AR061010A1 - Derivados de triazol i i - Google Patents

Derivados de triazol i i

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Publication number
AR061010A1
AR061010A1 ARP070102142A ARP070102142A AR061010A1 AR 061010 A1 AR061010 A1 AR 061010A1 AR P070102142 A ARP070102142 A AR P070102142A AR P070102142 A ARP070102142 A AR P070102142A AR 061010 A1 AR061010 A1 AR 061010A1
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Argentina
Prior art keywords
het
replaced
hal
atoms
groups
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ARP070102142A
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English (en)
Inventor
Eggenweiler Hans-Michael Dr
Wolf Michael Dr
Buchstaller Hans-Peter Dr
Christian Sirrenberg
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Merck Patent Gmbh
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Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR061010A1 publication Critical patent/AR061010A1/es

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    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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    • 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
    • A61K31/4196—1,2,4-Triazoles
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/12—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 chain containing hetero atoms as chain links
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
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Abstract

Los derivados de triazol de la formula (1) en donde R1 es OH, OCH3, OCF3, OCHF2, OBzl, OAc, p-metoxibenciloxi, SH, S(O)mCH3, SO2NH2, Hal, CF3 o CH3; R2 es CONA[(CH2)oAr], CONA[(CH2)oHet'], SO2NA[(CH2)oAr'] o SO2NA[(CH2)oHet']; R3 es H, Hal, CN, NO2, A, Alk, (CH2)nAr, (CH2)nHet', COOH, COOA, COOAr, COOHet', CONH2, CONHA, CONAA', CONHAr, CONAAr, CON(Ar)2, CONHHet', CON(Het')2, NH2, NHA, NHAr, NHHet', NAA', NHCOA, NACOA', NHCOAr, NHCOHet', NHCOOA, NHCOOAr, NHCOOHet', NHCONHA, NHCONHAr, NHCONHHet', OH, OA, OAr, OHet', SH, S(O)mA, S(O)mAr, S(O)mHet', SO2NH2, SO2NHA, SO2NAA', SO2NHAr, SO2NAAr, SO2NHHet', SO2NAHet', SO2NA-bencilo, SO2N(Ar)2 o SO2N(Het')2; R4, R5, R6 son en cada caso, de modo independiente entre sí, H, Hal, CN, NO2, A, Alk, (CH2)nAr, (CH2)nHet', COOH, COOA, COOAr, COOHet', CONH2, CONHA, CONAA', CONHAr, CONAAr, CON(Ar)2, CONHHet', CON(Het')2, NH2, NHA, NHAr, NHHet', NAA', NHCOA, NHCONH2, NACOA', NHCO(CH2)nAr, NHCOHet', NHCOOA, NHCOOAr, NHCOOHet', NHCONHA, NHCONHAr, NHCONHHet', OH, OA, O(CH2)oHet, O(CH2)oNH2, O(CH2)oCN, OAr, OHet', SH, S(O)mA, S(O)mAr, S(O)mHet', SO2NH2, SO2NHA, SO2NAA', SO2NHAr, SO2NAAr, SO2NHHet', SO2N(Ar)2 o SO2N(Het')2; R4 y R5 también son juntos OCH2O, OCH2CH2O, -CH=CH-CH=CH-, NH-CH=CH o CH=CH-NH; Y es OH o SH; A, A' son en cada caso, de modo independiente entre sí, alquilo no ramificado o ramificado C1-10, en donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NR8 y/o por grupos -CH=CH y/o también 1-5 átomos de H pueden estar reemplazados por F, Cl, Br y/o R7, Alk o alquilo cíclico C3-7; A y A' también son juntos una cadena de alquileno C2-6, en donde un grupo CH2 puede estar reemplazado por O, S, SO, SO2, NH, NR8, NCOR8 o NCOOR8; Alk es alquenilo C2-6; R7 es CN, COOR9, CONR9R10, NR9R10, NHCOR9, NHCOOR9 u OR9; R8 es