[go: up one dir, main page]

AR101175A1 - Imidazopiridinas e imidazopirazinas como inhibidores de lsd1 - Google Patents

Imidazopiridinas e imidazopirazinas como inhibidores de lsd1

Info

Publication number
AR101175A1
AR101175A1 ARP150102198A ARP150102198A AR101175A1 AR 101175 A1 AR101175 A1 AR 101175A1 AR P150102198 A ARP150102198 A AR P150102198A AR P150102198 A ARP150102198 A AR P150102198A AR 101175 A1 AR101175 A1 AR 101175A1
Authority
AR
Argentina
Prior art keywords
nrc8rd8
alkyl
nrc8c
ora8
independently selected
Prior art date
Application number
ARP150102198A
Other languages
English (en)
Inventor
Yu Zhiyong
Lajkiewicz Neil
Konkol Leah
Zhang Colin
Yao Wenquing
Xu Meizhong
Lu Liang
Wu Liangxing
Original Assignee
Incyte Corp
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 Incyte Corp filed Critical Incyte Corp
Publication of AR101175A1 publication Critical patent/AR101175A1/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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente se refiere a imidazo[1,5-a]piridina y derivados de imidazo[1,5-a]pirazina que son inhibidores de LSD1 útiles en el tratamiento de enfermedades tales como cáncer. Reivindicación 1: Un compuesto de fórmula (1), o una de sus sales farmacéuticamente aceptables, caracterizado porque: X es N o CRX; el anillo A es arilo C₆₋₁₀ o heteroarilo de 5 - 10 miembros que comprende carbono y 1, 2, 3, ó 4 heteroátomos seleccionados de N, O, y S, donde dicho arilo C₆₋₁₀ y heteroarilo de 5 - 10 miembros están opcionalmente sustituidos con 1, 2, 3, ó 4 sustituyentes seleccionados de modo independiente de RA; el anillo B es arilo C₆₋₁₀; heteroarilo de 5 - 10 miembros que comprende carbono y 1, 2, 3 ó 4 heteroátomos seleccionados de N, O, y S; cicloalquilo C₃₋₁₀; o heterocicloalquilo de 4 - 10 miembros que comprende carbono y 1, 2, 3 ó 4 heteroátomos seleccionados de N, O, y S; donde dicho arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros, cicloalquilo C₃₋₁₀, y heterocicloalquilo de 4 - 10 miembros están opcionalmente sustituidos con 1, 2, 3, ó 4 sustituyentes seleccionados de modo independiente de RB; R¹ es halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, Cy¹, CN, ORᵃ¹, SRᵃ¹, C(O)Rᵇ¹, C(O)NRᶜ¹Rᵈ¹, C(O)ORᵃ¹, OC(O)Rᵇ¹, OC(O)NRᶜ¹Rᵈ¹, NRᶜ¹Rᵈ¹, NRᶜ¹C(O)Rᵇ¹, NRᶜ¹C(O)ORᵃ¹, NRᶜ¹C(O)NRᶜ¹Rᵈ¹, C(=NRᵉ¹)Rᵇ¹, C(=NRᵉ¹)NRᶜ¹Rᵈ¹, NRᶜ¹C(=NRᵉ¹)NRᶜ¹Rᵈ¹, NRᶜ¹S(O)Rᵇ¹, NRᶜ¹S(O)₂Rᵇ¹, NRᶜ¹S(O)₂NRᶜ¹Rᵈ¹, S(O)Rᵇ¹, S(O)NRᶜ¹Rᵈ¹, S(O)₂Rᵇ¹, y S(O)₂NRᶜ¹Rᵈ¹; donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, y alquinilo C₂₋₆ están opcionalmente sustituidos con 1, 2, ó 3 sustituyentes seleccionados de modo independiente de Cy¹, halo, CN, ORᵃ¹, SRᵃ¹, C(O)Rᵇ¹, C(O)NRᶜ¹Rᵈ¹, C(O)ORᵃ¹, OC(O)Rᵇ¹, OC(O)NRᶜ¹Rᵈ¹, NRᶜ¹Rᵈ¹, NRᶜ¹C(O)Rᵇ¹, NRᶜ¹C(O)ORᵃ¹, NRᶜ¹C(O)NRᶜ¹Rᵈ¹, C(=NRᵉ¹)Rᵇ¹, C(=NRᵉ¹)NRᶜ¹Rᵈ¹, NRᶜ¹C(=NRᵉ¹)NRᶜ¹Rᵈ¹, NRᶜ¹S(O)Rᵇ¹, NRᶜ¹S(O)₂Rᵇ¹, NRᶜ¹S(O)₂NRᶜ¹Rᵈ¹, S(O)Rᵇ¹, S(O)NRᶜ¹Rᵈ¹, S(O)₂Rᵇ¹ y S(O)₂NRᶜ¹Rᵈ¹; R³ es H, halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, Cy², CN, ORᵃ³, SRᵃ³, C(O)Rᵇ³, C(O)NRᶜ³Rᵈ³, C(O)ORᵃ³, OC(O)Rᵇ³, OC(O)NRᶜ³Rᵈ³, NRᶜ³Rᵈ³, NRᶜ³C(O)Rᵇ³, NRᶜ³C(O)ORᵃ³, NRᶜ³C(O)NRᶜ³Rᵈ³, C(=NRᵉ³)Rᵇ³, C(=NRᵉ³)NRᶜ³Rᵈ³, NRᶜ³C(=NRᵉ³)NRᶜ³Rᵈ³, NRᶜ³S(O)Rᵇ³, NRᶜ³S(O)₂Rᵇ³, NRᶜ³S(O)₂NRᶜ³Rᵈ³, S(O)Rᵇ³, S(O)NRᶜ³Rᵈ³, S(O)₂Rᵇ³, y S(O)₂NRᶜ³Rᵈ³, donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, y alquinilo C₂₋₆ están opcionalmente sustituidos con 1, 2, ó 3 sustituyentes seleccionados de Cy², halo, CN, ORᵃ³, SRᵃ³, C(O)Rᵇ³, C(O)NRᶜ³Rᵈ³, C(O)ORᵃ³, OC(O)Rᵇ³, OC(O)NRᶜ³Rᵈ³, NRᶜ³Rᵈ³, NRᶜ³C(O)Rᵇ³, NRᶜ³C(O)ORᵃ³, NRᶜ³C(O)NRᶜ³Rᵈ³, C(=NRᵉ³)Rᵇ³, C(=NRᵉ³)NRᶜ³Rᵈ³, NRᶜ³C(=NRᵉ³)NRᶜ³Rᵈ³, NRᶜ³S(O)Rᵇ³, NRᶜ³S(O)₂Rᵇ³, NRᶜ³S(O)₂NRᶜ³Rᵈ³, S(O)Rᵇ³, S(O)NRᶜ³Rᵈ³, S(O)₂Rᵇ³ y S(O)₂NRᶜ³Rᵈ³; R⁴ es Cy³, H, halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, CN, ORᵃ², SRᵃ², C(O)Rᵇ², C(O)NRᶜ²Rᵈ², C(O)ORᵃ², OC(O)Rᵇ², OC(O)NRᶜ²Rᵈ², NRᶜ²Rᵈ², NRᶜ²C(O)Rᵇ², NRᶜ²C(O)ORᵃ², NRᶜ²C(O)NRᶜ²Rᵈ², C(=NRᵉ²)Rᵇ², C(=NRᵉ²)NRᶜ²Rᵈ², NRᶜ²C(=NRᵉ²)NRᶜ²Rᵈ², NRᶜ²S(O)Rᵇ², NRᶜ²S(O)₂Rᵇ², NRᶜ²S(O)₂NRᶜ²Rᵈ², S(O)Rᵇ², S(O)NRᶜ²Rᵈ², S(O)₂Rᵇ², y S(O)₂NRᶜ²Rᵈ²; donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, y alquinilo C₂₋₆ están opcionalmente sustituidos con 1, 2, ó 3 sustituyentes seleccionados de modo independiente de Cy³, halo, CN, ORᵃ², SRᵃ², C(O)Rᵇ², C(O)NRᶜ²Rᵈ², C(O)ORᵃ², OC(O)Rᵇ², OC(O)NRᶜ²Rᵈ², NRᶜ²Rᵈ², NRᶜ²C(O)Rᵇ², NRᶜ²C(O)ORᵃ², NRᶜ²C(O)NRᶜ²Rᵈ², C(=NRᵉ²)Rᵇ², C(=NRᵉ²)NRᶜ²Rᵈ², NRᶜ²C(=NRᵉ²)NRᶜ²Rᵈ², NRᶜ²S(O)Rᵇ², NRᶜ²S(O)₂Rᵇ², NRᶜ²S(O)₂NRᶜ²Rᵈ², S(O)Rᵇ², S(O)NRᶜ²Rᵈ², S(O)₂Rᵇ² y S(O)₂NRᶜ²Rᵈ²; cada RA se selecciona de modo independiente de halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, CN, NO₂, ORᵃ⁴, SRᵃ⁴, C(O)Rᵇ⁴, C(O)NRᶜ⁴Rᵈ⁴, C(O)ORᵃ⁴, OC(O)Rᵇ⁴, OC(O)NRᶜ⁴Rᵈ⁴, NRᶜ⁴Rᵈ⁴, NRᶜ⁴C(O)Rᵇ⁴, NRᶜ⁴C(O)ORᵃ⁴, NRᶜ⁴C(O)NRᶜ⁴Rᵈ⁴, C(=NRᵉ⁴)Rᵇ⁴, C(=NRᵉ⁴)NRᶜ⁴Rᵈ⁴, NRᶜ⁴C(=NRᵉ⁴)NRᶜ⁴Rᵈ⁴, NRᶜ⁴S(O)Rᵇ⁴, NRᶜ⁴S(O)₂Rᵇ⁴, NRᶜ⁴S(O)₂NRᶜ⁴Rᵈ⁴, S(O)Rᵇ⁴, S(O)NRᶜ⁴Rᵈ⁴, S(O)₂Rᵇ⁴, y S(O)₂NRᶜ⁴Rᵈ⁴, donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, y alquinilo C₂₋₆ están opcionalmente sustituidos con 1, 2, ó 3, sustituyentes seleccionados de modo independiente de halo, haloalquilo C₁₋₆, CN, NO₂, ORᵃ⁴, SRᵃ⁴, C(O)Rᵇ⁴, C(O)NRᶜ⁴Rᵈ⁴, C(O)ORᵃ⁴, OC(O)Rᵇ⁴, OC(O)NRᶜ⁴Rᵈ⁴, NRᶜ⁴Rᵈ⁴, NRᶜ⁴C(O)Rᵇ⁴, NRᶜ⁴C(O)ORᵃ⁴, NRᶜ⁴C(O)NRᶜ⁴Rᵈ⁴, C(=NRᵉ⁴)Rᵇ⁴, C(=NRᵉ⁴)NRᶜ⁴Rᵈ⁴, NRᶜ⁴C(=NRᵉ⁴)NRᶜ⁴Rᵈ⁴, NRᶜ⁴S(O)Rᵇ⁴, NRᶜ⁴S(O)₂Rᵇ⁴, NRᶜ⁴S(O)₂NRᶜ⁴Rᵈ⁴, S(O)Rᵇ⁴, S(O)NRᶜ⁴Rᵈ⁴, S(O)₂Rᵇ⁴ y S(O)₂NRᶜ⁴Rᵈ⁴; cada RB se selecciona