AR069636A1 - Triazolo triazinas y triazolopirazinas sustituidas, procedimiento para su preparacion, medicamentos que las contienen y uso de las mismas para el tratamiento y/o profilaxis de trastornos hematologicos,tales como neutropenias y leucopenias. - Google Patents
Triazolo triazinas y triazolopirazinas sustituidas, procedimiento para su preparacion, medicamentos que las contienen y uso de las mismas para el tratamiento y/o profilaxis de trastornos hematologicos,tales como neutropenias y leucopenias.Info
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- AR069636A1 AR069636A1 ARP080105333A ARP080105333A AR069636A1 AR 069636 A1 AR069636 A1 AR 069636A1 AR P080105333 A ARP080105333 A AR P080105333A AR P080105333 A ARP080105333 A AR P080105333A AR 069636 A1 AR069636 A1 AR 069636A1
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- alkyl
- alkoxy
- amino
- aminocarbonyl
- carbonyl
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Abstract
Reivindicacion 1: Compuesto de la formula (1) en la que u representa N, V representa CR12, w representa N, A representa CR15; o u representa N, v representa N, w representa CR16, A representa N, donde R12 representa hidrogeno, hidroxilo, amino, hidroxicarbonilo, aminocarbonilo, trifluorometilo, trifluorometoxi, ciano, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo, (alquil C1-4)carbonilamino, alquil C1-4-sulfonilamino, heterociclilcarbonilo de 5 o 6 miembros, -CH2R13 o -CH2CH2R14, donde heterociclilcarbonilo está sustituido con 1 a 3 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, oxo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)-carbonilo y (alquil C1-4)aminocarbonilo, y donde alcoxi, alquilamino, alquilcarbonilo, alcoxicarbonilo, alquilaminocarbonilo, alquilcarbonilamino y alquilsulfonilamino pueden estar sustituidos con un sustituyente, seleccionándose el sustituyente del grupo constituido por hidroxilo, amino, hidroxicarbonilo, aminocarbonilo, alcoxi C1-4, (alquil C1-4)amino, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo, alquil C1-4-carbonilamino, heterociclilo de 5 o 6 miembros y fenilo, donde fenilo puede estar sustituido con 1 a 3 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, ciano, trifluorometilo, trifluorometoxi, aminocarbonilo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo y (alquil C1-4)carbonilamino, y donde heterociclilo puede estar sustituido con 1 a 3 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, oxo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)-carbonilo y (alquil C1-4)aminocarbonilo, y donde R13 representa hidroxilo, amino, ciano, hidroxicarbonilo, aminocarbonilo, alcoxi C1-4, (alquil C1-4)amino, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo, (alquil C1-4)carbonilamino o heterociclilo de 5 o 6 miembros, donde alcoxi, alquilamino, alcoxicarbonilo, alquilaminocarbonilo y alquilcarbonilamino pueden estar sustituidos con un sustituyente, seleccionándose el sustituyente del grupo constituido por hidroxilo, amino, hidroxicarbonilo, aminocarbonilo, alcoxi C1-4, (alquil C1-4)amino, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo y (alquil C1-4)carbonilamino, y donde heterociclilo puede estar sustituido con 1 a 3 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, oxo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)-carbonilo y (alquil C1-4)aminocarbonilo, y donde R14 representa hidroxilo, amino, ciano, hidroxicarbonilo, aminocarbonilo, alcoxi C1-4, (alquil C1-4)amino, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo, (alquil C1-4)carbonilamino o heterociclilo de 5 o 6 miembros, donde alcoxi, alquilamino, alcoxicarbonilo, alquilaminocarbonilo y alquilcarbonilamino pueden estar sustituidos con un sustituyente, seleccionándose el sustituyente del grupo constituido por hidroxilo, amino, hidroxicarbonilo, aminocarbonilo, alcoxi C1-4, (alquil C1-4)amino, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo y (alquil C1-4)carbonilamino, y donde heterociclilo puede estar sustituido con 1 a 2 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, oxo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)-carbonilo y (alquil C1-4)aminocarbonilo, R15 representa hidrogeno, halogeno, ciano, trifluorometilo, alquilo C1-3, metoxi, metiltio o ciclopropilo, R16 representa hidrogeno o metilo; representa un resto del grupo de formulas (2) en las que * es el punto de union al heterociclo, n representa el numero 0 o 1; X representa NR10, S u O, donde R10 representa hidrogeno, alquilo C1-3 o ciclopropilo, Y representa NR11 o S, donde R11 representa hidrogeno, alquilo C1-3 o ciclopropilo, R3 representa