[go: up one dir, main page]

AR086817A1 - Compuestos inhibidores de la fosfodiesterasa tipo 10a - Google Patents

Compuestos inhibidores de la fosfodiesterasa tipo 10a

Info

Publication number
AR086817A1
AR086817A1 ARP120102358A ARP120102358A AR086817A1 AR 086817 A1 AR086817 A1 AR 086817A1 AR P120102358 A ARP120102358 A AR P120102358A AR P120102358 A ARP120102358 A AR P120102358A AR 086817 A1 AR086817 A1 AR 086817A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
members
radicals
group
Prior art date
Application number
ARP120102358A
Other languages
English (en)
Inventor
Geneste Herve
Ochse Michael
Drescher Karla
Belh Berthold
Laplanche Loic
Dinges Jurgen
Jakob Clarissa
Original Assignee
Abbott Gmbh & Co Kg
Abbott Lab
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46456562&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR086817(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Abbott Gmbh & Co Kg, Abbott Lab filed Critical Abbott Gmbh & Co Kg
Publication of AR086817A1 publication Critical patent/AR086817A1/es

Links

Classifications

    • 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
    • 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
    • A61P25/22—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
    • A61P25/24—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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • C07D401/06—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 only aliphatic carbon atoms
    • 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
    • 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
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Compuestos de carboxamida. Composiciones farmacéuticas que los contienen. Su uso en la terapia. Estos compuestos presentan propiedades terapéuticas valiosas y son particularmente apropiados para tratar o controlar diversos trastornos neurológicos y psiquiátricos, para mejorar sus síntomas y para reducir el riesgo de que se desarrollen. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) donde X¹ es N o C-R¹; X² es N o C-R²; X³ es N o C-R³; X⁴ es N o C-R⁴; con la condición de que 0, 1 ó 2 de las porciones X¹, X², X³ o X⁴ es N; A se selecciona entre el grupo que consiste en O, S, S(=O), S(=O)₂, NR⁵ᵃ y CR⁵R⁶; Het se selecciona entre i) hetarilo monocíclico con 1 ó 2 átomos de nitrógeno y opcionalmente un heteroátomo adicional seleccionado entre O, S y N como miembros del anillo, que no está sustituido o puede tener 1, 2, 3 ó 4 sustituyentes Rˣ idénticos o diferentes, ii) hetarilo bicíclico fusionado con 1 ó 2 átomos de nitrógeno y opcionalmente un heteroátomo adicional seleccionado entre O, S y N como miembros del anillo, benzotienilo o benzofurilo, donde hetarilo, benzotienilo y benzofurilo bicíclico son, en forma independiente entre sí, puede no estar sustituido o puede tener 1, 2, 3 ó 4 sustituyentes Rˣ idénticos o diferentes, y iii) fenilo, que tiene un radical hetarilo monocíclico con 1 ó 2 átomos de nitrógeno y opcionalmente un heteroátomo adicional seleccionado entre O, S y N como miembros del anillo, que además de hetarilo monocíclico, puede tener 1, 2 ó 3 sustituyentes Rˣ idénticos o diferentes, donde Rˣ se selecciona entre el grupo que consiste en H, halógeno, alquilo C₁₋₄, alcoxi