de modo independiente de Cy⁴, halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, =O, CN, NO₂, ORᵃ⁵, SRᵃ⁵, C(O)Rᵇ⁵, C(O)NRᶜ⁵Rᵈ⁵, C(O)ORᵃ⁵, OC(O)Rᵇ⁵, OC(O)NRᶜ⁵Rᵈ⁵, NRᶜ⁵Rᵈ⁵, NRᶜ⁵C(O)Rᵇ⁵, NRᶜ⁵C(O)ORᵃ⁵, NRᶜ⁵C(O)NRᶜ⁵Rᵈ⁵, C(=NRᵉ⁵)Rᵇ⁵, C(=NRᵉ⁵)NRᶜ⁵Rᵈ⁵, NRᶜ⁵C(=NRᵉ⁵)NRᶜ⁵Rᵈ⁵, NRᶜ⁵S(O)Rᵇ⁵, NRᶜ⁵S(O)₂Rᵇ⁵, NRᶜ⁵S(O)₂NRᶜ⁵Rᵈ⁵, S(O)Rᵇ⁵, S(O)NRᶜ⁵Rᵈ⁵, S(O)₂Rᵇ⁵ y S(O)₂NRᶜ⁵Rᵈ⁵, donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, y alquinilo C₂₋₆ están opcionalmente sustituidos con 1, 2, ó 3 sustituyentes seleccionados de modo independiente de Cy⁴, halo, haloalquilo C₁₋₆, CN, NO₂, ORᵃ⁵, SRᵃ⁵, C(O)Rᵇ⁵, C(O)NRᶜ⁵Rᵈ⁵, C(O)ORᵃ⁵, OC(O)Rᵇ⁵, OC(O)NRᶜ⁵Rᵈ⁵, NRᶜ⁵Rᵈ⁵, NRᶜ⁵C(O)Rᵇ⁵, NRᶜ⁵C(O)ORᵃ⁵, NRᶜ⁵C(O)NRᶜ⁵Rᵈ⁵, C(=NRᵉ⁵)Rᵇ⁵, C(=NRᵉ⁵)NRᶜ⁵Rᵈ⁵, NRᶜ⁵C(=NRᵉ⁵)NRᶜ⁵Rᵈ⁵, NRᶜ⁵S(O)Rᵇ⁵, NRᶜ⁵S(O)₂Rᵇ⁵, NRᶜ⁵S(O)₂NRᶜ⁵Rᵈ⁵, S(O)Rᵇ⁵, S(O)NRᶜ⁵Rᵈ⁵, S(O)₂Rᵇ⁵, y S(O)₂NRᶜ⁵Rᵈ⁵; RX es H, halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, CN, ORᵃ⁸, SRᵃ⁸, C(O)Rᵇ⁸, C(O)NRᶜ⁸Rᵈ⁸, C(O)ORᵃ⁸, OC(O)Rᵇ⁸, OC(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)Rᵇ⁸, NRᶜ⁸C(O)ORᵃ⁸, NRᶜ⁸C(O)NRᶜ⁸Rᵈ⁸, C(=NRᵉ⁸)Rᵇ⁸, C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, NRᶜ⁸S(O)Rᵇ⁸, NRᶜ⁸S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂NRᶜ⁸Rᵈ⁸, S(O)Rᵇ⁸, S(O)NRᶜ⁸Rᵈ⁸, S(O)₂Rᵇ⁸ o S(O)₂NRᶜ⁸Rᵈ⁸; cada Cy¹, Cy³, Cy⁴, y Cy⁵ se selecciona de modo independiente de arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, y heterocicloalquilo de 4 - 10 miembros, cada uno de los cuales está opcionalmente sustituido con 1, 2, 3, ó 4 sustituyentes seleccionados de modo independiente de RCʸ; cada Cy² se selecciona de modo independiente de fenilo, cicloalquilo C₃₋₇, heteroarilo de 5 - 6 miembros, y heterocicloalquilo de 4 - 7 miembros, cada uno de los cuales está opcionalmente sustituido con 1, 2, ó 3 sustituyentes seleccionados de modo independiente de RCʸ; cada RCʸ se selecciona de halo, alquilo C₁₋₄, haloalquilo C₁₋₄, cianoalquilo C₁₋₄, alquenilo C₂₋₆ alquinilo C₂₋₆, fenilo, cicloalquilo C₃₋₇, heteroarilo de 5 - 6 miembros, heterocicloalquilo de 4 - 7 miembros, fenil-alquil C₁₋₄-, cicloalquil C₃₋₇-alquil C₁₋₄-, (heteroarilo de 5 - 6 miembros)-alquil C₁₋₄-, (heterocicloalquilo de 4 - 7 miembros)-alquil C₁₋₄, oxo, CN, NO₂, ORᵃ⁶, SRᵃ⁶, C(O)Rᵇ⁶, C(O)NRᶜ⁶Rᵈ⁶, C(O)ORᵃ⁶, OC(O)Rᵇ⁶, OC(O)NRᶜ⁶Rᵈ⁶, C(=NRᵉ⁶)NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=NRᵉ⁶)NRᶜ⁶Rᵈ⁶, NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(O)Rᵇ⁶, NRᶜ⁶C(O)ORᵃ⁶, NRᶜ⁶C(O)NRᶜ⁶Rᵈ⁶, NRᶜ⁶S(O)Rᵇ⁶, NRᶜ⁶S(O)₂Rᵇ⁶, NRᶜ⁶S(O)₂NRᶜ⁶Rᵈ⁶, S(O)Rᵇ⁶, S(O)NRᶜ⁶Rᵈ⁶, S(O)₂Rᵇ⁶ y S(O)₂NRᶜ⁶Rᵈ⁶, donde dicho alquilo C₁₋₄, alquenilo C₂₋₆, alquinilo C₂₋₆, fenilo, cicloalquilo C₃₋₇, heteroarilo de 5 - 6 miembros, heterocicloalquilo de 4 - 7 miembros, fenil-alquil C₁₋₄-, cicloalquil C₃₋₇-alquil C₁₋₄-, (heteroarilo de 5 - 6 miembros)-alquil C₁₋₄-, y (heterocicloalquilo de 4 -7 miembros)-alquil C₁₋₄- están opcionalmente sustituidos con 1, 2, ó 3 sustituyentes seleccionados de modo independiente de alquilo C₁₋₄, haloalquilo C₁₋₄, cianoalquilo C₁₋₄, halo, CN, NO₂, ORᵃ⁶, SRᵃ⁶, C(O)Rᵇ⁶, C(O)NRᶜ⁶Rᵈ⁶, C(O)ORᵃ⁶, OC(O)Rᵇ⁶, OC(O)NRᶜ⁶Rᵈ⁶, C(=NRᵉ⁶)NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(=NRᵉ⁶)NRᶜ⁶Rᵈ⁶, NRᶜ⁶Rᵈ⁶, NRᶜ⁶C(O)Rᵇ⁶, NRᶜ⁶C(O)ORᵃ⁶, NRᶜ⁶C(O)NRᶜ⁶Rᵈ⁶, NRᶜ⁶S(O)Rᵇ⁶, NRᶜ⁶S(O)₂Rᵇ⁶, NRᶜ⁶S(O)₂NRᶜ⁶Rᵈ⁶, S(O)Rᵇ⁶, S(O)NRᶜ⁶Rᵈ⁶, S(O)₂Rᵇ⁶ y S(O)₂NRᶜ⁶Rᵈ⁶; cada Rᵃ¹ se selecciona de modo independiente de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, y Cy⁵, donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, y alquinilo C₂₋₆ están opcionalmente sustituidos con 1, 2, ó 3 sustituyentes seleccionados de modo independiente de Cy⁵, halo, CN, ORᵃ⁷, SRᵃ⁷, C(O)Rᵇ⁷, C(O)NRᶜ⁷Rᵈ⁷, C(O)ORᵃ⁷, OC(O)Rᵇ⁷, OC(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)Rᵇ⁷, NRᶜ⁷C(O)ORᵃ⁷, NRᶜ⁷C(O)NRᶜ⁷Rᵈ⁷, C(=NRᵉ⁷)Rᵇ⁷, C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, NRᶜ⁷S(O)Rᵇ⁷, NRᶜ⁷S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂NRᶜ⁷Rᵈ⁷, S(O)Rᵇ⁷, S(O)NRᶜ⁷Rᵈ⁷, S(O)₂Rᵇ⁷ y S(O)₂NRᶜ⁷Rᵈ⁷; cada Rᵇ¹, Rᶜ¹, y Rᵈ¹ se selecciona de modo independiente de H, alquilo C₁₋₆, haloalquilo C₁₋₄, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, aril C₆₋₁₀-alquil C₁₋₄-, cicloalquil C₃₋₁₀ alquil C₁₋₄-, (heteroarilo de 5 - 10 miembros)-alquil C₁₋₄-, y (heterocicloalquilo de 4 - 10 miembros)-alquil C₁₋₄-, donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, aril C₆₋₁₀-alquil C₁₋₄-, cicloalquil C₃₋₁₀-alquil C₁₋₄, (heteroarilo de 5 - 10 miembros)-alquil C₁₋₄-, y (heterocicloalquilo de 4 - 10 miembros)-alquil C₁₋₄- están opcionalmente sustituidos con 1, 2, 3, 4, ó 5 sustituyentes seleccionados de modo independiente de alquilo C₁₋₄, haloalquilo C₁₋₄, cianoalquilo C₁₋₄, halo, CN, ORᵃ⁸, SRᵃ⁸, C(O)Rᵇ⁸, C(O)NRᶜ⁸Rᵈ⁸, C(O)ORᵃ⁸, OC(O)Rᵇ⁸, OC(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)Rᵇ⁸, NRᶜ⁸C(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)ORᵃ⁸, C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, S(O)Rᵇ⁸, S(O)NRᶜ⁸Rᵈ⁸, S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂NRᶜ⁸Rᵈ⁸ y S(O)₂NRᶜ⁸Rᵈ⁸; o Rᶜ¹ y Rᵈ¹ juntos con un átomo de N al que están unidos forman un grupo heterocicloalquilo de a 4, 5, 6, ó 7 miembros opcionalmente sustituido con 1, 2, ó 3 sustituyentes seleccionados de modo independiente de alquilo C₁₋₆, cicloalquilo C₃₋₇, heterocicloalquilo de 4 - 7 miembros, arilo C₆₋₁₀, heteroarilo de 5 - 6 miembros, haloalquilo