AR117122A1 - INHIBIDORES DE LA ÁCIDO a-AMINO-b-CARBOXIMUCÓNICO SEMIALDEHÍDO DESCARBOXILASA - Google Patents

INHIBIDORES DE LA ÁCIDO a-AMINO-b-CARBOXIMUCÓNICO SEMIALDEHÍDO DESCARBOXILASA

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AR117122A1
AR117122A1 ARP190103396A ARP190103396A AR117122A1 AR 117122 A1 AR117122 A1 AR 117122A1 AR P190103396 A ARP190103396 A AR P190103396A AR P190103396 A ARP190103396 A AR P190103396A AR 117122 A1 AR117122 A1 AR 117122A1
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Argentina
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alkyl
optionally substituted
membered
aryl
independently
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ARP190103396A
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Franco Francesca De
Nicola Giacche
Paride Liscio
Roberto Pellicciari
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Tes Pharma S R L
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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Abstract

En la presente divulgación se describen compuestos capaces de modular la actividad del ácido a-amino-b-carboximucónico semialdehído descarboxilasa (ACMSD), que son útiles para la prevención y/o el tratamiento de enfermedades y trastornos asociados con defectos en la biosíntesis de NAD⁺, por ejemplo, trastornos metabólicos, enfermedades neurodegenerativas, enfermedades inflamatorias crónicas, enfermedades renales y enfermedades asociadas con el envejecimiento. En la presente solicitud también se describen composiciones farmacéuticas que comprenden dichos compuestos y el uso de los mismos como medicamento. Reivindicación 1: Un compuesto representado por la fórmula (1), o una sal o tautómero farmacéuticamente aceptable de este, caracterizado porque: X es H, S, SR², NR², NR²R²’, O, OH, ORʰ, F, Br o CI; W es N o C; (i) cuando W es N, entonces: L es -(C(R⁵)₂)ₘCH=CH(C(R⁵)₂)ₚ-, un resto de fórmula (2), -(C(R⁵)₂)ₘY¹(C(R⁵)₂)ₚ-, -(C(R⁵)₂)ₘY¹(C(R⁵)₂)ₚ-ciclopropil-, -(C(R⁵)₂)ₘY¹CH=CH-, -(C(R⁵)₂)ₘNR³C=(O)(C(R⁵)₂)ₚ-, -(C(R⁵)₂)ₘfenil(C(R⁵)₂)ₚ-, -(C(R⁵)₂)ₘpiridinil(C(R⁵)₂)ₚ-, o -(C(R⁵)₂)ₘtiofenil(C(R⁵)₂)ₚ-; (ii) cuando W es C, entonces: L es -(C(R⁵)₂)ₘCH=CH(C(R⁵)₂)ₚ-, -(C(R⁵)₂)o-, -(C(R⁵)₂)ₘY¹(C(R⁵)₂)ₚ-, un resto de fórmula (2), -(C(R⁵)₂)ₘY¹CH=CH-, -(C(R⁵)₂)ₘC=(O)(CH₂)ₚ-, -(C(R⁵)₂)ₘC=(O)O(C(R⁵)₂)ₚ-, -(C(R⁵)₂)ₘC=(O)NR³(C(R⁵)₂)ₚ-, -(C(R⁵)₂)ₘNR³C=(O)(C(R⁵)₂)ₚ-, -(C(R⁵)₂)ₘfenil(C(R⁵)₂)ₚ-, -(C(R⁵)₂)ₘpiridinil(C(R⁵)₂)ₚ-, o -(C(R⁵)₂)ₘtiofeni|(C(R⁵)₂)ₚ-; Y¹ es O, NR⁴ o S(O)q; cada Y² es independientemente O, NH o S; R¹ está ausente, es arileno C₆₋₁₀, heteroarileno o cicloalquileno C₃₋₈, donde el heteroarileno