AR050540A1 - Derivados de adamantilamida triciclica como inhibidores de deshidrogenasa 11- beta hidroxiesteroide - Google Patents

Derivados de adamantilamida triciclica como inhibidores de deshidrogenasa 11- beta hidroxiesteroide

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Publication number
AR050540A1
AR050540A1 ARP050103613A ARP050103613A AR050540A1 AR 050540 A1 AR050540 A1 AR 050540A1 AR P050103613 A ARP050103613 A AR P050103613A AR P050103613 A ARP050103613 A AR P050103613A AR 050540 A1 AR050540 A1 AR 050540A1
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Argentina
Prior art keywords
alkyl
phenyl
alkyloxy
hydroxycarbonyl
alkylcarbonyl
Prior art date
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ARP050103613A
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English (en)
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Janssen Pharmaceutica Nv
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Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR050540A1 publication Critical patent/AR050540A1/es

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    • 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
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/28—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P9/10—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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/58—[b]- or [c]-condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/58—[b]- or [c]-condensed
    • C07D209/60—Naphtho [b] pyrroles; Hydrogenated naphtho [b] pyrroles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/58—[b]- or [c]-condensed
    • C07D209/62—Naphtho [c] pyrroles; Hydrogenated naphtho [c] pyrroles
    • C07D209/64—Naphtho [c] pyrroles; Hydrogenated naphtho [c] pyrroles with an oxygen atom in position 1
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D495/04—Ortho-condensed systems

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

Abstract

Las formas de N-oxido, las sales de adicion farmacéuticamente aceptables y sus formas estereoquímicamente isoméricas, en las que X representa C o N; Y representa C o N; L representa un metilo o un enlace directo; Z1 representa un enlace directo, alquilo de C1-2 o un radical divalente de formula -CH2-CH= (a) o -CH= (b); Z2 representa un enlace directo, alquilo C1-2 o un radical divalente de formula -CH2-CH= (a) o -CH= (b); R1 representa H, halo, ciano, amino, fenilo, hidroxi, alquiloxicarbonilo C1-4, hidroxicarbonilo, NR3R4 o alquilo C1-4 opcionalmente sustituidos con uno o más sustituyentes seleccionados a partir de hidroxicarbonilo, fenilo, alquiloxi C1-4 o NR5R6 o R1 representa alquiloxi C1-4 opcionalmente sustituido con uno o más sustituyentes seleccionados a partir de hidroxicarbonilo, fenilo, alquiloxi C1-4 o NR7R8; R2 representa H, halo, alquilo C1-4 o alquiloxi C1-4; R3 y R4 representan cada uno independientemente H, alquilo C1-4 o alquilcarbonilo C1-4; R5 y R6 representan cada uno independientemente H, alquilo C1-4 o alquilcarbonilo C1-4; R7 y R8 representan cada uno independientemente H, alquilo C1-4 o alquilcarbonilo C1-4; A representa fenilo o un heterociclo monocíclico seleccionado a partir del grupo consistente de tiofenilo, furanilo, oxazolilo, tiazolilo, imidazolilo, isoxazolilo, isotiazolilo, pirridinilo, piridazinilo, pirimidinilo y piperazinilo. También reivindica composicion farmacéutica, uso de los compuestos para preparar medicamentos utiles para obesidad, diabetes, enfermedades cardiovasculares, demencia, cognicion, osteoporosis, estrés y glaucoma. Reivindicacion1: Un compuesto que tiene la formula (1), las formas de N-oxidos, las sales de adicion farmacéuticamente aceptables y las formas estereoquímicamente isoméricas del mismo, en donde: X representa C o N; Y representa C o N; L representa un metilo o un enlace directo; Z1 representa un enlace directo, alquilo C1-2 o un radical divalente de formula -CH2-CH= (a) o -CH= (b); Z2 representa un enlace directo, alquilo C1-2 o un radical divalente de formula -CH2-CH= (a) o -CH= (b); R1 representa H, halo, ciano, amino, fenilo, hidroxi, alquiloxicarbonilo C1-4, -O-(C=O)-alquilo C1-4, hidroxicarbonilo, NR3R4 o alquilo C1-4 donde dicho alquilo C1-4 o -O-(C=O)-alquilo C1-4 están opcionalmente sustituidos con uno o más sustituyentes seleccionados a partir de halo, hidroxicarbonilo, fenilo, alquiloxi C1-4 o NR5R6 o R1 representa alquiloxi C1-4 opcionalmente sustituido con uno o más sustituyentes seleccionados a partir de halo, hidroxicarbonilo, fenilo, alquiloxi C1-4 o NR7R8; R2 representa H, halo, alquilo C1-4 o alquiloxi C1-4; R3 y R4 representan cada uno independientemente H, alquilo C1-4 o alquilcarbonilo C1-4; R5 y R6 representan cada uno independientemente H, alquilo C1-4 o alquilcarbonilo C1-4; R7 y R8 representan cada uno independientemente H, alquilo C1-4 o alquilcarbonilo C1-4; A representa fenilo o un heterociclo monocíclico seleccionado a partir del grupo consistente de tiofenilo, furanilo, oxazolilo, tiazolilo, imidazolilo, isoxazolilo, isotiazolilo, pirridinilo, piridazinilo, pirimidinilo y piperazinilo.
ARP050103613A 2004-08-30 2005-08-29 Derivados de adamantilamida triciclica como inhibidores de deshidrogenasa 11- beta hidroxiesteroide AR050540A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP04104147 2004-08-30

Publications (1)

Publication Number Publication Date
AR050540A1 true AR050540A1 (es) 2006-11-01

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ID=34929502

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ARP050103613A AR050540A1 (es) 2004-08-30 2005-08-29 Derivados de adamantilamida triciclica como inhibidores de deshidrogenasa 11- beta hidroxiesteroide

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Country Link
US (1) US8563591B2 (es)
EP (1) EP1786774B1 (es)
JP (1) JP5137574B2 (es)
KR (1) KR101197672B1 (es)
CN (1) CN101039908B (es)
AR (1) AR050540A1 (es)
AT (1) ATE445600T1 (es)
AU (1) AU2005279209B2 (es)
CA (1) CA2576850C (es)
ES (1) ES2334246T3 (es)
HK (1) HK1112618A1 (es)
IL (1) IL181581A0 (es)
MY (1) MY141198A (es)
RU (1) RU2386617C2 (es)
TW (1) TWI365871B (es)
WO (1) WO2006024628A1 (es)

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