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AR101174A1 - Imidazopirazinas como inhibidores de lsd1 - Google Patents

Imidazopirazinas como inhibidores de lsd1

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AR101174A1
AR101174A1 ARP150102197A ARP150102197A AR101174A1 AR 101174 A1 AR101174 A1 AR 101174A1 AR P150102197 A ARP150102197 A AR P150102197A AR P150102197 A ARP150102197 A AR P150102197A AR 101174 A1 AR101174 A1 AR 101174A1
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Argentina
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nrc7rd7
alkyl
nrc7c
ora7
independently selected
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ARP150102197A
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Sun Yaping
Li Jingwei
R Courter Joel
Zhuo Jincong
Zhang Colin
Yao Wenquing
Wang Xiaozhao
Lu Liang
He Chunhong
Wu Liangxing
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Incyte Corp
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    • 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
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  • General Chemical & Material Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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Abstract

La presente se dirige a derivados de imidazo[1,2-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: 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, o 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, OH, 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; R² y R³ se seleccionan de modo independiente de H, halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, Cy², 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 Cy², 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 Cy³, halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, 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, 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, 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; cada Cy¹, Cy², Cy³, y Cy⁴ 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 RCʸ se selecciona de modo independiente 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-, y (heterocicloalquilo de 4 - 7 miembros)-alquil C₁₋₄-, 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 C₁₋₆, haloalquilo C₁₋₄, cianoalquilo C₁₋₆, 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 alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, y Cy⁴; 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, 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; 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, ORᵃ⁷, SRᵃ⁷, C(O)Rᵇ⁷, C(O)NRᶜ⁷Rᵈ⁷, C(O)ORᵃ⁷, OC(O)Rᵇ⁷, OC(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)Rᵇ⁷, NRᶜ⁷C(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)ORᵃ⁷, C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, S(O)Rᵇ⁷, S(O)NRᶜ⁷Rᵈ⁷, S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂NRᶜ⁷Rᵈ⁷, y S(O)₂NRᶜ⁷Rᵈ⁷; 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 CN, 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)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)ORᵃ⁷, C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, S(O)Rᵇ⁷, S(O)NRᶜ⁷Rᵈ⁷, S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂NRᶜ⁷Rᵈ⁷, y S(O)₂NRᶜ⁷Rᵈ⁷, 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, ORᵃ⁷, SRᵃ⁷, C(O)Rᵇ⁷, C(O)NRᶜ⁷Rᵈ⁷, C(O)ORᵃ⁷, OC(O)Rᵇ⁷, OC(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)Rᵇ⁷, NRᶜ⁷C(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)ORᵃ⁷, C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, S(O)Rᵇ⁷, S(O)NRᶜ⁷Rᵈ⁷, S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂NRᶜ⁷Rᵈ⁷ y S(O)₂NRᶜ⁷Rᵈ⁷; 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 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, ORᵃ⁷, SRᵃ⁷, C(O)Rᵇ⁷, C(O)NRᶜ⁷Rᵈ⁷, C(O)ORᵃ⁷, OC(O)Rᵇ⁷, OC(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)Rᵇ⁷, NRᶜ⁷C(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)ORᵃ⁷, C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(=NRᵉ⁷)NRᶜ⁷Rᵇ⁷, S(O)Rᵇ⁷, S(O)NRᶜ⁷Rᵈ⁷, S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂NRᶜ⁷Rᵈ⁷, y