AR050917A1 - Compuestos basados en 2-amido-tiazol que presentan actividad inhibidora de enzimas que utilizan atp, y composiciones y usos de los mismos - Google Patents

Compuestos basados en 2-amido-tiazol que presentan actividad inhibidora de enzimas que utilizan atp, y composiciones y usos de los mismos

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Publication number
AR050917A1
AR050917A1 ARP050103368A ARP050103368A AR050917A1 AR 050917 A1 AR050917 A1 AR 050917A1 AR P050103368 A ARP050103368 A AR P050103368A AR P050103368 A ARP050103368 A AR P050103368A AR 050917 A1 AR050917 A1 AR 050917A1
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AR
Argentina
Prior art keywords
substituted
heteroaryl
aryl
alkyl
pyridin
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ARP050103368A
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English (en)
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Amphora Discovery Corp
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Publication of AR050917A1 publication Critical patent/AR050917A1/es

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Abstract

Se describen compuestos basados en 2-amido-4-sustituido-aril-tiazol que muestran actividad inhibidora de enzimas que utilizan ATP, métodos de uso de compuestos que muestran actividad inhibidora de enzimas que utilizan ATP y composiciones que comprenden compuestos que muestran actividad inhibidora de enzimas que utilizan ATP. Reivindicacion 1: Al menos una entidad química seleccionada entre compuestos de formula (1), y sus sales farmacéuticamente aceptables, solvatos, quelatos, complejos no covalentes, profármacos y mezclas de los mismos, donde: R3 se selecciona entre hidroxi, alcoxi, amino, amino sustituido y Ar; Ar se selecciona entre cicloalquilo, cicloalquilo sustituido, arilo, arilo sustituido, heteroarilo y heteroarilo sustituido; L se selecciona entre alquileno C0-4, alquileno C1-4 sustituido, -(alquileno C0-4)-NH-C(=O)-; y -(alquileno C0-4)C(=O)-; W se selecciona entre hidrogeno, halo, alquilo, alquilo sustituido, cicloalquilo, cicloalquilo sustituido, heterocicloalquilo, heterocicloalquilo sustituido, arilo, arilo sustituido, heteroarilo y heteroarilo sustituido; Q selecciona entre alquilo, alquilo sustituido, cicloalquilo, cicloalquilo sustituido, cicloheteroalquilo, cicloheteroalquilo sustituido, arilo, arilo sustituido, heteroarilo y heteroarilo sustituido; y Z se selecciona entre alquilo y alquilo sustituido, con las condiciones de que: cuando Q es piridin-3-ilo opcionalmente sustituido, L es un enlace covalente, W es 3-metilfenilo, R3 es piridin-4-ilo opcionalmente sustituido, entonces Z no sea metilo; cuando Ar es piridin-4-ilo, W es hidrogeno y Q se selecciona entre bencilo, bencilo sustituido, fenetilo y fenetilo sustituido, entonces Z no se seleccione entre alquilo inferior y alquilo inferior sustituido; cuando Ar es 2-oxo-(3-hidroquinolilo), W es hidrogeno, Z es metilo, entonces Q no sea fenilo; cuando W se selecciona entre 2-(ciclohexilamino)piridin-4-ilo y 2- (ciclopentilamino)piridin-4-ilo, Ar es 3-metilfenilo, Z es metilo, entonces Q no sea piridin-3-ilo o 6-metilpiridin-3-ilo; Ar no sea piridona sustituida o benzoiloxipiridina; cuando R1 o R2 es hidrogeno, entonces Ar no sea 4-pivaloiloxifenilo; Q no sea un heteroarilo, heteroarilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido que comprende uno o más heteroátomos seleccionados entre S y N, condensados con un anillo arilo, arilo sustituido, heteroarilo, o heteroarilo sustituido; y cuando Z es alquilo inferior o 3-morfolinopropilo, entonces Ar no sea fenilo, 4-metoxifenilo, o 2,5-dimetoxifenilo.
ARP050103368A 2004-08-13 2005-08-11 Compuestos basados en 2-amido-tiazol que presentan actividad inhibidora de enzimas que utilizan atp, y composiciones y usos de los mismos AR050917A1 (es)

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WO2005089515A2 (en) * 2004-03-18 2005-09-29 The Brigham And Women's Hospital, Inc. Methods for the treatment of synucleinopathies
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