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AR074966A1 - Compuestos amino-heterociclicos - Google Patents

Compuestos amino-heterociclicos

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Publication number
AR074966A1
AR074966A1 ARP100100153A ARP100100153A AR074966A1 AR 074966 A1 AR074966 A1 AR 074966A1 AR P100100153 A ARP100100153 A AR P100100153A AR P100100153 A ARP100100153 A AR P100100153A AR 074966 A1 AR074966 A1 AR 074966A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
group
haloalkyl
cycloalkyl
Prior art date
Application number
ARP100100153A
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English (en)
Original Assignee
Pfizer
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of AR074966A1 publication Critical patent/AR074966A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/473Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente proporciona compuestos inhibidores de PDE9 de fórmula (1). También se proporcionan composiciones farmacéuticas que contienen los compuestos de fórmula (1), y usos de los mismos en el tratamiento de trastornos neurodegenerativos y cognitivos, tales como la enfermedad de Alzheimer y esquizofrenia. Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable del mismo, en la que R1 se selecciona entre el grupo constituido por (i) hidrógeno, (ii) alquilo C1-4, (iii) alquenilo C2-4, (iv) alquinilo C2-4, (v) alcoxi C1-4, (vi) haloalquilo C1-4, (vii) cicloalquilo C3-6, opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente entre el grupo constituido por alquilo C1-4, alcoxi C1-4, halo, haloalquilo C1-4, haloalcoxi C1-4, ciano, carboxi y carbamoilo, (viii) heterocicloalquilo de 4 a 10 miembros, opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente entre el grupo constituido por alquilo C1-4, alcoxi C1-4, halo, haloalquilo C1-4, haloalcoxi C1-4, ciano, carboxi y carbamoilo, (ix) arilo, opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente entre el grupo constituido por alquilo C1-4, alcoxi C1-4, halo, haloalquilo C1-4, haloalcoxi C1-4, ciano, carboxi y carbamoilo, y (x) heteroarilo, opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente entre el grupo constituido por alquilo C1-4, alcoxi C1-4, halo, haloalquilo C1-4, haloalcoxi C1-4, ciano, carboxi y carbamoilo; R2 se selecciona entre el grupo constituido por hidrógeno, alquilo C1-4, haloalquilo C1-4, ciano y cicloalquilo C3-6; R3 se selecciona entre el grupo constituido por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, heterocicloalquilo, arilo y heteroarilo. cada uno de los cuales puede estar opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente entre el grupo constituido por alquilo C1-4, alcoxi C1-4, halo y haloalquilo C1-4; n es 1 ó 2; A es -CR4R5- o-CHRa-CHRb-; R4 se selecciona entre el grupo constituido por (i) hidrógeno, (ii) alquilo C1-7, (iii) cicloalquilo C3-8, (iv) heterocicloalquilo de 4 a 10 miembros, (v) arilo, opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente entre el grupo constituido por alquilo C1-4, alcoxi C1-4, halo, haloalquilo C1-4, haloalcoxi C1-4, cicloalquilo C3-6, ciano, carboxi y carbamoilo, (vi) heteroarilo, opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente entre el grupo constituido por alquilo C1-4, alcoxi C1-4, halo, haloalquilo C1-4, haloalcoxi C1-4, cicloalquilo C3-6, ciano, carboxi y carbamoilo, y (vii) LR6, donde L se selecciona entre el grupo constituido por -CH2-, -NR7- y -O-; R6 es arilo, heteroarilo, alquilo C1-8, cicloalquilo C3-8, heterocicloalquilo de 4 a 10 miembros o alcoxi C1-8, cada uno de los cuales puede estar opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente entre el grupo constituido por alquilo C1-4, alcoxi C1-4, halo, haloalquilo C1-4, haloalcoxi C1-4. cicloalquilo C3-6, ciano, carboxi y carbamoilo; y R7 es hidrógeno, metilo o etilo; R5 se selecciona entre el grupo constituido por hidrógeno, hidroxilo, alcoxi C1-4, halógeno y alquilo C1-6; o R4 y R5, junto con el carbono al que están unidos, forman un anillo cicloalquilo o heterocicloalquilo que incorpora opcionalmente un grupo oxo y está opcionalmente sustituido con alquilo C1-8, cicloalquilo C3-8, halo, alcoxi C1-8 o haloalquilo C1-3; Ra es alcoxi C1-4 o R8-O-C(O)-, donde R8 es alquilo C1-4; y Rb es arilo, heteroarilo o heterocicloalquilo, opcionalmente sustituido con halo, alquilo C1-8, cicloalquilo C3-8, alcoxi C1-8 o haloalquilo C1-3; o Ra y Rb junto con los carbonos a los que están unidos, forman un anillo cicloalquilo o heterocicloalquilo que incorpora opcionalmente un grupo oxo y está opcionalmente sustituido con alquilo C1-8, cicloalquilo C3-8, halo, alcoxi C1-8 o haloalquilo C1-3.
ARP100100153A 2009-01-26 2010-01-25 Compuestos amino-heterociclicos AR074966A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US20609209P 2009-01-26 2009-01-26

Publications (1)

Publication Number Publication Date
AR074966A1 true AR074966A1 (es) 2011-02-23

Family

ID=42062324

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100100153A AR074966A1 (es) 2009-01-26 2010-01-25 Compuestos amino-heterociclicos

Country Status (21)

Country Link
US (3) US8278295B2 (es)
EP (1) EP2389382B1 (es)
JP (1) JP5656874B2 (es)
KR (1) KR101417237B1 (es)
CN (1) CN102292340B (es)
AR (1) AR074966A1 (es)
AU (1) AU2010207507B2 (es)
CA (1) CA2748864C (es)
DK (1) DK2389382T3 (es)
ES (1) ES2420860T3 (es)
HR (1) HRP20130530T1 (es)
IL (2) IL213923A (es)
MX (1) MX2011007862A (es)
PL (1) PL2389382T3 (es)
PT (1) PT2389382E (es)
SG (1) SG172805A1 (es)
SI (1) SI2389382T1 (es)
TW (1) TWI404721B (es)
UY (1) UY32391A (es)
WO (1) WO2010084438A1 (es)
ZA (1) ZA201105931B (es)

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JP2012515761A (ja) 2012-07-12
CA2748864A1 (en) 2010-07-29
UY32391A (es) 2010-08-31
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US20140088081A1 (en) 2014-03-27
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