AR047585A1 - Derivados de bisarilurea - Google Patents

Derivados de bisarilurea

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Publication number
AR047585A1
AR047585A1 ARP050100299A ARP050100299A AR047585A1 AR 047585 A1 AR047585 A1 AR 047585A1 AR P050100299 A ARP050100299 A AR P050100299A AR P050100299 A ARP050100299 A AR P050100299A AR 047585 A1 AR047585 A1 AR 047585A1
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Argentina
Prior art keywords
cr5r6
group
independently selected
independently
hal
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ARP050100299A
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Inventor
Hans-Peter Buchstaller
Lars Thore Burgdorf
Frank Stieber
Chirstiane Amendt
Matthias Grell
Christian Sirrenberg
Zenke Frank Dr
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Merck Patent Gmbh
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Publication of AR047585A1 publication Critical patent/AR047585A1/es

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    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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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    • 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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    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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Abstract

La presente se refiere a derivados de bisarilurea de la formula (1), en donde Ar1, Ar2 se seleccionan, de modo independiente entre sí, de hidrocarburos aromáticos que contienen 6 a 14 átomos de C y residuos heterocíclicos etilénicos insaturados o aromáticos que contienen 3 a 10 átomos de C y uno o dos heteroátomos, seleccionados, de modo independiente, de N, O y S; E, G, M, Q y U se seleccionan, de modo independiente entre sí, de átomos de C y átomos de N, con la condicion de que uno o varios de E, G, M Q y U sean átomos de C y que X esté unido a un átomo de C; R7 está seleccionado, de modo independiente, de un grupo integrado por Het, OHet, N(R11)Het, (CR5R6)kHet, O(CR5R6)kHet, N(R11)(CR5R6)kHet, (CR5R6)kNR11R12, (CR5R6)kOR13, O(CR5R6)kNR11R12, NR11(CR5R6)kNR11R12, O (CR5R6)kR13, NR11 (CR5R6)kR13, O (CR5R6)kOR13, NR11(CR5R6)kOR13, (CR5R6)nO(CR5R6)kNR11R12, O (CR5R6)nO(CR5R6)kNR11R12, NR11(CR5R6)nO(CR5R6)kNR11R12, (CR5R6)nNR11(CR5R6)kNR11R12, O(CR5R6)nNR11(CR5R6)kNR11R12, NR11(CR5R6)nNR12(CR5R6)kNR11R12, (CR5R6)nO(CR5R6)kOR11, O(CR5R6)nO(CR5R6)kOR11, NR11(CR5R6)nO(CR5R6)kOR12, (CR5R6)nNR11(CR5R6)kOR12, O(CR5R6)nNR11(CR5R6)kOR12, NR12(CR5R6)nNR11(CR5R6)kOR12, O(CR5R6)kAr3-NR11R12, SO2R13, SO2(CR5R6)kOR13 y SO2(CR5R6)kNR11R12, en donde R5, R6 están seleccionados, en cada caso de modo independiente entre sí, de H y AQ; o R5 y R6 representan juntos opcionalmente un grupo oxo; o R7 está seleccionado de radicales divalentes de la formula -SO2-CR8=CR8-, en donde ambas valencias están unidas de modo vecinal a Ar1, n y/o k son, de modo independiente, 0, 1, 2, 3 o 4, preferentemente 1, 2, 3 o 4, y con mayor preferencia aun es 2 o 3; R8, R9 y Rr10 están seleccionados, de modo independiente, de un grupo integrado por H, A, cicloalquilo que comprende 3 a 7 átomos de C, Hal, CH2Hal, CH(Hal)2, C(Hal)3, NO2, (CH2)nCN, (CH2)nNR11R12, (CH2)nO(CH2)kNR11R12, (CH2)nNR11(CH2)kNR11R12, (CH2)nO(CH2)kOR11, (CH2)nNR11(CH2)kOR12, (CH2)nCOOR13, (CH2)nCOR13, (CH2)nCONR11R12, (CH2)nNR11COR13, (CH2)nNR11CONR11R12, (CH2)nNR11SO2A, (CH2)nSO2NR11R12, (CH2)nS(O)uR13, (CH2)nOC(O)R13, (CH2)nCOR13, (CH2)nSR11, CH=N-OA, CH2CH=N-OA, (CH2)nNHOA, (CH2)nCH=N-R11, (CH2)nOC(O) NR11R12, (CH2)nNR11COOR13, (CH2)nN(R11)CH2CH2OR13, (CH2)nN(R11)CH2CH2OCF3, (CH2)nN(R11)C(R13)HCOOR12, (CH2)nN(R11)C(R13)HCOR11, (CH2)nN(R11)CH2CH2N(R12)CH2COOR11, (CH2)nN(R11)CH2CH2NR11R12, CH=CHCOOR13, CH=CHCH2NR11R12, CH=CHCH2NR11R12, CH=CHCH2OR13, (CH2)nN(COOR13)COOR14, (CH2)nN(CONH2)COOR13, (CH2)nN(CONH2)CONH2, (CH2)nN(CH2COOR13)COOR14, (CH2)nN(CH2CONH2)COOR13, (CH2)nN(CH2CONH2)CONH2, (CH2)nCHR13COR14, (CH2)nCHR13COOR14, (CH2)nCHR13CH2OR14, (CH2)nOCN