S(O)₂NRᶜ⁷Rᵈ⁷; 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, fenilo, heteroarilo de 5 - 6 miembros, haloalquilo C₁₋₆, 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)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)ORᵃ⁷, C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, S(O)Rᵇ⁷, S(O)NRᶜ⁷Rᵈ⁷, S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂NRᶜ⁷Rᵈ⁷, y S(O)₂NRᶜ⁷Rᵈ⁷, donde dicho alquilo C₁₋₆, cicloalquilo C₃₋₇, heterocicloalquilo de 4 - 7 miembros, fenilo, 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, ORᵃ⁷, SRᵃ⁷, C(O)Rᵇ⁷, C(O)NRᶜ⁷Rᵈ⁷, C(O)ORᵃ⁷, OC(O)Rᵇ⁷, OC(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)Rᵇ⁷, NRᶜ⁷C(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)ORᵃ⁷, C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, S(O)Rᵇ⁷, -S(O)NRᶜ⁷Rᵈ⁷, S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂NRᶜ⁷Rᵈ⁷, y S(O)₂NRᶜ⁷Rᵈ⁷; cada Rᵃ³, Rᵇ³, Rᶜ³, y Rᵈ³ 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 CH, halo, CN, ORᵃ⁷, SRᵃ⁷, C(O)Rᵇ⁷, C(O)NRᶜ⁷Rᵈ⁷, C(O)ORᵃ⁷, OC(O)Rᵃ⁷, OC(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)Rᵇ⁷, NRᶜ⁷C(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)ORᵃ⁷, C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, S(O)Rᵇ⁷, S(O)NRᶜ⁷Rᵈ⁷, S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂NRᶜ⁷Rᵈ⁷, y S(O)₂NRᶜ⁷Rᵈ⁷; 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, cicloalquilo C₃₋₇, heterocicloalquilo de 4 - 7 miembros, fenilo, heteroarilo de 5 - 6 miembros, haloalquilo C₁₋₆, halo, CN, ORᵃ⁷, SRᵃ⁷, C(O)Rᵇ⁷, C(O)NRᶜ⁷Rᵈ⁷, C(O)ORᵃ⁷, OC(O)Rᵃ⁷, OC(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)Rᵇ⁷, NRᶜ⁷C(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)ORᵃ⁷, C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, S(O)Rᵇ⁷, S(O)NRᶜ⁷Rᵈ⁷, S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂NRᶜ⁷Rᵈ⁷, y S(O)₂NRᶜ⁷Rᵈ⁷, donde dicho alquilo C₁₋₆, cicloalquilo C₃₋₇, heterocicloalquilo de 4 - 7 miembros, fenilo, 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, ORᵃ⁷, SRᵃ⁷, C(O)Rᵇ⁷, C(O)NRᶜ⁷Rᵈ⁷, C(O)ORᵃ⁷, OC(O)Rᵇ⁷, OC(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)Rᵇ⁷, NRᶜ⁷C(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)ORᵃ⁷, C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, S(O)Rᵇ⁷, S(O)NRᶜ⁷Rᵈ⁷, S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂NRᶜ⁷Rᵈ⁷, y S(O)₂NRᶜ⁷Rᵈ⁷; 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 C₁₋₄, 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, ORᵃ⁷, SRᵃ⁷, C(O)Rᵇ⁷, C(O)NRᶜ⁷Rᵈ⁷, C(O)ORᵃ⁷, OC(O)Rᵇ⁷, OC(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)Rᵇ⁷, NRᶜ⁷C(O)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(O)ORᵃ⁷, C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, NRᶜ⁷C(=NRᵉ⁷)NRᶜ⁷Rᵈ⁷, S(O)Rᵇ⁷, S(O)NRᶜ⁷Rᵈ⁷, S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂Rᵇ⁷, NRᶜ⁷S(O)₂NRᶜ⁷Rᵈ⁷, y S(O)₂NRᶜ⁷Rᵈ⁷; o Rᶜ⁴ y Rᵈ⁴ 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, ORᵃ⁷, SRᵃ⁷, C(O)Rᵇ⁷, C(O)NRᶜ⁷Rᵈ⁷, C(O)ORᵃ⁷, OC(O)Rᵇ⁷, OC(O)NRᶜ⁷Rᵈ⁷,
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Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
CN106488915B (zh) 2014-02-13 2020-10-02 因赛特公司 作为lsd1抑制剂的环丙胺
TW201613860A (en) 2014-02-13 2016-04-16 Incyte Corp Cyclopropylamines as LSD1 inhibitors
SG10201806849WA (en) 2014-02-13 2018-09-27 Incyte Corp Cyclopropylamines as lsd1 inhibitors
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
MX394094B (es) 2014-11-06 2025-03-24 Bial R&D Invest S A PYRAZOLO [1, 5-a] PIRIMIDINAS SUSTITUIDAS Y SU USO EN EL TRATAMIENTO DE TRASTORNOS MÉDICOS.
ES2958391T3 (es) 2014-11-06 2024-02-08 Bial R&D Invest S A Imidazo[1,5-a]pirimidinas sustituidas y su uso en el tratamiento de trastornos médicos
US20180185368A1 (en) 2014-11-06 2018-07-05 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders
US9944647B2 (en) * 2015-04-03 2018-04-17 Incyte Corporation Heterocyclic compounds as LSD1 inhibitors
MX2017015922A (es) 2015-06-12 2018-12-11 Oryzon Genomics Sa Biomarcadores asociados con inhibidores de lsd1 y usos de los mismos.
