AR061206A1 - Pirido[3,2-e]pirazinas, su uso como inhibidores de la fosfodiesterasa 10, y procesos para prepararlas - Google Patents

Pirido[3,2-e]pirazinas, su uso como inhibidores de la fosfodiesterasa 10, y procesos para prepararlas

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Publication number
AR061206A1
AR061206A1 ARP070102310A ARP070102310A AR061206A1 AR 061206 A1 AR061206 A1 AR 061206A1 AR P070102310 A ARP070102310 A AR P070102310A AR P070102310 A ARP070102310 A AR P070102310A AR 061206 A1 AR061206 A1 AR 061206A1
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Argentina
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alkyl
cyclic radical
halo
optionally mono
polysubstituted
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ARP070102310A
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Elbion Ag
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-condensed systems
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
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  • Addiction (AREA)
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  • Virology (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
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  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Pirido[3,2-e]pirazinas, procesos para prepararlas, preparaciones farmacéuticas que comprenden estos compuestos y al uso farmacéutico de estos compuestos, que son inhibidores de la fosfodiesterasa 10, como compuestos activos para tratar enfermedades de mamíferos, que incluyen a un ser humano, que pueden ser influidos por el uso de los compuesto para inhibir la actividad de la fosfodiesterasa 10 en el sistema nervioso central. Más particularmente, tratamiento de trastornos neurologicos y psiquiátricos, por ejemplo psicosis y trastornos que comprenden déficits cognitivos como síntomas. Reivindicacion 1: Compuestos caracterizados porque formula (1) donde el enlace entre A y N es un enlace simple o un doble enlace, A es C cuando el enlace es un doble enlace y CH cuando el enlace es un enlace simple, m es 0 o 1, n es 0 o 1, donde R1 es R2 se seleccionan independientemente de H, un radical cíclico, alquilo C1-8, opcionalmente mono- o polisustituido con halo, OH, O-alquilo C1-3 y/o un radical cíclico, alquenilo C2-8, opcionalmente mono- o polisustituido con halo, OH, O-alquilo C1-3 y/o un radical cíclico, alquilinilo C2-8, opcionalmente mono- o polisustituido con halo, OH, O-alquilo C1-3 y/o un radical cíclico, un sistema anular carbocíclico saturado, monoinsaturado o poliinsaturado con 3 a 8 átomos o un sistema anular heterocíclico con 5 a 15 átomos anulares, cada uno opcionalmente mono- o poliinsaturado con halo, amino, alquilamino C1-3, di-alquilamino C1-3, nitro, alquilo C1-3, O-alquilo C1-3 y/o un radical cíclico y R3 se selecciona de H, un radical cíclico, N3, CN, R6, OR6, SR6, SOR6, SO2R6, NH(CO)OR6, N((CO)OR6)2, NR6 ((CO)OR6), NH-(C=O)-NH2, NR6-(C=O)-NH2, NR6-(C=O)-NH2, NH-(C=O)-NHR6, NR6-(C=O)-NHR6, NH- SO2R6, N(SO2R6)2 y NR6(SO2R6), donde R6 es en cada caso independientemente, un radical cíclico, alquilo C1-8 ciclo(hetero)alquilo C3-8, alquenilo C2-8, ciclo(hetero)alquenilo C3-8, o alquinilo C2-8, cada uno opcionalmente mono- o polisustituido con halo, OH, O-alquilo C1-3 y/o un radical cíclico, R7, OR7, SR7, NHSO2R7, N(SO2R7) o N(R8)SO2R7, donde R7 es arilo, heteroarilo, arilalquilo C1-5, heteroarilalquilo C1-5, donde arilo es fenilo o naftilo, heteroarilo es un sistema anular heterocíclico aromático de 5 a 5 átomos en el anillo que contiene por lo menos un átomo seleccionado de N, que incluye N-oxido, s y O y donde arilo y heteroarilo están opcionalmente mono- o polisustituidos, con halo, amino, alquilamino C1-3, nitro, alquilo C1-3, O-alquilo C1-3 y/o un radical cíclico y R8 es alquilo C1-5, opcionalmente mono- o polisustituido con halo, OH, O-C1-3 alquilo y/o un radical cíclico, R4 se selecciona de H, halo, un radical cíclico, R9, OH u OR9, NH(C=O)-alquilo C1-3, opcionalmente mono- o polisustituido con halo, OH, O-alquilo C1-3 o/y un radical cíclico, NH2, NHR9 o NR9R10, donde R9 y R10 se seleccionan independientemente de - un radical cíclico, - alquilo C1-6 o ciclo(hetero)alquilo C3-6, opcionalmente mono- o polisustituido con halo, OH, O-alquilo C1-3 y/o un radical cíclico, - arilalquilo-C1-5, donde arilo es fenilo, opcionalmente mono- o polisustituido con halo, amino, alquilamino C1-3, di-alquilamino C1-3, nitro, alquilo C1-3, O-alquilo C1-3 y/o radical cíclico o -NR9R10 juntos forman un anillo de cinco, seis o siete miembros saturado o insaturado que puede contener hasta 3 heteroátomos, con preferencia N, que incluye N-oxido, Sy/u O, opcionalmente mono- o polisustituido con halo, amino, alquilamino C1-3, di-alquilamino C1-3, nitro, alquilo C1-3, O-alquilo C1-3 y/o aril-alquilo C1-5, donde arilo es fenilo, opcionalmente mono- o polisustituido con halo, amino, alquilamino c1-3, di-alquilamino C1-3, nitro, alquilo C1-3, O-alquilo C1-3 y/o un radical cíclico, y R5 se selecciona de H, alquilo C1-5, cicloalquilo C3-6 o (CO)-alquilo C1-5, opcionalmente mono- o poli sustituido con halo, OH, O-alquilo C1-3 y/o un radical cíclico, o sales y derivados aceptables para uso farmacéutico de los mismos.
ARP070102310A 2006-05-30 2007-05-29 Pirido[3,2-e]pirazinas, su uso como inhibidores de la fosfodiesterasa 10, y procesos para prepararlas AR061206A1 (es)

