AR074343A1 - Derivados de piridina y pirimidina como inhibidores de la fosfodiesterasa 10 - Google Patents

Derivados de piridina y pirimidina como inhibidores de la fosfodiesterasa 10

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Publication number
AR074343A1
AR074343A1 ARP090104404A ARP090104404A AR074343A1 AR 074343 A1 AR074343 A1 AR 074343A1 AR P090104404 A ARP090104404 A AR P090104404A AR P090104404 A ARP090104404 A AR P090104404A AR 074343 A1 AR074343 A1 AR 074343A1
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Argentina
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alqc1
nrara
ora
6nrara
6ora
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ARP090104404A
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Amgen Inc
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    • 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
    • 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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • 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
    • A61P25/24—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)

Abstract

Compuestos y composiciones que los contienen, y procesos para preparar tales como compuestos. También se proveen métodos para tratar trastornos o enfermedades tratables por la inhibición de la PDE10, tales como obesidad, diabetes no insulino dependiente, esquizofrenia, trastorno bipolar, trastornos obsesivo compulsivo, y similares. Reivindicación 1: Un compuesto que tiene la estructura de la fórmula 2 o 3 o cualquier sal aceptable para uso farmacéutico del mismo! donde: Z es NH, NR6, S u O; m es 0, 1, 2, 3 o 4; n es 0, 1 o 2; p es 0, 1 o 2, y es 0, 1, 2, 3 o 4; X1 es N o C, X5 es N o C; X6 es N o C; El anillo A es un anillo carbocíclico unido a carbono, saturado, o unido a carbono, parcialmente no saturado, de 4, 5, 6, 7, 8, 9, 10, 11 o 12 miembros que contiene 0, 1 o 2 átomos de N y que contiene 0 o 1 átomos de S u O; o un anillo heterociclo unido a nitrógeno, saturado, unido a nitrógeno, parcialmente saturado, o unido a nitrógeno, no saturado, de 4, 5, 6, 7, 8, 9,10, 11 o 12 miembros que contiene el nitrógeno vinculante y 0, 1 o 2 átomos de N adicionales y que contienen 0 o 1 átomos de S u O, donde en cada uno de dichos carbociclos o heterociclos R2 es, independientemente en cada caso, F, Cl, Br, CN, OH, OalqC1-4, alqC1-4 o haloalqC1-4; R3 es, independientemente en cada caso, F, CI, Br, CN, OH, OaIqC1-4, aIqC1-4, haloalqC1-4, o -NRaalqC1-4; R4 es, independientemente en cada caso, F, Cl, CH3, CN, CF3, CHF2, CH2F, ORa, o NRaRa; R5 es alqC1-8, haloalqC1-4, C(=O)Rb, o Rc; R6 es alqC1-8, haloalqC1-4, C(=O)Rb, o Rc; R7 es un anillo monocíclico saturado, parcialmente saturado o no saturado de 3, 4, 5, 6, o 7 miembros o bicíclico de 8, 9, 10, 11, o 12 miembros que contiene 0, 1, 2, 3, o 4 átomos de N y O o 1 átomos seleccionados de O y S, que están sustituidos con 0, 1, 2 o 3 grupos seleccionados de F, CI, Br, alqC1-6, haloalqC1-4, -ORa, -OhaloalqC1-4, CN, C(=O)Rb, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -OC(=O)Rb, -OC(=O)NRaRa, -OalqC2-6NRaRa, -OalqC2-6ORa, -SRa, S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRaaIqC2-6NRaRa, NRaalqC2-6ORa, alqC1-6NRaRa, alqC1-6ORa, -alqC1-6N(Ra)C(=O)Rb, -alqC1-6OC(=O)Rb, -alqC1-6C(=O)NRaRa, -alqC1-6C(=O)ORa, R8 y oxo; R8 es un alqC1-6 sustituido con 0, 1, 2 o 3 grupos seleccionados de F, CI, Br, alqC1-6, haloalqC1-4, -ORa, -OhaloalqC1-4, CN, C(=O)Rb, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -OC(=O)Rb, -OC(=O)NRaRa, -OalqC2-6NRaRa, -OalqC2-6ORa, -SRa, S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRaaIqC2-6NRaRa, NRaalqC2-6ORa, alqC1-6NRaRa, alqC1-6ORa, -alqC1-6N(Ra)C(=O)Rb, -alqC1-6OC(=O)Rb, -alqC1-6C(=O)NRaRa, -alqC1-6C(=O)ORa, y oxo; R9 se selecciona independientemente el grupo que consiste en H, F, CI, Br, alqC1-6, haloalqC1-4, -ORa, -OhaloalqC1-4, CN, C(=O)Rb, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -OC(=O)Rb, -OC(=O)NRaRa, -OalqC2-6NRaRa, -OalqC2-6ORa, -SRa, S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -NRaRa, -NRaRc, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRaaIqC2-6NRaRa, NRaalqC2-6ORa, alqC1-6NRaRa, alqC1-6ORa, -alqC1-6N(Ra)C(=O)Rb, -alqC1-6OC(=O)Rb, -alqC1-6C(=O)NRaRa, -alqC1-6C(=O)ORa, R7, R8 y oxo; Ra es independientemente en cada caso, H o Rb; Rb es, independientemente en cada caso, fenilo, bencilo o alqC1-6, el fenilo, bencilo y alqC1-6 estando sustituidos con 0, 1, 2 o 3 sustituyentes seleccionados de halo, alqC1-4, haloalqC1-3, -OH, -OalqC1-4, -NH2, -NHalqC1-4, -OC(=O)alqC1-4, o -N(alqC1-4)alqC1-4; Rc es un anillo monocíclico unido a alqC0-4, saturado, parcialmente saturado o no saturado de 3, 4, 5, 6, o 7 miembros o bicíclico que contiene 0, 1, 2 o 3 átomos de N y 0 o 1 átomos seleccionados de O y S, donde dicho alqC0-4 y dicho resto anular pueden estar sustituidos con 0, 1, 2 o 3 grupos seleccionados de F, CI, Br, alqC1-6, haloalqC1-4, R7, -ORa, -OhaloalqC1-4, CN, C(=O)Rb, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -OC(=O)Rb, -OC(=O)NRaRa, -OalqC2-6NRaRa, -OalqC2-6ORa, -SRa, S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRaaIqC2-6NRaRa, NRaalqC2-6ORa, alqC1-6NRaRa, alqC1-6ORa, -alqC1-6N(Ra)C(=O)Rb, -alqC1-6OC(=O)Rb, -alqC1-6C(=O)NRaRa, -alqC1-6C(=O)ORa, R7, R8 y oxo.
ARP090104404A 2008-11-14 2009-11-13 Derivados de piridina y pirimidina como inhibidores de la fosfodiesterasa 10 AR074343A1 (es)

