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AR096757A1 - Inhibidores de bromodominios - Google Patents

Inhibidores de bromodominios

Info

Publication number
AR096757A1
AR096757A1 ARP140102430A ARP140102430A AR096757A1 AR 096757 A1 AR096757 A1 AR 096757A1 AR P140102430 A ARP140102430 A AR P140102430A AR P140102430 A ARP140102430 A AR P140102430A AR 096757 A1 AR096757 A1 AR 096757A1
Authority
AR
Argentina
Prior art keywords
alkyleneyl
alkylenyl
alkyl
nrjrk
haloalkyl
Prior art date
Application number
ARP140102430A
Other languages
English (en)
Inventor
D Findanze Steven
Sheppard George
Wang Le
Marjanovic Jasmina
Dai Yujia
Holms James
Liu Dachun
Mclellan William
Mdaniel Keith
Hasvold Lisa
Original Assignee
Abbvie Inc
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 Abbvie Inc filed Critical Abbvie Inc
Publication of AR096757A1 publication Critical patent/AR096757A1/es

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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
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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Abstract

Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), o una sal farmacéuticamente aceptable del mismo, donde Rˣ es hidrógeno o C₁₋₃ alquilo; Rʸ es hidrógeno o C₁₋₃ alquilo; A¹ es N o CR¹, A² es N o CR², A³ es N o CR³; y A⁴ es N o CR⁴; donde cero, uno, dos o tres de A¹, A², A³, y A⁴ son N; R¹ es hidrógeno, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, halógeno, C₁₋₆ haloalquilo, CN, NO₂; R² es hidrógeno, -S(O)₂R²ᵃ, -S(O)₂NR²ᵇR²ᶜ, -N(R²ᵇ)S(O)₂R²ᵃ, o -(C₁₋₆ alquilenil)-S(O)₂R²ᵃ; donde R²ᵃ es C₁₋₆ alquilo o C₁₋₆ haloalquilo; y R²ᵇ y R²ᶜ son en forma independiente entre sí hidrógeno, C₁₋₆ alquilo, o C₁₋₆ haloalquilo; L¹ es O, N(H), o OCH₂ donde la unidad CH₂ de OCH₂ se une a G¹; Rˣ¹, G¹, R³, y R⁴, se seleccionan entre (i), (ii), (iii), ó (iv); (i) Rˣ¹ es -CN, -Gˣ¹-Gˣ², -(C₁₋₆ alquilenil)-Gˣ¹-Gˣ², -C(O)N(Rˣᵃ)(Rˣᵇ), C₁₋₆ alquilo sustituido con un sustituyente seleccionado entre el grupo que consiste en -CN, -ORˣᵇ, -SRˣᵇ, -S(O)Rˣᵇ, -S(O)₂Rˣᵇ, -NRˣᵃRˣᵇ, -C(O)Rˣᵇ, -C(O)ORˣᵇ, -C(O)NRˣᵃRˣᵇ, y -S(O)₂NRˣᵃRˣᵇ; C₂₋₆ alquenilo, o C₂₋₆ alquinilo; donde C₂₋₆ alquenilo y C₂₋₆ alquinilo están sustituidos en forma independiente entre sí con un sustituyente seleccionado entre el grupo que consiste en -CN, -ORˣᶜ, -SRˣᶜ, -S(O)Rˣᶜ, -S(O)₂Rˣᶜ, -NRˣᵃRˣᶜ, -C(O)Rˣᶜ, -C(O)ORˣᶜ,-C(O)NRˣᵃRˣᶜ, -S(O)₂NRˣᵃRˣᶜ, y