C₁₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, cicloalquilo C₃₋₆, alcoxi C₁₋₄-alcoxi C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, OH, hidroxi-alquilo C₁₋₄, O-cicloalquilo C₃₋₆, benciloxi, C(O)O-(alquilo C₁₋₄), O-(alquil C₁₋₄)-CO₂H, N(Rˣ¹)(Rˣ²), C(O)N(Rˣ¹)(Rˣ²), alquil C₁₋₄-N(Rˣ¹)(Rˣ²), -NRˣ³-C(O)-N(Rˣ¹)(Rˣ²), NRˣ³-C(O)O-(alquilo C₁₋₄), -N(Rˣ³)-SO₂-Rˣ⁴, fenilo, CN, -SF₅, -OSF₅, SO₂-Rˣ⁴, SRˣ⁴ y trimetilsililo, donde Rˣ¹, Rˣ², Rˣ³ y Rˣ⁴, se seleccionan en forma independiente entre sí entre el grupo que consiste en hidrógeno, alquilo C₁₋₄, fluoroalquilo C₁₋₄ y cicloalquilo C₃₋₆ o Rˣ¹ y Rˣ² forman junto con el átomo de N al cual están unidos un heterociclo con nitrógeno de entre 3 y 7 miembros que puede tener 1, 2 ó 3 heteroátomos diferentes o idénticos adicionales o grupos que contienen heteroátomos seleccionados entre el grupo de O, N, S, SO y SO₂ como miembros del anillo y que puede tener 1, 2, 3, 4, 5 ó 6 sustituyentes seleccionados entre alquilo C₁₋₄; R¹, R⁴ en forma independiente entre sí, se seleccionan entre el grupo que consiste en hidrógeno, halógeno, OH, alquilo C₁₋₄, trimetilsililo, alquil C₁₋₄sulfanilo, alcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄, alcoxi C₁₋₄-alcoxi C₁₋₄, alquil C₁₋₄sulfanil-alcoxi C₁₋₄, alqueniloxi C₂₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, ciclopropilo, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, ciclopropilo fluorado, CN, NRˣ¹Rˣ², NRˣ¹Rˣ²-alcoxi C₁₋₄ y la porción Y-Cyc; R², R³ en forma independiente entre sí, se seleccionan entre el grupo que consiste en hidrógeno, halógeno, OH, alquilo C₁₋₄, trimetilsililo, alcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄, alcoxi C₁₋₄-alcoxi C₁₋₄, alqueniloxi C₂₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, ciclopropilo, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, ciclopropilo fluorado, CN, NRˣ¹Rˣ² y la porción Y-Cyc; con la condición de que uno o dos de los radicales R¹, R², R³, R⁴ son una poción Y-Cyc; R⁵, R⁶ se seleccionan en forma independiente entre sí entre el grupo que consiste en hidrógeno, OH, halógeno, alquilo C₁₋₄, trimetilsililo, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, cicloalquilo C₃₋₆, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, y cicloalquilo C₃₋₆ fluorado o los radicales R⁵, R⁶ junto con el átomo de carbono al cual están unidos forman un grupo carbonilo o un carbociclo saturado de entre 3 y 6 miembros o un heterociclo saturado de entre 3 y 6 miembros con 1 ó 2 heteroátomos no adyacentes como miembros del anillo, donde el carbociclo y el heterociclo no están sustituidos o pueden tener 1, 2, 3 ó 4 sustituyentes seleccionados entre flúor y metilo; R⁵ᵃ se selecciona entre el grupo que consiste en alquilo C₁₋₄, alcoxi C₁₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, cicloalquilo C₃₋₆, opcionalmente sustituido con 1, 2 ó 3 grupos metilo, cicloalquilo C₃₋₆ fluorado, fenilo, bencilo, hetarilo de 5 ó 6 miembros con 1, 2 ó 3 heteroátomos seleccionados entre O, S y N como miembros del anillo, y hetarilmetilo de 5 ó 6 miembros con 1, 2 ó 3 heteroátomos seleccionados entre O, S y N como miembros del anillo, donde los anillos en los últimos cuatro radicales mencionados no están sustituidos o tienen 1, 2, 3 ó 4 sustituyentes