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US11459508P 2008-11-14 2008-11-14
US16621509P 2009-04-02 2009-04-02

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US (2) US8318718B2 (es)
EP (1) EP2364306B1 (es)
JP (1) JP2012508777A (es)
KR (1) KR20110086603A (es)
AR (1) AR074343A1 (es)
AU (1) AU2009313773B2 (es)
BR (1) BRPI0921598A2 (es)
CA (1) CA2742833C (es)
CR (1) CR20110279A (es)
EA (1) EA201100749A1 (es)
ES (1) ES2413808T3 (es)
IL (1) IL212670A0 (es)
MA (1) MA32891B1 (es)
MX (1) MX2011005093A (es)
TN (1) TN2011000220A1 (es)
TW (1) TW201030001A (es)
WO (1) WO2010057126A1 (es)

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EA201100749A1 (ru) 2011-10-31
EP2364306B1 (en) 2013-04-24
MX2011005093A (es) 2011-09-27
US20130079325A1 (en) 2013-03-28
KR20110086603A (ko) 2011-07-28
US20100125062A1 (en) 2010-05-20
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AU2009313773B2 (en) 2013-03-21
WO2010057126A1 (en) 2010-05-20
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CA2742833C (en) 2013-12-31
US8759532B2 (en) 2014-06-24
US8318718B2 (en) 2012-11-27
CA2742833A1 (en) 2010-05-20
JP2012508777A (ja) 2012-04-12
EP2364306A1 (en) 2011-09-14
CR20110279A (es) 2011-09-22
MA32891B1 (fr) 2011-12-01
TN2011000220A1 (en) 2012-12-17
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ES2413808T3 (es) 2013-07-17
BRPI0921598A2 (pt) 2016-02-10

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