Gˣ¹; G¹ es fenilo, C₃₋₆ cicloalquilo, C₅₋₆ heteroarilo, o C₄₋₆ heterociclo; donde cada G¹ no está sustituido o está sustituido en forma independiente con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre el grupo que consiste en los grupos Rᵘ y Rᵛ, R³ es R¹ᵃ, -C(O)OH, -C(O)NR³ᵃR³ᵇ, -NR³ᵃR³ᵇ, G³ᵃ, -G³ᵃ-G³ᵇ, -(C₁₋₆ alquilenil)-OR³ᵃ, -(C₁₋₆ alquilenil)-NR³ᵃR³ᵇ, -(C₁₋₆ alquilenil)-G³ᵃ, o -(C₁₋₆ alquilenil)-G³ᵃ-G³ᵇ; y R⁴ es R¹ᵃ o G⁴; (ii) Rˣ¹ es -CN, -Gˣ¹-Gˣ², -(C₁₋₆ alquilenil)-Gˣ¹-Gˣ², -C(O)N(Rˣᵃ)(Rˣᵇ), hidrógeno, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -C(O)ORᵃˣ¹, -C(O)NRᵇˣ¹Rᶜˣ¹, -C(O)Rᵈˣ¹, -S(O)₂Rᵈˣ¹, -S(O)₂NRᵇˣ¹Rᶜˣ¹, Gˣ¹, C₁₋₆ haloalquilo, o C₁₋₆ alquilo; donde C₁₋₆ alquilo, C₂₋₆ alquenilo, y C₂₋₆ alquinilo están opcionalmente sustituidos en cada caso con un sustituyente seleccionado entre el grupo que consiste en -CN, -ORˣᶜ, -SRˣᶜ, -S(O)Rˣᶜ, -S(O)₂Rˣᶜ, -NRˣᵃRˣᶜ, -C(O)Rˣᶜ, -C(O)ORˣᶜ, -C(O)NRˣᵃRˣᶜ, -S(O)₂NRˣᵃRˣᶜ, y Gˣ¹; G¹ es fenilo, C₃₋₆ cicloalquilo, C₅₋₆ heteroarilo, o C₄₋₆ heterociclo; donde cada G¹ está sustituido con un grupo Rᵘ y además está opcionalmente sustituido con 1, 2, 3, 4, ó 5 grupos Rᵛ; R³ es R¹ᵃ, -C(O)OH, -C(O)NR³ᵃR³ᵇ, -NR³ᵃR³ᵇ, G³ᵃ, -G³ᵃ-G³ᵇ, -(C₁₋₆ alquilenil)-OR³ᵃ, -(C₁₋₆ alquilenil)-NR³ᵃR³ᵇ, -(C₁₋₆ alquilenil)-G³ᵃ, o -(C₁₋₆ alquilenil)-G³ᵃ-G³ᵇ; y R⁴ es R¹ᵃ o G⁴; (iii) Rˣ¹ es -CN, -Gˣ¹-Gˣ², -(C₁₋₆ alquilenil)-Gˣ¹-Gˣ², C(O)N(Rˣᵃ)(Rˣᵇ), hidrógeno, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -C(O)ORᵃˣ¹, -C(O)NRᵇˣ¹Rᶜˣ¹, -C(O)Rᵈˣ¹, -S(O)₂Rᵈˣ¹, -S(O)₂NRᵇˣ¹Rᶜˣ¹, Gˣ¹, C₁₋₆ haloalquilo, o C₁₋₆ alquilo; donde C₁₋₆ alquilo, C₂₋₆ alquenilo, y C₂₋₆ alquinilo están opcionalmente sustituidos en cada caso con un sustituyente seleccionado entre el grupo que consiste en -CN, -ORˣᶜ, -SRˣᶜ, -S(O)Rˣᶜ, -S(O)₂Rˣᶜ, -NRˣᵃRˣᶜ, -C(O)Rˣᶜ, -C(O)ORˣᶜ, -C(O)NRˣᵃRˣᶜ, -S(O)₂NRˣᵃRˣᶜ, y Gˣ¹; G¹ es fenilo, C₃₋₆ cicloalquilo, C₅₋₆ heteroarilo, o C₄₋₆ heterociclo; donde cada G¹ no está sustituido o está sustituido en forma independiente con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre el grupo que consiste en los grupos Rᵘ y Rᵛ; R³ es -C(O)OH, -C(O)NR³ᵃR³ᵇ, -NR³ᵃR³ᵇ, G³ᵃ, -G³ᵃ-G³ᵇ, -(C₁₋₆ alquilenil)-OR³ᵃ, -(C₁₋₆ alquilenil)-NR³ᵃR³ᵇ, -(C₁₋₆ alquilenil)-G³ᵃ, o -(C₁₋₆ alquilenil)-G³ᵃ-G³ᵇ; y R⁴ es R¹ᵃ o G⁴; (iv) Rˣ¹ es -CN, -Gˣ¹-Gˣ², -(C₁₋₆ alquilenil)-Gˣ¹-Gˣ², C(O)N(Rˣᵃ)(Rˣᵇ), hidrógeno, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -C(O)ORᵃˣ¹, -C(O)NRᵇˣ¹Rᶜˣ¹, -C(O)Rᵈˣ¹, -S(O)₂Rᵈˣ¹, -S(O)₂NRᵇˣ¹Rᶜˣ¹, Gˣ¹, C₁₋₆ haloalquilo, o C₁₋₆ alquilo; donde C₁₋₆ alquilo, C₂₋₆ alquenilo, y C₂₋₆ alquinilo están opcionalmente sustituidos en cada caso con un sustituyente seleccionado entre el grupo que consiste en -CN, -ORˣᶜ, -SRˣᶜ, -S(O)Rˣᶜ, -S(O)₂Rˣᶜ, -NRˣᵃRˣᶜ, -C(O)Rˣᶜ, -C(O)ORˣᶜ, -C(O)NRˣᵃRˣᶜ, -S(O)₂NRˣᵃRˣᶜ, y Gˣ¹; G¹ es fenilo, C₃₋₆ cicloalquilo, C₅₋₆ heteroarilo, o C₄₋₆ heterociclo; donde cada G¹ no está sustituido o está sustituido en forma independiente con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre el grupo que consiste en los grupos Rᵘ y Rᵛ; R³ es R¹ᵃ, -C(O)OH, -C(O)NR³ᵃR³ᵇ, -NR³ᵃR³ᵇ, G³ᵃ, -G³ᵃ-G³ᵇ, -(C₁₋₆ alquilenil)-OR³ᵃ -(C₁₋₆ alquilenil)-NR³ᵃR³ᵇ, -(C₁₋₆alquilenil)-G³ᵃ, o -(C₁₋₆ alquilenil)-G³ᵃ-G³ᵇ; y R⁴ es G⁴; Rˣᵃ, en cada caso, es en forma independiente hidrógeno, C₁₋₆ alquilo, o C₁₋₆ haloalquilo; Rˣᵇ, en cada caso, es en forma independiente C₁₋₆ alquilo sustituido con un sustituyente seleccionado entre el grupo que consiste en - CN, -ORᵃˣ¹, -SRᵃˣ¹, -S(O)Rᵈˣ¹, -S(O)₂Rᵈˣ¹, -NRᵇˣ¹Rᶜˣ¹, -C(O)Rᵃˣ¹, -C(O)ORᵃˣ¹, -C(O)NRᵇˣ¹Rᶜˣ¹, y -S(O)₂NRᵇˣ¹Rᶜˣ¹; Rˣᶜ, en cada caso, es en forma independiente hidrógeno, C₁₋₆ alquilo, C₁₋₆ haloalquilo, Gᵃ, -(C₁₋₆ alquilenil)-Gᵃ, o Rˣᵇ; Rᵃˣ¹, Rᵇˣ¹, y Rᶜˣ¹, en cada caso, son en forma independiente entre sí hidrógeno, C₁₋₆ alquilo, C₁₋₆ haloalquilo, Gᵃ, o -(C₁₋₆ alquilenil)-Gᵃ; Rᵈˣ¹, en cada caso, es en forma independiente C₁₋₆ alquilo, C₁₋₆ haloalquilo, Gᵃ, o -(C₁₋₆ alquilenil)-Gᵃ; R¹ᵃ, en cada caso, es en forma independiente hidrógeno, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, halógeno, C₁₋₆ haloalquilo, CN, o NO₂; R³ᵃ y R³ᵇ, en cada caso, son en forma independiente entre sí hidrógeno, C₁₋₆ alquilo, C₁₋₆ haloalquilo, G³ᵃ, -G³ᵃ-G³ᵇ, -(C₁₋₆ alquilenil)-G³ᵃ, -(C₁₋₆ alquilenil)-G³ᵃ-G³ᵇ, o C₁₋₆ alquilo sustituido con un sustituyente seleccionado entre el grupo que consiste en -CN, -ORʰ, -SRʰ, -S(O)Rⁱ, -S(O)₂Rʰ, -NRʲRᵏ, -C(O)Rʰ, -C(O)ORʰ, -C(O)NRʲRᵏ, y -S(O)₂NRʲRᵏ; G⁴, en cada caso, es en forma independiente fenilo, C₃₋₆ cicloalquilo, C₅₋₆ heteroarilo, o C₄₋₆ heterociclo; cada uno de los cuales está opcionalmente sustituido con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre el grupo que consiste en C₁₋₆ alquilo, NO₂, halógeno, C₁₋₆ haloalquilo, -CN, oxo, -ORʰ, -SRʰ, -S(O)₂Rʰ, y -NRʲRᵏ; Rᵘ, en cada caso, es en forma independiente -(C₁₋₆ alquilenil)-Gᵘ, -(C₂₋₆ alquinilen)-Gᵘ, -(C₁₋₆ alquilenil)-SRʰ, -C(O)-Z¹, -C(O)-NZ¹Z², -S(O)₂-Z¹, -N(Z²)Z¹, o -N(Z²)S(O)₂-Z¹; donde Z¹ es Gᵘ, -(C₁₋₆ alquilenil)-Gᵘ, -(C₂₋₆ alquenilen)-Gᵘ, -(C₁₋₆ alquilenil)-CN, -(C₁₋₆ alquilenil)-SRʰ, -(C₁₋₆ alquilenil)-ORʰ, -(C₁₋₆ alquilenil)-NRʲRᵏ, o -(C₁₋₆ alquilenil)-C₁₋₄ alcoxi-C₁₋₄ alcoxi, y Z² es hidrógeno, C₁₋₆ alquilo, o C₁₋₆ haloalquilo; Gᵘ, en cada caso, es en forma independiente arilo, heteroarilo, heterociclo, cicloalquilo, o cicloalquenilo, donde cada Gᵘ no está sustituido o está sustituido en forma independiente con 1, 2, 3, 4, ó 5 sustituyentes seleccionados en forma independiente entre el grupo que consiste en C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, halógeno, C₁₋₆ haloalquilo, -CN, oxo, NO₂, -ORʰ, -O-(C₂₋₆ alquilenil)-NRʲRᵏ, -OC(O)Rⁱ, -OC(O)NRʲRᵏ, -O-(C₁₋₆ alquilenil)-NRʲRᵏ, -SRʰ, -S(O)₂Rʰ, -S(O)₂NRʲRᵏ, -C(O)Rʰ, -C(O)ORʰ, -C(O)NRʲRᵏ, -NRʲRᵏ, -N(Rʰ)C(O)Rⁱ, -N(Rʰ)S(O)₂Rⁱ, -N(Rʰ)C(O)O(Rⁱ), -N(Rʰ)C(O)NRʲRᵏ, Gᵘᵃ, -(C₁₋₆ alquilenil)-ORʰ, -(C₁₋₆ alquilenil)-OC(O)Rⁱ, -(C₁₋₆ alquilenil)-OC(O)NRʲRᵏ, -(C₁₋₆ alquilenil)-SRʰ, -(C₁₋₆ alquilenil)-S(O)₂Rʰ, -(C₁₋₆ alquilenil)-S(O)₂NRʲRᵏ, -(C₁₋₆ alquilenil)-C(O)Rʰ, -(C₁₋₆ alquilenil)-C(O)ORʰ, -(C₁₋₆ alquilenil)-C(O)NRʲRᵏ, -(C₁₋₆ alquilenil)-NRʲRᵏ, -(C₁₋₆ alquilenil)-N(Rʰ)C(O)Rⁱ, -(C₁₋₆ alquiIenil)-N(Rʰ)S(O)₂Rⁱ, -(C₁₋₆ alquilenil)-N(Rʰ)C(O)O(Rⁱ), -(C₁₋₆ alquilenil)-N(Rʰ)C(O)NRʲRᵏ, -(C₁₋₆ alquilenil)-CN, y -(C₁₋₆ alquilenil)-Gᵘᵃ; Gᵃ, Gˣ¹, Gˣ², G³ᵃ, G³ᵇ, y Gᵘᵃ, en cada caso, son en forma independiente entre sí arilo, heteroarilo, heterociclo, cicloalquilo, o cicloalquenilo, cada uno de los cuales está opcionalmente sustituido con 1, 2, 3, 4, ó 5 grupos Rᶻ; Rᶻ y Rᵛ, en cada caso, son en forma independiente entre sí C₁₋₆ alquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, halógeno, C₁₋₆ haloalquilo, -CN, oxo, NO₂, -ORʰ, -OC(O)Rⁱ, -OC(O)NRʲRᵏ, -SRʰ, -S(O)₂Rʰ, -S(O)₂NRʲRᵏ, -C(O)Rʰ, -C(O)ORʰ, -C(O)NRʲRᵏ, -NRʲRᵏ, -N(Rʰ)C(O)Rⁱ, -N(Rʰ)S(O)₂Rⁱ, -N(Rʰ)C(O)O(Rⁱ), -N(Rʰ)C(O)NRʲRᵏ, -(C₁₋₆ alquilenil)-ORʰ, -(C₁₋₆ alquilenil)-OC(O)Rⁱ, -(C₁₋₆ alquilenil)-OC(O)NRʲRᵏ, -(C₁₋₆ alquilenil)-SRʰ, -(C₁₋₆alquilenil)-S(O)₂Rʰ, -(C₁₋₆ alquilenil)-S(O)₂NRʲRᵏ, -(C₁₋₆ alquilenil)-C(O)Rʰ, -(C₁₋₆ alquilenil)-C(O)ORʰ, -(C₁₋₆ alquilenil)-C(O)NRʲRᵏ, -(C₁₋₆ alquilenil)-NRʲRᵏ, -(C₁₋₆ alquilenil)-N(Rʰ)C(O)Rⁱ, -(C₁₋₆ alquilenil)-N(Rʰ)S(O)₂Rⁱ, -(C₁₋₆ alquilenil)-N(Rʰ)C(O)O(Rⁱ), -(C₁₋₆ alquilenil)-N(Rʰ)C(O)NRʲRᵏ, o -(C₁₋₆ alquilenil)-CN; Rʰ, Rʲ, Rᵏ, en cada caso, son en forma independiente entre sí hidrógeno, C₁₋₆ alquilo, o C₁₋₆ haloalquilo; y Rⁱ, en cada caso, es en forma independiente C₁₋₆ alquilo o C₁₋₆ haloalquilo.
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Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013097052A1 (en) * 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
TWI719464B (zh) 2013-03-15 2021-02-21 美商英塞特控股公司 作為bet蛋白抑制劑之三環雜環
SG11201510678TA (en) * 2013-06-28 2016-01-28 Abbvie Inc Bromodomain inhibitors
JP2016523964A (ja) 2013-07-08 2016-08-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｂｅｔタンパク質阻害剤としての三環式複素環
PE20161065A1 (es) 2013-10-18 2016-11-19 Celgene Quanticel Res Inc Inhibidores de bromodominio
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
KR20240134245A (ko) 2014-04-23 2024-09-06 인사이트 홀딩스 코포레이션 BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
CN107108613B (zh) 2014-11-10 2020-02-25 基因泰克公司 布罗莫结构域抑制剂及其用途
MA40940A (fr) * 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
MA40943A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
JP6709792B2 (ja) 2015-01-29 2020-06-17 ジェネンテック， インコーポレイテッド 治療用化合物およびその使用
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
WO2017177955A1 (en) * 2016-04-15 2017-10-19 Abbvie Inc. Bromodomain inhibitors
CN105924671A (zh) * 2016-06-02 2016-09-07 扬州兰都塑料科技有限公司 一种电力电缆用增韧剂
CN105924842A (zh) * 2016-06-02 2016-09-07 扬州兰都塑料科技有限公司 一种力学性能改善的电力电缆
CN105924841A (zh) * 2016-06-02 2016-09-07 扬州兰都塑料科技有限公司 一种力学性能改善的电力电缆的制备方法
EP4234554A3 (en) 2016-06-20 2023-12-27 Incyte Corporation Crystalline solid forms of a bet inhibitor
CN108069958A (zh) * 2016-11-10 2018-05-25 凯惠科技发展(上海)有限公司 一种含氮杂环类化合物、其制备方法、药物组合物及应用
CN110167939B (zh) * 2017-01-11 2021-12-31 江苏豪森药业集团有限公司 吡咯并[2,3-c]吡啶类衍生物、其制备方法及其在医药上的应用
CN109384784B (zh) * 2017-08-10 2021-01-12 浙江海正药业股份有限公司 磺酰胺类衍生物、其制备方法及其在医药上的用途
KR102026243B1 (ko) * 2018-01-19 2019-09-27 연세대학교 산학협력단 백혈병 치료용 약학적 조성물
WO2019184919A1 (zh) * 2018-03-27 2019-10-03 成都海创药业有限公司 一种含有金刚烷的化合物及其在治疗癌症中的用途
BR112020019824A2 (pt) * 2018-03-29 2021-01-05 Board Of Regents, The University Of Texas System Composto de fórmula estrutural i ou um sal do mesmo, composição farmacêutica, método de inibição de cbp, método de inibição de p300, método de tratamento de uma doença mediada por cbp, método de tratamento de uma doença mediada por p300 e método para alcançar um efeito em um paciente
US10442799B1 (en) 2018-04-07 2019-10-15 Fuqiang Ruan Heterocyclic compounds and uses thereof