C₁₋₆, halo, CN, ORᵃ⁸, SRᵃ⁸, C(O)Rᵇ⁸, C(O)NRᶜ⁸Rᵈ⁸, C(O)ORᵃ⁸, OC(O)Rᵇ⁸, OC(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)Rᵇ⁸, NRᶜ⁸C(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)ORᵃ⁸, C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, S(O)Rᵇ⁸, S(O)NRᶜ⁸Rᵈ⁸, S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂NRᶜ⁸Rᵈ⁸, y S(O)₂NRᶜ⁸Rᵈ⁸, donde dicho alquilo C₁₋₆, cicloalquilo C₃₋₇, heterocicloalquilo de 4 - 7 miembros, arilo C₆₋₁₀, y heteroarilo de 5 - 6 miembros están opcionalmente sustituidos con 1, 2, ó 3 sustituyentes seleccionados de modo independiente de halo, alquilo C₁₋₄, haloalquilo C₁₋₄, cianoalquilo C₁₋₄, CN, ORᵃ⁸, SRᵃ⁸, C(O)Rᵇ⁸, C(O)NRᶜ⁸Rᵈ⁸, C(O)ORᵃ⁸, OC(O)Rᵇ⁸, OC(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)Rᵇ⁸, NRᶜ⁸C(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)ORᵃ⁸, C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, S(O)Rᵇ⁸, S(O)NRᶜ⁸Rᵈ⁸, S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂NRᶜ⁸Rᵈ⁸ y S(O)₂NRᶜ⁸Rᵈ⁸; cada Rᵃ², Rᵇ², Rᶜ², y Rᵈ² se selecciona de modo independiente de H, alquilo C₁₋₆, haloalquilo C₁₋₄, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo Calo, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, aril C₆₋₁₀-alquil C₁₋₄-, cicloalquil C₃₋₁₀-alquil C₁₋₄-, (heteroarilo de 5- 10 miembros)-alquil C₁₋₄-, y (heterocicloalquilo de 4 - 10 miembros)-alquil C₁₋₄-, donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, aril C₆₋₁₀-alquil C₁₋₄-, cicloalquil C₃₋₁₀-alquil C₁₋₄-, (heteroarilo de 5 -10 miembros)-alquil C₁₋₄-, y (heterocicloalquilo de 4 - 10 miembros)-alquil C₁₋₄- están opcionalmente sustituidos con 1, 2, 3, 4, ó 5 sustituyentes seleccionados de modo independiente de alquilo C₁₋₄, haloalquilo C₁₋₄, cianoalquilo C₁₋₄, halo, CN, ORᵃ⁸, SRᵃ⁸, C(O)Rᵇ⁸, C(O)NRᶜ⁸Rᵈ⁸, C(O)ORᵃ⁸, OC(O)Rᵇ⁸, OC(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)Rᵇ⁸, NRᶜ⁸C(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)ORᵃ⁸, C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, S(O)Rᵇ⁸, S(O)NRᶜ⁸Rᵈ⁸, S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂NRᶜ⁸Rᵈ⁸ y S(O)₂NRᶜ⁸Rᵈ⁸, o Rᶜ² y Rᵈ² juntos con un átomo de N al que están unidos forman un grupo heterocicloalquilo de a 4, 5, 6, ó 7 miembros opcionalmente sustituido con 1, 2, ó 3 sustituyentes seleccionados de modo independiente de alquilo C₁₋₆, cicloalquilo C₃₋₇, heterocicloalquilo de 4 - 7 miembros, arilo C₆₋₁₀, heteroarilo de 5 - 6 miembros, haloalquilo C₁₋₆, halo, CN, ORᵃ⁸, SRᵃ⁸, C(O)Rᵇ⁸, C(O)NRᶜ⁸Rᵈ⁸, C(O)ORᵃ⁸, OC(O)Rᵇ⁸, OC(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)Rᵇ⁸, NRᶜ⁸C(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)ORᵃ⁸, C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, S(O)Rᵇ⁸, S(O)NRᶜ⁸Rᵈ⁸, S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂NRᶜ⁸Rᵈ⁸ y S(O)₂NRᶜ⁸Rᵈ⁸, donde dicho alquilo C₁₋₆, cicloalquilo C₃₋₇, heterocicloalquilo de 4 - 7 miembros, arilo C₆₋₁₀, y heteroarilo de 5 - 6 miembros están opcionalmente sustituidos con 1, 2, ó 3 sustituyentes seleccionados de modo independiente de halo, alquilo C₁₋₄, haloalquilo C₁₋₄, cianoalquilo C₁₋₄, CN, ORᵃ⁸, SRᵃ⁸, C(O)Rᵇ⁸, C(O)NRᶜ⁸Rᵈ⁸, C(O)ORᵃ⁸, OC(O)Rᵇ⁸, OC(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)Rᵇ⁸, NRᶜ⁸C(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)ORᵃ⁸, C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, S(O)Rᵇ⁸, S(O)NRᶜ⁸Rᵈ⁸, S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂NRᶜ⁸Rᵈ⁸, y S(O)₂NRᶜ⁸Rᵈ⁸; cada Rᵃ³, Rᵇ³, Rᶜ³, y Rᵈ³ se selecciona de modo independiente de H, alquilo C₁₋₆, haloalquilo C₁₋₄, alquenilo C₂₋₆, y alquinilo C₂₋₆, donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, y alquinilo C₂₋₆ están opcionalmente sustituidos con 1, 2, 3, 4, ó 5 sustituyentes seleccionados de modo independiente de alquilo C₁₋₄, haloalquilo C₁₋₄, cianoalquilo C₁₋₄, halo, CN, ORᵃ⁸, SRᵃ⁸, C(O)Rᵇ⁸, C(O)NRᶜ⁸Rᵈ⁸, C(O)ORᵃ⁸, OC(O)Rᵇ⁸, OC(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)Rᵇ⁸, NRᶜ⁸C(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)ORᵃ⁸, C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, S(O)Rᵇ⁸, S(O)NRᶜ⁸Rᵈ⁸, S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂NRᶜ⁸Rᵈ⁸, y S(O)₂NRᶜ⁸Rᵈ⁸; o Rᶜ³ y Rᵈ³ juntos con un átomo de N al que están unidos forman un grupo heterocicloalquilo de a 4, 5, 6, ó 7 miembros opcionalmente sustituido con 1, 2, ó 3 sustituyentes seleccionados de modo independiente de alquilo C₁₋₆, haloalquilo C₁₋₆, halo, CN, ORᵃ⁸, SRᵃ⁸, C(O)Rᵇ⁸, C(O)NRᶜ⁸Rᵈ⁸, C(O)ORᵃ⁸, OC(O)Rᵇ⁸, OC(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)Rᵇ⁸, NRᶜ⁸C(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)ORᵃ⁸, C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(=NRᵉ⁸)NRᶜ⁸Rᵈ⁸, S(O)Rᵇ⁸, S(O)NRᶜ⁸Rᵈ⁸, S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂Rᵇ⁸, NRᶜ⁸S(O)₂NRᶜ⁸Rᵈ⁸, y S(O)₂NRᶜ⁸Rᵈ⁸; cada Rᵃ⁴, Rᵇ⁴, Rᶜ⁴, y Rᵈ⁴ se selecciona de modo independiente de H, alquilo C₁₋₆, haloalquilo C₁₋₄, alquenilo C₂₋₆, y alquinilo C₂₋₆, donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, y alquinilo C₂₋₆ están opcionalmente sustituidos con 1, 2, 3, 4, ó 5 sustituyentes seleccionados de modo independiente de alquilo C₁₋₄, haloalquilo C₁₋₄, cianoalquilo C₁₋₄, halo, CN, ORᵃ⁸, SRᵃ⁸, C(O)Rᵇ⁸, C(O)NRᶜ⁸Rᵈ⁸, C(O)ORᵃ⁸, OC(O)Rᵇ⁸, OC(O)NRᶜ⁸Rᵈ⁸, NRᶜ⁸Rᵈ⁸, NRᶜ⁸C(O)Rᵇ⁸,
ARP150102198A 2014-07-10 2015-07-10 Imidazopiridinas e imidazopirazinas como inhibidores de lsd1 AR101175A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462022933P 2014-07-10 2014-07-10