y (CH2)nNCO, en donde R11 y R12 están seleccionados, de modo independiente, de un grupo integrado por H, A, C(O)A, (CH2)mAr3, C(O)(CH2)mAr3, (CH2)mHet, C(O) (CH2)mHet y S(O)uA, o en NR11R12, R11 y R12 forman, junto con el átomo de N al que están unidos, un heterociclo de 5, 6 o 7 miembros que opcionalmente contiene 1 o 2 heteroátomos adicionales, seleccionados de N, O y S, que está opcionalmente sustituido con uno o varios sustituyentes, seleccionados de A, R13, =O, =S y =N-R14,; R13, R14 están seleccionados, de modo independiente, de un grupo integrado por H, Hal, A, (CH2)mAr4 y (CH2)mHet; A está seleccionado del grupo integrado por alquilo, alquenilo, cicloalquilo, alquilencicloalquilo, alcoxi, alcoxialquilo y heterociclilo saturado, preferentemente del grupo integrado por alquilo, alquenilo, cicloalquilo, alquilencicloalquilo, alcoxi y alcoxialquilo; Ar3, Ar4 son, de modo independiente entre sí, residuos hidrocarbonados aromáticos que comprenden 5 a 12 y preferentemente 5 a 10 átomos de C que están opcionalmente sustituidos con uno o varios sustituyentes, seleccionados de un grupo integrado por A, Hal, NO2, CN, OR15, NR15R16, COOR15, CONR15R16, NR15COR16, NR15CONR15R16, NR16SO2A, COR15, SO2NR15R16, S(O)uA y OOCR15; Het es un residuo heterocíclico saturado, insaturado o aromático que está opcionalmente sustituido con uno o varios sustituyentes, seleccionados de un grupo integrado por A, C(O)A, R13, =O, =S, =N-R14,Hal, NO2, CN, OR15, NR15R16, COOR15, CONR15R16, NR15COR16, NR15CONR15R16, NR16SO2A, COR15, SO2NR15R16, S(O)uA y OOCR15; R15 y R16 están seleccionados, de modo independiente, de un grupo integrado por H, A, y (CH2)mAr6, en donde Ar6 es un hidrocarburo aromático de 5 o 6 miembros que está opcionalmente sustituido con uno o varios sustituyentes seleccionados de un grupo integrado por metilo, etilo, propilo, 2-propilo, ter-butilo, Hal, CN, OH, NH2 y CF3; k, n y m son, de modo independiente entre sí, 0, 1, 2, 3, 4, o 5; X representa un enlace o es (CR11R12)h, o (CHR11)h-Q-(CHR12)i, en donde Q está seleccionado de un grupo integrado por O, S, N-R15, (CHal2)j,(O-CHR18)j, (CHR18-O)j, CR18=CR19, (O-CHR18CHR19)j, (CHR18CHR19-O)j, C=O, C=S, C=NR15, CH(OR15), C(OR15)(OR20), C(=O)O, OC(=O), OC(=O)O, C(=O)N(R15), N(R15)C(=O), OC(=O)N(R15), N(R15)C(=O)O, CH=N-O, CH=N-NR15, OC(O)NR15, NR15C(O)O, S=O, SO2, SO2NR15 y NR15SO2, en donde h, i son, de modo independiente entre sí, 0,1, 2, 3, 4, 5, o 6, y j es 1, 2, 3, 4, 5 o 6; Y está seleccionado de O, S, NR21, C(R22)-NO2, C(R22)-NO2, C(R22)- CN y C(CN)2, en donde R21 está seleccionado, de modo independiente, de los significados dados para R13, R14 y R22 está seleccionado, de modo independiente, de los significados dados para R11, R12; g es 1, 2 o 3, preferentemente 1 o 2; p, r son, de modo independiente entre sí, 0,1, 2, 3, 4 o 5; q es 0, 1, 2, 3 o 4, preferentemente 0, 1 o 2; u es 0, 1,2 o 3, preferentemente 0, 1 o 2, y Hal está seleccionado, de modo independiente, de un grupo integrado por F, Cl, Br e I; y sus derivados, sales y solvatos farmacéuticamente aceptables. Al uso de los compuestos de la formula (1) como inhibidores de la raf-quinasa, al uso de los compuestos de la formula (1) para preparar una composicion farmacéutica y a un método de tratamiento que comprende la administracion de dicha composicion farmacéutica a un paciente.
ARP050100299A 2004-01-30 2005-01-28 Derivados de bisarilurea AR047585A1 (es)

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US (1) US20070161677A1 (es)
EP (1) EP1730111A2 (es)
JP (1) JP2007519653A (es)
KR (1) KR20060132882A (es)
CN (1) CN1972925A (es)
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RU2006131045A (ru) 2008-03-10
WO2005075425A2 (en) 2005-08-18
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CA2554878A1 (en) 2005-08-18
KR20060132882A (ko) 2006-12-22
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