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AR040406A1 - Antagonistas de histamina h3 de benzimidazolona - Google Patents

Antagonistas de histamina h3 de benzimidazolona

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Publication number
AR040406A1
AR040406A1 AR20030101341A ARP030101341A AR040406A1 AR 040406 A1 AR040406 A1 AR 040406A1 AR 20030101341 A AR20030101341 A AR 20030101341A AR P030101341 A ARP030101341 A AR P030101341A AR 040406 A1 AR040406 A1 AR 040406A1
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AR
Argentina
Prior art keywords
alkyl
independently selected
aryl
group
alkoxy
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Application number
AR20030101341A
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English (en)
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Schering Corp
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Publication of AR040406A1 publication Critical patent/AR040406A1/es

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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

También se describen composiciones farmacéuticas que comprenden los compuestos de la fórmula (1). Asimismo se describen métodos para el tratamiento de varias enfermedades o trastornos, tales como por ejemplo la alergia, afecciones de las vías respiratorias inducidas por alergia, y congestión (por ejemplo, congestión nasal) usando los compuestos de la fórmula (1). Asimismo se describen métodos para el tratar varias enfermedades o trastornos, tales como por ejemplo la alergia, afecciones de las vías respiratorias inducidas por alergia, y congestión (por ejemplo, congestión nasal) mediante el uso de los compuestos de fórmula (1) en combinación con un antagonista de H1. Reivindicación 1: Un compuesto que está representado por la fórmula estructural (1) o una sal o solvato de los mismos farmacéuticamente aceptable, en los cuales: la línea de puntos representa un doble enlace opcional; a es 0 a 3; b es 0 a 3; n es 1, 2 o 3; p es 1, 2 o 3 con la condición de que cuando M2 es N, entonces p no es 1; r es 1, 2, o 3 con la condición de que cuando r es 2 o 3, entonces M2 es C(R3) y p es 2 o 3; A es un enlace o alquileno C1-6; M1 es C(R3) o N; M2 es C (R3) o N; Y es -C(=O)-, -C(=S)-, -(CH2)q-, -NR4C(=O)-, -C(=O)NR4-, -C(=O)CH2-, -CH2(C=O)-, -SO1-2-, -NH-C(=N-CN)- o -C(=N-CN)-NH-; con la condición de que cuando M1 es N, I no es -NR4C(=O)- o -NH-C(=N-CN)- ; y cuando M2 es N, Y no es -C(=O)NR4- o -C(=N-CN)-NH- ; q es 1 a 5, con la condición de que cuando M1 y M2 son ambos N, q no es 1; Z es un enlace, alquileno C1-6, alquenileno C1-6, -C(=O)-, -CH(CN)-, o -CH2-C(=O)NR4-; R1 es un resto seleccionado del grupo de fórmulas (2); k es 0, 1, 2, 3 o 4; k1 es 0, 1, 2 o 3; k2 es 0, 1 o 2; R es H, alquilo C1-6, hidroxialquilo C2-6-, haloalquilo C1-6-, haloalcoxi C1-6-alquilo C1-6-, R29-O-C(O)-alquilo C1-6-, alcoxi C1-6-alquilo C1-6-, N (R30)(R31)-alquilo C1-6-, alcoxi C1-6-alcoxi C1-6-alquilo C1-6-, R32-arilo, R32-arilalquilo C1-6-, R32-ariloxialquilo C1-6-, R32-heteroarilo, R32-heteroarilalquilo C1-6-, cicloalquilo C3-6, cicloalquil C3-6 alquilo C1-6-, N(R30)(R31)-C(O)-alquilo C1-6-, o heterocicloalquilalquilo C1-6-; R2 es un anillo heteroarilo de seis miembros que tiene 1 o 2 heteroátomos independientemente seleccionados entre N o N-O, siendo los átomos de anillo remanentes carbono; un anillo heteroarilo de cinco miembros que tiene 1, 2, 3 o 4 heteroátomos independientemente seleccionados entre N, O o S, siendo el resto de los anillos carbono; R32-quinolilo ; R32-arilo; heterocicloalquilo ; cicloalquilo C3-6; alquilo C1-6; hidrógeno; o de fórmulas (3), (4) y (5) donde dicho anillo heteroarilo de seis miembros o dicho anillo heteroarilo de cinco miembros está opcionalmente substituido con R6; X es CH o N; Q es un enlace o alquileno C1-6; Q1 es un enlace alquileno C1-6 o -N(R4)-; R3 es H, halógeno, alquilo C1-6, -OH o alcoxi C1-6; R4 está independientemente seleccionado del grupo que consiste en hidrógeno, alquilo C1-6, cicloalquilo C3-6, cicloalquil (C3-6)alquilo C1-6, R33-arilo, R33-arilalquilo C1-6, y R32-heteroarilo ;R5 es hidrogeno, alquilo C1-6, -C(O)R20, -C(O)2R20, -C(O)N(R20)2 o alquilo C1-6 -SO2-; o R4 y R5, conjuntamente con el nitrógeno al cual están