AR078733A1 - Compuestos heterociclicos fusionados como moduladores del receptor de orexina - Google Patents

Compuestos heterociclicos fusionados como moduladores del receptor de orexina

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Publication number
AR078733A1
AR078733A1 ARP100103876A ARP100103876A AR078733A1 AR 078733 A1 AR078733 A1 AR 078733A1 AR P100103876 A ARP100103876 A AR P100103876A AR P100103876 A ARP100103876 A AR P100103876A AR 078733 A1 AR078733 A1 AR 078733A1
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Argentina
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group
substituted
unsubstituted
alkyl
members
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ARP100103876A
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Janssen Pharmaceutica Nv
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Publication of AR078733A1 publication Critical patent/AR078733A1/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
    • C07D471/08—Bridged systems
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • 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
    • 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
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
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  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
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  • Vascular Medicine (AREA)
  • Anesthesiology (AREA)
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  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)

Abstract

Dichos compuestos pueden ser utiles en composiciones y métodos farmacéuticos para el tratamiento de enfermedades, trastornos y afecciones mediadas por la actividad de la orexina, tal como el insomnio. Reivindicacion 1: Una entidad química que es un compuesto de la Formula (1): en donde: n es 0-1; R1 es un miembro seleccionado del grupo que consiste de: A) fenilo sustituido o no sustituido con uno o dos miembros Ra, y sustituido en la posicion orto con Rb; Ra se selecciona independientemente del grupo que consiste de: halo, alquilo de -C1-4 y alcoxi de -C1-4, en donde dos miembros Ra adyacentes pueden unirse para formar un anillo aromático de seis miembros; Rb es un miembro seleccionado del grupo que consiste de: a) halo, alcoxi de -C1-4, -CF3 o -CF2CHF2; b) un anillo heteroarilo de 5 miembros que contiene un miembro de oxígeno o azufre; c) un anillo heteroarilo de 5 a 6 miembros que contiene uno a tres miembros de nitrogeno, opcionalmente, que contiene un miembro de oxígeno, sustituido o no sustituido con halo, alquilo de -C1-4, tetrahidropiran-2-il, o -N(CH3)2; y d) fenilo sustituido o no sustituido con -F o -CH3; B) piridina sustituida o no sustituida con uno o dos miembros Rc y sustituida con Rd, en donde Rd se coloca adyacente al punto de union mediante R1; Rc es un miembro seleccionado independientemente del grupo que consiste de: alquilo de -C1-4, -CF3 y alcoxi de -C1-4; Rd es un miembro seleccionado del grupo que consiste de: a) un anillo heteroarilo de 5-6 miembros seleccionado del grupo que consiste de: 1H-1,2,3-triazol-1-il, 2H-1,2,3-triazol-2-il, 1H-pirazol-3-il y 6-metil-piridin-2-il; y b) -CF3, -Br o alcoxi de -C1-4; C) un anillo heteroarilo de 6 miembros seleccionado del grupo que consiste de: pirimidin-il o pirazin-il sustituido o no sustituido con un miembro seleccionado independientemente de -CH3, -OCH3 o fenilo; D) un anillo heteroarilo de 5 miembros seleccionado del grupo que consiste de: 2-metil-1,3-tiazol-il, 5-metil-isoxazol-4-il, 2H-pirazol-3- il, 1H-pirazol-4-il, isoxazolil y 1,3-oxazol-4-il, cada uno de ellos sustituido con fenilo sustituido o no sustituido con -F o -CI; y E) 3-metilfuran-2-il, 9H-fluoreno, 9H-fluoren-9-ona, 3,5'-biisoxazol, [3-metil-5-(4-metil-1,2,3-tiadiazol-5-iI)isoxazol-4-iI] o naftiridina; R2 es un miembro seleccionado del grupo que consiste de: A) un anillo heteroarilo de 6 miembros que contiene dos miembros de nitrogeno sustituidos o no sustituidos con uno o más miembros seleccionados independientemente del grupo que consiste de: halo, alquilo de -C1-4, alcoxi de -C1-4, -CF3, -NH2, -NHCH3, alquilo de -N(C1-4)1-2, ciclopropil-NH y fenilo; B) piridina sustituida o no sustituida con uno o dos miembros seleccionados independientemente del grupo que consiste de: alquilo de -C1-4, -N(alquilo de C1-4)2 y -CF3; y C) quinoxalin-2-il, benzooxazol-2-il o 5-cloro-1 ,3-benzoxazol; y sales farmacéuticamente aceptables de los compuestos de la Formula 1.
ARP100103876A 2009-10-23 2010-10-22 Compuestos heterociclicos fusionados como moduladores del receptor de orexina AR078733A1 (es)

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US25452909P 2009-10-23 2009-10-23

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AR078733A1 true AR078733A1 (es) 2011-11-30

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ID=43430851

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Application Number Title Priority Date Filing Date
ARP100103876A AR078733A1 (es) 2009-10-23 2010-10-22 Compuestos heterociclicos fusionados como moduladores del receptor de orexina

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US (1) US8680275B2 (es)
EP (1) EP2491034B1 (es)
JP (1) JP5847087B2 (es)
AR (1) AR078733A1 (es)
CL (1) CL2010001159A1 (es)
HK (1) HK1175461A1 (es)
PE (1) PE20110296A1 (es)
TW (1) TW201121966A (es)
UY (1) UY32968A (es)
WO (1) WO2011050200A1 (es)

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US8680275B2 (en) 2014-03-25
CL2010001159A1 (es) 2011-05-06
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PE20110296A1 (es) 2011-05-21
TW201121966A (en) 2011-07-01
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WO2011050200A1 (en) 2011-04-28
US20120202783A1 (en) 2012-08-09

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