AR084226A1 - Derivados de bencimidazol-amidas, composiciones farmaceuticas que los contienen y uso de los mismos para tratar enfermedades inflamatorias asociadas con el dolor - Google Patents

Derivados de bencimidazol-amidas, composiciones farmaceuticas que los contienen y uso de los mismos para tratar enfermedades inflamatorias asociadas con el dolor

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AR084226A1
AR084226A1 ARP110104608A ARP110104608A AR084226A1 AR 084226 A1 AR084226 A1 AR 084226A1 AR P110104608 A ARP110104608 A AR P110104608A AR P110104608 A ARP110104608 A AR P110104608A AR 084226 A1 AR084226 A1 AR 084226A1
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Argentina
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alkyl
optionally substituted
groups
last
substituents selected
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Roland Pfau
Dirk Stenkamp
Henri Doods
Alexander Heim-Riether
Raimund Kuelzer
Klaus Rudolf
Henning Priepke
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Boehringer Ingelheim Int
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Abstract

Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1) en la que R1 representa halo, OH, -CN, alquilo C1-3, alquinilo C2-6, O-alquilo C1-3, estando estos tres últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de fluoro, -CN, =O, OH, -OCH3, -OCF3; R2 representa halo, -CN, alquilo C1-3, O-alquilo C1-3, estando estos dos últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de fluoro, -CN, =O, OH, -OCH3, -OCF3; R3 y R4 representan independientemente hidrógeno, halo, -CN, alquilo C1-3, O-alquilo C1-3, estando estos dos últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de fluoro, -CN, =O, OH, -OCH3, -OCF3; Ra, Rb representan independientemente hidrógeno, alquilo C1-3 opcionalmente sustituido con uno o más átomos de fluoro, o ambos junto con el átomo de carbono al que están unidos, forman un anillo de cicloalquileno C3-7, o un anillo de heterocicloalquileno de 4 - 6 miembros, estando estos dos últimos anillos opcionalmente sustituidos con uno o más átomos de flúor; W representa -C(O)-, -S(O)-, -S(O)2-, -C(O)O-, C(O)NRd- y estos grupos están unidos al nitrógeno del resto -NH- mediante un átomo de carbono o de azufre; Rd representa hidrógeno, alquilo C1-3; M representa alquilo C1-8, alquinilo C2-8, cicloalquil C3-8-alquilo C0-4, (heterocicloalquil de 4 - 10 miembros)-alquil C0-4-, estando estos cuatro últimos grupos opcionalmente sustituidos con uno o más grupos seleccionados de fluoro, -OH, =O, -CN, -NH2, alquilo C1-3, -NH(alquil C1-3), -N(alquil C1-3)2, azetidinilo, pirrolidinilo, piperidinilo, -O-alquilo C1-3 [y estos siete últimos grupos alquilo pueden estar sustituidos con uno o más sustituyentes seleccionados de fluoro, OH, -CN, O-alquilo C1-2 (y este último grupo alquilo está opcionalmente sustituido con uno o más átomos de flúor)], arilo, heteroarilo [estando estos dos últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de halo, OH, -CN, alquilo C1-3, O-alquilo C1-3 (estando estos dos últimos grupos alquilo opcionalmente sustituidos con uno o más átomos de flúor)], o arilo, heteroarilo, estando estos dos últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de halo, -OH, -CN, -NH2, arilo, heteroarilo [estando estos dos últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de halo, OH, -CN, alquilo C1-3, -O-alquilo C1-3 (estando estos dos últimos grupos alquilo opcionalmente sustituidos con uno o más átomos de flúor)], alquilo C1-7, alquinilo C2-7, cicloalquilo C3-7, heterocicloalquilo de 4 - 7 miembros, -NH(alquil C1-3), -N(alquil C1-3)2, -O-alquilo C1-3, -O-alquil C0-2-arilo, -S-alquilo C1-3, (estando estos últimos grupos alquilo, alquinilo, heterocicloalquilo, arilo o cicloalquilo, opcionalmente sustituidos con uno o más sustituyentes seleccionados de fluoro, -CN, =O, -NH2, -NH(alquil C1-3), -N(alquil C1-3)2, -OH, -O-alquilo C1-3)]; R6 representa hidrógeno, alquilo C1-5, alquinilo C3-6, (heterocicloalquil de 4 - 7 miembros)-alquilo C0-2 o cicloalquil C3-7-alquilo C0-2 [estando estos cuatro últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de fluoro, -CN, =O, -C(O)-NH2, -C(O)-NH(alquil C1-3), -C(O)-N(alquil C1-3)2, alquilo C1-3 opcionalmente sustituido con OH o fluoro, -OH, -NH2, -O-alquilo C1-3, -NH(alquil C1-3), -N(alquil C1-3)2]; R7 y R9 representan independientemente hidrógeno, halo, -CN, alquilo C1-5, cicloalquil C3-5-alquil C0-2-, alquil