AR094852A1 - Oestra-1,3,5(10),16-tetraeno-3-carboxamidas - Google Patents

Oestra-1,3,5(10),16-tetraeno-3-carboxamidas

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Publication number
AR094852A1
AR094852A1 ARP140100555A ARP140100555A AR094852A1 AR 094852 A1 AR094852 A1 AR 094852A1 AR P140100555 A ARP140100555 A AR P140100555A AR P140100555 A ARP140100555 A AR P140100555A AR 094852 A1 AR094852 A1 AR 094852A1
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Argentina
Prior art keywords
alkyl
cycloalkyl
nhr
heteroaryl
aryl
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ARP140100555A
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English (en)
Inventor
Dr Bothe Ulrich
Martin Dr Fischer Oliver
Dr Busemann Matthias
Dr Barak Naomi
Dr Rotgeri Andrea
Dr Marquardt Tobias
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Bayer Pharma Aktiengellschaft
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Publication of AR094852A1 publication Critical patent/AR094852A1/es

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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member

Abstract

Inhibidores de AKR1C3 de fórmula (1) y procesos para su preparación, producción de medicamentos útiles para el tratamiento y/o profilaxis de enfermedades, en especial de trastornos de sangrado y endometriosis. Reivindicación 1: Compuestos de la fórmula general (1) donde X es en forma independiente carbono o nitrógeno, donde el carbono puede estar sustituido con R¹; Y es carbono o nitrógeno, donde el carbono puede estar sustituido con R²; R¹ y R² es cada uno en forma independiente hidrógeno, halógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, nitrilo, nitro, -SO₂CH₃, -SO₂CH₂CH₃, -(C=O)CH₃, carboxilo, hidroxilo, -NH₂, -CH₂NH₂, -CH₂OH, -CH(OH)CH₃, -C(CH₃)₂OH, -(C=O)NH₂, -(C=O)NHCH₃, -(C=O)NHCH₂CH₃, -(C=O)N(CH₃)₂, -SO₂NH₂, -SO₂NHCH₃ -SO₂N(CH₃)₂; R³ es hidrógeno o halógeno; R⁴ es hidrógeno, alquilo C₁₋₆, cicloalquilo C₃₋₆ o cicloalquil C₃₋₆-alquilo C₁₋₆, que están opcionalmente sustituidos con hasta 6 átomos de halógeno y están opcionalmente monosustituidos o disustituidos con hidroxilo, alcoxi C₁₋₆, haloalcoxi C₁₋₆; R⁵ es hidrógeno, alquilo C₁₋₆ o cicloalquilo C₃₋₆, donde alquilo C₁₋₆ y cicloalquilo C₃₋₆ están opcionalmente sustituidos con hasta 6 átomos de halógeno y están opcionalmente monosustituidos o disustituidos con hidroxilo, hidroxi-alquilo C₁₋₆, alquilo C₁₋₆, alcoxi C₁₋₆, hidroxi-alcoxi C₂₋₆, haloalcoxi C₁₋₆, cicloalquilo C₃₋₆, arilo, heteroarilo, heterocicloalquilo de 3 - 10 miembros, aril-alquilo C₁₋₆, heteroaril-alquilo C₁₋₆, -C(=O)R, -C(=O)NH₂, -C(=O)N(H)R, -C(=O)N(R)R, -NH₂, -NHR, -N(R)R, -N(H)C(=O)R, -N(R)C(=O)R, -N(H)C(=O)OR, -N(R)C(=O)OR, -NO₂, -N(H)S(=O)R, -N(R)S(=O)R, -N(H)S(=O)₂R, -N(R)S(=O)₂R, -N=S(=O)(R)R, -S(=O)R, -S(=O)₂R, -S(=O)₂NH₂, -S(=O)₂NHR, -S(=O)₂N(R)R, -S(=O)(=NR)R, donde arilo, heteroarilo, aril-alquilo C₁₋₆ y heteroaril-alquilo C₁₋₆ están opcionalmente monosustituidos o polisustituidos en forma independiente entre sí con R⁶, y el heterocicloalquilo de 3 - 10 miembros está opcionalmente monosustituido o polisustituido en forma independiente con R, o R⁴ y R⁵ junto con el átomo de nitrógeno unido directamente forman un anillo de 4 - 7 miembros que está opcionalmente sustituido con uno o dos sustituyentes del grupo que consiste en: halógeno, nitrilo, hidroxilo, alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, arilo, heteroarilo, -C(=O)NH₂, -C(=O)N(H)R, -C(=O)N(R)R, -C(=O)OH, -C(=O)OR, -NH₂, -NHR, -N(R)R, -N(H)C(=O)R, -N(R)C(=O)R, -N(H)S(=O)R, -N(R)S(=O)R, -N(H)S(=O)₂R, -N(R)S(=O)₂R, -N=S(=O)(R)R, -OH, alcoxi C₁₋₆, haloalcoxi C₁₋₆, -OC(=O)R, -OC(=O)NH₂, -OC(=O)NHR, -OC(=O)N(R)R, -SH, alquil C₁₋₆-S-, -S(=O)R, -S(=O)₂R, -S(=O)₂NH₂, -S(=O)₂NHR, -S(=O)₂N(R)R, donde arilo y heteroarilo están opcionalmente monosustituidos o polisustituidos en forma independiente entre sí con R⁶, y donde en dicho anillo de 5, 6 ó 7 miembros uno o más grupos metileno se reemplazan opcionalmente por NH, NR, O ó S; R⁶ es halógeno, nitrilo, alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, heterocicloalquilo de 3 - 10 miembros, arilo, heteroarilo, -C(=O)R, -C(=O)NH₂, -C(=O)N(H)R,-C(=O)N(R)R, -C(=O)OR, -NH₂, -NHR, -N(R)R, -N(H)C(=O)R, -N(R)C(=O)R, -N(H)C(=O)NH₂, -N(H)C(=O)NHR, -N(H)C(=O)N(R)R, -N(R)C(=O)NH₂, -N(R)C(=O)NHR, -N(R)C(=O)N(R)R, -N(H)C(=O)OR, -N(R)C(=O)OR, -NO₂, -N(H)S(=O)R, -N(R)S(=O)R, -N(H)S(=O)₂R, -N(R)S(=O)₂R, -N=S(=O)(R)R, -OH, alcoxi C₁₋₆, haloalcoxi C₁₋₆, -OC(=O)R, -OC(=O)NH₂, -OC(=O)NHR, -OC(=O)N(R)R, -SH, alquil C₁₋₆-S-, -S(=O)R, -S(=O)₂R, -S(=O)₂NH₂, -S(=O)₂NHR, -S(=O)₂N(R)R, -S(=O)(=NR)R; R y R son en forma independiente entre sí alquilo C₁₋₆, cicloalquilo C₃₋₁₀ o haloalquilo C₁₋₆; o los estereoisómeros, tautómeros, N-óxidos, hidratos, solvatos o sales de los mismos, o una mezcla que consiste en los mismos.
ARP140100555A 2013-02-21 2014-02-21 Oestra-1,3,5(10),16-tetraeno-3-carboxamidas AR094852A1 (es)

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US (1) US9714266B2 (es)
EP (1) EP2958928B1 (es)
JP (1) JP6254195B2 (es)
KR (1) KR20150118153A (es)
CN (1) CN105008382B (es)
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