Publications (1)

Publication Number Publication Date
AR101175A1 true AR101175A1 (es) 2016-11-30

Family

ID=53682878

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150102198A AR101175A1 (es) 2014-07-10 2015-07-10 Imidazopiridinas e imidazopirazinas como inhibidores de lsd1

Country Status (4)

Country Link
US (3) US9695168B2 (es)
AR (1) AR101175A1 (es)
TW (1) TWI687419B (es)
WO (1) WO2016007731A1 (es)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
PT3105218T (pt) 2014-02-13 2019-12-05 Incyte Corp Ciclopropilaminas como inibidores de lsd1
DK3105226T3 (da) 2014-02-13 2019-10-14 Incyte Corp Cyclopropylaminer som lsd1-inhibitorer
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪
EP3626720A1 (en) 2015-04-03 2020-03-25 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
EP3307909A1 (en) 2015-06-12 2018-04-18 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
KR102710120B1 (ko) 2015-08-12 2024-09-27 인사이트 홀딩스 코포레이션 Lsd1 저해제의 염
SG11201807965YA (en) 2016-03-15 2018-10-30 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of solid tumors
ES3042059T3 (en) 2016-03-16 2025-11-18 Oryzon Genomics Sa Methods to determine kdm1a target engagement and chemoprobes useful therefor
PE20190377A1 (es) 2016-04-22 2019-03-08 Incyte Corp Formulaciones de un inhibidor de lsd 1
EP3246330A1 (en) 2016-05-18 2017-11-22 Istituto Europeo di Oncologia S.r.l. Imidazoles as histone demethylase inhibitors
TW202413340A (zh) 2016-07-12 2024-04-01 美商銳新醫藥公司 作為異位shp2抑制劑之2,5-雙取代型3-甲基吡嗪及2,5,6-三取代型3-甲基吡嗪
HUE063848T2 (hu) 2016-10-26 2024-02-28 Constellation Pharmaceuticals Inc LSD1 gátlók és gyógyászati alkalmazásaik
EP3535420A1 (en) 2016-11-03 2019-09-11 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
RU2019126455A (ru) 2017-01-23 2021-02-24 Революшн Медсинз, Инк. Пиридиновые соединения в качестве аллостерических ингибиторов shp2
SG11201906209SA (en) 2017-01-23 2019-08-27 Revolution Medicines Inc Bicyclic compounds as allosteric shp2 inhibitors
EP3628044B1 (en) 2017-05-15 2023-11-22 The Regents of The University of Michigan Pyrrolo[2,3-c]pyridines and related analogs as lsd-1 inhibitors
DK3661510T3 (da) 2017-08-03 2025-01-02 Oryzon Genomics Sa Fremgangsmåder til behandling af adfærdsændringer
WO2019068326A1 (en) 2017-10-05 2019-04-11 Université D'aix-Marseille INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES
JP2020536881A (ja) 2017-10-12 2020-12-17 レヴォリューション・メディスンズ，インコーポレイテッド アロステリックｓｈｐ２阻害剤としてのピリジン、ピラジンおよびトリアジン化合物
RU2020123241A (ru) 2017-12-15 2022-01-17 Революшн Медсинз, Инк. Полициклические соединения в качестве аллостерических ингибиторов shp2
US11613549B2 (en) 2018-01-23 2023-03-28 Basf Se Bromination of pyridine derivatives
EP3794003A1 (en) 2018-05-15 2021-03-24 The Regents Of The University Of Michigan Imidazo[4,5-c]pyridine compounds as lsd-1 inhibitors
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
CN113498352A (zh) 2019-01-23 2021-10-12 施万生物制药研发Ip有限责任公司 作为jak抑制剂的咪唑并[1,5-a]吡啶、1,2,4-三唑并[4,3-a]吡啶和咪唑并[1,5-a]吡嗪
JP7532386B2 (ja) * 2019-02-01 2024-08-13 ハンミ ファーマシューティカルズ カンパニー リミテッド イミダゾピリジン誘導体化合物及びその用途
CN113365996B (zh) * 2019-02-01 2024-09-03 韩美药品株式会社 咪唑吡啶衍生化合物以及药物组成物
SG11202109159VA (en) 2019-03-20 2021-10-28 Oryzon Genomics Sa Methods of treating borderline personality disorder
JP7535797B2 (ja) 2019-03-20 2024-08-19 オリソン ヘノミクス，ソシエダ アノニマ 化合物バフィデムスタット（ｖａｆｉｄｅｍｓｔａｔ）などｋｄｍ１ａ阻害剤を使用した注意欠陥多動性障害の処置方法
MX2021015508A (es) 2019-06-14 2022-01-31 Janssen Pharmaceutica Nv Carbamatos de piridina y su uso como moduladores del receptor glun2b.
CN112110936B (zh) * 2019-06-20 2021-12-07 沈阳药科大学 四氢喹啉类衍生物及其制备方法和应用
JP2022546908A (ja) 2019-07-05 2022-11-10 オリゾン・ゲノミクス・ソシエダッド・アノニマ Ｋｄｍ１ａ阻害剤を使用した小細胞肺がんの個別化された処置のためのバイオマーカーおよび方法
EP3964204A1 (en) 2020-09-08 2022-03-09 Université d'Aix-Marseille Lsd1 inhibitors for use in the treatment and prevention of fibrosis of tissues
CA3231846A1 (en) 2021-04-08 2022-10-13 Tamara Maes Combinations of lsd1 inhibitors for treating myeloid cancers
CN116836167B (zh) * 2022-03-25 2025-09-09 腾讯科技（深圳）有限公司 咪唑并[1,2-a]吡嗪或吡唑并[1,5-a]嘧啶衍生物及其用途
JP2025516647A (ja) 2022-05-09 2025-05-30 オリゾン・ゲノミクス・ソシエダッド・アノニマ Ｌｓｄ１阻害薬を用いる悪性末梢神経鞘腫（ｍｐｎｓｔ）の治療法
CN119497613A (zh) 2022-05-09 2025-02-21 奥莱松基因组股份有限公司 使用lsd1抑制剂治疗nf1-突变肿瘤的方法
WO2024110649A1 (en) 2022-11-24 2024-05-30 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer
WO2024208187A1 (zh) * 2023-04-03 2024-10-10 上海复星医药（集团）股份有限公司 氮杂芳基化合物及其作为lsd1抑制剂的用途