unidos, forman un anillo azetidinilo, pirrolidinilo, piperidinilo, piperazinilo o morfolinilo; R6 representa de1 a 3 substituyentes independientemente seleccionados del grupo que consiste en -OH, halógeno, alquilo C1-6-, alcoxi C1-6, alquil C1-6tio, -CF3, -NR4R5, NO2, -CO2R4, -CON(R4)2, -CH2-NR4R5, -CN, o de fórmulas (6), (7) y (8), o 2 substituyentes R6 conjuntamente en el mismo carbono son =O; R12 está independientemente seleccionado del grupo que consiste en alquilo C1-6, hidroxi, alcoxi C1-6, o flúor, con la condición de que cuando R12 es hidroxi o flúor, entonces R12 no está unido a un carbono adyacente a un nitrógeno; o dos substituyentes R12 conjuntamente forman un puente alquilo C1 a C2 de un carbono de anillo a otro carbono de anillo no adyacente; o R12 es =O; R13 está independientemente seleccionado del grupo que consiste en alquilo C1-6, hidroxi, alcoxi C1-6, o flúor, con la condición de que cuando R13 es hidroxi o flúor entonces R13 no están unido a un carbono adyacente a un nitrógeno; o dos substituyentes R13 conjuntamente forman un puente alquilo C1 a C2 de un carbono de anillo a otro carbono de anillo no adyacente; o R13 es =O; R20 está independientemente seleccionado del grupo que consiste en hidrogeno, alquilo C1-6, o arilo, donde dicho grupo arilo está opcionalmente substituido con 1 a 3 grupos independientemente seleccionados de halógeno, -CF3, -OCF3, hidroxi, o metoxi; o cuando dos grupos R20 están presentes, dichos dos grupos R20 tomados conjuntamente con el nitrógeno al cual están unidos pueden formar un anillo heterocíclico de cinco o seis miembros; R22 es alquilo C1-6, R34-arilo o heterocicloalquilo; R24 es H, alquilo C1-6, -SO2R22 o R34-arilo; R25 está independientemente seleccionado del grupo que consiste en alquilo C1-6, -CN, -NO2, halógeno, -CF3, -OH, alcoxi C1-6, alquil C1-6-C(O)-, aril-C(O)-, N(R4)(R5)-C(O)-, N(R4)(R5)-S(O)1-2-, halo-alquilo C1-6- o halo-alcoxi C1-6-alquilo C1-6-; R29 es H, alquilo C1-6, R35-arilo o R35-arilalquilo C1-6-; R30 es H, alquilo C1-6 -, R35-arilo o R35-arilalquilo C1-6-; R31 es H, alquilo C1-6-, R35-arilo, R35-arilalquilo C1-6 -, alquilo C1-6-C(O)-, R35- aril-C(O)-, N(R4)(R5)-C(O)-, alquilo C1-6-S(O)2- o R35-aril-S(O)2-; o R30 y R31 conjuntamente son -(CH2)4-5-, -(CH2)2-O-(CH2)2- o -(CH2)2-N(R29)-(CH2)2- y forman un anillo con el nitrógeno al cual están unidos; R32 representa de 1 a 3 substituyentes independientemente seleccionados del grupo que consiste en H, -OH, halógeno, alquilo C1-6, alcoxi C1-6, -SR22, -CF3, -OCF3, -OCHF2, -NR37R38, -NO2, -CO2R37, -CON(R37)2, -S(O)2R22, -S(O)2N(R20)2, -N(R24)S(O)2R22, -CN, hidroxialquilo C1-6- y -OCH2CH2OR22; R33 representa de 1 a 3 substituyentes independientemente seleccionados del grupo que consiste en alquilo C1-6, halógeno, -CN, -NO2, -OCHF2 y -O-alquilo C1-6; R34 representa de 1 a 3 substituyentes independientemente seleccionados del grupo que consiste en H, halógeno, -CF3, -OCF3, -OH y -OCH3; R35 representa de 1 a 3 substituyentes independientemente seleccionados de hidrogeno, halo, alquil C1-6, hidroxi, alcoxi C1-6, fenoxi, -CF3, -N (R36)2, -COOR20 y -NO2; R36 está independientemente seleccionado del grupo que consiste en H y alquilo C1-6; R37 está independientemente seleccionado del grupo que consiste en hidrogeno, alquilo C1-6, cicloalquilo C3-6, cicloalquil C3-6alquilo C1-6, R33-arilo, R33-arilalquilo C1-6, y R32-heteroarilo; y R38 es hidrogeno, alquilo C1-6, -C(O)R20, -C(O)2R20, -C(O)N(R2)2 o alquil C1-6 -SO2-; o R37 y R38, conjuntamente con el nitrógeno al cual están unidos forman un anillo azetidinilo, pirrolidinilo, piperidinilo, piperazinilo o morfolinilo.
AR20030101341A 2002-04-18 2003-04-16 Antagonistas de histamina h3 de benzimidazolona AR040406A1 (es)

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US (1) US7220735B2 (es)
EP (1) EP1494671B1 (es)
JP (2) JP4563800B2 (es)
KR (1) KR20040099449A (es)
CN (1) CN100360130C (es)
AR (1) AR040406A1 (es)
AT (1) ATE529112T1 (es)
AU (1) AU2003223631B2 (es)
CA (1) CA2482551C (es)
IL (1) IL164583A (es)
MX (1) MXPA04010172A (es)
MY (1) MY132566A (es)
NZ (1) NZ535764A (es)
PE (1) PE20040464A1 (es)
TW (1) TW200305409A (es)
WO (1) WO2003103669A1 (es)
ZA (1) ZA200407985B (es)

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