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 | , , , , , , , , , , , , , , , , , |
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Format | Patent |
Language | English Korean |
Published |
14.10.2004
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Edition | 7 |
Subjects | |
Online Access | Get full text |
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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. |
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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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Snippet | PURPOSE: Farnesyl transferase inhibitors, preparation processes thereof and pharmaceutical compositions containing the same compounds are provided, which... |
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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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