seleccionados entre flúor, alquilo C₁₋₄, fluoroalquilo C₁₋₄, alcoxi C₁₋₄ y fluoroalcoxi C₁₋₄; R⁷, R⁸, R⁹, R¹⁰ se seleccionan en forma independiente entre sí entre el grupo que consiste en hidrógeno, halógeno, alquilo C₁₋₄, trimetilsililo, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, cicloalquilo C₃₋₆, o los radicales junto con los átomos de carbono a los cuales están unidos forman un carbociclo saturado de entre 3 y 6 miembros o un heterociclo saturado de entre 3 y 6 miembros con 1 ó 2 heteroátomos no adyacentes como miembros del anillo, donde el carbociclo y el heterociclo no están sustituidos o pueden tener 1, 2, 3 ó 4 sustituyentes seleccionados entre flúor y metilo o los radicales R⁷, R⁸ o los radicales R⁹, R¹⁰ junto con el átomo de carbono al cual están unidos forman un carbociclo saturado de entre 3 y 6 miembros o un heterociclo saturado de entre 3 y 6 miembros con 1 ó 2 heteroátomos no adyacentes como miembros del anillo, donde el carbociclo y el heterociclo no están sustituidos o pueden tener 1, 2, 3 ó 4 sustituyentes seleccionados entre flúor y metilo; Y es un enlace químico, CH₂, O, O-CH₂, NRʸ, NRʸ-CH₂, NRʸ-S(O)₂, S, S(O), S(O)₂, 1,2-etandiilo, 1,2-etendiilo o 1,2-etindiilo, donde Rʸ se selecciona entre el grupo que consiste en hidrógeno, alquilo C₁₋₄, alquil C₁₋₄carbonilo, alquil C₁₋₄sulfonilo, fluoroalquil C₁₋₄sulfonilo; Cyc es un radical seleccionado entre el grupo que consiste en fenilo, naftilo, radicales monocarbocíclicos saturados o parcialmente insaturados de entre 4 y 8 miembros, radicales bicarbocíclicos saturados o parcialmente insaturados de entre 7 y 10 miembros, radicales heteromonocíclicos saturados o parcialmente insaturados de entre 4 y 8 miembros, radicales heterobicíclicos saturados o parcialmente insaturados de entre 7 y 10 miembros, hetarilo monocíclico de 5 ó 6 miembros, y hetarilo bicíclico de entre 8 y 10 miembros, donde los radicales heteromonocíclicos y heterobicíclicos saturados o parcialmente insaturados tienen 1 2, 3 ó 4 heteroátomos o grupos que contienen heteroátomos como miembros del anillo, que se seleccionan entre O, S, SO, SO₂ y N, y donde el hetarilo monocíclico de 5 ó 6 miembros y el hetarilo bicíclico de entre 8 y 10 miembros tienen 1, 2, 3 ó 4 heteroátomos como miembros del anillo, que se seleccionan entre O, S y N, donde fenilo, naftilo, los radicales mono- y bicarbocíclicos saturados o parcialmente insaturados, los radicales heteromonocíclicos y heterobicíclicos y los radicales heteroaromáticos mono- y bicíclicos no están sustituidos o tienen 1, 2, 3, 4 ó 5 radicales RC¹ o un radical Y-RC² y 0, 1, 2, 3 ó 4 radicales RC¹; donde RC¹ se selecciona entre hidrógeno, halógeno, OH, CN, NO₂, alquilo C₁₋₄, alcoxi C₁₋₄, alquil C₁₋₄sulfanilo, hidroxi-alquilo C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, alcoxi C₁₋₄-alcoxi C₁₋₄, ciano-alquilo C₁₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, alquil C₁₋₄sulfonilo, C(O)Rᵃ, Z-C(O)ORᵇ, Z-C(O)NRᶜRᵈ, S(O)₂NRᶜRᵈ y Z-NRᵉRᶠ, donde Rᵃ se selecciona entre el grupo que consiste en alquilo C₁₋₄ y fluoroalquilo C₁₋₄, Rᵇ se
ARP120102358A 2011-06-30 2012-06-29 Compuestos inhibidores de la fosfodiesterasa tipo 10a AR086817A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161503040P 2011-06-30 2011-06-30

