AR064952A1 - Derivados de 5-([1, 3, 4]oxadiazol-2-il)-1h-indazol y 5-([1, 3, 4]tiadiazol-2-il)-1h-indazol, un metodo para su preperacion, un kit de elementos que los comprende y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de la sgk. - Google Patents

Derivados de 5-([1, 3, 4]oxadiazol-2-il)-1h-indazol y 5-([1, 3, 4]tiadiazol-2-il)-1h-indazol, un metodo para su preperacion, un kit de elementos que los comprende y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de la sgk.

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AR064952A1
AR064952A1 ARP080100224A ARP080100224A AR064952A1 AR 064952 A1 AR064952 A1 AR 064952A1 AR P080100224 A ARP080100224 A AR P080100224A AR P080100224 A ARP080100224 A AR P080100224A AR 064952 A1 AR064952 A1 AR 064952A1
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het
cr7r8r9r10
so2n
formula
hal
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Markus Klein
Norbert Beier
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Merck Patent Gmbh
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Abstract

Derivados de indazol de la formula (1) en donde L es R1, R2 o -(X)mR3, X es CR7R8, CR7R8CR9R10, CR7R8C(OR9)R10, NR7, O, NR6CR7R8, CR7R8NR9, OCR7R8, OCR7R8CR9R10, CR7R8O, CR7R8CR9R10O, NR6CR7R8CR9R10, CR7R8SO2, NR7CONR8, NR7CONR8CR9R10, COCR7R8, CONR7, CONR7CR8R9, NR7CR8R9CONR10, NR7CO o NR7COCR8R9, Y es H, A, Ar o Het, R1 es CR9=CR9R10 o CR12=CR13R14; R2 es C:::CR12 o C:::C-Het, R3, R4, R5 son cada uno, de modo independiente entre sí, H, A, Hal, OH, OA, -[C(R7)2]nAr, -[C(R7)2]nHet, OAr, OHet, SH, SA, SAr, SHet, NH2, NHA, NAA', NHAr, N(Ar)2, NHHet, N(Het)2, NAAr, NAHet, SOA, SOAr, SOHet, SO2A, SO2Ar, SO2Het, NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NACOA, NHCONH2, NHCONHA, NHCONA2, NHSO2A, NASO2A, CHO, COA, COAr, COHet, SO3H, SO2NH2, SO2NHAr, SO2N(Ar)2, SO2NHHet o SO2N(Het)2, R6, R7, R8, R9, R10 son cada uno, de modo independiente entre sí, H o A, R11 es alquilo C1-6, en donde 1-5 átomos de H pueden estar reemplazados por F; R12, R13, R14 son cada uno, de modo independiente entre sí, H o Ar, A, A' son cada uno, de modo independiente entre sí, alquilo no sustituido o mono-, di- o trisustituido con R3, =S, =NR7 y/u =O (oxígeno del carbonilo) C1-10, en donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NR11 y/o por grupos -CH=CH y/o también 1-7 átomos de H pueden estar reemplazados por F y/o Cl, o alquilo cíclico C3-7, Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di-, tri- o tetrasustituido con A, Hal, OH, OA, Ar', OAr', Het, OHet, SH, SA, SAr', SHet, NH2, NHA, NAA', NHAr', N(Ar')2, NHHet, N(Het)2, NAAr', NAHet, SOA, SOAr', SOHet, SO2A, SO2Ar', SO2Het, NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NACOA, NHCONH2, NHCONHA, NHCONA2, NHSO2A, NASO2A, CHO, COA, COAr' , COHet, SO3H, SO2NH2, SO2NHAr', SO2N(Ar')2, SO2NHHet y/o SO2N(Het)2, Het es un heterociclo monocíclico o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar mono-, di- o trisustituido con A, Hal, OH, OA, Ar, OAr, Het', OHet', SH, SA, SAr', SHet', NH2, NHA, NAA', NHAr', N(Ar')2, NHHet', N(Het' )2, NAAr', NAHet', SOA, SOAr', SOHet', SO2A, SO2Ar', SO2Het', NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NACOA, NHCONH2, NHCONHA, NHCONA2, NHSO2A, NASO2A, CHO, COA, COAr', COHet', SO3H, SO2NH2, SO2NHAr', SO2N(Ar')2, SO2NHHet' o SO2N(Het')2, =S, =NR7 y/u =O (oxígeno del carbonilo), Ar' es fenilo no sustituido o mono-, di-, tri- o tetrasustituido con A, Hal, OH, OA, Ofenilo, SH, SA, NH2, NHA, NAA', NHfenilo, SOA, SOfenilo, SO2A, SO2fenilo, NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NACOA, NHCONH2, NHCONHA, NHCONA2, NHSO2A, NASO2A, CHO, COA, COfenilo, SO3H, SO2NH2, SO2NHfenilo y/o SO2N(fenilo)2, Het' es un heterociclo monocíclico o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar mono-, di- o trisustituido con A, Hal, OH, OA, NH2, NHA, NAA', SOA, SOAr', SO2A, SO2Ar', NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NACOA, NHCONH2, NHCONHA, NHCONA2, NHSO2A, NASO2A, CHO, COA, COAr', SO3H, SO2NH2, SO2NHAr', SO2N(Ar')2, =S, =NR7 y/u =O (oxígeno del carbonilo), Hal es F, Cl, Br o I, m es 0, 1, 2 o 3, n es 0, 1 o 2, así como sus derivados, sales, solvatos y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la SGK y pueden utilizarse para el tratamiento de enfermedades causadas por SGK y dolencias tales como diabetes, obesidad, síndrome metabolico (dislipidemia), hipertonía sistémica y pulmonar, enfermedades cardiocirculatorias y enfermedades renales, en general en cualquier tipo de fibrosis y procesos inflamatorios. Reivindicacion 19: Procedimiento para preparar compuestos de la formula 1 de acuerdo con las reivindicaciones 1-18, así como sus derivados, solvatos, sales y estereoisomeros de utilidad farmacéutica, caracterizado porque a) se liberan de uno de sus derivados funcionales por tratamiento con un agente solvolizante o hidrogenolizante, reemplazando un grupo protector amino convencional por tratamiento con un agente solvolizante o hidrogenolizante por hidrogeno o liberando un grupo amino protegido por un grupo protector convencional, o b) para preparar compuestos de la formula 1, en donde L es NH2, se hace reaccionar un compuesto de la formula 2 en donde R3, R4, R5, X e Y tienen los significados indicados en la reivindicacion 1, con hidrazina, o c) se cicla un compuesto de la formula 3 en donde L, R3, R4, R5, X e Y tienen los significados indicados en la reivindicacion 1, en presencia de una sal de Hg (II) o d) se cicla un compuesto de la formula 4 en donde L, R3, R4, R5, X e Y tienen los significados indicados en la reivindicacion 1, en presencia de POCl3, y/o una base o un ácido de la formula 1 se convierte en una de sus sales.
ARP080100224A 2007-01-18 2008-01-18 Derivados de 5-([1, 3, 4]oxadiazol-2-il)-1h-indazol y 5-([1, 3, 4]tiadiazol-2-il)-1h-indazol, un metodo para su preperacion, un kit de elementos que los comprende y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de la sgk. AR064952A1 (es)

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DE102007002717A DE102007002717A1 (de) 2007-01-18 2007-01-18 Heterocyclische Indazolderivate

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US (1) US20100063115A1 (es)
EP (1) EP2102197B1 (es)
JP (1) JP2010516638A (es)
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AT (1) ATE516286T1 (es)
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