Family Cites Families (265)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4537889A (en) 1982-12-27 1985-08-27 Eli Lilly And Company Inotropic agents
US4625040A (en) 1984-09-24 1986-11-25 Pennwalt Corporation N-(phenyl) or N-(phenylcyclopropyl)-2,5-dihydro-2-oxo-4[(substituted phenyl)amino]-3-furancarboxamide derivatives
US4614810A (en) 1984-09-24 1986-09-30 Pennwalt Corporation 4,5-dihydro-4-oxo-2-[(2-trans-phenylcyclopropyl)amino]-3-furancarboxylic acids and derivatives thereof
FR2607813B1 (fr) 1986-12-05 1989-03-31 Montpellier I Universite Alkylamino-8 imidazo (1,2-a) pyrazines et derives, leur preparation et leur application en therapeutique
AU622330B2 (en) 1989-06-23 1992-04-02 Takeda Chemical Industries Ltd. Condensed heterocyclic compounds having a nitrogen atom in the bridgehead for use as fungicides
IL96432A0 (en) 1989-11-30 1991-08-16 Schering Ag Pesticidal compositions containing pyridine derivatives and novel pyridine derivatives
FR2662163A1 (fr) 1990-05-16 1991-11-22 Lipha Nouvelles 8-amino-1,2,4-triazolo(4,3-a) pyrazines, procedes de preparation et medicaments les contenant.
EP0649425B1 (en) 1992-06-17 1999-03-10 PHARMACIA & UPJOHN COMPANY Pyridino-, pyrrolidino- and azepino-substituted oximes useful as anti-atherosclerosis and anti-hypercholesterolemic agents
DE4327027A1 (de) 1993-02-15 1994-08-18 Bayer Ag Imidazoazine
FR2711993B1 (fr) 1993-11-05 1995-12-01 Rhone Poulenc Rorer Sa Médicaments contenant des dérivés de 7H-imidazol[1,2-a]pyrazine-8-one, les nouveaux composés et leur préparation.
TR200001728T2 (tr) 1997-11-11 2000-09-21 Ono Pharmaceutical Co., Ltd. Birleşik pirazin türevleri
JP2000319278A (ja) 1999-05-11 2000-11-21 Ono Pharmaceut Co Ltd 縮合ピラジン化合物およびその化合物を有効成分とする薬剤
JP2000319277A (ja) 1999-05-11 2000-11-21 Ono Pharmaceut Co Ltd 縮合ピラジン化合物およびその化合物を有効成分とする薬剤
JP4032566B2 (ja) 1999-06-21 2008-01-16 東レ株式会社 発光素子
JP4041624B2 (ja) 1999-07-21 2008-01-30 三井化学株式会社 有機電界発光素子
JP2001057292A (ja) 1999-08-20 2001-02-27 Toray Ind Inc 発光素子
SE9903611D0 (sv) 1999-10-06 1999-10-06 Astra Ab Novel compounds III
DE19948434A1 (de) 1999-10-08 2001-06-07 Gruenenthal Gmbh Substanzbibliothek enthaltend bicyclische Imidazo-5-amine und/oder bicyclische Imidazo-3-amine
JP4409680B2 (ja) 1999-10-18 2010-02-03 株式会社ヤクルト本社 三環性縮合イミダゾール誘導体
US6403588B1 (en) 2000-04-27 2002-06-11 Yamanouchi Pharmaceutical Co., Ltd. Imidazopyridine derivatives
ES2244613T3 (es) 2000-04-27 2005-12-16 Astellas Pharma Inc. Derivados de imidazopiridina.
EP1294358B1 (en) 2000-06-28 2004-08-18 Smithkline Beecham Plc Wet milling process
HUP0301801A2 (hu) 2000-07-14 2003-09-29 Bristol-Myers Squibb Pharma Company Imidazo[1,2-a]pirazin-származékok és az ezeket tartalmazó gyógyszerkészítmények
DE10050663A1 (de) 2000-10-13 2002-04-18 Gruenenthal Gmbh Verwendung von substituierten Imidazo[1,2-a]pyridin-, -pyrimidin- und pyrazin-3-yl-amin-Derivaten zur Herstellung von Medikamenten zur NOS-Inhibierung
AU2001295992A1 (en) 2000-10-24 2002-05-06 Sankyo Company Limited Imidazopyridine derivatives
JP2002205992A (ja) 2000-11-08 2002-07-23 Takeda Chem Ind Ltd 二環式トリアゾロン誘導体およびそれを含有する除草剤
ES2251518T3 (es) 2000-11-10 2006-05-01 MERCK SHARP & DOHME LTD. Derivados de imidazo-triazina como ligandos para receptores gaba.
EP1343785A2 (de) 2000-12-13 2003-09-17 Basf Aktiengesellschaft Verwendung von substituierten imidazoazinen, neue imidazoazine, verfahren zu deren herstellung, sowie sie enthaltende mittel
EP1217000A1 (en) 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
EP1377549A1 (en) 2001-03-12 2004-01-07 Millennium Pharmaceuticals, Inc. Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor
AR035543A1 (es) 2001-06-26 2004-06-16 Japan Tobacco Inc Agente terapeutico para la hepatitis c que comprende un compuesto de anillo condensado, compuesto de anillo condensado, composicion farmaceutica que lo comprende, compuestos de benzimidazol, tiazol y bifenilo utiles como intermediarios para producir dichos compuestos, uso del compuesto de anillo con
IL159811A0 (en) 2001-07-13 2004-06-20 Neurogen Corp Heteroaryl substituted fused bicyclic heteroaryl compounds as gabaa receptor ligands
US6921762B2 (en) 2001-11-16 2005-07-26 Amgen Inc. Substituted indolizine-like compounds and methods of use
EP1513522A2 (en) 2002-01-18 2005-03-16 Sri International Methods of treating conditions associated with an edg receptor
US20050113283A1 (en) 2002-01-18 2005-05-26 David Solow-Cordero Methods of treating conditions associated with an EDG-4 receptor
WO2004017950A2 (en) 2002-08-22 2004-03-04 Piramed Limited Phosphadidylinositol 3,5-biphosphate inhibitors as anti-viral agents
UA80296C2 (en) 2002-09-06 2007-09-10 Biogen Inc Imidazolopyridines and methods of making and using the same
AU2003301226A1 (en) 2002-12-20 2004-07-22 Pharmacia Corp Acyclic pyrazole compounds for the inhibition of mitogen activated protein kinase-activated protein kinase-2
US7160885B2 (en) 2003-02-10 2007-01-09 Cgi Pharmaceuticals, Inc. Certain 6, 8-(heteroaryl or aryl) disubstituted imidazo[1,2-a]pyrazines as modulators of Hsp90 complex activity
GB0303910D0 (en) 2003-02-20 2003-03-26 Merck Sharp & Dohme Therapeutic agents
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
EP2385040A1 (en) 2003-03-14 2011-11-09 ONO Pharmaceutical Co., Ltd. Nitrogen-containing heterocyclic derivatives and drugs containing the same as the active ingredient
ES2338656T3 (es) 2003-04-11 2010-05-11 High Point Pharmaceuticals, Llc Uso farmaceutico de 1,2,4-triazoles fusionados.
JP2006522750A (ja) 2003-04-11 2006-10-05 ノボ　ノルディスク　アクティーゼルスカブ 代謝性症候群ならびに関連の疾患および障害を治療するために、１１β−ヒドロキシステロイドデヒドロゲナーゼ１型阻害剤および抗高血圧剤を使用する併用療法
AU2004233828B2 (en) 2003-04-24 2009-05-28 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
SE0301653D0 (sv) 2003-06-05 2003-06-05 Astrazeneca Ab Novel compounds
US7132426B2 (en) 2003-07-14 2006-11-07 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
US7538120B2 (en) 2003-09-03 2009-05-26 Array Biopharma Inc. Method of treating inflammatory diseases
EP1663193B1 (en) 2003-09-12 2012-04-04 Merck Serono SA Sulfonamide derivatives for the treatment of diabetes
JP2005089352A (ja) 2003-09-16 2005-04-07 Kissei Pharmaceut Co Ltd 新規なイミダゾ［１，５−ａ］ピラジン誘導体、それを含有する医薬組成物およびそれらの用途
ATE369370T1 (de) 2003-10-10 2007-08-15 Pfizer Prod Inc Substituierte 2h-(1,2,4)triazolo(4,3-a)pyrazine als gsk-3-inhibitoren
US7419978B2 (en) 2003-10-22 2008-09-02 Bristol-Myers Squibb Company Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors
WO2005044793A2 (en) 2003-10-31 2005-05-19 Takeda Pharmaceutical Company Limited Nitrogen-containing fused heterocyclic compounds
EP1698335A4 (en) 2003-12-26 2007-08-01 Ono Pharmaceutical Co AGENT FOR PREVENTING AND / OR TREATING DISEASES INVOLVING A MITOCHONDRIAL BENZODIAZEPINE RECEPTOR
EP1717238A4 (en) 2004-02-16 2008-03-05 Daiichi Seiyaku Co FUNGICIDES HETEROCYCLIC COMPOUNDS
US7306631B2 (en) 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
WO2006015263A2 (en) 2004-07-29 2006-02-09 Threshold Pharmaceuticals, Inc. Lonidamine analogs
WO2006018727A2 (en) 2004-08-18 2006-02-23 Pharmacia & Upjohn Company Llc Triazolopyridine compounds useful for the treatment of inflammation
US7524860B2 (en) 2004-10-07 2009-04-28 Pfizer Inc. Antibacterial agents
AU2005309761A1 (en) 2004-11-22 2006-06-01 Threshold Pharmaceuticals, Inc. Tubulin binding anti cancer agents and prodrugs thereof
ATE443063T1 (de) 2004-12-01 2009-10-15 Merck Serono Sa Ä1,2,4ütriazoloä4,3-aüpyridin-derivative zur behandlung hyperproliferativer erkrankungen
WO2006073938A2 (en) 2004-12-30 2006-07-13 East Carolina University Method for the synthesis of 3-substituted indolizine and benzoindolizine compounds
US7456289B2 (en) 2004-12-31 2008-11-25 National Health Research Institutes Anti-tumor compounds
AP2007004067A0 (en) 2005-02-22 2007-08-31 Pfizer Oxyindole derivatives as 5HT4 receptor agonists
JP2008536950A (ja) 2005-04-18 2008-09-11 ニューロジェン・コーポレーション 置換ヘテロアリールのｃｂ１拮抗薬
US7572807B2 (en) 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
US7579360B2 (en) 2005-06-09 2009-08-25 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
EP1901748B1 (en) 2005-06-09 2010-09-08 Oncalis AG Angiogenesis inhibitors
US7452892B2 (en) 2005-06-17 2008-11-18 Bristol-Myers Squibb Company Triazolopyrimidine cannabinoid receptor 1 antagonists
US7572808B2 (en) 2005-06-17 2009-08-11 Bristol-Myers Squibb Company Triazolopyridine cannabinoid receptor 1 antagonists
US7632837B2 (en) 2005-06-17 2009-12-15 Bristol-Myers Squibb Company Bicyclic heterocycles as cannabinoid-1 receptor modulators
JP2009507032A (ja) 2005-09-02 2009-02-19 アボット・ラボラトリーズ 新規なイミダゾ系複素環
AR056785A1 (es) 2005-11-10 2007-10-24 Schering Corp COMPUESTOS DE IMIDAZO[1,2-A]PIRAZINAS, uTILES COMO INHIBIDORES, REGULADORES O MODULADORES DE PROTEINQUINASAS
CA2633536A1 (en) * 2005-12-27 2007-07-05 F. Hoffmann-La Roche Ag Aryl-isoxazol-4-yl-imidazo[1, 5-a]pyridine derivatives
WO2007074491A1 (en) 2005-12-28 2007-07-05 Universita Degli Studi Di Siena HETEROTRICYCLIC AMIDE DERIVATIVES AS NEUROKININ-l (NKl) RECEPTOR LIGANDS
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
WO2007113226A1 (en) 2006-03-31 2007-10-11 Novartis Ag Organic compounds
US20090175852A1 (en) 2006-06-06 2009-07-09 Schering Corporation Imidazopyrazines as protein kinase inhibitors
AR061229A1 (es) 2006-06-06 2008-08-13 Schering Corp Imidazopirazinas como inhibidores de la proteina quinasa
CA2655857C (en) 2006-06-22 2014-12-02 Mallinckrodt Inc. Pyrazine derivatives with extended conjugation and uses thereof
DK2029554T3 (da) 2006-06-22 2014-06-10 Medibeacon Llc Pyrazinderivater og anvendelser heraf til nyreovervågning
EP2032560B1 (en) 2006-06-29 2013-05-01 Merck Sharp & Dohme Corp. Substituted bicyclic and tricyclic thrombin receptor antagonists