Publications (1)

Publication Number Publication Date
AR086817A1 true AR086817A1 (es) 2014-01-22

Family

ID=46456562

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120102358A AR086817A1 (es) 2011-06-30 2012-06-29 Compuestos inhibidores de la fosfodiesterasa tipo 10a

Country Status (25)

Country Link
US (2) US9938269B2 (es)
EP (1) EP2726479A1 (es)
JP (1) JP2014518237A (es)
KR (1) KR20140050028A (es)
CN (1) CN103958504B (es)
AR (1) AR086817A1 (es)
AU (1) AU2012277802A1 (es)
BR (1) BR112013033696A2 (es)
CA (1) CA2839655A1 (es)
CL (1) CL2013003731A1 (es)
CO (1) CO6870032A2 (es)
CR (1) CR20140023A (es)
DO (1) DOP2013000315A (es)
EC (1) ECSP14013188A (es)
GT (1) GT201300324A (es)
MX (1) MX2013015390A (es)
NZ (1) NZ618930A (es)
PE (1) PE20141308A1 (es)
PH (1) PH12013502620A1 (es)
RU (1) RU2014102962A (es)
SG (1) SG10201605196PA (es)
TW (1) TW201311662A (es)
UY (1) UY34177A (es)
WO (1) WO2013000994A1 (es)
ZA (1) ZA201309561B (es)