KR20210038921A (ko) 2018-07-25 2021-04-08 치아타이 티안큉 파마수티컬 그룹 주식회사 브로모도메인 단백질 억제제로서의 설폭시민 화합물과 약학적 조성물 및 이의 의학적 용도
CN110776508B (zh) 2018-07-27 2021-07-16 海创药业股份有限公司 一种brd4抑制剂及其制备方法和用途
WO2020092638A1 (en) 2018-10-30 2020-05-07 Nuvation Bio Inc. Heterocyclic compounds as bet inhibitors
US20220079951A1 (en) * 2018-12-20 2022-03-17 Saint Louis University Bet inhibitors for modulating dux4 expression in fshd
AU2020242411A1 (en) * 2019-03-17 2021-11-11 Shanghai Ringene Biopharma Co., Ltd. Pyrrole amidopyridone compound, preparation method therefor and use thereof
GB201905721D0 (en) 2019-04-24 2019-06-05 Univ Dundee Compounds
WO2020253711A1 (zh) * 2019-06-17 2020-12-24 中国科学院上海药物研究所 一种吡咯并吡啶酮类化合物、其制备方法、其组合物和用途
CA3145827A1 (en) 2019-07-02 2021-01-07 Nuvation Bio Inc. Heterocyclic compounds as bet inhibitors
AU2020360170A1 (en) 2019-09-30 2022-05-19 Kyowa Kirin Co., Ltd. Bet degrader
CN112625036A (zh) * 2019-10-08 2021-04-09 上海海和药物研究开发股份有限公司 一类具有brd4抑制活性的化合物、其制备方法及用途
CN113387879B (zh) * 2020-03-14 2023-05-30 成都先导药物开发股份有限公司 一种胺类衍生物、其制备方法及其在医药上的应用
CA3172610A1 (en) * 2020-04-08 2021-10-14 Soo Jin Lee Agent for treating contrast-induced acute kidney injury
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
GB202016977D0 (en) 2020-10-26 2020-12-09 In4Derm Ltd Compounds
IL309651A (en) 2021-06-29 2024-02-01 Tay Therapeutics Ltd History Pyrolopyridone is useful in the treatment of cancer

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW263498B (es) * 1993-11-10 1995-11-21 Takeda Pharm Industry Co Ltd
JPH08337583A (ja) * 1995-04-13 1996-12-24 Takeda Chem Ind Ltd 複素環化合物およびその製造法
US6271380B1 (en) * 1998-12-30 2001-08-07 Dupont Pharmaceuticals Company 1H-imidazo[4,5-d]pyridazin-7-ones, 3H-imidazo-[4,5-c]pyridin-4-ones and corresponding thiones as corticotropin releasing factor (CRF) receptor ligands
WO2006129623A1 (ja) 2005-05-30 2006-12-07 Mitsubishi Tanabe Pharma Corporation チエノトリアゾロジアゼピン化合物及びその医薬としての用途
GB0919434D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
HUE031073T2 (en) * 2010-05-14 2017-06-28 Dana Farber Cancer Inst Inc Thieno triazolo-diazepine compounds for the treatment of neoplasia
CN103119160B (zh) 2010-05-14 2016-06-01 达那-法伯癌症研究所 用于调节代谢的组合物和方法
WO2013097052A1 (en) * 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
SG11201510678TA (en) * 2013-06-28 2016-01-28 Abbvie Inc Bromodomain inhibitors

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