AR051135A1 - Fenilpirazoles - Google Patents

Fenilpirazoles

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Publication number
AR051135A1
AR051135A1 ARP050104228A ARP050104228A AR051135A1 AR 051135 A1 AR051135 A1 AR 051135A1 AR P050104228 A ARP050104228 A AR P050104228A AR P050104228 A ARP050104228 A AR P050104228A AR 051135 A1 AR051135 A1 AR 051135A1
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AR
Argentina
Prior art keywords
atoms
replaced
het
hal
con
Prior art date
Application number
ARP050104228A
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English (en)
Inventor
Hans-Michael Eggenweiler
Michael Wolf
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Merck Patent Gmbh
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Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR051135A1 publication Critical patent/AR051135A1/es

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    • 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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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • 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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Abstract

Los derivados de fenil-pirazoles de la formula (1) en la que R1 es OH, OCH3, OCF3, OCHF2, OBzl, OAc, p-metoxibenciloxi, SH, S(O)mCH3, SO2NH2, Hal, CF3 o CH3; R2, R3 son cada uno, 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, 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', SO2NH(CH2)nAr, SO2NAAr, SO2NH(CH2)nHet, SO2N(Ar)2 o SO2N(Het)2; R4, R5, R6 son cada uno, 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', NHCOAr, NHCOHet, NHCOOA, NHCOOAr, NHCOOHet, NHCONHA, NHCONHAr, NHCONH-Het, OH, OA, 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, NH-CH=CH o CH=CH-NH; X es O, S, SO o SO2; Y es A, Ar o Het; A, A' son cada uno, de modo independiente entre sí, alquilo no ramificado o ramificado con 1-10 átomos de C, 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, y/o R7, Alk o alquilo cíclico con 3-7 átomos de C; A y A' también son juntos una cadena alquileno con 2, 3, 4, 5 o 6 átomos de C, en donde un grupo CH2 puede estar reemplazado por O, S, SO, SO2, NH, NR8, NCOR8 o NCOOR8; Alk es alquenilo con 2-6 átomos de C; R7 es COOR9, CONR9R10, NR9R10, NHCOR9, NHCOOR9 u OR9; R8 es cicloalquilo con 3-7 átomos de C, cicloalquilalquileno con 4-10 átomos de C, Alk o alquilo no ramificado o ramificado con 1-6 átomos de C, 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 cada uno, de modo independiente entre sí, H o alquilo con 1-5 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; R9 y R10 también son juntos una cadena alquileno con 2, 3, 4, 5, o 6 átomos de C, 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, OR11, N(R11)2, NO2, CN, fenilo, CON(R11)2, NR11COA, NR11CON(R11)2, NR11SO2A, COR11, SO2N(R11)2, S(O)mA, [C(R11)2]n-COOR y/u -O[C(R11)2]o-COOR11; Het es un heterociclo mono- 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 Hal, A, (CH2)nOR11, (CH2)nN(R11)2, NO2, CN, COOR11, CON(R11)2, NR11COA, NR11SO2A, COR11, SO2NR11, S(O)mA, =S, =NR11 y/u =O (el oxígeno del carbonilo); 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, excluyendo los compuestos de la formula (1), en la que R1 es OH u OCH3; R2 es H o etilo; R3 es H o metilo; R4 es H, NO2, F, Cl, Br, fenilo, i-propilo, n-propilo, COOH, COOCH3 o etoxi; R5 es H o Cl; R6 es H; X es O; Y es H, Ch3 o CF3, 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.
ARP050104228A 2004-10-08 2005-10-07 Fenilpirazoles AR051135A1 (es)

Applications Claiming Priority (1)

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DE102004049078A DE102004049078A1 (de) 2004-10-08 2004-10-08 Phenylpyrazole

Publications (1)

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AR051135A1 true AR051135A1 (es) 2006-12-20

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US (1) US20080090880A1 (es)
EP (1) EP1799649B1 (es)
JP (1) JP2008515823A (es)
KR (1) KR20070098782A (es)
CN (1) CN101035766A (es)
AR (1) AR051135A1 (es)
AU (1) AU2005293937A1 (es)
BR (1) BRPI0515582A (es)
CA (1) CA2583292A1 (es)
DE (1) DE102004049078A1 (es)
DK (1) DK1799649T3 (es)
ES (1) ES2494920T3 (es)
MX (1) MX2007004041A (es)
PT (1) PT1799649E (es)
RU (1) RU2007116868A (es)
WO (1) WO2006039977A1 (es)
ZA (1) ZA200703677B (es)

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