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2632461A4 (en) * 2010-10-29 2014-04-02 Merck Sharp & Dohme Isoindolinone PDE10 INHIBITORS
EP2841435B1 (en) * 2012-04-25 2017-09-06 RaQualia Pharma Inc. Pyrrolopyridinone derivatives as ttx-s blockers
DE102012016908A1 (de) 2012-08-17 2014-02-20 Aicuris Gmbh & Co. Kg Tris-(Hetero)Aryl-Pyrazole und ihre Verwendung
US9200005B2 (en) 2013-03-13 2015-12-01 AbbVie Deutschland GmbH & Co. KG Inhibitor compounds of phosphodiesterase type 10A
WO2014140184A1 (en) 2013-03-14 2014-09-18 AbbVie Deutschland GmbH & Co. KG Novel inhibitor compounds of phosphodiesterase type 10a
GB201322334D0 (en) 2013-12-17 2014-01-29 Agency Science Tech & Res Maleimide derivatives as modulators of WNT pathway
RU2016133624A (ru) * 2014-01-31 2018-03-06 Ф. Хоффманн-Ля Рош Аг (гетеро)арилимидазолы/пиразолы для лечения заболеваний нервной системы
SG11201606080SA (en) 2014-02-03 2016-08-30 Vitae Pharmaceuticals Inc Dihydropyrrolopyridine inhibitors of ror-gamma
WO2015177110A1 (en) * 2014-05-22 2015-11-26 F. Hoffmann-La Roche Ag INDOLIN-2-ONE AND 1,3-DIHYDRO-PYRROLO[3,2-c]PYRIDIN-2-ONE DERIVATIVES
TWI713455B (zh) 2014-06-25 2020-12-21 美商伊凡克特治療公司 ＭｎＫ抑制劑及其相關方法
CN107074852B (zh) 2014-10-14 2019-08-16 生命医药有限责任公司 ROR-γ的二氢吡咯并吡啶抑制剂
US9845308B2 (en) 2014-11-05 2017-12-19 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ROR-gamma
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
US20160304496A1 (en) 2015-04-17 2016-10-20 Abbvie Inc. Indazolones as modulators of tnf signaling
US9879016B2 (en) 2015-04-17 2018-01-30 Abbvie Inc. Indazolones as modulators of TNF signaling
WO2016168641A1 (en) 2015-04-17 2016-10-20 Abbvie Inc. Tricyclic modulators of tnf signaling
US10301261B2 (en) 2015-08-05 2019-05-28 Vitae Pharmaceuticals, Llc Substituted indoles as modulators of ROR-gamma
HUE068392T2 (hu) 2015-10-21 2024-12-28 Otsuka Pharma Co Ltd Benzolaktám vegyületek mint fehérje kináz gátlók
EP3368530A1 (en) 2015-10-29 2018-09-05 Effector Therapeutics Inc. Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of mnk1 and mnk2
EP3368533A1 (en) 2015-10-29 2018-09-05 Effector Therapeutics Inc. Pyrrolo-, pyrazolo-, imidazo-pyrimidine and pyridine compounds that inhibit mnk1 and mnk2
US10000487B2 (en) 2015-11-20 2018-06-19 Effector Therapeutics, Inc. Heterocyclic compounds that inhibit the kinase activity of Mnk useful for treating various cancers
EP3377482B1 (en) 2015-11-20 2021-05-12 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
TWI757266B (zh) 2016-01-29 2022-03-11 美商維它藥物有限責任公司 ＲＯＲ－γ調節劑
MY196648A (en) 2016-02-05 2023-04-27 Denali Therapeutics Inc Inhibitors of Receptor-Interacting Protein Kinase 1