WO2008005423A1 (en) 2006-07-03 2008-01-10 Cambrex Charles City, Inc. Improved method of making sufentanil
US7501438B2 (en) 2006-07-07 2009-03-10 Forest Laboratories Holdings Limited Pyridoimidazole derivatives
US8198448B2 (en) 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
CA2658764A1 (en) 2006-07-20 2008-01-24 Mehmet Kahraman Benzothiophene inhibitors of rho kinase
US7563797B2 (en) 2006-08-28 2009-07-21 Forest Laboratories Holding Limited Substituted imidazo(1,2-A)pyrimidines and imidazo(1,2-A) pyridines as cannabinoid receptor ligands
DE102006041292A1 (de) 2006-09-01 2008-03-06 Henkel Kgaa Wasserstoffperoxid-Aktivierung mit N-Heterocyclen
WO2008037607A1 (de) 2006-09-25 2008-04-03 Basf Se Carbonylgruppen-enthaltende heterocyclische verbindungen und deren verwendung zur bekämpfung von phytopathogenen pilzen
AU2007307031B2 (en) 2006-10-11 2011-11-24 Amgen Inc. Imidazo- and triazolo-pyridine compounds and methods of use therof
WO2008056176A1 (en) 2006-11-10 2008-05-15 Scottish Biomedical Limited Pyrazolopyrimidines as phosphodiesterase inhibitors
GEP20125658B (en) 2006-11-22 2012-10-10 Incyte Corp Imidazotriazines and imidazo pyrimidines as kinase inhibitors
DE602007012133D1 (de) 2006-12-01 2011-03-03 Andrew Burritt Triazolopyridinverbindungen zur behandlung von degenerations- und entzündungskrankheiten
US7803810B2 (en) * 2007-03-09 2010-09-28 Probiodrug Ag Inhibitors
DE102007012645A1 (de) 2007-03-16 2008-09-18 Bayer Healthcare Ag Substituierte Imidazo- und Triazolopyrimidine
EP1972628A1 (en) 2007-03-21 2008-09-24 Schwarz Pharma Ag Indolizines and aza-analog derivatives thereof as CNS active compounds
ES2380395T3 (es) 2007-04-16 2012-05-11 Leo Pharma A/S Triazolopiridinas como inhibidores de fosfodiesterasa para el tratamiento de enfermedades dérmicas
US8546394B2 (en) 2007-04-17 2013-10-01 Bristol-Myers Squibb Company Substituted [1,2,4]triazolo[4,3-A]pyrazine 11-beta-hydroxysteroid dehydrogenase inhibitors
EP2155747B1 (en) 2007-05-10 2012-10-24 GE Healthcare Limited Imidazol (1,2-a)pyridines and related compounds with activity at cannabinoid cb2 receptors
JP5343845B2 (ja) 2007-05-21 2013-11-13 東レ株式会社 特定の有機酸を含有する経口製剤並びに経口製剤の溶出性及び化学的安定性の改善方法
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
WO2008154241A1 (en) 2007-06-08 2008-12-18 Abbott Laboratories 5-heteroaryl substituted indazoles as kinase inhibitors
PE20090365A1 (es) 2007-06-14 2009-04-04 Schering Corp Imidazopirazinas como inhibidores de proteina quinasa
CL2008001839A1 (es) 2007-06-21 2009-01-16 Incyte Holdings Corp Compuestos derivados de 2,7-diazaespirociclos, inhibidores de 11-beta hidroxil esteroide deshidrogenasa tipo 1; composicion farmaceutica que comprende a dichos compuestos; utiles para tratar la obesidad, diabetes, intolerancia a la glucosa, diabetes tipo ii, entre otras enfermedades.
AR067562A1 (es) 2007-07-18 2009-10-14 Novartis Ag Compuestos heterociclicos inhibidores de kinasa
KR20100042287A (ko) 2007-07-31 2010-04-23 쉐링 코포레이션 항암요법으로서의 항-유사분열제 및 아우로라 키나제 억제제 조합물
WO2009017954A1 (en) 2007-08-01 2009-02-05 Phenomix Corporation Inhibitors of jak2 kinase
EA201000201A1 (ru) 2007-08-10 2010-12-30 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Азотсодержащие бициклические химические вещества для лечения вирусных инфекций
FR2920090A1 (fr) 2007-08-24 2009-02-27 Oreal Composition tinctoriale comprenant une base d'oxydation aminopyrazolopyridine particuliere, un coupleur et un tensioactif particulier.
FR2920091A1 (fr) 2007-08-24 2009-02-27 Oreal Composition tinctoriale comprenant une base d'oxydation aminopyrazolopyridine, un coupleur et un polyol particulier.
US8119658B2 (en) 2007-10-01 2012-02-21 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
GB0719803D0 (en) 2007-10-10 2007-11-21 Cancer Rec Tech Ltd Therapeutic compounds and their use
JP4705695B2 (ja) 2007-10-11 2011-06-22 アストラゼネカ アクチボラグ プロテインキナーゼｂ阻害剤としてのピロロ［２，３−ｄ］ピリミジン誘導体
EP3733161A1 (en) 2007-10-12 2020-11-04 Novartis AG Compositions comprising sphingosine 1 phosphate (s1p) receptor modulators
CA2704125A1 (en) 2007-12-19 2009-07-09 Genentech, Inc. 8-anilinoimidazopyridines and their use as anti-cancer and/or anti-inflammatory agents
CA2710194C (en) 2007-12-19 2014-04-22 Amgen Inc. Inhibitors of p13 kinase
MX2010010012A (es) 2008-03-11 2010-10-20 Incyte Corp Derivados de azetidina y ciclobutano como inhibidores de jak.
EP2265603B1 (en) 2008-03-13 2014-05-07 The General Hospital Corporation Inhibitors of the bmp signaling pathway
JPWO2009128520A1 (ja) 2008-04-18 2011-08-04 塩野義製薬株式会社 Ｐｉ３ｋ阻害活性を有する複素環化合物
DE102008023801A1 (de) 2008-05-15 2009-11-19 Bayer Schering Pharma Aktiengesellschaft Substituierte Imidazo- und Triazolopyrimidine, Imidazo- und Pyrazolopyrazine und Imidazotriazine
US8349210B2 (en) 2008-06-27 2013-01-08 Transitions Optical, Inc. Mesogenic stabilizers
WO2010010184A1 (en) 2008-07-25 2010-01-28 Galapagos Nv [1, 2, 4] triazolo [1, 5-a] pyridines as jak inhibitors
WO2010010187A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases
WO2010010189A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases
WO2010010188A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases.
UY32049A (es) 2008-08-14 2010-03-26 Takeda Pharmaceutical Inhibidores de cmet
JP2010070503A (ja) 2008-09-19 2010-04-02 Daiichi Sankyo Co Ltd 抗真菌作用２−アミノトリアゾロピリジン誘導体
US20120021519A1 (en) 2008-09-19 2012-01-26 Presidents And Fellows Of Harvard College Efficient induction of pluripotent stem cells using small molecule compounds
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
EP2361242B1 (en) 2008-10-17 2018-08-01 Oryzon Genomics, S.A. Oxidase inhibitors and their use
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
ES2403633T3 (es) 2008-12-04 2013-05-20 Proximagen Limited Compuestos de imidazopiridina
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
EP2389362B1 (en) 2009-01-21 2019-12-11 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
CA2750517A1 (en) 2009-02-04 2010-08-12 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
ES2435804T3 (es) 2009-02-13 2013-12-23 Bayer Intellectual Property Gmbh Pirimidinas condensadas como inhibidores de Akt
WO2010104307A2 (ko) 2009-03-07 2010-09-16 주식회사 메디젠텍 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물
TW201035078A (en) 2009-03-20 2010-10-01 Incyte Corp Substituted heterocyclic compounds
KR101772963B1 (ko) 2009-03-31 2017-08-31 깃세이 야쿠힌 고교 가부시키가이샤 인돌리진 유도체 및 그 의약용도
CN102428087B (zh) 2009-04-16 2015-06-17 卡洛斯三世国家癌症研究中心基金会 用作激酶抑制剂的咪唑并吡嗪类化合物
TWI461426B (zh) 2009-05-27 2014-11-21 Merck Sharp & Dohme （二氫）咪唑並異〔５，１－ａ〕喹啉類
RU2011153723A (ru) 2009-06-10 2013-07-20 Суновион Фармасьютикалз Инк. Обратные агонисты и антагонисты н3 рецепторов гистамина и способы их применения
AU2010266040B2 (en) 2009-06-25 2015-01-15 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds
HRP20190016T1 (hr) 2009-08-17 2019-03-08 Intellikine, Llc Heterociklički spojevi i njihova upotreba
US9708255B2 (en) 2009-08-18 2017-07-18 Robert A. Casero (bis)urea and (bis)thiourea compounds as epigenic modulators of lysine-specific demethylase 1 and methods of treating disorders
EP2473495A1 (en) 2009-09-18 2012-07-11 Almac Discovery Limited Pharmaceutical compounds
KR101736218B1 (ko) 2009-09-25 2017-05-16 오리존 지노믹스 에스.에이. 라이신 특이적 디메틸라아제-1 억제제 및 이의 용도
US8946296B2 (en) 2009-10-09 2015-02-03 Oryzon Genomics S.A. Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
WO2011050245A1 (en) 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
US8541404B2 (en) 2009-11-09 2013-09-24 Elexopharm Gmbh Inhibitors of the human aldosterone synthase CYP11B2
EP2526102B1 (en) * 2010-01-22 2017-03-08 Fundación Centro Nacional de Investigaciones Oncológicas Carlos III Inhibitors of PI3 kinase
WO2011097607A1 (en) 2010-02-08 2011-08-11 Southern Research Institute Anti-viral treatment and assay to screen for anti-viral agent
WO2011106574A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
WO2011106573A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae
TW201200518A (en) 2010-03-10 2012-01-01 Kalypsys Inc Heterocyclic inhibitors of histamine receptors for the treatment of disease
AU2011229423B2 (en) 2010-03-18 2015-12-10 Institut National De La Sante Et De La Recherche Medicale (Inserm) Anti-infective compounds
CA2793279A1 (en) 2010-03-18 2011-09-22 Ulrich Klar Imidazopyrazines
MX342161B (es) 2010-04-02 2016-09-19 Euroscreen Sa Compuestos antagonistas selectivos de receptor nk-3 novedosos, composicion farmaceutica y metodos para utilizarse en trastornos transmitidos por receptores nk-3.
BR122019020471B1 (pt) 2010-04-19 2021-06-22 Oryzon Genomics S.A. Inibidores da desmetilase específica para lisina 1, seus usos e método para sua identificação, e composições farmacêuticas
PL2560949T3 (pl) 2010-04-20 2017-01-31 Università Degli Studi Di Roma "La Sapienza" Pochodne tranylocyprominy jako inhibitory demetylazy histonowej LSD1 i/lub LSD2
SG185515A1 (en) * 2010-05-13 2012-12-28 Amgen Inc Nitrogen heterocyclic compounds useful as pde10 inhibitors
US20130131057A1 (en) 2010-05-13 2013-05-23 Centro Nacional De Investigaciones Oncologicas (Cnio New bicyclic compounds as pi3-k and mtor inhibitors
CN102295642B (zh) 2010-06-25 2016-04-06 中国人民解放军军事医学科学院毒物药物研究所 2-芳基咪唑并[1,2-a]吡啶-3-乙酰胺衍生物、其制备方法及用途
NZ604478A (en) 2010-07-02 2014-12-24 Gilead Sciences Inc Fused heterocyclic compounds as ion channel modulators
EP2593451B1 (en) 2010-07-12 2015-08-19 Bayer Intellectual Property GmbH Substituted imidazo[1,2-a]pyrimidines and -pyridines
WO2012009475A1 (en) 2010-07-14 2012-01-19 Oregon Health & Science University Methods of treating cancer with inhibition of lysine-specific demethylase 1
US9006449B2 (en) 2010-07-29 2015-04-14 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as LSD1 inhibitors
WO2012013728A1 (en) 2010-07-29 2012-02-02 Oryzon Genomics S.A. Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use