comprende uno o dos anillos de 5 a 7 miembros y 1 a 4 heteroátomos seleccionados de N, O y S, y donde el arileno C₆₋₁₀, heteroarileno y cicloalquileno C₃₋₈ se sustituyen opcionalmente con uno a dos Rᵉ; R² es H o alquilo C₁₋₄; R²’ es H, alquilo C₁₋₄ o cicloalquilo C₃₋₇; o R² y R²’ junto con el átomo de nitrógeno al que están unidos forman un anillo heterocicloalquilo de 3 a 7 miembros que comprende 1 a 3 heteroátomos adicionales seleccionados de N, O y S; R³ es H o alquilo C₁₋₄; R⁴ es H o alquilo C₁₋₄; cada R⁵ es independientemente en cada caso H o alquilo C₁₋₄; cada R⁶ es independientemente en cada caso H o alquilo C₁₋₄; R⁷ es H, A, B o C; A es -(C(R⁶)₂)ʳCO₂Rˣ, -Y²(C(R⁶)₂)ʳCO₂Rˣ, -(C(R⁶)₂)ʳtetrazol, -(C(R⁶)₂)ʳoxadiazolon, -(C(R⁶)₂)ʳtetrazolon, -(C(R⁶)₂)ʳtiadiazolol, -(C(R⁶)₂)ʳisoxazol-3-ol, -(C(R⁶)₂)ʳP(O)(OH)ORˣ, -(C(R⁶)₂)ʳS(O)₂OH, -(C(R⁶)₂)ʳC(O)NHCN, o -(C(R⁶)₂)ʳC(O)NHS(O)₂alquilo, donde -(C(R⁶)₂)ʳtetrazol, -(C(R⁶)₂)ʳoxadiazolon, -(C(R⁶)₂)ʳtetrazolon, -(C(R⁶)₂)ʳtiadiazolol, -(C(R⁶)₂)ʳisoxazol-3-ol se sustituyen opcionalmente con alquilo C₁₋₆; B es -(C(R⁶)₂)ʳS(O)₂OC₁₋₄ alquilo, -O(C(R⁶)₂)ʳS(O)₂OC₁₋₄ alquilo, -Y²(C(R⁶)₂)ʳC(O)NRᵍRᵍ’, -Y²(C(R⁶)₂)ʳS(O)₂NRᵍRᵍ’, -(C(R⁶)₂)ʳC(O)NRᵍRᵍ’, -(C(R⁶)₂)ʳS(O)₂NRᵍRᵍ’, -(C(R⁶)₂)ʳC(O)NHS(O)₂NRᵍRᵍ’, -(C(R⁶)₂)ʳCO₂Rⁱ, -(C(R⁶)₂)ʳNH₂CO₂Rˣ, -(C(R⁶)₂)ʳP(O)(ORˣ)₂, -O(C(R⁶)₂)ʳP(O)(ORˣ)₂, -(C(R⁶)₂)ʳS(O)₂OH, -O(C(R⁶)₂)ʳS(O)₂OH, -(C(R⁶)₂)ʳP(O)₂ORˣ, o -O(C(R⁶)₂)ʳP(O)₂ORˣ; C es -(CH₂)ʳCN, -(CH₂)ₛOH, halógeno, -(C(R⁶)₂)ʳC₆₋₁₀ arilo, -(C(R⁶)₂)ʳS-C₆₋₁₀ arilo, -(C(R⁶)₂)ʳheteroarilo, -O(C(R⁶)₂)ʳheteroarilo, -O(C(R⁶)₂)ʳheterocicloalquilo, -O(C(R⁶)₂)ʳOH, -ORʸ, -(C(R⁶)₂)ʳC(O)NHCN, -CH=CHCO₂Rˣ, o -(C(R⁶)₂)ʳC(O)NHS(O)₂C₁₋₄alquilo, donde el arilo y el heteroarilo se sustituyen con uno a tres sustituyentes seleccionados cada uno independientemente del alquilo C₁₋₆, haloalquilo C₁₋₆, halógeno y OH, y donde el heterocicloalquilo se sustituye con uno a dos =O ó =S; Rᶜ es H, alquilo C₁₋₆, haloalquilo C₁₋₆, halógeno, -CN, -ORˣ o -CO₂Rˣ; Rᵈ es metilo, CF₃, CRᶠF₂, -(C(R⁶)₂)ₜC₆₋₁₀ arilo, -(C(R⁶)₂)ₜ-heteroarilo de 5 ó 6 miembros, -(C(R⁶)₂)ₜ-cicloalquilo de 5 ó 6 miembros, opcionalmente sustituido con arilo C₆₋₁₀, opcionalmente sustituido con heteroarilo de 5 ó 6 miembros u opcionalmente sustituido con cicloalquilo de 5 ó 6 miembros; cada Rᵉ es independientemente en cada caso alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, halógeno, haloalquilo C₁₋₆, -NHRᶻ, -OH o -CN; Rᶠ está ausente, es H o metilo; Rᵍ es H, alquilo C₁₋₆, OH, -S(O)₂(alquilo C₁₋₆) o alquilo S(O)₂N(alquilo C₁₋₆)₂; Rᵍ’ es H, alquilo C₁₋₆, cicloalquilo C₃₋₇, anillo de heterocicloalquilo de 4 a 7 miembros que comprende de 