AR121745A1 - MODULADORES DE a-1 ANTITRIPSINA - Google Patents

MODULADORES DE a-1 ANTITRIPSINA

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Publication number
AR121745A1
AR121745A1 ARP210100866A ARP210100866A AR121745A1 AR 121745 A1 AR121745 A1 AR 121745A1 AR P210100866 A ARP210100866 A AR P210100866A AR P210100866 A ARP210100866 A AR P210100866A AR 121745 A1 AR121745 A1 AR 121745A1
Authority
AR
Argentina
Prior art keywords
alkyl
cyano
cycloalkyl
halogen
alkoxy
Prior art date
Application number
ARP210100866A
Other languages
English (en)
Inventor
Simon Giroux
Michael Philip Clark
Michael Aaron Brodney
Philippe Marcel Nuhant
Emily Elizabeth Allen
Jr Robert Francis Fimognari
Mariam Zaky
Michael John Boyd
David D Deininger
Hu Zhang
Hongbo Deng
Philip Noel Collier
Brad Maxwell
Nathan D Waal
Steven M Ronkin
Jian Wang
Qing Tang
Gabrielle Simone Fleming
Peter Jones
Diane Marie Boucher
Lev T D Fanning
Amy B Hall
Dennis James Hurley
Jr Mac Arthur Johnson
John Patrick Maxwell
Rebecca Jane Swett
Timothy Lewis Tapley
Stephen A Thomson
Veronique Damagnez
Kevin Michael Cottrell
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of AR121745A1 publication Critical patent/AR121745A1/es

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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
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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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P31/02—Local antiseptics
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    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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Abstract

Compuestos novedosos, composiciones novedosas, y métodos novedosos para usar y preparar dichos compuestos y composiciones, que pueden ser útiles para tratar deficiencia de a-1 antitripsina (AATD). Reivindicación 1: Un compuesto representado por la siguiente fórmula estructural (1), un tautómero del mismo, un derivado deuterado de ese compuesto o tautómero, o una sal farmacéuticamente aceptable de los anteriores, en donde: ⁻ ⁻ ⁻ ⁻ ⁻, por cada una de las dos apariciones, es un enlace simple o un enlace doble, siempre que uno sea un enlace simple y el otro sea un enlace doble; V¹ y V² son, cada uno independientemente, N o -CR²; W¹ y W² son, cada uno independientemente, N o C, siempre que uno de W¹ y W² sea N y el otro sea C; U es hidrógeno, -OH, -CH₃, -NH₂, o halógeno; X está ausente o es un enlace, -(CRᵃRᵇ)ₚ-, o -SO₂-; Y está ausente o es un enlace, -(CRᶜRᵈ)q-, -C(=O)-, o -SO₂-; Rᵃ y Rᵇ, por cada aparición, son, cada uno independientemente, hidrógeno, halógeno, -OH, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₁₋₆ haloalquilo, C₁₋₆ alcoxi, o C₁₋₆ haloalcoxi; Rᶜ y Rᵈ, por cada aparición, son, cada uno independientemente, hidrógeno, halógeno, -OH, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₁₋₆ haloalquilo, C₁₋₆ alcoxi, o C₁₋₆ haloalcoxi; el Anillo A es C₃₋₁₂ carbociclilo, heterociclilo de 3 a 12 miembros, C₆ o C₁₀ arilo, o heteroarilo de 5 a 10 miembros; siempre que, cuando W¹ sea N y W² sea C, el Anillo A no sea 1,5,6,7-tetrahidro-4H-indol-4-onilo o un tautómero del mismo; el Anillo B es C₄₋₁₂ cicloalquilo, C₆ o C₁₀ arilo, heteroarilo de 5 a 10 miembros, o bencilo; Z es un resto de fórmula (2) ó (3); en donde: el Anillo C es C₃-C₁₂ cicloalquilo, heterociclilo de 3 a 12 miembros, C₆ o C₁₀ arilo, o heteroarilo de 5 a 10 miembros; siempre que, cuando el Anillo C sea fenilo, el fenilo esté sustituido con R⁴; siempre que, cuando el Anillo C sea fenilo, Y no pueda ser -SO₂-; y siempre que, cuando el Anillo B sea bencilo, el Anillo C no pueda ser piridinilo ni indolilo; RE, RF, y RG son, cada uno independientemente, hidrógeno, halógeno, ciano, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₁₋₆ alcoxi, C₁₋₆ haloalquilo, C₁₋₆ haloalcoxi, -C(=O)Rˢ, -C(=O)ORˢ, -C(=O)NRᵖRq, -CRᵖ(=N)ORˢ, -NRᵖC(=O)Rˢ, -NRᵖC(=O)ORˢ, -NRᵖC(=O)NRqRʳ, -ORˢ, -OC(=O)Rˢ, o -OC(=O)NRᵖRq; en donde: el C₁₋₆ alquilo o el C₂₋₆ alquenilo de uno cualquiera de RE, RF, y RG está opcionalmente sustituido con 1 a 3 grupos seleccionados entre ciano, -C(=O)Rˢ, -C(=O)ORˢ, -C(=O)NRᵖRq, -NRᵖC(=O)Rˢ, -NRᵖC(=O)ORˢ, -NRᵖC(=O)NRqRʳ, -NRᵖS(=O)ʳRˢ, -ORˢ, -OC(=O)Rˢ, -OC(=O)ORˢ, -OC(=O)NRᵖRq, -S(=O)ʳRˢ, y -S(=O)ʳNRᵖRq; en donde: Rᵖ, Rq, y Rʳ, por cada aparición, son, cada uno independientemente, hidrógeno, C₁₋₄ alquilo, C₃₋₆ cicloalquilo, o heterociclilo de 3 a 6 miembros; en donde: el C₁₋₄ alquilo de uno cualquiera de Rᵖ, Rq, y Rʳ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre halógeno, ciano, -OH, C₁₋₃ alcoxi, -C(=O)NH(C₁₋₂ alquilo), y -C(=O)N(C₁₋₂ alquilo)₂; y el C₃₋₆ cicloalquilo o el heterociclilo de 3 a 6 miembros de uno cualquiera de Rᵖ, Rq, y Rʳ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre halógeno, ciano, -OH, C₁₋₃ alquilo, C₁₋₃ alcoxi, C₁₋₃ haloalquilo, C₁₋₃ haloalcoxi, -C(=O)O(C₁₋₂ alquilo), -C(=O)NH(C₁₋₂ alquilo), y -C(=O)N(C₁₋₂ alquilo)₂; Rˢ, por cada aparición, es independientemente hidrógeno, C₁₋₄ alquilo, C₃₋₆ cicloalquilo, fenilo, o heteroarilo de 5 ó 6 miembros; en donde: el C₁₋₄ alquilo de Rˢ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre halógeno, ciano, -OH, -NH₂, -NH(C₁₋₂ alquilo), -N(C₁₋₂ alquilo)₂, C₁₋₃ alcoxi, -C(=O)OH, -C(=O)O(C₁₋₂ alquilo), -C(=O)NH₂, -C(=O)NH(C₁₋₂ alquilo), y -C(=O)N(C₁₋₂ alquilo)₂; y el C₃₋₆ cicloalquilo, el fenilo, o el heteroarilo de 5 ó 6 miembros de Rˢ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre halógeno, ciano, -OH, -OCH₃, -NH₂, -NH(C₁₋₂ alquilo), -N(C₁₋₂ alquilo)₂, C₁₋₃ alquilo, C₁₋₃ alcoxi, C₁₋₃ haloalquilo, C₁₋₃ haloalcoxi, -C(=O)OH, -C(=O)O(C₁₋₂ alquilo), -C(=O)NH₂, -C(=O)NH(C₁₋₂ alquilo), y -C(=O)N(C₁₋₂ alquilo)₂; R¹ es halógeno, ciano, C₁₋₃ alquilo, C₁₋₃ haloalquilo, C₁₋₃ alcoxi, C₁₋₃ haloalcoxi, o -O-(C₃₋₆ cicloalquilo); R², por cada aparición, es independientemente hidrógeno, halógeno, ciano, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₁₋₆ alcoxi, C₁₋₆ haloalquilo, C₁₋₆ haloalcoxi, C₃₋₆ cicloalquilo, -NRʰRⁱ, fenilo, o heteroarilo de 5 ó 6 miembros; en donde: el C₁₋₆ alquilo, el C₂₋₆ alquenilo o el C₃₋₆ cicloalquilo de R² está opcionalmente sustituido con 1 a 3 grupos seleccionados entre ciano, -C(=O)Rᵏ, -C(=O)ORᵏ, -C(=O)NRʰRⁱ, -NRʰRⁱ, -NRʰC(=O)Rᵏ, -NRʰC(=O)ORᵏ, -NRʰC(=O)NRⁱRʲ, -NRʰS(=O)ₛRᵏ, -ORᵏ, -OC(=O)Rᵏ, -OC(=O)ORᵏ, -OC(=O)NRʰRⁱ, -S(=O)ₛRᵏ, y S(=O)ₛNRʰRⁱ; en donde: Rʰ, Rⁱ, y Rʲ, por cada aparición, son, cada uno independientemente, hidrógeno, C₁₋₄ alquilo, o C₃₋₆ cicloalquilo; en donde: el C₁₋₄ alquilo de uno cualquiera de Rʰ, Rⁱ, y Rʲ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre halógeno, ciano, -OH, -NH₂, -NH(C₁₋₂ alquilo), -N(C₁₋₂ alquilo)₂, C₁₋₃ alquilo, C₁₋₃ alcoxi, C₁₋₃ haloalquilo, C₁₋₃ haloalcoxi, -C(=O)OH, -C(=O)O(C₁₋₂ alquilo), -C(=O)NH₂, -C(=O)NH(C₁₋₂ alquilo), y -C(=O)N(C₁₋₂ alquilo)₂; y el C₃₋₆ cicloalquilo de uno cualquiera de Rʰ, Rⁱ, y Rʲ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre halógeno, ciano, -OH, -NH₂, -NH(C₁₋₂ alquilo), -N(C₁₋₂ alquilo)₂, C₁₋₃ alquilo, C₁₋₃ alcoxi, C₁₋₃ haloalquilo, C₁₋₃ haloalcoxi, -C(=O)OH, -C(=O)O(C₁₋₂ alquilo), -C(=O)NH₂, -C(=O)NH(C₁₋₂ alquilo), y -C(=O)N(C₁₋₂ alquilo)₂; Rᵏ, por cada aparición, es independientemente hidrógeno, C₁₋₄ alquilo, C₃₋₆ cicloalquilo, fenilo, o heteroarilo de 5 ó 6 miembros; en donde: -ORᵏ no puede ser -OH; el C₁₋₄ alquilo de Rᵏ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre halógeno, ciano, -OH, -NH₂, -NH(C₁₋₂ alquilo), -N(C₁₋₂ alquilo)₂, C₁₋₃ alquilo, C₁₋₃ alcoxi, C₁₋₃ haloalquilo, C₁₋₃ haloalcoxi, -C(=O)OH, -C(=O)O(C₁₋₂ alquilo), -C(=O)NH₂, -C(=O)NH(C₁₋₂ alquilo), y -C(=O)N(C₁₋₂ alquilo)₂; y el C₃₋₆ cicloalquilo de Rᵏ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre halógeno, ciano, -OH, -NH₂, -NH(C₁₋₂ alquilo), -N(C₁₋₂ alquilo)₂, C₁₋₃ alquilo, C₁₋₃ alcoxi, C₁₋₃ haloalquilo, C₁₋₃ haloalcoxi, -C(=O)OH, -C(=O)O(C₁₋₂ alquilo), -C(=O)NH₂, -C(=O)NH(C₁₋₂ alquilo), y -C(=O)N(C₁₋₂ alquilo)₂; R³ y R⁴, por cada aparición son, cada uno independientemente, ciano, =O, C₁₋₆ alquilo, C₂₋₆ alquenilo, C₁₋₆ alcoxi, C₁₋₆ haloalquilo, C₁₋₆ haloalcoxi, C₃₋₆ cicloalquilo, -C(=O)Rʸ, -C(=O)ORʸ, -C(=O)NRᵛRʷ, -C(=O)NRᵛORʸ, -C(=O)NRᵛS(=O)ₜRʸ, -NRᵛRʷ, -NRᵛC(=O)Rʸ, -NRᵛC(=O)ORʸ, -NRᵛC(=O)NRʷRˣ, -NRᵛS(=O)ₜRʸ, -ORʸ, -OC(=O)Rʸ, -OC(=O)ORʸ, -OC(=O)NRᵛRʷ, -S(=O)ₜRʸ, -S(=O)ₜNRᵛRʷ, -S(=O)ₜNRᵛC(=O)Rʸ, -P(=O)RᶻRᶻ, fenilo, o un heteroarilo de 5 ó 6 miembros; en donde: el C₁₋₆ alquilo, el C₂₋₆ alquenilo, o el C₃₋₆ cicloalquilo de uno cualquiera de R³ y R⁴ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre ciano, -C(=O)Rʸ, -C(=O)ORʸ, -C(=O)NRᵛRʷ, -NRᵛRʷ, -NRᵛC(=O)Rʸ, -NRᵛC(=O)ORʸ, -NRᵛC(=O)NRʷRˣ, -NRᵛS(=O)ʳRʸ, -ORʸ, -C(=O)Rʸ, -OC(=O)ORʸ, -OC(=O)NRᵛRʷ, -S(=O)ₜRʸ, y -S(=O)ₜNRᵛRʷ; en donde: Rᵛ, Rʷ, y Rˣ, por cada aparición son, cada uno independientemente, hidrógeno, C₁₋₄ alquilo, C₃₋₆ cicloalquilo, heterociclilo de 5 ó 6 miembros, o heteroarilo de 5 ó 6 miembros; en donde: el C₁₋₄ alquilo de uno cualquiera de Rᵛ, Rʷ, y Rˣ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre halógeno, ciano, -OH, -NH₂, -NH(C₁₋₂ alquilo), -N(C₁₋₂ alquilo)₂, C₁₋₃ alquilo, C₁₋₃ alcoxi, C₁₋₃ haloalquilo, C₁₋₃ haloalcoxi, -C(=O)OH, -C(=O)O(C₁₋₂ alquilo), -C(=O)NH₂, -C(=O)NH(C₁₋₂ alquilo), y -C(=O)N(C₁₋₂ alquilo)₂; y el C₃₋₆ cicloalquilo, el heterociclilo de 5 ó 6 miembros, o el heteroarilo de 5 ó 6 miembros de uno cualquiera de Rᵛ, Rʷ, y Rˣ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre halógeno, ciano, -OH, -NH₂, -NH(C₁₋₂ alquilo), -N(C₁₋₂ alquilo)₂, C₁₋₃ alquilo, C₁₋₃ alcoxi, C₁₋₃ haloalquilo, C₁₋₃ haloalcoxi, -C(=O)OH, -C(=O)O(C₁₋₂ alquilo), -C(=O)NH₂, -C(=O)NH(C₁₋₂ alquilo), y -C(=O)N(C₁₋₂ alquilo)₂; Rʸ, por cada aparición, es independientemente hidrógeno, C₁₋₄ alquilo, C₃₋₆ cicloalquilo, fenilo, heterociclilo de 5 ó 6 miembros, o un heteroarilo de 5 ó 6 miembros; en donde el C₁₋₄ alquilo de Rʸ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre halógeno, ciano, -OH, -NH₂, -NH(C₁₋₂ alquilo), -N(C₁₋₂ alquilo)₂, C₁₋₃ alquilo, C₁₋₃ alcoxi, C₁₋₃ haloalquilo, C₁₋₃ haloalcoxi, -C(=O)OH, -C(=O)O(C₁₋₂ alquilo), -C(=O)NH₂, -C(=O)NH(C₁₋₂ alquilo), y -C(=O)N(C₁₋₂ alquilo)₂; y el C₃₋₆ cicloalquilo, el fenilo, el heterociclilo de 5 ó 6 miembros, o el heteroarilo de 5 ó 6 miembros de Rʸ está opcionalmente sustituido con 1 a 3 grupos seleccionados entre halógeno, ciano, -OH, -NH₂, NH(C₁₋₂ alquilo), -N(C₁₋₂ alquilo)₂, C₁₋₃ alquilo, C₁₋₃ alcoxi, C₁₋₃ haloalquilo, C₁₋₃ haloalcoxi, -C(=O)OH, -C(=O)O(C₁₋₂ alquilo), -C(=O)NH₂, -C(=O)NH(C₁₋₂ alquilo), y -C(=O)N(C₁₋₂ alquilo)₂; Rᶻ, por cada aparición, es independientemente C₁₋₂ alquilo, -OH, o -O(C₁₋₂ alquilo); k es un número entero seleccionado entre 1, 2 y 3; m y n son, cada uno independientemente, un número entero seleccionado entre 0, 1, 2, y 3; p, r, s, y t son, cada uno independientemente, un número entero seleccionado entre 1 y 2; y q es un número entero seleccionado entre 1, 2, y 3.
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