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US80924206P 2006-05-30 2006-05-30

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AR061206A1 true AR061206A1 (es) 2008-08-13

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US (2) US7550465B2 (es)
EP (1) EP2021342A1 (es)
JP (1) JP2009538853A (es)
KR (1) KR20090013834A (es)
CN (1) CN101454324A (es)
AR (1) AR061206A1 (es)
AU (1) AU2007267392A1 (es)
BR (1) BRPI0712132A2 (es)
CA (1) CA2651849A1 (es)
CL (1) CL2007001554A1 (es)
CR (1) CR10358A (es)
GT (1) GT200800265A (es)
IL (1) IL193740A0 (es)
MX (1) MX2008014569A (es)
NO (1) NO20085326L (es)
PE (1) PE20080711A1 (es)
RU (1) RU2008152440A (es)
SV (1) SV2009003048A (es)
TW (1) TW200817400A (es)
WO (1) WO2007137820A1 (es)
ZA (1) ZA200807517B (es)

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WO2014142255A1 (ja) 2013-03-14 2014-09-18 武田薬品工業株式会社 複素環化合物
JP6427491B2 (ja) 2013-07-03 2018-11-21 武田薬品工業株式会社 複素環化合物
JP6411342B2 (ja) 2013-07-03 2018-10-24 武田薬品工業株式会社 アミド化合物
WO2015006689A1 (en) 2013-07-12 2015-01-15 University Of South Alabama Treatment and diagnosis of cancer and precancerous conditions using pde10a inhibitors and methods to measure pde10a expression
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BRPI0712132A2 (pt) 2012-01-17
SV2009003048A (es) 2009-02-11
US7550465B2 (en) 2009-06-23
CR10358A (es) 2009-01-07
JP2009538853A (ja) 2009-11-12
CA2651849A1 (en) 2007-12-06
CN101454324A (zh) 2009-06-10
TW200817400A (en) 2008-04-16
PE20080711A1 (es) 2008-06-14
IL193740A0 (en) 2009-05-04
US20080027064A1 (en) 2008-01-31
KR20090013834A (ko) 2009-02-05
GT200800265A (es) 2010-07-22
US20090239874A1 (en) 2009-09-24
RU2008152440A (ru) 2010-07-10
NO20085326L (no) 2008-12-19
MX2008014569A (es) 2008-12-03
WO2007137820A1 (en) 2007-12-06
CL2007001554A1 (es) 2008-01-18
EP2021342A1 (en) 2009-02-11
ZA200807517B (en) 2009-06-24
AU2007267392A1 (en) 2007-12-06

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