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
UA126277C2 (uk) 2015-08-12 2022-09-14 Інсайт Корпорейшн Солі інгібітору lsd1
CN107174584B (zh) * 2016-03-12 2020-09-01 福建金乐医药科技有限公司 含哌嗪结构化合物在制备lsd1抑制剂中的应用
EP3429571B1 (en) 2016-03-15 2025-10-08 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases
JP2019512546A (ja) 2016-03-16 2019-05-16 オリゾン・ゲノミクス・ソシエダッド・アノニマ Ｋｄｍ１ａ標的会合を決定するための方法、およびそれに有用な化学プローブ
JP7046827B2 (ja) 2016-04-06 2022-04-04 リソソーマル・セラピューティクス・インコーポレイテッド イミダゾ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用
MX2018012211A (es) 2016-04-06 2019-03-28 Lysosomal Therapeutics Inc Compuestos de pirazol[1,5-a]pirimidinil carboxamida y su uso en el tratamiento de trastornos médicos.
JP7034935B2 (ja) 2016-04-06 2022-03-14 リソソーマル・セラピューティクス・インコーポレイテッド ピロロ［１，２－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用
BR112018071585B1 (pt) 2016-04-22 2024-01-02 Incyte Corporation Formulações de um inibidor de lsd1, seus usos e método de preparação das mesmas
JP7164774B2 (ja) 2016-05-05 2022-11-02 ビアル－アール・アンド・ディ・インベストメンツ・ソシエダーデ・アノニマ 置換イミダゾ［１，２－ｂ］ピリダジン、置換イミダゾ［１，５－ｂ］ピリダジン、関連化合物、および医学的障害の治療におけるその使用
US11345698B2 (en) 2016-05-05 2022-05-31 Bial—R&D Investments, S.A. Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders
EP3535420A1 (en) 2016-11-03 2019-09-11 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
EP3551178A1 (en) 2016-12-09 2019-10-16 Constellation Pharmaceuticals, Inc. Markers for personalized cancer treatment with lsd1 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
US20200369665A1 (en) * 2017-06-30 2020-11-26 Ryvu Therapeutics S.A. Imidazo[1,2-a]pyrazine modulators of the adenosine a2a receptor
BR112020000827A2 (pt) 2017-08-03 2020-07-21 Oryzon Genomics, S.A. métodos de tratamento de alterações de comportamento
TWI794294B (zh) * 2017-09-13 2023-03-01 南韓商韓美藥品股份有限公司 吡唑衍生化合物及其用途
WO2019068326A1 (en) 2017-10-05 2019-04-11 Université D'aix-Marseille INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES
US11685782B2 (en) 2017-10-23 2023-06-27 Children's Medical Center Corporation Methods of treating cancer using LSD1 inhibitors in combination with immunotherapy
CN108220422B (zh) * 2018-01-05 2020-10-16 武汉惠康达科技有限公司 组蛋白去甲基化酶在筛选治疗脂肪肝及其相关疾病药物中的应用
CN112119080B (zh) * 2018-05-15 2023-07-11 密歇根大学董事会 作为lsd-1抑制剂的咪唑并[4,5-c]吡啶化合物
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
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
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
PH12021552251A1 (en) 2019-03-20 2022-07-25 Oryzon Genomics Sa Methods of treating borderline personality disorder
WO2021004610A1 (en) 2019-07-05 2021-01-14 Oryzon Genomics, S.A. Biomarkers and methods for personalized treatment of small cell lung cancer using kdm1a inhibitors
WO2021094208A1 (en) 2019-11-12 2021-05-20 Bayer Aktiengesellschaft Substituted imidazo pyrimidine ep3 antagonists
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
BR112023020554A2 (pt) 2021-04-08 2023-12-05 Oryzon Genomics Sa Combinações de inibidores de lsd1 para o tratamento de cânceres mieloides
GB202115017D0 (en) 2021-10-20 2021-12-01 Univ London Queen Mary Sequential treatments and biomarkers to reverse resistance to kinase inhibitors
US20240418723A1 (en) 2021-10-20 2024-12-19 Queen Mary University Of London Sequential treatments and biomarkers to reverse resistance to kinase inhibitors
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
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
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
EP4622635A1 (en) 2022-11-24 2025-10-01 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer

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.
ATE177426T1 (de) 1992-06-17 1999-03-15 Upjohn Co Pyrridino-, pyrrolidino- und azepino- substituierte oxime als antiatherosklerosemittel und antihypercholesterolemiemittel
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.
