AR074700A1 - Derivados heterociclicos fusionados con oxadiazola, composiciones farmaceuticas, procesos de preparacion y su uso en el tratamiento de esclerosis multiple y otras enfermedades - Google Patents

Derivados heterociclicos fusionados con oxadiazola, composiciones farmaceuticas, procesos de preparacion y su uso en el tratamiento de esclerosis multiple y otras enfermedades

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Publication number
AR074700A1
AR074700A1 ARP090104954A ARP090104954A AR074700A1 AR 074700 A1 AR074700 A1 AR 074700A1 AR P090104954 A ARP090104954 A AR P090104954A AR P090104954 A ARP090104954 A AR P090104954A AR 074700 A1 AR074700 A1 AR 074700A1
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AR
Argentina
Prior art keywords
hal
denotes
coor3
ocf3
atoms
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ARP090104954A
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English (en)
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Merck Serono Sa
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Publication of AR074700A1 publication Critical patent/AR074700A1/es

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Abstract

Reivindicación 1: Los compuestos de la fórmula (1), en donde: R1, R2 denotan independientemente la una de la otra H, COOR3, CONHR3, Hal, CF3, OCF3, CN, NO2, OH, A, OA, o (CH2)mV(CH2)mW; V denota O-, -NR3-, -COO- o -CONR3; W denota COOR3, SO2NH2, CON(R3)2; Q denota un anillo heterocíclico de 5 ó 6 miembros saturado o no saturado, que contiene 1, 2 ó 3 átomos N; X denota -CH- o -N-; Y denota Het, Ar o Cyc; Ra es, A, Hal, CF3, OR3, OCF3, (CH2)nOH, (CH2)nOA, (CH2)nOR3, CN, NO2, N(R3)2, CH2N(H)2-p(A)p, (CH2)nSO2N(R3)2, SO2N(R3)2, (CH2)nNR3SO2A, (CH2)nSO2A, (CH2)nN(SO2A)2, NR3CON(R3)2 o NR3COA, NR3SO2N(R3)2; A es un alquilo ramificado o lineal que tiene desde 1 hasta 12 átomos C, en donde uno o más, preferentemente 1 a 7 átomos H pueden ser reemplazados por Hal, OR3, CN, COOR3, o N(R3)2 y en donde uno o más, preferentemente 1 hasta 7 grupos no adyacentes CH2 pueden ser reemplazados por O, NR3 o S y/o por los grupos -CH=CH- o -CsC-, o denotan cicloalquilo o cicloalquilalquileno que tiene un anillo de 3-7 átomos C; Ar denota un anillo monocíclico o bicíclico, saturado o no saturado o aromático carbocíclico que tiene desde 6 a 14 átomos de carbono, que está monosubstituido, disubstituido o trisubstituido por A, OR3, N(R3)2, NO2, CN, COOR3, CF3, OCF3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2N(R3)2, SOA O SO2A, o, cuando Ra es, Hal, OR3, OCF3, (CH2)nOH, (CH2)nOA, (CH2)nOR3, CN, NO2, N(R3)2, CH2N(H)2-p(A)p, (CH2)nSO2N(R3)2, SO2N(R3)2, (CH2)nNR3SO2A, (CH2)nSO2A, (CH2)nN(SO2A)2, NR3CON(R3)2 o NR3COA, NR3SO2N(R3)2, Ar también puede ser substituido por Hal, con tal que, al menos, un átomo adyacente al átomo que enlaza el grupo Ar al resto de la molécula soporte uno de dichos substituyentes; Het denota un anillo heterocíclico, saturado, no saturado o aromático, monocíclico o bicíclico que tiene desde 1 hasta 4 átomos N, O y/o S que están monosubstituidos, disubstituidos o trisubstituidos por Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-cicloalquilo, OR3, CF3, OCF3, N(R3)2, NR3CON(R3)2, NO2, CN, -[C(R3)2]n-COOR3, [C(R3)2]n-CON(R3)2, NR3COA, NR3SO2A, COR3, SO2N(R3)2, SOA y/o SO2A, con tal que, al menos, un átomo adyacente al átomo que enlaza el grupo Het al resto de la molécula soporte uno de dichos substituyentes; Cyc denota un anillo saturado o no saturado carbocíclico que contiene desde 3 hasta 7 átomos de carbono que están substituidos por Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-cicloalquilo, OR3, CF3, OCF3, N(R3)2, NR3CON(R3)2, NO2, CN, -[C(R3)2]n-COOR3, [C(R3)2]n-CON(R3)2, NR3COA, NR3SO2A, COR3, SO2N(R3)2, SOA y/o SO2A, con tal que, al menos, un átomo adyacente al átomo que enlaza el grupo Cyc al resto de la molécula soporte uno de dichos substituyentes; Hal es F, Cl, Br o I; R3 es H o A; p es 0, 1 ó 2; n es 0, 1, 2, 3 ó 4; m es 0, 1, 2, 3 ó 4; y los derivados, solvatos, tautómeros, sales y estereoisómeros farmacéuticamente aceptables de los mismos, incluyendo las mezclas de los mismos en todas las proporciones.
ARP090104954A 2008-12-18 2009-12-17 Derivados heterociclicos fusionados con oxadiazola, composiciones farmaceuticas, procesos de preparacion y su uso en el tratamiento de esclerosis multiple y otras enfermedades AR074700A1 (es)

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EP08172177 2008-12-18
US23826109P 2009-08-31 2009-08-31

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AR074700A1 true AR074700A1 (es) 2011-02-02

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US (1) US8741923B2 (es)
EP (1) EP2376484B1 (es)
JP (1) JP5855942B2 (es)
KR (1) KR20110100624A (es)
CN (1) CN102245602B (es)
AR (1) AR074700A1 (es)
AU (1) AU2009327133B2 (es)
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JP2013544811A (ja) * 2010-11-03 2013-12-19 ブリストル−マイヤーズ スクイブ カンパニー 自己免疫疾患および血管疾患の治療用のｓ１ｐ１アゴニストとしての複素環式化合物
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PL2958913T3 (pl) 2013-02-20 2019-03-29 Lg Chem, Ltd. Agoniści receptora sfingozyno-1-fosforanowego, sposoby ich przygotowania i zawierające je jako środek aktywny farmaceutyczne kompozycje
TWI613182B (zh) 2013-02-21 2018-02-01 必治妥美雅史谷比公司 雙環化合物
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TWI689487B (zh) 2014-08-20 2020-04-01 美商必治妥美雅史谷比公司 經取代雙環化合物

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EP2376484A1 (en) 2011-10-19
CN102245602A (zh) 2011-11-16
KR20110100624A (ko) 2011-09-14
WO2010069949A1 (en) 2010-06-24
JP2012512829A (ja) 2012-06-07
AU2009327133A1 (en) 2010-06-24
IL213590A0 (en) 2011-07-31
CA2743397A1 (en) 2010-06-24
JP5855942B2 (ja) 2016-02-09
ES2543205T3 (es) 2015-08-17
AU2009327133B2 (en) 2016-04-14
US8741923B2 (en) 2014-06-03
ZA201103405B (en) 2012-08-29
US20110230518A1 (en) 2011-09-22
MX2011006560A (es) 2011-08-03
EP2376484B1 (en) 2015-04-22
CN102245602B (zh) 2014-09-10
EA201170828A1 (ru) 2011-12-30
CA2743397C (en) 2017-02-28
BRPI0923178A2 (pt) 2016-02-16

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