US9481674B1 (en) 2016-06-10 2016-11-01 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
CN110383066B (zh) 2016-12-09 2023-03-31 戴纳立制药公司 化合物、组合物和方法
EA201991894A1 (ru) 2017-02-14 2020-02-05 Эффектор Терапьютикс, Инк. ПИПЕРИДИН-ЗАМЕЩЕННЫЕ ИНГИБИТОРЫ Mnk И СВЯЗАННЫЕ С НИМИ СПОСОБЫ
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
US11584744B2 (en) * 2017-06-23 2023-02-21 University Of Washington Inhibitors of type 1 methionyl-tRNA synthetase and methods of using them
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
MA49685A (fr) 2017-07-24 2021-04-14 Vitae Pharmaceuticals Llc INHIBITEURS DE ROR gamma
PT3684767T (pt) 2017-09-22 2024-07-29 Jubilant Epipad LLC Compostos heterocíclicos como inibidores de pad
CA3076476A1 (en) 2017-10-18 2019-04-25 Jubilant Epipad LLC Imidazo-pyridine compounds as pad inhibitors
US11629135B2 (en) 2017-11-06 2023-04-18 Jubilant Prodell Llc Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation
AU2018372211B2 (en) 2017-11-24 2023-02-02 Jubilant Episcribe LLC, Heterocyclic compounds as PRMT5 inhibitors
KR20250073542A (ko) 2018-03-09 2025-05-27 리커리엄 아이피 홀딩스, 엘엘씨 치환된 1,2-다이하이드로-3H-피라졸로[3,4-d]피리미딘-3-온
JP7279063B6 (ja) 2018-03-13 2024-02-15 ジュビラント プローデル エルエルシー Ｐｄ１／ｐｄ－ｌ１相互作用／活性化の阻害剤としての二環式化合物
EP3856185A1 (en) 2018-09-28 2021-08-04 Takeda Pharmaceutical Company Limited Balipodect for treating or preventing autism spectrum disorders
JP2022505846A (ja) 2018-10-24 2022-01-14 イーフェクター セラピューティクス， インコーポレイテッド Ｍｎｋ阻害剤の結晶形態
WO2020102150A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
WO2020102198A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
CN109608444B (zh) * 2018-11-27 2022-02-11 中国药科大学 含异吲哚啉酮的erk抑制剂及其制备方法与用途
WO2021032935A1 (en) * 2019-08-21 2021-02-25 Kalvista Pharmaceuticals Limited Enzyme inhibitors
US11005924B1 (en) 2020-04-01 2021-05-11 Netapp, Inc. Disparity of quality of service (QoS) settings of volumes across a cluster
US11140219B1 (en) 2020-04-07 2021-10-05 Netapp, Inc. Quality of service (QoS) setting recommendations for volumes across a cluster
US12029718B2 (en) 2021-11-09 2024-07-09 Cct Sciences, Llc Process for production of essentially pure delta-9-tetrahydrocannabinol
US20240076291A1 (en) * 2020-11-24 2024-03-07 Merck Sharp & Dohme Llc Modified isoindolinones as glucosylceramide synthase inhibitors
US11693563B2 (en) 2021-04-22 2023-07-04 Netapp, Inc. Automated tuning of a quality of service setting for a distributed storage system based on internal monitoring
AU2023206890A1 (en) 2022-01-12 2024-08-22 Denali Therapeutics Inc. Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2, 3,4,5- tetrahydropyrido [3,2-b] [l,4]oxazepin-3-yl)-4h-l,2,4-triazole-3-carboxamide
CN114805052A (zh) * 2022-06-07 2022-07-29 华衍化学(上海)有限公司 一种合成对乙烯基苯甲酸的方法