US6451796B1 (en) 1997-11-11 2002-09-17 Ono Pharmaceutical Co., Ltd. Fused pyrazine compounds
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
JP2001000687A (ja) 1999-06-23 2001-01-09 Ace Denken:Kk 遊技機
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
JP3729343B2 (ja) 2000-04-27 2005-12-21 アステラス製薬株式会社 縮合ヘテロアリール誘導体
US6403588B1 (en) 2000-04-27 2002-06-11 Yamanouchi Pharmaceutical Co., Ltd. Imidazopyridine derivatives
NZ522783A (en) 2000-06-28 2004-07-30 Smithkline Beecham P Wet milling process for pharmaceuticals with agitator or chamber having nylon with internal lubricant
AU2001276903A1 (en) 2000-07-14 2002-01-30 Bristol-Myers Squibb Pharma Company Imidazo(1,2-a)pyrazines for the treatment of neurological disorders
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
ATE310740T1 (de) 2000-11-10 2005-12-15 Merck Sharp & Dohme Imidazotriazin-derivate als liganden für gaba- rezeptoren
WO2002048146A2 (de) 2000-12-13 2002-06-20 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
CA2473740A1 (en) 2002-01-18 2003-07-31 David Solow-Cordero 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
EP1572693A1 (en) 2002-12-20 2005-09-14 Pharmacia Corporation Mitogen activated protein kinase-activated protein kinase-2 inhibiting compounds
US7189723B2 (en) * 2003-02-10 2007-03-13 Cgi Pharmaceuticals, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity
GB0303910D0 (en) 2003-02-20 2003-03-26 Merck Sharp & Dohme Therapeutic agents
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
RU2366655C2 (ru) 2003-03-14 2009-09-10 Оно Фармасьютикал Ко., Лтд. Азотсодержащие гетероциклические производные и лекарственные средства, содержащие их в качестве активного ингредиента
ES2338656T3 (es) 2003-04-11 2010-05-11 High Point Pharmaceuticals, Llc Uso farmaceutico de 1,2,4-triazoles fusionados.
WO2004089416A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S Combination of an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent
US7579355B2 (en) 2003-04-24 2009-08-25 Merck & Co., Inc. Inhibitors of Akt activity
SE0301653D0 (sv) 2003-06-05 2003-06-05 Astrazeneca Ab Novel compounds
EA010023B1 (ru) 2003-07-14 2008-06-30 Арена Фармасьютикалз, Инк. Конденсированные арильные и гетероарильные производные в качестве модуляторов метаболизма и для профилактики и лечения расстройств, связанных с нарушением метаболизма
US7538120B2 (en) 2003-09-03 2009-05-26 Array Biopharma Inc. Method of treating inflammatory diseases
AU2004271741A1 (en) 2003-09-12 2005-03-24 Laboratoires 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
MXPA06004043A (es) 2003-10-10 2006-06-28 Pfizer Prod Inc 2h-[1,2,4]triazolo[4,3-a]pirazinas sustituidas como inhibidores de la glucogeno sintetasa cinasa 3.
US7419978B2 (en) 2003-10-22 2008-09-02 Bristol-Myers Squibb Company Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors
US7714009B2 (en) 2003-10-31 2010-05-11 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
US20090215817A1 (en) 2004-08-18 2009-08-27 Pfizer Inc Novel Triazolopyridine Compounds for the Treatment of Inflammation
CA2582482A1 (en) 2004-10-07 2006-04-13 Warner-Lambert Company Llc Triazolopyridine derivatives as antibacterial agents
JP2008520719A (ja) 2004-11-22 2008-06-19 スレショルド ファーマシューティカルズ インコーポレイティッド チューブリン結合抗癌剤およびそれらのプロドラッグ
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
ES2366375T3 (es) 2005-02-22 2011-10-19 Pfizer, Inc. Derivados de oxiindol, como agonistas del receptor 5-ht4.
