AR092348A1 - DERIVADOS DE ARIL-SULTAMO COMO MODULADORES DE RORc - Google Patents

DERIVADOS DE ARIL-SULTAMO COMO MODULADORES DE RORc

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Publication number
AR092348A1
AR092348A1 ARP130102439A ARP130102439A AR092348A1 AR 092348 A1 AR092348 A1 AR 092348A1 AR P130102439 A ARP130102439 A AR P130102439A AR P130102439 A ARP130102439 A AR P130102439A AR 092348 A1 AR092348 A1 AR 092348A1
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Argentina
Prior art keywords
alkyl
aminocarbonyl
alkoxy
several times
substituted once
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ARP130102439A
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English (en)
Inventor
Rene Olivier
Gobbi Alberto
Gaines Simon
Ward Stuart
Bodil Van Niel Monique
Vesey David
Fauber Benjamin
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Hoffmann La Roche
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Publication of AR092348A1 publication Critical patent/AR092348A1/es

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    • C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
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  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
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Abstract

Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en la que: m es el número 0 ó 1; n es el número 0 ó 1; p es un número de 0 a 3; q es el número de 0, 1 ó 2; r es un número de 1 a 3; A es: un enlace; -(CRʲRᵏ)ₜ-; -C(O)-(CRʲRᵏ)ₜ-; -(CRʲRᵏ)ₜ-C(O)-; -NRᵃ-(CRʲRᵏ)ₜ-; -(CRʲRᵏ)ₜ-NRᵃ-; -C(O)NRᵃ-(CRʲRᵏ)ₜ-; -(CRʲRᵏ)ₜ-NRᵃC(O)-; -O-(CRʲRᵏ)ₜ-; -(CRʲRᵏ)ₜ-O-; -S-(CRʲRᵏ)ₜ-; -(CRʲRᵏ)ₜ-S-; -SO₂-(CRʲRᵏ)ₜ-; o -(CRʲRᵏ)ₜ-SO₂-; t es un número de 0 a 4; W es: -CRᵇRᶜ-; -O-; -S-; -SO₂-; o -NRᵈ-; uno de X¹, X², X³ y X⁴ es N y los demás son CRᵉ; o dos de X¹, X², X³ y X⁴ son N y los demás son CRᵉ; o tres de X¹, X², X³ y X⁴ son N y el restante es CRᵉ; o cada uno de X¹, X², X³ y X⁴ es CRᵉ; Y es: -O-; -S-; SO₂-; -CRᶠRᵍ-; o -NRʰ-; Z es: CH; o N; R¹, R², R³, R⁴, R⁵, R⁶, R⁷ y R⁸ con independencia entre sí son: hidrógeno; o alquilo C₁₋₆, que puede estar sin sustituir o sustituido una o varias veces por halógeno; o R³ y R⁴ junto con el átomo al que están unidos pueden formar un grupo etileno; o R³ y R⁴ junto con los átomos a los que están unidos pueden formar un anillo saturado o parcialmente saturado de tres, cuatro, cinco, seis o siete eslabones, que puede incluir opcionalmente uno o dos heteroátomos elegidos entre -O-, -NRᵃ- y -S-, y que puede estar opcionalmente sustituido una o varias veces por Rⁱ; o R⁵ y R⁶ junto con los átomos a los que están unidos pueden formar un anillo saturado o parcialmente saturado de tres, cuatro, cinco, seis o siete eslabones, que puede incluir opcionalmente uno o dos heteroátomos elegidos entre -O-, -NRᵃ- y -S-, y que puede estar opcionalmente sustituido una o varias