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1560726A (en) * 1976-04-28 1980-02-06 Beecham Group Ltd Isothiazolo-pyridines
JPH02268162A (ja) * 1989-04-10 1990-11-01 Fujisawa Pharmaceut Co Ltd ジフェニルピリジン誘導体
US6339093B1 (en) 1999-10-08 2002-01-15 Hoffmann-La Roche Inc. Isoquinoline derivatives
US20030032579A1 (en) 2001-04-20 2003-02-13 Pfizer Inc. Therapeutic use of selective PDE10 inhibitors
DE10134482A1 (de) 2001-07-16 2003-01-30 Bayer Ag Substituierte Isoindole und ihre Verwendung
US20030166476A1 (en) 2002-01-31 2003-09-04 Winemiller Mark D. Lubricating oil compositions with improved friction properties
AU2003286711A1 (en) 2002-10-25 2004-05-13 Vertex Pharmaceuticals Incorporated Indazolinone compositions useful as kinase inhibitors
CA2534432A1 (en) 2003-07-31 2005-02-10 Bayer Pharmaceuticals Corporation Methods for treating diabetes and related disorders using pde10a inhibitors
MXPA06014236A (es) 2004-06-07 2007-02-14 Pfizer Prod Inc Inhibicion de la fosfodiesterasa 10 como tratamiento para las afecciones relacionadas con el sindrome metabolico y con la obesidad.
US7244759B2 (en) 2004-07-28 2007-07-17 Celgene Corporation Isoindoline compounds and methods of making and using the same
AU2005282721A1 (en) 2004-09-03 2006-03-16 Memory Pharmaceuticals Corporation 4-substituted 4, 6-dialkoxy-cinnoline derivatives as phospodiesterase 10 inhibitors for the treatment of psychiatric or neurological syndroms
ATE460415T1 (de) 2004-11-29 2010-03-15 Warner Lambert Co Therapeutische pyrazoloä3,4-büpyridine und - indazole
CN101228164A (zh) * 2005-05-20 2008-07-23 布里斯托尔-迈尔斯·斯奎布公司 二肽基肽酶iv的吡咯并吡啶类抑制剂及方法
US7521557B2 (en) 2005-05-20 2009-04-21 Bristol-Myers Squibb Company Pyrrolopyridine-based inhibitors of dipeptidyl peptidase IV and methods
AU2006279548A1 (en) 2005-08-16 2007-02-22 Amgen, Inc. Phosphodiesterase 10 inhibitors
NL2000397C2 (nl) 2006-01-05 2007-10-30 Pfizer Prod Inc Bicyclische heteroarylverbindingen als PDE10 inhibitoren.
WO2007082546A1 (en) 2006-01-20 2007-07-26 H. Lundbeck A/S Use of tofisopam as a pde10a inhibitor
US20100222353A1 (en) 2006-01-27 2010-09-02 Pfizer Products Inc. Aminophthalazine derivative compounds
MX2008010668A (es) 2006-02-21 2008-10-01 Amgen Inc Derivados de cinolina como inhibidores de fosfodiesterasa 10.
MX2008010671A (es) 2006-02-21 2008-10-01 Amgen Inc Derivados de cinolina como inhibidores de fosfodiesterasa 10.
EP1996587A1 (en) 2006-02-23 2008-12-03 Pfizer Products Incorporated Substituted quinazolines as pde10 inhibitors
US20070287707A1 (en) 2006-02-28 2007-12-13 Arrington Mark P Phosphodiesterase 10 inhibitors
US20070265258A1 (en) 2006-03-06 2007-11-15 Ruiping Liu Quinazoline derivatives as phosphodiesterase 10 inhibitors
AU2007223801A1 (en) 2006-03-08 2007-09-13 Amgen Inc. Quinoline and isoquinoline derivatives as phosphodiesterase 10 inhibitors
TW200806625A (en) 2006-05-26 2008-02-01 Astrazeneca Ab Therapeutic compounds
TW200817400A (en) 2006-05-30 2008-04-16 Elbion Ag Pyrido [3,2-e] pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them
TW200815436A (en) 2006-05-30 2008-04-01 Elbion Ag 4-amino-pyrido[3,2-e]pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them
CA2654394A1 (en) 2006-06-26 2008-01-03 Pfizer Products Inc. Tricyclic heteroaryl compounds as pde10 inhibitors
US20080090834A1 (en) 2006-07-06 2008-04-17 Pfizer Inc Selective azole pde10a inhibitor compounds
SI2057153T1 (sl) 2006-07-10 2012-12-31 H. Lundbeck A/S (3-ril-piperazin-1-il) derivati 6,7-dialkoksikuinazolin, 6,7-dialkoksiftalazin in 6,7-dialkoksiizokuinolin
WO2008020302A2 (en) 2006-08-17 2008-02-21 Pfizer Products Inc. Heteroaromatic quinoline-based compounds as phosphodiesterase (pde) inhibitors
US20090062277A1 (en) 2007-08-21 2009-03-05 Essa Hu Phosphodiesterase 10 inhibitors
US20090062291A1 (en) 2007-08-22 2009-03-05 Essa Hu Phosphodiesterase 10 inhibitors
WO2009029214A1 (en) 2007-08-23 2009-03-05 Amgen Inc. Isoquinolone derivatives as phosphodiesterase 10 inhibitors
TW200918519A (en) 2007-09-19 2009-05-01 Lundbeck & Co As H Cyanoisoquinoline
WO2009068320A1 (en) 2007-11-30 2009-06-04 Elbion Gmbh Aryl and heteroaryl fused imidazo (1,5-a) pyrazines as inhibitors of phosphodiesterase 10
US20090143361A1 (en) 2007-11-30 2009-06-04 Elbion Gmbh Pyrido[3,2-E]Pyrazines, Process For Preparing The Same, And Their Use As Inhibitors Of Phosphodiesterase 10
CN101918408A (zh) 2007-11-30 2010-12-15 惠氏有限责任公司 作为磷酸二酯酶10的抑制剂的芳基和杂芳基稠合的咪唑并[1,5-a]吡嗪
WO2009068246A2 (en) 2007-11-30 2009-06-04 Elbion Gmbh Methods of treating obesity and metabolic disorders
US20110319411A1 (en) 2008-12-08 2011-12-29 Sirtis Pharmaceuticals, Inc. Isoindolinone and related analogs as sirtuin modulators
WO2010138585A1 (en) 2009-05-29 2010-12-02 Merck Sharp & Dohme Corp. Pyrimidinones as pde10 inhibitors
TWI481607B (zh) * 2009-12-17 2015-04-21 Lundbeck & Co As H 作為ｐｄｅ１０ａ酵素抑制劑的２－芳基咪唑衍生物
TWI485151B (zh) * 2009-12-17 2015-05-21 Lundbeck & Co As H 作為ｐｄｅ１０ａ酵素抑制劑之雜芳香族苯基咪唑衍生物
EP2632461A4 (en) * 2010-10-29 2014-04-02 Merck Sharp & Dohme Isoindolinone PDE10 INHIBITORS
ES2623387T3 (es) 2010-12-20 2017-07-11 Pfizer Inc. Nuevos compuestos de piridina condensada como inhibidores de la cinasa de caseína

