AR061735A1 - Derivados de indazol, composiciones farmaceuticas y uso de los mismos - Google Patents

Derivados de indazol, composiciones farmaceuticas y uso de los mismos

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Publication number
AR061735A1
AR061735A1 ARP070102907A ARP070102907A AR061735A1 AR 061735 A1 AR061735 A1 AR 061735A1 AR P070102907 A ARP070102907 A AR P070102907A AR P070102907 A ARP070102907 A AR P070102907A AR 061735 A1 AR061735 A1 AR 061735A1
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AR
Argentina
Prior art keywords
nhet
nar
hal
atoms
cooa
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ARP070102907A
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English (en)
Inventor
Michael Wolf
Christian Sirrenberg
Eggenweiler Hans-Michael Dr
Buchstaller Hans-Peter Dr
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Merck Patent Gmbh
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Publication of AR061735A1 publication Critical patent/AR061735A1/es

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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
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    • A61P35/00Antineoplastic agents
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
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    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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Abstract

Derivados de indazol de la formula (1) así como sus derivados, sales, solvatos 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. Reivindicacion 1: Un compuesto de la formula 1 en donde R1 es H, OH, OCH3, OCF3, OCHF2, OBzl, OAc, p-metoxibenciloxi, SH, S(O)mCH3, SO2NH2, Hal, CF3 o CH3; R2 es Alk, (CH2)nHet, CN, NO2, NH2, OH, OA, O(CH2)nAr, O(CH2)nHet, SH, COA, CO(CH2)nAr, CO(CH2)nHet, S(O)mA, S(O)m(CH2)nAr, S(O)m(CH2)nHet, NHA, NHAr, NHHet, NAA', COOH, COOA, CONH2, CONHA, CONAA', CONH(CH2)nAr, CONA(CH2)nAr, CONH(CH2)nHet, CONA(CH2)nHet, SO2NH2, SO2NHA, SO2NAA', SO2NH(CH2)nAr, SO2NA(CH2)nAr, SO2NH(CH2)nHet, SO2NA(CH2)nHet, NHCOA, NACOA', NHCO(CH2)nAr, NACO(CH2)nAr, NHCO(CH2)nHet, NACO(CH2)nHet, NHSO2A, NASO2A', NHSO2(CH2)nAr, NASO2(CH2)nAr, NHSO2(CH2)nHet, NASO2(CH2)nHet, NHCOOA, NHCOOAr, NHCOOHet, NHCONHA, NHCONHAr o NHCONHHet, R3 es H, Hal, A, AOH, COOA, CONH2, CONHA, CONAA', CONHAr, CONH(CH2)Ar, CONAAr, CONA(CH2)Ar, CONHHet, CONH(CH2)Het, CONAHet, CONA(CH2)Het, (CH2)nCOOA, (CH2)nCONHA, (CH2)nCONAA', (CH2)nNHCONH2, (CH2)nNHCONHA, (CH2)nNHCONAA', (CH2)nNHCOA, (CH2)nNHCOAr, (CH2)nNHSO2A, (CH2)nNHSO2Ar, (CH2)nNASO2Ar, (CH2)nNHSO2CH2Ar, (CH2)nNASO2CH2Ar, (CH2)nAr, (CH2)nHet, NHAr o NHHet, Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di-, tri-, tetra- o pentasustituido con A, OA, OH, SH, S(O)mA, Hal, NO2, CN, COA, COOH, COOA, CONR4R5, SO2NR4R5, NR4R5, OCONR4R5, NR4COR5, NR4SO2R5, NR4CONR4R5, (CH2)nNHSO2A, O(CH2)pCN, SO2Het1, O(CH2)pNR4R5 y/o (CH2)mHet1, A, A' son en cada caso, de modo independiente entre sí, alquilo no ramificado o ramificado con 1-10 átomos de C, 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, Alk o alquilo cíclico C3-8, Alk es alquenilo o alquinilo C2-6, 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 A, OA, OH, SH, S(O)mA, Hal, NO2, CN, COA, COOA, CONR4R5, SO2NR4R5, NR4R5, OCONR4R5, NR4COR5, NR4SO2R5, NR4CONR4R5, =S, =NH, =NA y/u =O (oxígeno del carbonilo), Het1 es un heterociclo saturado monocíclico con 1 a 3 átomos de N y/u O, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con A, OA, OH y/u =O (oxígeno del carbonilo), R4, R5 son en cada caso, de modo independiente entre sí, H o alquilo C1-6, 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, Hal es F, Cl, Br o I, m es 0, 1 o 2, n es 0, 1, 2, 3 o 4, p es 1, 2, 3 o 4, así como sus derivados, sales, solvatos y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones.
ARP070102907A 2006-07-01 2007-06-29 Derivados de indazol, composiciones farmaceuticas y uso de los mismos AR061735A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102006030479A DE102006030479A1 (de) 2006-07-01 2006-07-01 Indazolderivate

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AR061735A1 true AR061735A1 (es) 2008-09-17

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US (1) US8722903B2 (es)
EP (1) EP2035391B1 (es)
JP (1) JP5303456B2 (es)
KR (1) KR20090025371A (es)
CN (1) CN101484425A (es)
AR (1) AR061735A1 (es)
AT (1) ATE534633T1 (es)
AU (1) AU2007271504B2 (es)
BR (1) BRPI0713977A2 (es)
CA (1) CA2656458C (es)
DE (1) DE102006030479A1 (es)
ES (1) ES2376043T3 (es)
IL (1) IL196202A (es)
MX (1) MX2008015442A (es)
WO (1) WO2008003396A1 (es)
ZA (1) ZA200900750B (es)

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EP2035391B1 (de) 2011-11-23
AU2007271504A1 (en) 2008-01-10
US20090197882A1 (en) 2009-08-06
JP2009541377A (ja) 2009-11-26
ES2376043T3 (es) 2012-03-08
CN101484425A (zh) 2009-07-15
BRPI0713977A2 (pt) 2012-11-27
IL196202A (en) 2014-03-31
ATE534633T1 (de) 2011-12-15
DE102006030479A1 (de) 2008-03-20
KR20090025371A (ko) 2009-03-10
AU2007271504B2 (en) 2012-05-24
ZA200900750B (en) 2009-12-30
US8722903B2 (en) 2014-05-13
JP5303456B2 (ja) 2013-10-02
EP2035391A1 (de) 2009-03-18
CA2656458A1 (en) 2008-01-10
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CA2656458C (en) 2014-10-07

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