FARNESYL TRANSFERASE INHIBITORS, PREPARATION PROCESSES THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, IN WHICH THE COMPOUNDS ARE USEFUL FOR PREVENTION AND TREATMENT OF CANCER, VIRUS OR HYPERLIPIDEMIA

PURPOSE: Farnesyl transferase inhibitors, preparation processes thereof and pharmaceutical compositions containing the same compounds are provided, which compounds have improved farnesyl transferase inhibiting activity and low CYP 3A4 enzyme inhibiting activity, so that an interaction between drugs...

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Main Authors CHOI, OK HUI, CHOI, HWAN GEUN, CHOI, SE HYEON, HAN, HUI UN, KWON, TAE SIK, HONG, CHANG YONG, LEE, SEONG BAE, LEE, IN SANG, KIM, HAK JUNG, KIM, MIN HYEONG, KIM, GYEONG HUI, LEE, JIN HO, JUNG, SIN U, KIM, JONG HYEON, KOO, SEON YEONG, KIM, DONG MYEONG, PARK, JI HYEON, LEE, SEON HWA
Format Patent
LanguageEnglish
Korean
Published 14.10.2004
Edition7
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Abstract PURPOSE: Farnesyl transferase inhibitors, preparation processes thereof and pharmaceutical compositions containing the same compounds are provided, which compounds have improved farnesyl transferase inhibiting activity and low CYP 3A4 enzyme inhibiting activity, so that an interaction between drugs for farnesyl transferase and CYP 3A4 enzyme can be minimized, and the compounds can be useful for prevention and treatment of cancer, virus or hyperlipidemia. CONSTITUTION: The farnesyl transferase inhibitors represented by formula (1), or pharmaceutically acceptable salts or isomers thereof are provided, wherein (B) is one selected from benzene ring, N-benzene ring, Y-benzene ring and X-Y-benzene ring; X and Y are independently C-H, N, O or S; R1 and R2 are independently hydrogen, optionally halogen substituted C1-6 alkyl, optionally halogen substituted C1-6 alkoxy, hydroxy, halogen, nitro, cyano, thienyl, C3-6 cycloalkyl, di(C1-6alkyl)amine, C3-6 cycloamine, C3-6 cycloalkylamine, C5-6 heterocycloamine, C5-6 heterocycloalkylamine, optionally C1-6 alkyl or halogen substituted phenoxy, or optionally C1-6 alkyl or halogen substituted aniline, or a compound of formula (2); X' is C-H or N; R6, R7, R8 and R9 are independently hydrogen, C1-6 alkyl, C1-6alkoxy, hydroxy, halogen, nitro, cyano, amino or di(C1-6alkyl)amine; R3 is C1-6 alkyl; R4 is optionally C2-6 alkenyl or halogen substituted phenyl or naphthyl; R5 is one selected from R10-N-N-R10R11, R10-N-Y'-R11 and N-Y'-benzene ring; Y' is O, S, S=O or SO2; and R10 and R11 are independently hydrogen, hydroxy, C1-6 alkyl or C1-6 alkoxy.
AbstractList PURPOSE: Farnesyl transferase inhibitors, preparation processes thereof and pharmaceutical compositions containing the same compounds are provided, which compounds have improved farnesyl transferase inhibiting activity and low CYP 3A4 enzyme inhibiting activity, so that an interaction between drugs for farnesyl transferase and CYP 3A4 enzyme can be minimized, and the compounds can be useful for prevention and treatment of cancer, virus or hyperlipidemia. CONSTITUTION: The farnesyl transferase inhibitors represented by formula (1), or pharmaceutically acceptable salts or isomers thereof are provided, wherein (B) is one selected from benzene ring, N-benzene ring, Y-benzene ring and X-Y-benzene ring; X and Y are independently C-H, N, O or S; R1 and R2 are independently hydrogen, optionally halogen substituted C1-6 alkyl, optionally halogen substituted C1-6 alkoxy, hydroxy, halogen, nitro, cyano, thienyl, C3-6 cycloalkyl, di(C1-6alkyl)amine, C3-6 cycloamine, C3-6 cycloalkylamine, C5-6 heterocycloamine, C5-6 heterocycloalkylamine, optionally C1-6 alkyl or halogen substituted phenoxy, or optionally C1-6 alkyl or halogen substituted aniline, or a compound of formula (2); X' is C-H or N; R6, R7, R8 and R9 are independently hydrogen, C1-6 alkyl, C1-6alkoxy, hydroxy, halogen, nitro, cyano, amino or di(C1-6alkyl)amine; R3 is C1-6 alkyl; R4 is optionally C2-6 alkenyl or halogen substituted phenyl or naphthyl; R5 is one selected from R10-N-N-R10R11, R10-N-Y'-R11 and N-Y'-benzene ring; Y' is O, S, S=O or SO2; and R10 and R11 are independently hydrogen, hydroxy, C1-6 alkyl or C1-6 alkoxy.
Author KOO, SEON YEONG
LEE, IN SANG
HONG, CHANG YONG
KIM, MIN HYEONG
KIM, JONG HYEON
KIM, DONG MYEONG
LEE, SEON HWA
PARK, JI HYEON
CHOI, HWAN GEUN
KIM, GYEONG HUI
CHOI, OK HUI
LEE, JIN HO
KIM, HAK JUNG
JUNG, SIN U
LEE, SEONG BAE
CHOI, SE HYEON
HAN, HUI UN
KWON, TAE SIK
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– fullname: CHOI, HWAN GEUN
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– fullname: HAN, HUI UN
– fullname: KWON, TAE SIK
– fullname: HONG, CHANG YONG
– fullname: LEE, SEONG BAE
– fullname: LEE, IN SANG
– fullname: KIM, HAK JUNG
– fullname: KIM, MIN HYEONG
– fullname: KIM, GYEONG HUI
– fullname: LEE, JIN HO
– fullname: JUNG, SIN U
– fullname: KIM, JONG HYEON
– fullname: KOO, SEON YEONG
– fullname: KIM, DONG MYEONG
– fullname: PARK, JI HYEON
– fullname: LEE, SEON HWA
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Snippet PURPOSE: Farnesyl transferase inhibitors, preparation processes thereof and pharmaceutical compositions containing the same compounds are provided, which...
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SubjectTerms CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Title FARNESYL TRANSFERASE INHIBITORS, PREPARATION PROCESSES THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, IN WHICH THE COMPOUNDS ARE USEFUL FOR PREVENTION AND TREATMENT OF CANCER, VIRUS OR HYPERLIPIDEMIA
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