AR074775A1 - Compuestos aminopiridina y carboxipiridina como inhibidores de fosfodiesterasa 10 - Google Patents

Compuestos aminopiridina y carboxipiridina como inhibidores de fosfodiesterasa 10

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Publication number
AR074775A1
AR074775A1 ARP090104944A ARP090104944A AR074775A1 AR 074775 A1 AR074775 A1 AR 074775A1 AR P090104944 A ARP090104944 A AR P090104944A AR P090104944 A ARP090104944 A AR P090104944A AR 074775 A1 AR074775 A1 AR 074775A1
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alq
nrara
haloalq
ora
independently
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Amgen Inc
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
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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
    • 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
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/36—Opioid-abuse
    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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    • C07—ORGANIC CHEMISTRY
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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C—CHEMISTRY; METALLURGY
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    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D413/14—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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
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  • Engineering & Computer Science (AREA)
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  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
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  • Addiction (AREA)
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  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Además se proveen en la presente métodos para tratar los trastornos o las enfermedades que pueden tratarse mediante la inhibición del PDE10, tales como obesidad, diabetes no insulino dependiente, esquizofrenia, trastorno bipolar, trastorno obsesivo-compulsivo, y similares. Reivindicación 1: Un compuesto que tiene una estructura (1) o una sal del mismo aceptable para uso farmacéutico, donde: X1 es N o C; X2 es N o C; donde 1 o 2 de X1 y X2 es C; Cada uno de X4, X5, X7, y X8 es independientemente N o C; cada uno de X3 y X6 es C; donde no más de tres de X4, X5, X7, y X8 son N; m es independientemente en cada instancia 0, 1, 2, 3 o 4; n es independientemente en cada instancia 0, 1, 2, 3 o 4; Y es NR8 o C(=O); o en forma alternativa cuando Y es NR8, Y y R3 pueden formar un anillo de 5 a 6 miembros fusionados al anillo que contiene tanto Y como R3; R1 se selecciona de: (c) H, F, CI, Br, I, alq C1-8, haloalq C1-4, -ORa, -NRaRa, -NRaRc, -N(Ra)C(=O)Rb, -C(=O)NRaRa, -C(=O)NRaRc, -C(=O)NRaRd, -C(=O)Ra, -C(=O)Rc, -C(=O)Rd, -C(=O)-O-Ra, -C(=O)-O-Rc, -C(=O)-O-Rd, -ORc, -NRaRc, -SRc, -S(=O)Rc, -S(=O)2Rc, -N(Rc)S(=O)2Rb, -S(=O)2NRaRc, -N(Rc)C(=O)Rb, -N(Ra)C(=O)Rc, o -C(=O)NRaRc; o, (d) el anillo A, donde dicho anillo A se selecciona del grupo integrado por Rb, Rc, y Rd; con la condición que cuando el anillo A es Rc, dicho Rc no es ciclopentadienilo; o anillo bicíclico de 9 o 10 miembros o monocíclico de 5 o 6 miembros insaturado enlazado a alq C0-4 que contiene 0, 1, 2 o 3 átomos N y 0, 1 o 2 átomos seleccionados de O y S; Y cuando Y es -NR8, el anillo A no es aminopirimidina; R2 es independientemente en cada instancia. F, CI, Br, CN, OH, Oalq C1-4, alq C1-4 o haloalq C1-4; R3 es, independientemente en cada instancia, F, Br, CN, OH, Oalq C1-4, alq C1-4 o haloalq C1-4; R4 se selecciona de H, F, Br, CN, -O-alq C1-4, alq C1-2, y haloalq C1-2; R5 se selecciona de