pirid-2-ilo, pirimid-2-ilo, 2-aminopirimid-4-ilo, 2-(mono-(alquil C1-4)-amino)pirimid-4-ilo, 2-(mono-cicloalquilamino C3-4)pirimid-4-ilo, piridazin-3(2H)-on-6-ilo; 1,3-oxazol-2-ilo, 1,3-oxazol-4-ilo, 1,2,4-oxadiazol-3-ilo, 1,2,3-oxadiazol-4-ilo, 1,3-tiazol-2-ilo, 1,3-tiazol-4-ilo, 1H-1,2,4-triazol-5-ilo, 2,4-dihidro-3H-1,2,4-triazol-3-on-5-ilo o 1,2-pirazol-5-ilo, donde pirid-2-ilo, pirimid-2-ilo, 1,3-oxazol-2-ilo, 1,3-oxazol-4-ilo, 1,3-tiazol-2-ilo y 1,3-tiazol-4-ilo están sustituidos con 1 o 2 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, ciano, nitro, amino, trifluorometilo, trifluorometoxi, aminocarbonilo, trifluorometilcarbonilo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, cicloalquilamino C3-4, (alquil C1-4)carbonilo, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo y ciclo alquilcarbonilo C3-6, donde alquilo, alcoxi, alquilamino, alquilcarbonilo, alcoxicarbonilo, alquilaminocarbonilo y cicloalquilcarbonilo pueden estar sustituidos con un sustituyente, seleccionándose el sustituyente del grupo constituido por halogeno, ciano, hidroxilo, amino, trifluorometilo y cicloalquilo C3-5, y donde 2-aminopirimid-4-ilo, 2-(mono-(alquil C1-4)-amino)pirimid-4-ilo, 2-(mono-C3-4-cicloalquilamino)pirinlid-4-ilo, piridazin-3(2H)-on-6-ilo, 1,2,4-oxadiazol-3-ilo, 1,2,3-oxadiazol-4-ilo, 1H-1,2,4-triazol-5-ilo, 2,4-dihidro-3H-1,2,4-triazol-3-on-5-ilo y 1,2-pirazol-5-ilo pueden estar sustituidos con un sustituyente, seleccionándose el sustituyente del grupo constituido por halogeno, ciano, nitro, amino, trifluorometilo, trifluorometoxi, aminocarbonilo, trifluorometilcarbonilo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, cicloalquilamino C3-4, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo y cicloalquilcarbonilo C3-6, R4 representa hidrogeno, alquilo C1-3 o ciclopropilo, R5 representa hidrogeno o alquilo C1-3, R6 representa hidrogeno, alquilo C1-3 o ciclopropilo, R7 representa hidrogeno o alquilo C1-3, R8 representa hidrogeno, alquilo C1-3 o ciclopropilo, R9 representa hidrogeno o alquilo C1-3, R2 representa arilo C5-10 o heteroarilo de 5 a 10 miembros, donde arilo y heteroarilo pueden estar sustituidos con 1 a 3 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por hidroxilo, hidroximetilo, amino, halogeno, ciano, trifluorometilo, trifluorometoxi, aminocarbonilo, alquilo C1-4, alcoxi C1-4, (alcoxi C1-4)metilo, (alquil C1-4)amino, (alquil C1-4)-aminometilo, (alquil C1-4)carbonilo, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo, (alquil C1-4)carbonilamino, (alquil C1-4)sulfonilo, (alquil C1-4)sulfonilamino, (alquil C1-4)-aminosulfonilo, fenilo, benciloxi, heterociclilo de 5 o 6 miembros, heterociclilcarbonilo de 5 o 6 miembros, heterociclilmetilo de 5 o 6 miembros y heteroarilo de 5 o 6 miembros, donde fenilo, benciloxi, heterociclilo, heterociclilcarbonilo, heterociclilmetilo y heteroarilo pueden estar sustituidos con 1 a 3 sustituyentes, seleccionándose los sustituyentes independientemente uno de otro del grupo constituido por halogeno, ciano, trifluorometilo, trifluorometoxi, aminocarbonilo, alquilo C1-4, alcoxi C1-4, (alquil C1-4)amino, (alquil C1-4)carbonilo, (alcoxi C1-4)carbonilo, (alquil C1-4)aminocarbonilo y (alquil C1-4)carbonilamino, o dos de los sustituyentes en arilo junto con los átomos de carbono a los que están unidos forman un 1,3-dioxolano o 1,4-dioxano; o una de sus sales, sus solvatos o los solvatos de sus sales.
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DE102007060172A DE102007060172A1 (de) | 2007-12-13 | 2007-12-13 | Triazolotriazine und Triazolopyrazine und ihre Verwendung |
DE200810035209 DE102008035209A1 (de) | 2008-07-29 | 2008-07-29 | Triazolotriazine und Triazolopyrazine und ihre Verwendung |
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WO2015157955A1 (en) | 2014-04-17 | 2015-10-22 | Abbvie Inc. | Heterocyclic btk inhibit ors |
CR20200441A (es) | 2018-02-27 | 2021-03-15 | Incyte Corp | Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b |
MX2020012376A (es) | 2018-05-18 | 2021-03-09 | Incyte Corp | Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b. |
TW202402759A (zh) | 2018-07-05 | 2024-01-16 | 美商英塞特公司 | 作為a2a/a2b抑制劑之稠合吡嗪衍生物 |
TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
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PA8806501A1 (es) | 2009-08-26 |
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JP2011506364A (ja) | 2011-03-03 |
CA2708783A1 (en) | 2009-06-18 |
US20090258877A1 (en) | 2009-10-15 |
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WO2009074259A1 (de) | 2009-06-18 |
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