WO2012016133A2 (en) 2010-07-29 2012-02-02 President And Fellows Of Harvard College Ros1 kinase inhibitors for the treatment of glioblastoma and other p53-deficient cancers
WO2012034116A2 (en) 2010-09-10 2012-03-15 The Johns Hopkins University Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders
CN103221412B (zh) 2010-09-29 2015-08-19 橘生药品工业株式会社 (氮杂)中氮茚衍生物及其药物用途
US20130303545A1 (en) 2010-09-30 2013-11-14 Tamara Maes Cyclopropylamine derivatives useful as lsd1 inhibitors
US20120108500A1 (en) 2010-10-07 2012-05-03 Naoki Sakane Compositions and Methods for Modulating Immunodeficiency Virus Transcription
ES2525441T3 (es) 2010-10-18 2014-12-23 E.I. Du Pont De Nemours And Company Sulfonamidas nematocidas
EP2444084A1 (en) 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
WO2012071469A2 (en) 2010-11-23 2012-05-31 Nevada Cancer Institute Histone demethylase inhibitors and uses thereof for treatment o f cancer
WO2012072713A2 (en) 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae
WO2012080729A2 (en) 2010-12-14 2012-06-21 Electrophoretics Limited CASEIN KINASE 1δ (CK1δ) INHIBITORS
WO2012080230A1 (en) 2010-12-17 2012-06-21 Bayer Pharma Aktiengesellschaft 6 substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
UY33805A (es) 2010-12-17 2012-07-31 Boehringer Ingelheim Int ?Derivados de dihidrobenzofuranil-piperidinilo, aza-dihidrobenzofuranilpiperidinilo y diaza-dihidrobenzofuranil-piperidinilo, composiciones farmacéuticas que los contienen y usos de los mismos?.
WO2012080236A1 (en) 2010-12-17 2012-06-21 Bayer Pharma Aktiengesellschaft 6-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
WO2012080234A1 (en) 2010-12-17 2012-06-21 Bayer Pharma Aktiengesellschaft Substituted 6-imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
JP5822944B2 (ja) 2010-12-17 2015-11-25 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 過剰増殖性障害の治療におけるｍｐｓ−１およびｔｋｋ阻害剤として使用するための２置換イミダゾピラジン
EP2655334B1 (en) 2010-12-22 2018-10-03 Eutropics Pharmaceuticals, Inc. Compositions and methods useful for treating diseases
TWI617559B (zh) 2010-12-22 2018-03-11 江蘇恆瑞醫藥股份有限公司 ２－芳基咪唑并［１，２－ｂ］嗒．２－苯基咪唑并［１，２－ａ］吡啶，和２－苯基咪唑并［１，２－ａ］吡衍生物
WO2012100229A2 (en) 2011-01-21 2012-07-26 The General Hospital Corporation Compositions and methods for cardiovascular disease
EP3981395A1 (en) 2011-02-08 2022-04-13 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative disorders
EP2712316A1 (en) 2011-02-08 2014-04-02 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders
JP5808826B2 (ja) 2011-02-23 2015-11-10 インテリカイン， エルエルシー 複素環化合物およびその使用
US9464065B2 (en) 2011-03-24 2016-10-11 The Scripps Research Institute Compounds and methods for inducing chondrogenesis
PE20141322A1 (es) 2011-03-25 2014-10-05 Glaxosmithkline Intellectual Property (N 2) Limited Ciclopropilaminas como inhibidores de desmetilasa 1 especifica de lisina
WO2012147890A1 (ja) 2011-04-27 2012-11-01 持田製薬株式会社 新規アゾール誘導体
WO2012156531A2 (en) 2011-05-19 2012-11-22 Oryzon Genomics, S.A. Lysine demethylase inhibitors for inflammatory diseases or conditions
EP2524918A1 (en) 2011-05-19 2012-11-21 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyrazines derivates as kinase inhibitors
WO2012156537A2 (en) 2011-05-19 2012-11-22 Oryzon Genomics, S.A. Lysine demethylase inhibitors for thrombosis and cardiovascular diseases
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
TW201311149A (zh) 2011-06-24 2013-03-16 Ishihara Sangyo Kaisha 有害生物防治劑
EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
AU2012293223B2 (en) 2011-08-09 2017-03-02 Takeda Pharmaceutical Company Limited Cyclopropaneamine compound
BR112014003382B1 (pt) 2011-08-15 2022-03-15 University Of Utah Research Foundation Análogos de (e)-n-(1-feniletilideno) benzo-hidrazida substituída como inibidores de histona desmetilase e composições farmacêuticas compreendendo-os
WO2013033688A1 (en) 2011-09-01 2013-03-07 The Brigham And Women's Hospital, Inc. Treatment of cancer
WO2013033515A1 (en) 2011-09-02 2013-03-07 Promega Corporation Compounds and methods for assaying redox state of metabolically active cells and methods for measuring nad(p)/nad(p)h
CN104703987B (zh) 2011-10-10 2017-05-03 H.隆德贝克有限公司 具有咪唑并吡嗪酮骨架的pde9抑制剂
UA116765C2 (uk) 2011-10-20 2018-05-10 Орізон Джіномікс, С.А. (гетеро)арилциклопропіламіни як інгібітори lsd1
CN104203914B (zh) 2011-10-20 2017-07-11 奥瑞泽恩基因组学股份有限公司 作为lsd1抑制剂的(杂)芳基环丙胺化合物
ITMI20111971A1 (it) 2011-10-28 2013-04-29 Mesogenics Srl Inibitori dell'enzima lsd-1 per l'induzione del differenziamento osteogenico
US9266881B2 (en) 2011-11-14 2016-02-23 Merck Sharp & Dohme Corp. Triazolopyridinone PDE10 inhibitors
CA2857964A1 (en) 2011-12-05 2013-06-13 Brandeis University Treatment of amyloidosis by compounds that regulate retromer stabilization
WO2013131609A1 (en) 2012-03-07 2013-09-12 Merck Patent Gmbh Triazolopyrazine derivatives
GB201205669D0 (en) 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof
CN103373996A (zh) 2012-04-20 2013-10-30 山东亨利医药科技有限责任公司 作为crth2受体拮抗剂的二并环衍生物
JP6273274B2 (ja) 2012-06-28 2018-01-31 ノバルティス アーゲー 補体経路モジュレーターおよびその使用
GB201212513D0 (en) 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents
CA2886187C (en) 2012-09-28 2020-04-14 Vanderbilt University Fused heterocyclic compounds as selective bmp inhibitors
MX2015004151A (es) 2012-10-05 2015-07-06 Rigel Pharmaceuticals Inc Inhibidores del factor de diferenciacion de crecimiento-8 (gdf-8).
JP6325449B2 (ja) 2012-10-12 2018-05-16 武田薬品工業株式会社 シクロプロパンアミン化合物およびその用途
WO2014078479A2 (en) 2012-11-14 2014-05-22 The Board Of Regents Of The University Of Texas System INHIBITION OF HIF-2α HETERODIMERIZATION WITH HIF1β (ARNT)
WO2014084298A1 (ja) 2012-11-28 2014-06-05 京都府公立大学法人 リシン構造を有するｌｓｄ1選択的阻害薬
WO2014085613A1 (en) 2012-11-30 2014-06-05 Mccord Darlene E Hydroxytyrosol and oleuropein compositions for induction of dna damage, cell death and lsd1 inhibition
EP2740474A1 (en) 2012-12-05 2014-06-11 Instituto Europeo di Oncologia S.r.l. Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a
CN103054869A (zh) 2013-01-18 2013-04-24 郑州大学 含三唑基的氨基二硫代甲酸酯化合物在制备以lsd1为靶标药物中的应用
CN103933036B (zh) 2013-01-23 2017-10-13 中国人民解放军军事医学科学院毒物药物研究所 2‑芳基咪唑并[1,2‑α]吡啶‑3‑乙酰胺衍生物在制备防治PTSD的药物中的用途
EP2956441A4 (en) 2013-02-18 2016-11-02 Scripps Research Inst MODULATORS OF VASOPRESSIN RECEPTORS WITH THERAPEUTIC POTENTIAL
WO2014164867A1 (en) 2013-03-11 2014-10-09 Imago Biosciences Kdm1a inhibitors for the treatment of disease
JP2016516399A (ja) 2013-03-13 2016-06-09 オーストラリアン ニュークリア サイエンス アンド テクノロジー オーガニゼーション 非機能性ｔｓｐｏ遺伝子を有するトランスジェニック非ヒト生物
US20140343118A1 (en) 2013-03-14 2014-11-20 Duke University Methods of treatment using arylcyclopropylamine compounds
EP2968343A4 (en) 2013-03-14 2016-11-02 Epizyme Inc COMBINATION THERAPY FOR THE TREATMENT OF CANCER
EP3003301B1 (en) 2013-05-30 2021-02-24 Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Vegas Novel suicidal lsd1 inhibitors targeting sox2-expressing cancer cells
AU2014281398B2 (en) 2013-06-19 2018-10-04 University Of Utah Research Foundation Substituted (E)-N'-(1-phenylethylidene) benzohydrazide analogs as histone demethylase inhibitors
SMT202000071T1 (it) 2013-06-21 2020-03-13 Myokardia Inc Composti di pirimidinadione contro le condizioni cardiache
US9186391B2 (en) 2013-08-29 2015-11-17 Musc Foundation For Research Development Cyclic peptide inhibitors of lysine-specific demethylase 1
US9556170B2 (en) 2013-08-30 2017-01-31 University Of Utah Research Foundation Substituted-1H-benzo[d]imidazole series compounds as lysine-specific demethylase 1 (LSD1) inhibitors
KR101568724B1 (ko) 2013-11-13 2015-11-12 서울대학교산학협력단 신규한 화합물, 이의 생산 방법, 및 히스톤 디메틸라제 저해제로서 이의 용도
LT3080100T (lt) 2013-12-11 2023-02-27 Celgene Quanticel Research, Inc. Lizinui specifinės demetilazės-1 inhibitoriai
US9428470B2 (en) 2014-02-13 2016-08-30 Takeda Pharmaceutical Company Limited Heterocyclic compound
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
US9346776B2 (en) 2014-02-13 2016-05-24 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
DK3105226T3 (da) 2014-02-13 2019-10-14 Incyte Corp Cyclopropylaminer som lsd1-inhibitorer
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
PT3105218T (pt) 2014-02-13 2019-12-05 Incyte Corp Ciclopropilaminas como inibidores de lsd1
CN103893163B (zh) 2014-03-28 2016-02-03 中国药科大学 2-([1，1′-联苯]-4-基)2-氧代乙基4-((3-氯-4-甲基苯基)氨基)-4-氧代丁酸酯在制备lsd1抑制剂药物中的应用
KR102379518B1 (ko) 2014-04-02 2022-03-25 브리스톨-마이어스 스큅 컴퍼니 비아릴 키나제 억제제
TN2016000418A1 (en) 2014-04-11 2018-04-04 Takeda Pharmaceuticals Co Cyclopropanamine compound and use thereof.
CN103961340B (zh) 2014-04-30 2019-06-25 南通中国科学院海洋研究所海洋科学与技术研究发展中心 一类lsd1抑制剂及其应用
DK3148974T3 (en) 2014-05-30 2018-10-29 St Europeo Di Oncologia S R L CYCLOPROPYLAMINE COMPOUNDS AS HYDONDEMETHYLASE INHIBITORS
CN104119280B (zh) 2014-06-27 2016-03-16 郑州大学 含氨基类脲与端炔结构单元的嘧啶衍生物、制备方法及应用
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
GB201417828D0 (en) 2014-10-08 2014-11-19 Cereno Scient Ab New methods and compositions
KR102550852B1 (ko) 2014-10-08 2023-07-05 에프. 호프만-라 로슈 아게 알도스테론 신타아제 억제제로서의 스피로다이아민 유도체
BR112017020935A2 (pt) 2015-04-03 2018-07-10 Mutabilis ?compostos, composição farmacêutica e conjunto?
EP3626720A1 (en) 2015-04-03 2020-03-25 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
WO2016161279A1 (en) 2015-04-03 2016-10-06 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase for the treatment of cancer
KR102710120B1 (ko) 2015-08-12 2024-09-27 인사이트 홀딩스 코포레이션 Lsd1 저해제의 염
JPWO2017130933A1 (ja) 2016-01-25 2018-11-29 国立大学法人 熊本大学 神経変性疾患治療剤
PE20190377A1 (es) 2016-04-22 2019-03-08 Incyte Corp Formulaciones de un inhibidor de lsd 1
EP3570843A1 (en) 2017-01-18 2019-11-27 Vanderbilt University Fused heterocyclic compounds as selective bmp inhibitors
CN109963854B (zh) 2017-03-16 2022-04-12 江苏恒瑞医药股份有限公司 杂芳基并[4,3-c]嘧啶-5-胺类衍生物、其制备方法及其在医药上的应用