US20070078135A1 (en) 2005-04-18 2007-04-05 Neurogen Corporation Substituted heteroaryl CB1 antagonists
ATE480239T1 (de) 2005-06-09 2010-09-15 Oncalis Ag Angiogeneseinhibitoren
US7579360B2 (en) 2005-06-09 2009-08-25 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
US7572807B2 (en) 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
US7632837B2 (en) 2005-06-17 2009-12-15 Bristol-Myers Squibb Company Bicyclic heterocycles as cannabinoid-1 receptor modulators
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
US7709468B2 (en) 2005-09-02 2010-05-04 Abbott Laboratories Imidazo based heterocycles
BRPI0618520A2 (pt) 2005-11-10 2011-09-06 Schering Corp imidazopirazinas como inibidores de proteìna cinase
ATE537171T1 (de) 2005-12-27 2011-12-15 Hoffmann La Roche Aryl-isoxazol-4-yl-imidazoä1,5-aüpyridin-deriva e
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)
JP2009531390A (ja) 2006-03-31 2009-09-03 ノバルティス アクチエンゲゼルシャフト 有機化合物
US20090175852A1 (en) 2006-06-06 2009-07-09 Schering Corporation Imidazopyrazines as protein kinase inhibitors
JP2009539840A (ja) 2006-06-06 2009-11-19 シェーリング コーポレイション プロテインキナーゼ阻害剤としてのイミダゾピラジン
AU2007261398A1 (en) 2006-06-22 2007-12-27 Mallinckrodt Llc Pyrazine derivatives and uses thereof in renal monitoring
WO2007149478A2 (en) 2006-06-22 2007-12-27 Mallinckrodt Inc. Pyrazine derivatives with extended conjugation and uses thereof
AU2007269830A1 (en) 2006-06-29 2008-01-10 Schering Corporation 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
BRPI0713187A2 (pt) 2006-07-20 2012-10-16 Mehmet Kahraman método de inibir rho-quinase, método de tratamento de doença mediada por rho-quinase, composto e composição farmacêutica
WO2008027812A2 (en) 2006-08-28 2008-03-06 Forest Laboratories Holdings Limited Imidazopyridine and imidazopyrimidine derivatives
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
EP3443958A1 (en) 2006-11-22 2019-02-20 Incyte Holdings Corporation Imidazotriazines and imidazopyrimidines as kinase inhibitors
JP2010511018A (ja) 2006-12-01 2010-04-08 ガラパゴス・ナムローゼ・フェンノートシャップ 変性疾患及び炎症性疾患の治療に有用なトリアゾロピリジン化合物
DK2118101T3 (da) 2007-03-09 2013-01-02 Probiodrug Ag IMIDAZO (1,5-A)-PYRIDinderivater som glutaminylcyclaseinhibitorer
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
US8829190B2 (en) 2007-04-16 2014-09-09 Leo Pharma A/S Triazolopyridines as phosphodiesterase inhibitors for treatment of dermal diseases
CN101687873A (zh) 2007-04-17 2010-03-31 百时美施贵宝公司 具有稠合杂环的11β-羟基类固醇Ⅰ型脱氢酶抑制剂
JP2010526836A (ja) 2007-05-10 2010-08-05 ジーイー・ヘルスケア・リミテッド カンナビノイドＣＢ２レセプターに対して活性を有するイミダゾール（１，２−ａ）ピリジン及び関連化合物
ES2648037T3 (es) 2007-05-21 2017-12-28 Toray Industries, Inc. Preparación oral que comprende un ácido orgánico específico y método para mejorar la propiedad de disolución y la estabilidad química de la preparación oral
WO2008154241A1 (en) 2007-06-08 2008-12-18 Abbott Laboratories 5-heteroaryl substituted indazoles as kinase inhibitors
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
CN101772500A (zh) 2007-06-14 2010-07-07 先灵公司 作为蛋白质激酶抑制剂的咪唑并吡嗪
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.
CN101801966A (zh) 2007-07-18 2010-08-11 诺瓦提斯公司 双环杂芳基化合物和它们作为激酶抑制剂的用途
WO2009017701A2 (en) 2007-07-31 2009-02-05 Schering Corporation Anti-mitotic agent and aurora kinase inhibitor combination as anti-cancer treatment
WO2009017954A1 (en) 2007-08-01 2009-02-05 Phenomix Corporation Inhibitors of jak2 kinase
CA2695989A1 (en) 2007-08-10 2009-02-19 Glaxosmithkline Llc Certain nitrogen containing bicyclic chemical entities for treating viral infections
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
ES2522365T3 (es) 2007-10-11 2014-11-14 Astrazeneca Ab Derivados de pirrolo [2,3-D] pirimidina como inhibidores de proteína quinasas B
PL2465492T3 (pl) 2007-10-12 2015-11-30 Novartis Ag Mieszaniny zawierające modulatory receptora 1-fosforanu sfingozyny (S1P)
US8293763B2 (en) 2007-12-19 2012-10-23 Genentech, Inc. 8-anilinoimidazopyridines and their use as anti-cancer and/or anti-inflammatory agents
US7820665B2 (en) 2007-12-19 2010-10-26 Amgen Inc. Imidazopyridazine inhibitors of PI3 kinase for cancer treatment
UA101493C2 (ru) 2008-03-11 2013-04-10 Инсайт Корпорейшн Производные азетидина и циклобутана как ингибиторы jak
WO2009114180A1 (en) 2008-03-13 2009-09-17 The General Hospital Corporation Inhibitors of the bmp signaling pathway
US20110105457A1 (en) 2008-04-18 2011-05-05 Shionogi & Co., Ltd. Heterocyclic compound having inhibitory activity on pi3k
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
WO2010010188A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases.
