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AR092955A1 - Antagonistas de receptores de orexina los cuales son derivados de [orto bi-(hetero-)aril]-[2-(meta bi-(hetero-)aril)-pirrolidin-1-il]-metanona - Google Patents

Antagonistas de receptores de orexina los cuales son derivados de [orto bi-(hetero-)aril]-[2-(meta bi-(hetero-)aril)-pirrolidin-1-il]-metanona

Info

Publication number
AR092955A1
AR092955A1 ARP130103661A ARP130103661A AR092955A1 AR 092955 A1 AR092955 A1 AR 092955A1 AR P130103661 A ARP130103661 A AR P130103661A AR P130103661 A ARP130103661 A AR P130103661A AR 092955 A1 AR092955 A1 AR 092955A1
Authority
AR
Argentina
Prior art keywords
alkyl
heteroaryl
group
twice
membered
Prior art date
Application number
ARP130103661A
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English (en)
Original Assignee
Actelion Pharmaceuticals Ltd
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Filing date
Publication date
Application filed by Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of AR092955A1 publication Critical patent/AR092955A1/es

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    • 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
    • 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
    • A61P25/20—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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/14—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 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
    • C07D413/02—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
    • 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
    • C07D417/14—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 three or more hetero rings
    • 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
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyrrole Compounds (AREA)

Abstract

La presente se refiere a derivados de [orto bi-(hetero-)aril]-[2-(meta bi-(hetero-)aril)-pirrolidin-1-il]-metanona de fórmula (1). Composiciones farmacéuticas que contienen uno o más compuestos de fórmula (1), y a su uso como productos farmacéuticos, especialmente a su uso como antagonistas de los receptores de orexina. Reivindicación 1: Un compuesto de fórmula (1) en la cual el átomo de carbono en posición 2 del anillo de pirrolidina está en configuración (S) absoluta; R representa hidrógeno o metilo; el anillo A³ representa un anillo heteroarileno de 5 miembros sustituido dos veces en posición meta que contiene uno, dos o tres heteroátomos; donde por lo menos uno de dichos heteroátomos es nitrógeno, y el resto es/ son seleccionado/s independientemente entre oxígeno, azufre y nitrógeno; el anillo A² representa arilo o heteroarilo de 5 a 10 miembros; donde dicho arilo o heteroarilo de 5 a 10 miembros es independientemente no sustituido, o sustituido una, dos o tres veces; donde los sustituyentes son seleccionados independientemente del grupo que consiste en alquilo C₁₋₄, alcoxi C₁₋₄, cicloalquilo C₃₋₆, halógeno, ciano, fluoroalquilo C₁₋₃, fluoroalcoxi C₁₋₃, hidroxi, alcoxi C₁₋₄-alquilo C₁₋₃, hidroxi-alquilo C₁₋₃, -CO-alquilo C₁₋₄, y cicloalquil C₃₋₆-oxi-; o el anillo A² representa un grupo 2,3-dihidro-benzo[1,4]dioxinilo, un grupo 2,3-dihidro-benzofuranilo, o un grupo benzo[1,3]dioxolilo opcionalmente sustituido dos veces con flúor; y el anillo A¹ representa fenilo o heteroarilo de 5 ó 6 miembros, donde dicho fenilo o heteroarilo de 5 ó 6 miembros está independientemente sustituido una, dos o tres veces; donde uno de dichos sustituyentes está unido en posición orto al punto de unión de A¹ al resto de la molécula; donde dicho sustituyente es fenilo o heteroarilo de 5 ó 6 miembros; donde dicho sustituyente fenilo o heteroarilo de 5 ó 6 miembros está independientemente sin sustituir, sustituido una, dos o tres veces, donde los sustituyentes son seleccionados independientemente del grupo que consiste en alquilo C₁₋₄, alcoxi C₁₋₄, halógeno, ciano, fluoroalquilo C₁₋₃, y fluoroalcoxi C₁₋₃; y el otro de dichos sustituyentes, si está presente, es/son seleccionado/s independientemente del grupo que consiste en alquilo C₁₋₄, alcoxi C₁₋₄, halógeno, ciano, fluoroalquilo C₁₋₃, y fluoroalcoxi C₁₋₃; siempre que el anillo A¹ no sea isoxazol-4-ilo, sustituido en posición 5 con alquilo C₁₋₄, unido al resto de la molécula en posición 4, y que porta dicho sustituyente orto adicional en posición 3; con la excepción del compuesto (1,1-bifenil)-2-il-{(S)-2-[3-(3-piridinil)-1H-1,2,4-triazol-5-il]-1-pirrolidinil}-metanona; o su sal farmacéuticamente aceptable.
ARP130103661A 2012-10-10 2013-10-09 Antagonistas de receptores de orexina los cuales son derivados de [orto bi-(hetero-)aril]-[2-(meta bi-(hetero-)aril)-pirrolidin-1-il]-metanona AR092955A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12188019 2012-10-10
EP13157809 2013-03-05

Publications (1)

Publication Number Publication Date
AR092955A1 true AR092955A1 (es) 2015-05-06

Family

ID=49765598

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130103661A AR092955A1 (es) 2012-10-10 2013-10-09 Antagonistas de receptores de orexina los cuales son derivados de [orto bi-(hetero-)aril]-[2-(meta bi-(hetero-)aril)-pirrolidin-1-il]-metanona

Country Status (16)

Country Link
US (1) US9493446B2 (es)
EP (1) EP2906553B1 (es)
JP (1) JP6244365B2 (es)
KR (1) KR102151288B1 (es)
CN (1) CN104703980B (es)
AR (1) AR092955A1 (es)
AU (1) AU2013328301A1 (es)
BR (1) BR112015007516A2 (es)
CA (1) CA2885180C (es)
EA (1) EA201500399A1 (es)
IL (1) IL238052A0 (es)
MX (1) MX2015004638A (es)
PH (1) PH12015500627A1 (es)
SG (1) SG11201502493XA (es)
TW (1) TW201414727A (es)
WO (1) WO2014057435A1 (es)

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BR112015007516A2 (pt) 2017-07-04
CN104703980B (zh) 2017-09-22
AU2013328301A8 (en) 2015-06-11
AU2013328301A1 (en) 2015-05-28
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CA2885180A1 (en) 2014-04-17
EA201500399A1 (ru) 2015-09-30
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US20150252032A1 (en) 2015-09-10
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CN104703980A (zh) 2015-06-10
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