veces por Rⁱ; o R⁷ y R⁸ junto con los átomos a los que están unidos pueden formar un anillo saturado o parcialmente saturado de tres, cuatro, cinco, seis o siete eslabones, que puede incluir opcionalmente uno o dos heteroátomos elegidos entre -O-, -NRᵃ- y -S-, y que puede estar opcionalmente sustituido una o varias veces por Rⁱ; o uno de R³ y R⁴ junto con uno de R⁵ y R⁶ y los átomos a los que están unidos pueden formar un anillo saturado o parcialmente saturado de tres, cuatro, cinco, seis o siete eslabones, que puede incluir opcionalmente uno o dos heteroátomos elegidos entre -O-, -NRᵃ- y -S-, y que puede estar opcionalmente sustituido una o varias veces por Rⁱ; o uno de R⁵ y R⁶ junto con uno de R⁷ y R⁸ y los átomos a los que están unidos pueden formar un anillo saturado o parcialmente saturado de tres, cuatro, cinco, seis o siete eslabones, que puede incluir opcionalmente uno o dos heteroátomos elegidos entre -O-, -NRᵃ- y -S-, y que puede estar opcionalmente sustituido una o varias veces por Rⁱ; cada R⁹ es con independencia: alquilo C₁₋₆; halógeno; alcoxi C₁₋₆; o ciano; dichos restos alquilo C₁₋₆ pueden estar sin sustituir o sustituidos una o varias veces por halógeno; R¹⁰ es: hidrógeno; carboxi; (alquil C₁₋₆)-carbonilo; (alcoxi C₁₋₆)-carbonilo; oxo; hidroxi; aminocarbonilo; N-(alquil C₁₋₆)-aminocarbonilo; N,N-di(alquil C₁₋₆)-aminocarbonilo; ciano; hidroxi-alquilo C₁₋₆; N-(alcoxi C₁₋₆)-(alquil C₁₋₆)-amino-carbonilo; N-hidroxi-(alquil C₁₋₆)-aminocarbonilo; N-(alcoxi C₁₋₆)-aminocarbonilo; halógeno; o alquilo C₁₋₆, que puede estar sin sustituir o sustituido una o varias veces por halógeno u oxo; R¹¹ es: hidrógeno; halógeno; carboxi; (alquil C₁₋₆)-carbonilo; (alcoxi C₁₋₆)-carbonilo; oxo; hidroxi; aminocarbonilo; N-(alquil C₁₋₆)-aminocarbonilo; N,N-di-(alquil C₁₋₆)-aminocarbonilo; (alquil C₁₋₆)-sulfonil-amino; (alquil C₁₋₆)-sulfonil-amino-alquilo C₁₋₆ ciano; hidroxi-alquilo C₁₋₆ N-(alcoxi C₁₋₆)-(alquil C₁₋₆)-aminocarbonilo; N-hidroxi-(alquil C₁₋₆)-aminocarbonilo; N-(alcoxi C₁₋₆)-aminocarbonilo; o alquilo C₁₋₆, que puede estar sin sustituir o sustituido una o varias veces por halógeno u oxo; R¹² es: hidrógeno; halógeno; carboxi; (alquil C₁₋₆)-carbonilo; (alcoxi C₁₋₆)-carbonilo; oxo; hidroxi; aminocarbonilo; N-(alquil C₁₋₆)-aminocarbonilo; N,N-di-(alquil C₁₋₆) -aminocarbonilo; ciano; hidroxi-alquilo C₁₋₆; N-(alcoxi C₁₋₆)-(alquil C₁₋₆)-aminocarbonilo; N-hidroxi-(alquil C₁₋₆)-aminocarbonilo; N-(alcoxi C₁₋₆)-aminocarbonilo; o alquilo C₁₋₆, que puede estar sin sustituir o sustituido una o varias veces por halógeno u oxo; o R¹⁰ y R¹¹ junto con los átomos a los que están unidos pueden formar un anillo saturado o parcialmente saturado de tres, cuatro, cinco, seis o siete eslabones, que puede incluir opcionalmente uno o dos heteroátomos elegidos entre -O-, -NRᵃ- y -S-, y que puede estar opcionalmente sustituido una o varias veces por Rⁱ; Rᵃ, Rᵇ, Rᶜ y Rᵈ con independencia entre sí son: hidrógeno; o alquilo C₁₋₆, que puede estar sin sustituir o sustituido una o varias veces por halógeno; o Rᵇ y Rᶜ junto con los átomos a los que están unidos pueden formar un anillo saturado o parcialmente saturado de tres, cuatro, cinco, seis o siete eslabones, que puede incluir opcionalmente uno o dos heteroátomos elegidos entre -O-, -NRᵃ- y -S-, y que puede estar opcionalmente sustituido una o varias veces por Rⁱ; o uno de Rᵇ y Rᶜ junto con uno de R⁷ y R⁸ y los átomos a los que están unidos pueden formar un anillo saturado o parcialmente saturado de tres, cuatro, cinco, seis o siete eslabones, que puede incluir opcionalmente uno o dos heteroátomos elegidos entre -O-, -NRᵃ- y -S-, y que puede estar opcionalmente sustituido una o varias veces por Rⁱ; o uno de Rᵇ y Rᶜ junto con uno de R⁵ y R⁶ y los átomos a los que están unidos pueden formar un anillo saturado o parcialmente saturado de tres, cuatro, cinco, seis o siete eslabones, que puede incluir opcionalmente uno o dos heteroátomos elegidos entre -O-, -NRᵃ- y -S-, y que puede estar opcionalmente sustituido una o varias veces por Rⁱ; cada Rᵉ es con independencia: hidrógeno; alquilo C₁₋₆; halógeno; alcoxi C₁₋₆; o ciano; dichos restos alquilo C₁₋₆ pueden estar sin sustituir o sustituidos una o varias veces por halógeno; Rᶠ es: hidrógeno; halógeno; o alquilo C₁₋₆, que puede estar sin sustituir o sustituido una o varias veces por halógeno; Rᵍ es: hidrógeno; alquilo C₁₋₆; cicloalquilo C₃₋₆; cicloalquenilo C₃₋₆; (cicloalquil C₃₋₆)-alquilo C₁₋₆; halógeno; (alquil C₁₋₆)-carbonilo; (cicloalquil C₃₋₆)-carbonilo; (cicloalquil C₃₋₆)-(alquil C₁₋₆)-carbonilo; ciano-(alquil C₁₋₆)-carbonilo; hidroxi-(alquil C₁₋₆)-carbonilo; alcoxi C₁₋₆-(alquil C₁₋₆)-carbonilo; carboxi; N-ciano-aminocarbonilo; N-ciano-N-(alquil C₁₋₆)-aminocarbonilo; N-(alquil C₁₋₆)-acetimidamidilo; N,N-di-(alquil C₁₋₆)-acetimidamidilo; N-ciano-N-(alquil C₁₋₆)-acetimidamidilo; N-hidroxi-acetimidamidilo; N-alcoxi C₁₋₆-acetimidamidilo; N-hidroxi-N-(alquil C₁₋₆)-acetimidamidilo; N-(alcoxi C₁₋₆)-N-(alquil C₁₋₆)-acetimidamidilo; 2-nitro-1-N-(alquil C₁₋₆)-amino-vinilo; formilo; (alquil C₁₋₆)-sulfonilo; (cicloalquil C₃₋₆)-sulfonilo; (cicloalquil C₃₋₆)-(alquil C₁₋₆)-sulfonilo; (alquil C₁₋₆)-sulfonil-alquilo C₁₋₆; aminocarbonilo; N-hidroxi-aminocarbonilo; N-(alcoxi C₁₋₆)-aminocarbonilo; N-(alquil C₁₋₆)-aminocarbonilo; aminocarbonil-alquilo C₁₋₆; N-(alquil C₁₋₆)-aminocarbonil-alquilo C₁₋₆; N,N-di-(alquil C₁₋₆)-aminocarbonil-alquilo C₁₋₆; (alcoxi C₁₋₆)-carbonilo; N-hidroxi-N-(alquil C₁₋₆)-aminocarbonilo; N-alcoxi C₁₋₆-N-(alquil C₁₋₆)-aminocarbonilo; N,N-di(alquil C₁₋₆)-aminocarbonilo; aminosulfonilo; N-(alquil C₁₋₆)-aminosulfonilo; N,N-di-(alquil C₁₋₆)-aminosulfonilo; ciano; alcoxi C₁₋₆ (alquil C₁₋₆)-sulfonil-amino; N-(alquil C₁₋₆)-sulfonil-aminocarbonilo; N-(alqui
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