WO2010010184A1 (en) 2008-07-25 2010-01-28 Galapagos Nv [1, 2, 4] triazolo [1, 5-a] pyridines as jak inhibitors
WO2010010189A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases
WO2010010187A1 (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
US20120021519A1 (en) 2008-09-19 2012-01-26 Presidents And Fellows Of Harvard College Efficient induction of pluripotent stem cells using small molecule compounds
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
CA2738429C (en) 2008-09-26 2016-10-25 Intellikine, Inc. Heterocyclic kinase inhibitors
WO2010043721A1 (en) 2008-10-17 2010-04-22 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
US20120010188A1 (en) 2008-12-04 2012-01-12 Promimagen Ltd. Imidazopyridine Compounds
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
WO2010084160A1 (en) 2009-01-21 2010-07-29 Oryzon Genomics S.A. Phenylcyclopropylamine derivatives and their medical use
WO2010091067A2 (en) 2009-02-04 2010-08-12 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CN102361872B (zh) 2009-02-13 2014-12-03 拜耳知识产权有限责任公司 作为akt抑制剂的稠合嘧啶
WO2010104306A2 (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
WO2010108059A1 (en) 2009-03-20 2010-09-23 Incyte Corporation Substituted pyrimidine derivatives as antagonists of the histamine h4 receptor
RU2529868C2 (ru) 2009-03-31 2014-10-10 Кисcеи Фармасьютикал Ко., Лтд. Производное индолизина и его применение в медицинских целях
DK2419429T3 (da) * 2009-04-16 2014-06-23 Ct Nac De Investigaciones Oncológicas Cnio Imidazopyraziner som inhibitorer af proteinkinaser
TWI461426B (zh) 2009-05-27 2014-11-21 Merck Sharp & Dohme （二氫）咪唑並異〔５，１－ａ〕喹啉類
CA2764808A1 (en) 2009-06-10 2010-12-16 Sunovion Pharmaceuticals Inc. Histamine h3 inverse agonists and antagonists and methods of use thereof
US8686009B2 (en) 2009-06-25 2014-04-01 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds
PE20170003A1 (es) 2009-08-17 2017-03-15 Intellikine Llc Compuestos heterociclicos y usos de los mismos
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
WO2011033265A1 (en) 2009-09-18 2011-03-24 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
WO2011042217A1 (en) 2009-10-09 2011-04-14 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
US9073927B2 (en) 2010-01-22 2015-07-07 Fundacion Centro Nacional De Investigaciones Oncologicas 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
WO2011106105A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
WO2011106106A2 (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
JP5841078B2 (ja) 2010-03-18 2016-01-06 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 イミダゾピラジン
CN102869661B (zh) 2010-03-18 2015-08-05 韩国巴斯德研究所 抗感染化合物
PL2552920T3 (pl) 2010-04-02 2017-08-31 Ogeda Sa Nowe wybiórcze związki antagonistów receptora NK-3, farmaceutyczne kompozycje i sposoby do zastosowania w zaburzeniach pośredniczonych przez receptory NK-3
JP5868948B2 (ja) 2010-04-19 2016-02-24 オリゾン・ジェノミックス・ソシエダッド・アノニマＯｒｙｚｏｎ Ｇｅｎｏｍｉｃｓ Ｓ．Ａ． リジン特異的脱メチル化酵素１阻害薬およびその使用
EP2560949B1 (en) 2010-04-20 2015-12-02 Università degli Studi di Roma "La Sapienza" Tranylcypromine derivatives as inhibitors of histone demethylase lsd1 and/or lsd2
WO2011141713A1 (en) 2010-05-13 2011-11-17 Centro Nacional De Investigaciones Oncologicas (Cnio) New bicyclic compounds as pi3-k and mtor inhibitors
MA34300B1 (fr) 2010-05-13 2013-06-01 Amgen Inc Composés azotés hétérocycliques convenant comme inhibiteurs de la pde10
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
US8703759B2 (en) 2010-07-02 2014-04-22 Gilead Sciences, Inc. Fused heterocyclic compounds as ion channel modulators
CN103097384B (zh) 2010-07-12 2017-02-15 拜耳知识产权有限责任公司 取代的咪唑并[1,2‑a]嘧啶和吡啶
WO2012009475A1 (en) 2010-07-14 2012-01-19 Oregon Health & Science University Methods of treating cancer with inhibition of lysine-specific demethylase 1
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
EP3375775A1 (en) 2010-07-29 2018-09-19 Oryzon Genomics, S.A. Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use
EP2598480B1 (en) 2010-07-29 2019-04-24 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as lsd1 inhibitors
US9527805B2 (en) 2010-09-10 2016-12-27 Robert A. Casero Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders
WO2012043638A1 (ja) 2010-09-29 2012-04-05 キッセイ薬品工業株式会社 （アザ）インドリジン誘導体及びその医薬用途
US20130303545A1 (en) 2010-09-30 2013-11-14 Tamara Maes Cyclopropylamine derivatives useful as lsd1 inhibitors
WO2012047852A2 (en) 2010-10-07 2012-04-12 The J. David Gladstone Institutes Compositions and methods for modulating immunodeficiency virus transcription
MX343596B (es) 2010-10-18 2016-11-11 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
CA2818903C (en) 2010-12-14 2021-03-23 Electrophoretics Limited 5-(1,3-benzoxazol-2-yl)-4-(pyridin-4-yl)pyrimidin-2-amine and its use as a casein kinase 1delta inhibitor
EP2651945A1 (en) 2010-12-17 2013-10-23 Bayer Intellectual Property GmbH 6-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
CA2821817A1 (en) 2010-12-17 2012-06-21 Bayer Intellectual Property Gmbh Substituted 6-imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
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?.
