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AR057771A1 - Agonistas adrenoreceptores alfa2c - Google Patents

Agonistas adrenoreceptores alfa2c

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Publication number
AR057771A1
AR057771A1 ARP060103662A ARP060103662A AR057771A1 AR 057771 A1 AR057771 A1 AR 057771A1 AR P060103662 A ARP060103662 A AR P060103662A AR P060103662 A ARP060103662 A AR P060103662A AR 057771 A1 AR057771 A1 AR 057771A1
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AR
Argentina
Prior art keywords
group
heteroaryl
alkynyl
cycloalkyl
alkenyl
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Application number
ARP060103662A
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English (en)
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Pharmacopeia Drug Discovery
Schering Corp
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Application filed by Pharmacopeia Drug Discovery, Schering Corp filed Critical Pharmacopeia Drug Discovery
Publication of AR057771A1 publication Critical patent/AR057771A1/es

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    • 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
    • C07D413/06—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 carbon chain containing only aliphatic carbon atoms
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    • 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
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    • A—HUMAN NECESSITIES
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    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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    • A61P25/00—Drugs for disorders of the nervous system
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    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
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    • 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
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • 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
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    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente se refiere a una clase de compuestos, fenilmorfolina y feniltiomorfolina, utiles como agonistas receptores adrenérgicos a2C y a las composiciones farmacéuticas que contienen los compuestos. Los compuestos son utiles en el tratamiento, prevencion e inhibicion, o mejoramiento de una o más enfermedades asociadas con los agonistas receptores adrenérgicos a2C adrenérgico usando dichos compuestos o composiciones farmacéuticas. Son tratables patologías tales como congestion, insuficiencia cardiaca congestiva y desordenes psicoticos. Reivindicacion 1: El compuesto representado por la formula estructural (1), o una sal o solvato farmacéuticamente aceptables de dicho compuesto, donde: A es un anillo heterocíclico de 5 miembros que contiene 1-3 heteroátomos, y está sustituido con por lo menos un R5; X es - O-, -S(O)p-, o -N(R6)-; J1, J2, J3, y J4 son independientemente -N-, -N(O)- o -C(R2)-, con la condicion de que 0-3 de J1, J2, J3 y J4 son -N-; R2 está independientemente seleccionado del grupo que consiste en H, -OH, halo, -CN, -NO2, -(CH2)qYR7, -(CH2)qNR7YR7', -(CH2)qOYR7, -(CH2) qON=CR7R7', -P(=O)(OR7)(OR7'), -P(=O)(NR7R7')2, -P(=O)R82, y grupos alquilo, alcoxi, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, y heterociclilo opcionalmente sustituidos con por lo menos un R5; Y está seleccionado del grupo que consiste en un enlace, -C(=O)-, -C(=O)NR7-, C(=O)O-, -C(=NR7)-, -C(=NOR7)-, - C(=NR7)NR7-, -C(=NR7)NR7O-, -S(O)P-, SO2NR7-, y -C(S)NR7-; R3 está independientemente seleccionado del grupo que consiste en H y (=O), y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo opcionalmente sustituidos con por lo menos un R5, con la condicion de que cuando n es 3 o 4, no más de 2 de los grupos R3 sean (=O); R4 está independientemente seleccionado del grupo que consiste en H y CN y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo opcionalmente sustituidos con por lo menos un R5; R5 está independientemente seleccionado del grupo que consiste en H, halo, -OH, -CN, -NO2, -NR7R7', -SR7, y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, cada uno de los cuales está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, -OH, -CN, -NO2, -NR7R7', y -SR7; R6 está independientemente seleccionado del grupo que consiste en H y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, cada uno de los cuales está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, -OH, -CN, -NO2, -NR7R7', y -SR7, -C(=O)R7, -C(=O)OR7, -C(=O)NR7R7', -SO2R8 y -SO2NR7R7'; R7 está independientemente seleccionado del grupo que consiste en H y grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, -OH, -CN, -NO2, -N(R11) 2 y -SR11; R7' está independientemente seleccionado del grupo que consiste en H y grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, -OH, -CN, -NO2, -N(R11)2, y -SR11; o R7y R7' conjuntamente con el átomo de nitrogeno al cual están unidos forman un anillo heterociclilo, heterociclenilo o heteroarilo de 3- a 8- miembros, que tiene además del átomo N, 1 o 2 heteroátomos adicionales seleccionados del grupo que consiste en O, N, -N(R9)- y S, en el cual dichos anillos están opcionalmente sustituidos con 1 a 5 porciones R5 independientemente seleccionadas; R8 está independientemente seleccionado del grupo que consiste en grupo alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, -OH, -CN, -NO2, -N(R11)2, y -SR11; R9 está independientemente seleccionado del grupo que consiste en H, -C(O)-R10, -C(O)-OR10, y -S(O)p- OR10 y grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, -OH, -CN, -NO2, -N(R11)2, y -SR11; y R10 está seleccionado del grupo que consiste en grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, cada uno de los cuales está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, -OH, -CN, -NO2, -N(R11)2, y -SR11; R11 es una porcion independientemente seleccionada del grupo que consiste en H, alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclialquilo; m es 1-5; n es 1-3; p es 0-2; q es 0-6; y w es 0-4, con las siguientes condiciones: a) si J1-J4 son cada uno -C(H)-, n es 1, m es 1, R4 es H, A es 3H-imidazol-4-il, y X es -N(R6)-, entonces R6 no es -C(= O)-naftilo; b) si J1-J4 son cada uno -C(H)-, n es 1, m es 1, R4 es H, A es 1H-imidazol-4-il, y X es -N(R6)-, entonces R6 no es -S(O2)-naftilo; y c) si J1, J2, y J4 son cada uno -C(H)-, J3 es -C(Br)-, n es 2, m es 1, R3 es 3-bencilo, R4 es H, A es 1H-imidazol-4-ilo, y X es -N(R6)-, entonces R6 no es -C(O2)bencilo.
ARP060103662A 2005-08-25 2006-08-23 Agonistas adrenoreceptores alfa2c AR057771A1 (es)

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EP (1) EP1934203B1 (es)
JP (2) JP2009506051A (es)
KR (1) KR20080037070A (es)
CN (1) CN101374830A (es)
AR (1) AR057771A1 (es)
AT (1) ATE478069T1 (es)
AU (1) AU2006283109A1 (es)
BR (1) BRPI0615021A2 (es)
CA (1) CA2620173A1 (es)
DE (1) DE602006016303D1 (es)
EC (1) ECSP088221A (es)
ES (1) ES2348997T3 (es)
IL (1) IL189678A0 (es)
NO (1) NO20081427L (es)
PE (1) PE20070519A1 (es)
RU (1) RU2008110902A (es)
SG (1) SG165315A1 (es)
TW (1) TWI329643B (es)
WO (1) WO2007024949A2 (es)
ZA (1) ZA200802495B (es)

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