Also Published As

Publication number Publication date
US20170369487A1 (en) 2017-12-28
US9695168B2 (en) 2017-07-04
TWI687419B (zh) 2020-03-11
WO2016007731A1 (en) 2016-01-14
US10047086B2 (en) 2018-08-14
US10640503B2 (en) 2020-05-05
US20190040058A1 (en) 2019-02-07
US20160009712A1 (en) 2016-01-14
TW201609726A (zh) 2016-03-16

Similar Documents

Publication Publication Date Title
AR101175A1 (es) Imidazopiridinas e imidazopirazinas como inhibidores de lsd1
AR101174A1 (es) Imidazopirazinas como inhibidores de lsd1
AR097431A1 (es) Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de quinasas pim
NI201600152A (es) Compuestos de heteroarilo o arilo bicíclicos fusionados y su uso como inhibidores de irak4
PE20160540A1 (es) Inhibidores de bromodominios
MX373846B (es) Nuevos derivados de pirazolo pirimidina y su uso como inhibidores de malt1.
CR20150474A (es) Inhibidores de bromodominios tetracíclicos
CY1124537T1 (el) Παραγωγο πυριδονης που εχει τετραϋδροπυρανυλ μεθυλ ομαδα
AR091424A1 (es) Compuestos triciclicos sustituidos como inhibidores de receptores del factor de crecimiento del fibroplasto (fgfr)
AR100160A1 (es) 1H-PIRROLO[2,3-c]PIRIDIN-7(6H)-ONAS Y PIRAZOLO[3,4-c]PIRIDIN-7(6H)-ONAS COMO INHIBIDORES DE PROTEÍNAS BET
EA201791692A1 (ru) 4H-ПИРРОЛО[3,2-c]ПИРИДИН-4-ОНОВЫЕ ПРОИЗВОДНЫЕ
PH12017500252A1 (en) New spiro[3h-indole-3,2`-pyrrolidin]-2(1h)-one compounds and derivatives as mdm2-p53 inhibitors
CR20160523A (es) Compuestos de imidazo[4,5-c]quinolin-2-ona y su uso para tratar cáncer
AR087913A1 (es) Inhibidores sustituidos de n-[1-ciano-2-(fenil)etil]-2-azabiciclo[2,2,1]heptan-3-carboxamida de catepsina c
UY35834A (es) Piperazinas de pirazolo sustituido como inhibidores de caseína quinasa 1 delta y epsilon
UY35675A (es) Derivados sustituidos de quinazolin-4-ona
AR089776A1 (es) 5,8-dihidro-6h-pirazolo[3,4-h]quinazolinas como inhibidores de igf-1r/ir
EA201491376A1 (ru) Производные 1h-пирроло[2,3-b]пиридина и их применение в качестве ингибиторов киназы
CR20150378A (es) Compuestos tetracíclicos sustituidos con heterociclo y métodos de uso de los mismos para el tratamiento de enfermedades víricas
PE20160201A1 (es) Bencil-1h-pirazol[3,4-b]piridinas y su uso
AR088320A1 (es) Derivados de isoindolinona y pirrolopiridinona como inhibidores de akt
MX2021005891A (es) Sondas para la proyeccion de imagen de la proteina huntingtina.
AR109296A1 (es) Derivados de oxadiazolopiridina para el uso como inhibidores de ghrelin o-aciltransferasa (goat)
AR089815A1 (es) Compuestos que mejoran la actividad de los proteasomas
CL2013003056A1 (es) Compuestos derivados de (fenil o piridin)-etinil-(piridin o pirimidin) sustituido; composición farmacéutica que los comprende; proceso de preparación de esto; y su uso en el tratamiento de la esquizofrenia o enfermedades cognitivas.

Legal Events

Date Code Title Description
FB Suspension of granting procedure