CN103370322B (zh) 2010-12-17 2016-02-10 拜耳知识产权有限责任公司 在过度增殖性病症的治疗中用作mps-1和tkk抑制剂的2-取代的咪唑并吡嗪
US8987271B2 (en) 2010-12-22 2015-03-24 Eutropics Pharmaceuticals, Inc. 2,2′-biphenazine compounds and methods useful for treating disease
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
EP2665726A4 (en) 2011-01-21 2014-09-03 Gen Hospital Corp COMPOSITIONS AND METHODS OF TREATING CARDIOVASCULAR DISEASES
US20140163041A1 (en) 2011-02-08 2014-06-12 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders
EP2712315B1 (en) 2011-02-08 2021-11-24 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative disorders
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
US9464065B2 (en) 2011-03-24 2016-10-11 The Scripps Research Institute Compounds and methods for inducing chondrogenesis
EA023143B1 (ru) 2011-03-25 2016-04-29 Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед Замещенный циклопропиламин в качестве ингибитора lsd1
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
WO2012156537A2 (en) 2011-05-19 2012-11-22 Oryzon Genomics, S.A. Lysine demethylase inhibitors for thrombosis and cardiovascular diseases
EP2524918A1 (en) 2011-05-19 2012-11-21 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyrazines derivates as kinase inhibitors
EP2741741A2 (en) 2011-05-19 2014-06-18 Oryzon Genomics, S.A. Lysine demethylase inhibitors for inflammatory diseases or conditions
KR20140040819A (ko) 2011-06-20 2014-04-03 인사이트 코포레이션 Ｊａｋ 저해제로서의 아제티디닐 페닐, 피리딜 또는 피라지닐 카르복스아미드 유도체
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
JP6111195B2 (ja) 2011-08-09 2017-04-05 武田薬品工業株式会社 シクロプロパンアミン化合物
PT2744330T (pt) 2011-08-15 2020-10-01 Univ Utah Res Found Análogos substituídos de (e)-n'-(1-feniletilideno) benzoidrazida como inibitores de histona desmetilase
US9289415B2 (en) 2011-09-01 2016-03-22 The Brigham And Women's Hospital, Inc. Treatment of cancer
JP6067019B2 (ja) 2011-09-02 2017-01-25 プロメガ コーポレイションＰｒｏｍｅｇａ Ｃｏｒｐｏｒａｔｉｏｎ 代謝的に活性な細胞の酸化還元状態を評価するための化合物及び方法、ならびにｎａｄ（ｐ）／ｎａｄ（ｐ）ｈを測定するための方法
EP2906562B1 (en) 2011-10-10 2016-10-05 H. Lundbeck A/S Pde9i with imidazo pyrazinone backbone
US9487512B2 (en) 2011-10-20 2016-11-08 Oryzon Genomics S.A. (Hetero)aryl cyclopropylamine compounds as LSD1 inhibitors
IL264982B (en) 2011-10-20 2022-08-01 Oryzon Genomics Sa Hetero(aryl)cyclopropylamine compounds as lsd1 inhibitors
ITMI20111971A1 (it) 2011-10-28 2013-04-29 Mesogenics Srl Inibitori dell'enzima lsd-1 per l'induzione del differenziamento osteogenico
WO2013074390A1 (en) 2011-11-14 2013-05-23 Merck Sharp & Dohme Corp. Triazolopyridinone pde10 inhibitors
EP2787990A4 (en) 2011-12-05 2015-09-02 Univ Brandeis TREATMENT OF AMYLOIDOSE BY COMPOUNDS FOR REGULATING RETROMER STABILIZATION
EP2822948B1 (en) 2012-03-07 2016-04-06 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
ES2710491T3 (es) 2012-06-28 2019-04-25 Novartis Ag Moduladores de la vía del complemento y sus usos
GB201212513D0 (en) 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents
JP6430383B2 (ja) 2012-09-28 2018-11-28 ヴァンダービルト ユニバーシティーＶａｎｄｅｒｂｉｌｔ Ｕｎｉｖｅｒｓｉｔｙ 選択的ｂｍｐ阻害剤としての縮合複素環化合物
JP6457942B2 (ja) 2012-10-05 2019-01-23 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｇｄｆ−８阻害剤
CA2887598A1 (en) 2012-10-12 2014-04-17 Takeda Pharmaceutical Company Limited Cyclopropanamine compound and use thereof
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)