H, F, Br, CN, -O-alq C1-4, alq C1-2, y haloalq C1-2; R6 se selecciona de H, F, Br, CN, -O-alq C1-4, alq C1-2, y haloalq C1-2; R7 se selecciona de H, F, Br, CN, -O-alq C1-4, alq C1-2, y haloalq C1-2; R8 se selecciona de H, alq C1-8, y haloalq C1-4; Ra es independientemente, en cada instancia, H o Rb; Rb es independientemente, en cada instancia, fenilo, bencilo o alq C1-6, donde dicho fenilo, bencilo y alq C1-6 está independientemente sustituido con 0, 1, 2 o 3 sustituyentes seleccionados de halo, OH, alq C1-4, haloalq C1-3, -O alq C1-4, -NH2, -NH alq C1-4, -N(alq C1-4)alq C1-4, alq C1-4-NH2, COOH, CN, -C(=O)-O-alq C1-6, alq-C(=O)-N(C1-4)alq C1-4, y -S-alq C1-4; Rc es un anillo bicíclico de 8, 9, 10, 11 o 12 miembros o monocíclico de 3, 4, 5, 6 o 7 miembros insaturado o parcialmente saturado, enlazado a alq C0-4 que contiene 0, 1, 2 o 3 N átomos y 0, 1 o 2 átomos seleccionados de O y S, el cual está sustituido con 0, 1, 2 o 3 grupos seleccionados de F, CI, Br, Re, alq C1-6, haloalq C1-4, -ORa, -O haloalq C1-4, CN, -C(=O)Rb, -C(=O)Re, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -OC(=O)Rb, -OC(=O)NRaRa, -C(=O)Rc, -O alq C2-6NRaRa, -O alq C2-6(ORa)1-3, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)(OH)Rb, -S(=O)2NRaRa, -NRaRa, -NRaRe, -NRaRd, -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, -NRa alq C2-6NRaRa. -NRa alq C2-6ORa, -alq C1-6NRaRa, alq C1-6(ORa)1-3, -alq C1-6N(Ra)C(=O)Rb, -alq C1-6OC(=O)Rb, alq C1-6C(=O)NRaRa, -alq C1-6(=O)ORa y oxo; Rd es un heterociclo del anillo de 4, 5, 6 o 7 miembros insaturado o parcialmente saturado, enlazado a nitrógeno que contiene el nitrógeno de enlace y 0, 1 o 2 átomos de nitrógeno adicionales y que contiene 0 o 1 átomo de azufre u oxigeno, el heterociclo está sustituido con 0, 1, 2 o 3 sustituyentes seleccionados de oxo, halo, OH, CN, alq C1-4, haloalq C1-3, -Oalq C1-4, Re, -ORe, -NH2, -NHalq C1-4, -N(alq C1-4)alq C1-4, C(=O)ORa, -alq C1-6(ORa)1-3, -NH-C(=O)Oalq C1-4, -C(=O)Ra, -C(=O)Re, -C(=O)NRaRa, y -C(=O)NRaRa; y Re es (a) monocíclico de 3, 4, 5, 6 o 7 miembros insaturado o parcialmente saturado, saturado enlazado a alq C0-4 que contiene 0, 1, 2 o 3 N átomos y 0, 1 o 2 átomos seleccionados de O y S; el cual está sustituido con 0, 1, 2 o 3 grupos seleccionados de oxo, halo, OH, alq C1-4, haloalq C1-3, -Oalq C1-4, -NH2, -NHalq C1-4, -N(alq C1-4)alq C1-4, alq C1-4-NH2, COOH, CN, -C(=O)-O-alq C1-6, -C(=O)-N(alq C1-4)alq C1-4, y -S-alq C1-4; o (b) heterociclo del anillo de 4, 5, 6 o 7 miembros insaturado o parcialmente saturado, saturado enlazado a nitrógeno que contiene el nitrógeno de enlace y 0, 1 o 2 átomos de nitrógeno adicionales y que contiene 0 o 1 átomo de azufre u oxigeno, el cual está sustituido con 0, 1, 2 o 3 grupos seleccionados de oxo, halo, OH, alq C1-4, haloalq C1-3, -Oalq C1-4, -NH2, -NHalq C1-4, -N(alq C1-4)alq C1-4, alq C1-4-NH2, COOH, CN, -C(=O)-O-alq C1-6, -C(=O)-N(alq C1-4)alq C1-4, y -S-alq C1-4.
ARP090104944A 2008-12-17 2009-12-17 Compuestos aminopiridina y carboxipiridina como inhibidores de fosfodiesterasa 10 AR074775A1 (es)

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US (1) US8637500B2 (es)
EP (1) EP2376455B1 (es)
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AR (1) AR074775A1 (es)
AU (1) AU2009333214B2 (es)
CA (1) CA2746307C (es)
ES (1) ES2397934T3 (es)
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US20100160280A1 (en) 2010-06-24
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JP2012512255A (ja) 2012-05-31
MX2011006575A (es) 2011-10-06
CA2746307A1 (en) 2010-07-08
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US8637500B2 (en) 2014-01-28
WO2010077992A1 (en) 2010-07-08

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