Also Published As

Publication number Publication date
JP2014518237A (ja) 2014-07-28
PE20141308A1 (es) 2014-10-26
BR112013033696A2 (pt) 2016-08-30
CL2013003731A1 (es) 2014-10-10
UY34177A (es) 2013-01-31
US9938269B2 (en) 2018-04-10
EP2726479A1 (en) 2014-05-07
MX2013015390A (es) 2014-07-14
AU2012277802A8 (en) 2014-03-06
ZA201309561B (en) 2014-08-27
US20130005705A1 (en) 2013-01-03
AU2012277802A1 (en) 2014-01-09
CA2839655A1 (en) 2013-01-03
DOP2013000315A (es) 2014-04-15
CR20140023A (es) 2014-08-21
CN103958504A (zh) 2014-07-30
PH12013502620A1 (en) 2014-02-03
TW201311662A (zh) 2013-03-16
US20180222905A1 (en) 2018-08-09
CO6870032A2 (es) 2014-02-20
SG10201605196PA (en) 2016-08-30
GT201300324A (es) 2014-09-26
NZ618930A (en) 2015-05-29
ECSP14013188A (es) 2014-12-30
RU2014102962A (ru) 2015-08-10
WO2013000994A1 (en) 2013-01-03
CN103958504B (zh) 2016-10-12
KR20140050028A (ko) 2014-04-28

Similar Documents

Publication Publication Date Title
AR086817A1 (es) Compuestos inhibidores de la fosfodiesterasa tipo 10a
AR088801A1 (es) Compuestos inhibidores de la fosfodiesterasa del tipo 10a
AR100438A1 (es) Pirazolopiridinas y pirazolopirimidinas
AR098721A1 (es) Inhibidores de biarilo de tirosina quinasa de bruton
AR110405A1 (es) Compuestos
AR095311A1 (es) 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante
AR090005A1 (es) Imidazo[1,2-a]pirimidinas y piridinas sustituidas
AR106595A1 (es) COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g
AR088423A1 (es) Ligadores p1 ciclicos como inhibidores del factor xia
AR098136A1 (es) Compuestos de heteroarilo como inhibidores de btk y usos de los mismos
AR095312A1 (es) Compuestos de biarilamida como inhibidores de cinasa
AR107032A1 (es) Inhibidores bicíclicos de pad4
AR090220A1 (es) Inhibidores de serina/treonina cinasa
AR096979A1 (es) Derivados de pirrol, su procedimiento de preparación y las composiciones farmacéuticas que los contienen
AR095464A1 (es) Compuestos de heteroarilo y usos de los mismos
AR112290A1 (es) Dinucleótidos cíclicos como agentes anticáncer
AR094557A1 (es) Tiadiazol, análogos del mismo, y métodos para el tratamiento de condiciones relacionadas con deficiencia de smn
AR092869A1 (es) Alcoxipirazoles como activadores de guanilato ciclasa soluble
AR094346A1 (es) Derivados de azaindol como inhibidores de las proteína quinasas
AR106301A1 (es) Composiciones de pirrolpirimidina como inhibidores de quinasas
AR107042A1 (es) Inhibidores de la tirosina quinasa de bruton y métodos de su uso
AR095267A1 (es) Compuestos inhibidores de la fosfodiesterasa del tipo 10a
AR116114A1 (es) Amidas heterocíclicas de entre 5 y 7 miembros como inhibidores de jak
AR103232A1 (es) ANTAGONISTAS DE TGFbR
AR113888A1 (es) Derivados de indol macrocíclicos sustituidos

Legal Events

Date Code Title Description
FB Suspension of granting procedure