EP2927212A4 (en) 2012-11-28 2016-06-08 Univ Kyoto LSD1-SELECTIVE HEMMER WITH LYSINE STRUCTURE
EP2925307B1 (en) 2012-11-30 2020-10-28 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
US20150376198A1 (en) 2013-02-18 2015-12-31 The Scripps Research Institute Modulators of vasopressin receptors with therapeutic potential
WO2014164867A1 (en) 2013-03-11 2014-10-09 Imago Biosciences Kdm1a inhibitors for the treatment of disease
CN105283552A (zh) 2013-03-13 2016-01-27 澳大利亚核科学和技术组织 具有非功能性tspo基因的转基因非人类生物体
US20160045531A1 (en) 2013-03-14 2016-02-18 Epizyme, Inc. Combination therapy for treating cancer
US20140343118A1 (en) 2013-03-14 2014-11-20 Duke University Methods of treatment using arylcyclopropylamine compounds
US9918983B2 (en) 2013-05-30 2018-03-20 The Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Vegas Suicidal LSD1 inhibitors targeting SOX2-expressing cancer cells
WO2014205213A1 (en) 2013-06-19 2014-12-24 University Of Utah Research Foundation Substituted (e)-n'-(1-phenylethylidene) benzohydrazide analogs as histone demethylase inhibitors
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
DK3080100T3 (da) 2013-12-11 2023-02-06 Celgene Quanticel Res Inc Hæmmere af lysinspecifik demethylase-1
US9346776B2 (en) 2014-02-13 2016-05-24 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
TW201613860A (en) 2014-02-13 2016-04-16 Incyte Corp Cyclopropylamines as LSD1 inhibitors
SG10201806849WA (en) 2014-02-13 2018-09-27 Incyte Corp Cyclopropylamines as lsd1 inhibitors
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
CN106488915B (zh) 2014-02-13 2020-10-02 因赛特公司 作为lsd1抑制剂的环丙胺
US9428470B2 (en) 2014-02-13 2016-08-30 Takeda Pharmaceutical Company Limited Heterocyclic compound
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
EA028942B1 (ru) 2014-04-02 2018-01-31 Бристол-Майерс Сквибб Компани Биарильные ингибиторы киназы
TWI669291B (zh) 2014-04-11 2019-08-21 日商武田藥品工業股份有限公司 環丙胺化合物及其用途
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
MX375102B (es) 2014-05-30 2025-03-06 Ieo St Europeo Di Oncologia S R L Compuestos de ciclopropilamina como inhibidores de histona demetilasa
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
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
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
EP3204383B1 (en) 2014-10-08 2020-11-18 F.Hoffmann-La Roche Ag Spirodiamine derivatives as aldosterone synthase inhibitors
US9944647B2 (en) 2015-04-03 2018-04-17 Incyte Corporation Heterocyclic compounds as LSD1 inhibitors
US10399933B2 (en) 2015-04-03 2019-09-03 Bristol-Myers Squibb Company Inhibitors of indoleamine-2,3-dioxygenase for the treatment of cancer
AU2016239861A1 (en) 2015-04-03 2017-10-12 Mutabilis Heterocyclic compounds and their use in preventing or treating bacterial infections
UA126277C2 (uk) 2015-08-12 2022-09-14 Інсайт Корпорейшн Солі інгібітору lsd1
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
BR112018071585B1 (pt) 2016-04-22 2024-01-02 Incyte Corporation Formulações de um inibidor de lsd1, seus usos e método de preparação das mesmas
WO2018136634A1 (en) 2017-01-18 2018-07-26 Vanderbilt University Fused heterocyclic compounds as selective bmp inhibitors
AU2018233367B2 (en) 2017-03-16 2021-08-12 Jiangsu Hengrui Medicine Co., Ltd. Heteroaryl[4,3-c]pyrimidine-5-amine derivative, preparation method therefor, and medical uses thereof

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