NOVEL COMPOUNDS, ISOMER THEREOF, OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AS VANILLOID RECEPTOR ANTAGONIST; AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

A compound as a vanilloid receptor antagonist is provided to obtain a high activity in preventing or treating pain, migraine, arthralgia, neuralgia, neural diseases, neural injury, skin diseases, irritable bowel syndrome, inflammatory diseases, cardiac diseases, etc. A compound as a vanilloid recept...

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Hauptverfasser: RYU, CHONG HYON, PARK, SEOL RIN, LEE, KI WHA, MOH, JOO HYUN, LIM, KYUNG MIN, KIM, SUNG IL, LEE, YONG SIL, KIM, HEE DOO, CHOI, JIN KYU, JEONG, YEON SU, SUH, YOUNG GER, KIM, JIN KWAN, KOH, HYUN JU, BAE, JOON HO, PARK, HYEUNG GEUN, KIM, SUN YOUNG, PARK, YOUNG HO, OH, UH TAEK, SHIN, SONG SEOK
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Sprache:eng
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Zusammenfassung:A compound as a vanilloid receptor antagonist is provided to obtain a high activity in preventing or treating pain, migraine, arthralgia, neuralgia, neural diseases, neural injury, skin diseases, irritable bowel syndrome, inflammatory diseases, cardiac diseases, etc. A compound as a vanilloid receptor antagonist is a compound represented by the following formula Ia or an isomer and/or pharmaceutically acceptable salt thereof. In formula Ia, X is CR11=CR12 or C=C, wherein each of R11 and R12 independently represents H, a halogen atom, C1-C5 alkyl or phenyl; each of R1 and R2 independently represents H, carboxyl, C1-C5 alkyl, halogen, nitro, C1-C5 alkoxy, halo(C1-C5)alkyl, C1-C5 alkylcarbonyl, C1-C5 alkylcarbonylamino, C1-C5 alkylsulfonylamino, phenylsulfonylamino, C1-C5 alkylthio, C1-C5 alkylsulfonyl or C1-C5 alkoxycarbonyl; R3 is H, C1-C5 alkyl, C1-C5 alkoxy or halo(C1-C5)alkyl; each of R4, R5, R6, R7 and R8 independently represents H, carboxyl, C1-C5 alkyl, nitro, C2-C5 alkenyl, C1-C5 alkoxy, C2-C5 alkynyl, halo(C1-C5)alkyl, C1-C5 alkylthio, C1-C5 alkylsulfonyl, C1-C5 alkylcarbonyl, C1-C5 alkoxycarbonyl, phenyl or halogen, wherein the phenyl is non-substituted or substituted with at least one substituent selected from carboxyl, C1-C5 alkyl, halogen, nitro, C2-C5 alkenyl, C1-C5 alkoxy, halo(C1-C5)alkyl, C1-C5 alkylcarbonyl, C1-C5 alkylthio, C1-C5 alkylsulfonyl and C1-C5 alkoxycarbonyl; R9 is C1-C5 alkylsulfonyl or C2-C5 alkenylsulfonyl; and R10 is H, with the proviso that when R3 is not H, R11 and R13 cannot represent H at the same time.