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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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Publication number
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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English (en)
Inventor
Franco Francesca De
Nicola Giacche
Paride Liscio
Roberto Pellicciari
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Tes Pharma S R L
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Publication of AR117122A1 publication Critical patent/AR117122A1/es

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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
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • 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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