C1-5-O-, cicloalquil C3-5-alquil C0-2-O- (y en estos cuatro últimos grupos los fragmentos alquilo y cicloalquilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados de fluoro, -CN, =O, OH, -O-alquilo C1-3 o con uno o más grupos alquilo C1-3 que están opcionalmente sustituidos con uno o más átomos de flúor); L representa -NH2, -NHR10, -NR10R11, o un grupo heterocicloalquilo de 4 - 10 miembros que está unido al bencimidazol a través de un átomo de nitrógeno y que puede estar opcionalmente anillado con un fenilo o con un anillo heteroarilo de 5 ó 6 miembros y que está opcionalmente sustituido con uno o más sustituyentes R12; R10 y R11 representan independientemente alquilo C1-7, alquinilo C3-6, cicloalquil C3-7-alquil C0-4- o heterocicloalquil C4-7-alquil C0-4- [estando estos cuatro últimos grupos opcionalmente sustituidos con uno o más grupos seleccionados de fluoro, -OH, NH2, -C(O)NH2, -CN, =O, alquilo C1-3, -NH(alquil C1-3), -N(alquil C1-3)2, -O-alquilo C1-5, -O-cicloalquilo C3-6, -O-heterocicloalquilo C4-6, -S-alquilo C1-3, -S(O)alquilo C1-3, -S(O)2-alquilo C1-3 (estando estos nueve últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de fluoro, -CF3, -CHF2, -CH2F, -CH3)], o aril-alquil C0-4, heteroaril-alquil C0-4- [estando estos dos últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de halo, -OH, -NH2, -CN, alquilo C1-3, cicloalquilo C3-5, alquil C1-3-O-, cicloalquil C3-5-O- (estando estos cuatro últimos grupos opcionalmente sustituidos con uno o más átomos de flúor)]; cada R12 representa independientemente halo, -OH, -NH2, =O, -CN, -C(=O)-NH2, alquilo C1-4, cicloalquil C3-5-alquil C0-2-, heterocicloalquil C4-5-alquil C0-2-, alquil C1-4-O-, alquil C1-3-C(=O)-, -C(O)-NH(alquil C1-3), -C(=O)-N(alquil C1-3)2 [estando estos siete últimos grupos opcionalmente sustituidos con uno ó más grupos seleccionados de: fluoro, -OH, oxo, -NH2, -CN, alquilo C1-3, -NH(alquil C1-3), -N(alquil C1-3)2, -O-alquilo C1-3, -O-cicloalquilo C3-5 (estando estos cinco últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de fluoro, -CF3, -CHF2, -CH2F)], o aril-alquil C0-4-, heteroaril-alquil C0-4- [estando estos dos últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de halo, -OH, -CN, alquilo C1-3, cicloalquilo C3-5, alquil C1-3-O-, cicloalquil C3-5-O- (estando estos cuatro últimos grupos opcionalmente sustituidos con uno o más átomos de flúor)]; A representa alquilo C1-8, alquinilo C3-8, aril-alquil C0-3-, cicloalquil C3-8-alquil C0-3, (heterocicloalquil de 4 - 7 miembros)-alquil C0-3-, heteroaril-alquil C0-3, y en estos seis últimos grupos los fragmentos alquil-, alquinil-, cicloalquil- y heterocicloalquil- están opcionalmente sustituidos con uno o más sustituyentes seleccionados de R14 y los fragmentos arilo y heteroarilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados de R15; cada R14 representa independientemente fluoro, -OH, -CN, =O, -NH2, -NH(alquil C1-3), -N(alquil C1-3)2, -O-alquilo C1-6, alquilo C1-6 [y en estos cuatro últimos grupos los fragmentos alquilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados de fluoro, -CN, =O, -NH2, -NH(alquil C1-3), N(alquil C1-3)2, -OH, -O-alquilo C1-3] o arilo, heteroarilo [estando estos dos últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de halo, OH, -CN, alquilo C1-3, O-alquilo C1-3 (estando estos dos últimos grupos alquilo opcionalmente sustituidos con uno o más átomos de flúor)]; cada R15 representa independientemente halo, -OH, -CN, -NH2, -NH(alquil C1-3), -N(alquil C1-3)2, -O-alquilo C1-3 [y en estos tres últimos grupos los fragmentos alquilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados de fluoro, -CN, =O, -NH2, -NH(alquil C1-3), N(alquil C1-3)2, -OH, -O-alquilo C1-3] o arilo, heteroarilo [estando estos dos últimos grupos opcionalmente sustituidos con uno o más sustituyentes seleccionados de halo, OH, -CN, alquilo C1-3, O-alquilo C1-3 (estando estos dos últimos grupos alquilo opcionalmente sustituidos con uno o más átomos de flúor)] o alquilo C1-7, alquinilo C2-7, cicloalquilo C3-7, heterocicloalquilo de 4 - 7 miembros [estando estos últimos grupos alquilo, alquinilo, heterocicloalquilo o cicloalquilo opcionalmente sustituidos con uno o más sustituyentes seleccionados de fluoro, -CN, =O, -NH2, -NH(alquil C1-3), N(alquil C1-3)2, -OH, O-alquilo C1-3]; o una de sus sales, particularmente una de sus sales fisiológicamente aceptables.
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