cicloalquilo C3-7, cicloalquilalquileno C4-10, Alk o alquilo no ramificado o ramificado C1-6, en donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH y/o también 1-5 átomos de H pueden estar reemplazados por F y/o Cl; R9, R10 son en cada caso, de modo independiente entre sí, H o alquilo C1-5, en donde 1-3 grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NMe o Net y/o también 1- 5 átomos de H pueden estar reemplazados por F y/o Cl; R9 y R10 también son juntos una cadena de alquileno C2-6, en donde un grupo CH2 puede estar reemplazado por O, S, SO, SO2, NH, NR8, NCOR8 o NCOOR8; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, XR7, Y, CN, fenilo, Het'', OXHet''', OA, OXR7, S(O)mA, S(O)mXR7, NO2, NH2, NR9R10, NR8R9, CONR9R10, CONR8R9, SO2NR9R10, SO2NR8R9, NR9COR10, NR9CONR9R10 y/o NR9SO2R10; Ar' es fenilo, naftilo o bifenilo mono-, di- o trisustituido con Hal, A, XR7, XR4, Y, CN, Ar, Het, OA, OXR7, OXR4, S(O)mA, S(O)mXR7, S(O)mXR4, NO2, NH2, NR9R10, NR8R9, CONR9R10, CONR8R9, SO2NR9R10, SO2NR8R9, NR9COR10, NR9CONR9R10, y/o NR9SO2R10; Het es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, XR7, Y, CN, Ar, OA, OXR7, S(O)mA, S(O)mXR7, NO2, NH2, NR9R10, NR8R9, CONR9R10, CONR8R9, SO2NR9R10, SO2NR8R9, NR9COR10, NR9CONR9R10, NR9SO2R10, =S, =NR11, =NR11R7 y/u =O (oxígeno del carbonilo); Het' es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, XR7, XR4, Y, CN, Ar, Het, OA, OXR7, OXR4, S(O)mA, S(O)mXR7, S(O)mXR4, NO2, NH2, NR9R10, NR8R9, CONR9R10, CONR8R9, SO2NR9R10, SO2NR8R9, NR9COR10, NR9CONR9R10, NR9SO2R10, =S, =NR11, =NR11R7 y/u =O (oxígeno del carbonilo), y/o en donde un nitrogeno del anillo puede estar sustituido con -O-; Het'' es un heterociclo aromático monocíclico con 1 a 3 átomos de N, O y/o S; Het''' es un heterociclo saturado monocíclico con 1 a 3 átomos de N, O y/o S; X es alquileno no ramificado o ramificado C1-10, en donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NR8 y/o por grupos -CH=CH y/o también 1-5 átomos de H pueden estar reemplazados por F, Cl, Br y/o R7; R11 es H o A; Hal es F, Cl, Br o I; m es 0, 1 o 2; n es 0, 1, 2, 3 o 4; o es 1, 2 o 3; así como sus derivados, sales, solvatos, tautomeros y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la HSP90 y pueden ser utilizados para preparar un medicamento para el tratamiento de enfermedades en las que la inhibicion, la regulacion y/o la modulacion de la HSP90 desempena un papel importante. utiles para enfermedades tumorales, virales, inflamatorias, angiogenesis, fibrogenesis.
ARP070102142A 2006-05-18 2007-05-18 Derivados de triazol i i AR061010A1 (es)

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DE102006023337A DE102006023337A1 (de) 2006-05-18 2006-05-18 Triazolderivate II

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US (1) US8119795B2 (es)
EP (1) EP2023922B1 (es)
JP (1) JP5314593B2 (es)
KR (1) KR20090023614A (es)
CN (1) CN101443003A (es)
AR (1) AR061010A1 (es)
AU (1) AU2007252021B2 (es)
BR (1) BRPI0711463A2 (es)
CA (1) CA2652394C (es)
DE (1) DE102006023337A1 (es)
EA (1) EA015094B1 (es)
EC (1) ECSP088984A (es)
ES (1) ES2389451T3 (es)
IL (1) IL195278A (es)
MX (1) MX2008014480A (es)
PE (1) PE20080257A1 (es)
TW (1) TW200812983A (es)
WO (1) WO2007134678A2 (es)
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