AR050454A1 - 1,5-difenil-pirazoles. - Google Patents

1,5-difenil-pirazoles.

Info

Publication number
AR050454A1
AR050454A1 ARP050103374A ARP050103374A AR050454A1 AR 050454 A1 AR050454 A1 AR 050454A1 AR P050103374 A ARP050103374 A AR P050103374A AR P050103374 A ARP050103374 A AR P050103374A AR 050454 A1 AR050454 A1 AR 050454A1
Authority
AR
Argentina
Prior art keywords
replaced
ohet
het
hal
con
Prior art date
Application number
ARP050103374A
Other languages
English (en)
Inventor
Hans-Michael Eggenweiler
Michael Wolf
Original Assignee
Merck Patent Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR050454A1 publication Critical patent/AR050454A1/es

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    • 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
    • C07D231/12—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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  • Psychiatry (AREA)

Abstract

Los derivados de 1,5-difenil-pirazol 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)n Het, (CH2)n COOH, (CH2)nCOOA, COOAr, COOHet, CONH2, CONHA, CONAA', CONHAr, CON(Ar)2, CONHHet, CON(Het)2, NH2, NHA, NHAr, NHHet, NAA', NHCOA, NACOA', NHCOAr, NHCOHet, NHCOOA, NHCOOAr, NHCOOHet, NHCONHA, NHCON-HAr, NHCONHHet, OH, OA, OAr, OHet, SH, S(O)mA, S(O)mAr, S(O)mHet, SO2NH2, SO2NHA, SO2NAA', SO2NHAr, SO2NAAr, SO2NHHet, SO2N(Ar)2, SO2N(Het)2, CONH(CH2)oHet, NH(CH2)oHet, O(CH2)oAr, S(O)m(CH2)oHet, S(O)m(CH2)oAr, (CH2)oCH(Ar)CH3, CONAR12, SO2NA(CH2CONAA'), SO2NH(CH2Ar), SO2NA[(CH2)oCN], SO2NA(CH2Ar), (CH2)oNHAr, (CH2)oNAAr, (CH2)oOAr, (CH2)oS(O)mAr, CH=CH-Ar, CHO, COA o R12, R4, R5R6, son cada uno, de modo independiente entre sí, H, Hal, CN, NO2, A, Alk, (CH29nAr, (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, SO2N(Ar)2, SO2N(Het)2, CO-NH(CH2)oAr, NHCO(CH2)oOA, u O(CH2)oHet, R4 y R5 juntos también son OCH2O u OCH2CH2O, A, A' son cada uno, de modo independiente entre sí, alquilo no ramificado o ramificado con C1- 10, en donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, N, 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 con C3-7, A y A' también son juntos una cadena alquileno con 2, 3, 4, 5 o 6 de C, que puede estar sustituida con CH2 OH, CH2Br, CH2NEt2, y/o en donde un grupo CH2 puede estar reemplazado por O, S, SO, SO2, N, NH, NR8, NCOR8 o NCOOR8, Alk es alquenilo C2-6, R7 es COOR9, CONR9R10, 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 cada uno, 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 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 substituido o mono-, di- o trisustituido con Hal, A, OR11, N(R11)2, NO2, CN, fenilo, CON(R11)2, NR11COA, NR11CON(R11)2, NR11SO2A, COR11, NR11CO(CH2oR11, SO2N(R11)2, S(O)mA, -[C(R11)2]n-COOR11 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 pueden estar mono-, di-, o trisustituido con Hal, A, OR11, N(R11)2, NO2, CN, COOR11, CON(R11)2, NR11COA, NR11SO2A, COR11, SO2NR11, S(O)mA, =S, =NR11 y/u =O (oxígeno del carbonilo), R11 es H o A, R12 es cicloalquilo C3-7 o cicloalquilalquileno C4-12, Hal es F, Cl, Br o I, m es 0, 1 o 2, n es 0, 1, 2, 3 o 4, o es1, 2 o 3 así sus derivados, sales, solvatos y estereoisomeros de utilidad farmacéutica, 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.
ARP050103374A 2004-08-13 2005-08-12 1,5-difenil-pirazoles. AR050454A1 (es)

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AU2005274540A1 (en) 2006-02-23
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