1 a 3 heteroátomos seleccionados de N, O y S, arilo C₆₋₁₀ o heteroarilo de 5 a 7 miembros que comprende de 1 a 3 heteroátomos seleccionados de N, O y S, donde el alquilo se sustituye opcionalmente con uno o más sustituyentes seleccionados independientemente de halógeno y -OH, y donde el cicloalquilo, heterocicloalquilo, arilo y heteroarilo se sustituyen opcionalmente con uno o más sustituyentes seleccionados independientemente de alquilo C₁₋₆ halógeno y -OH; Rʰ es H, alquilo C₁₋₄ o anillo de heterocicloalquilo de 3 a 7 miembros que comprende de 1 a 3 heteroátomos seleccionados de N, O y S, donde el alquilo se sustituye opcionalmente con uno o más sustituyentes seleccionados independientemente de NH₂, alquilamino C₁₋₄, dialquilamino C₁₋₄ y C(O)NH₂, y donde el heterocicloalquilo se sustituye opcionalmente con uno o más sustituyentes seleccionados cada uno independientemente de alquilo C₁₋₆ y haloalquilo C₁₋₆; Rⁱ es (i) alquilo-(CH₂)ₛOC(O)C₁₋₆, donde el alquilo se sustituye con uno o más NH₂; (ii) (CH₂CH₂O)ₙCH₂CH₂OH o (iii) alquilo C₁₋₆ se sustituye con uno o más sustituyentes seleccionados cada uno independientemente de OH y heterocicloalquilo de 4 a 7 miembros que comprende de 1 a 3 heteroátomos seleccionados de O, N o S; Rʲ está ausente, es H, alquilo C₁₋₆ o -CN; cada Rˣ es independientemente en cada caso H, alquilo C₁₋₆ o arilo C₆₋₁₀; cada Rʸ y Rᶻ es independientemente en cada caso H, alquilo C₁₋₆ o haloalquilo C₁₋₆; cada m, p, q, r y t es independientemente 0, 1 ó 2; n es 0, 1, 2 ó 3; s es 1 ó 2; o es 0, 1, 2, 3 ó 4; y ⁻ ⁻ ⁻ representa un enlace simple o un enlace doble; y siempre que cuando X es O; Rᶠ es H; W es C; Rʲ es -CN; L es -SCH₂-; R¹ es fenileno o piridina; entonces R⁷ no es -COOH; cuando X es O; Rᶠ es H; W es C; Rʲ es -CN; L es -SCH₂-; R¹ es fenileno o piridina; y R⁷ es tetrazol; entonces Rᶜ no es H; cuando X es O; Rᶠ es H; W es C; Rʲ es -CN; L es -S-C(R⁵)₂ o -SCH₂CH₂-; R¹ está ausente; entonces R⁷ no es COOH o tetrazol; cuando X es O, Rᶠ es H; W es N; Rʲ está ausente; Rᵈ es metilo, sustituido opcionalmente con arilo de 5 a 10 miembros, sustituido opcionalmente con heteroarilo de 5 ó 6 miembros o sustituido opcionalmente con cicloalquilo de 5 ó 6 miembros; L es -SCH₂- o -OCH₂-; y R¹ es fenileno; entonces R⁷ no es -COOH, -CH₂COOH, un resto de fórmula (3) ni un resto de fórmula (4); y cuando X es O, Rᶠ es H, W es N, Rʲ está ausente, L es -NHCH₂-, -CH₂NH- o -NH-C(O)-, y R¹ es fenileno, entonces Rᵈ no es fenilo.
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KR20210111248A (ko) 2021-09-10
CN118496217A (zh) 2024-08-16
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