalmente sustituidos con de uno a cuatro alquilos C1-4; u opcionalmente R1 y R2, junto con el nitrogeno al que están unidos, forman un anillo alifático saturado o insaturado de 4, 5, 6, o 7 miembros, en el que uno de los carbonos en dicho anillo alifático está opcionalmente reemplazado por O, S, NR3, o CO, y en el que dicho anillo está opcionalmente fusionado a un arileno C6-10 y está opcionalmente sustituido en un carbono del anillo con un sustituyente seleccionado del grupo que consiste en -OH, heteroarilo de 5-10 miembros opcionalmente sustituido con uno o más halogenos y opcionalmente sustituido con uno o más alquilos C1-2, alcoxi C1-4 opcionalmente sustituido con uno o más alcoxi C1-2 y opcionalmente sustituido con uno o más dialquilaminocarbonilos C1-4, y uno o dos alquilos C1-4 opcionalmente e independientemente sustituidos con uno o más alcoxi C1-2; en la que R3 es hidrogeno; alquilo C1-8 opcionalmente sustituido con de 1 a 4 halogenos; heteroarilo de 5-10 miembros opcionalmente sustituido con un sustituyente seleccionado del grupo que consiste en halogeno, alquilo C1-4, alcoxi C1-2, arilo C5-10, alquilaminocarbonilo C1-4, y ciano; un grupo alquilo C1-4 opcionalmente sustituido con un sustituyente seleccionado del grupo que consiste en alcoxicarbonilo C1-2, heteroarilo de 5-10 miembros opcionalmente sustituido con uno o más alquilos C1-2, de uno a cuatro alquilos C1-4, cicloalquilo C3-7, y arilo C6-14; arilo C6-10 opcionalmente sustituido con uno o dos alquilos C1-2; aIquilcarbonilo C1-4; o aril C6-14-alquilen C0-4-O-alquilo C0-4, en el que cada alquilo C0-4 y cada alquileno C0-4 están opcionalmente sustituidos con de uno a cuatro alquilos; R4 se selecciona independientemente del grupo que consiste en hidrogeno, alquilo C1-4, alcoxilo C1-4, halogeno, nitrilo, -SO2-alquilo C1-4, -SO2NH-alquilo C1-4, y -C(=O)NH-alquilo C1-4; n es 0, 1, 2, 3 o 4; R5 es OH, -O-alquilo C1-3, halogeno o hidrogeno; R6 es hidrogeno, alquilo C1-4 opcionalmente sustituido con de 1 a 4 halogenos, o cicloalquil C3-7-alquilo C0-4; R7 es hidrogeno, alquilo C1-8 opcionalmente sustituido con de 1 a 4 halogenos, o cicloalquil C3-7-alquilo C0-4, en el que cada alquilo C0-4 está opcionalmente sustituido con de uno a cuatro alquilo C1-4 y; R8 es hidrogeno, alquilo C1-8 opcionalmente sustituido con de 1 a 4 halogenos, o cicloalquil C3-7-alquilo C0-4; u opcionalmente R7 y R8, junto con el nitrogeno al que están unidos, forman un anillo heterocíclico de 4, 5, 6, o 7 miembros, en el que dicho anillo heterocíclico está opcionalmente sustituido con uno o dos alquilos C1-4 y en el que uno de los carbonos de dicho anillo heterocíclico que está separado de dicho nitrogeno en dicho anillo heterocíclico por al menos dos átomos, está opcionalmente reemplazado por O, S, NR9, o C=O, en el que R9 es hidrogeno, alquilo C1-8 opcionalmente sustituido con de 1 a 4 halogenos, o cicloalquil C3-7-alquilo C0-4, y en el que cada alquilo C0-4 está opcionalmente sustituido con de uno a cuatro alquilos C1-4.
ARP060104658A 2005-10-27 2006-10-25 Antagonistas del receptor 3 de la histamina AR056879A1 (es)

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EP (1) EP1951660B1 (es)
JP (2) JP4319245B2 (es)
KR (1) KR101025358B1 (es)
CN (1) CN101296898B (es)
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