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Treatment of malignant and non-malignant disease with Ras antagonists
专利权人:
Pisces Therapeutics LLC
发明人:
WIKEL, James,BROWNSTEIN, Michael
申请号:
ES12838578
公开号:
ES2642843T3
申请日:
2012.10.05
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A Ras antagonist represented by the formula (I): R1-R2-R3-R4 (I) in which: R1 represents CN, 5 C (>; = O) R5, S (>; = O) (>; = O) R5, CO2M, SO3M, or an N-substituted tetrazole (R8); R2 represents a 5-membered heterocyclic ring with one or two heteroatoms, R3 represents S, O, NH, SO, SO2, or Se; R4 represents farnesyl or geranyl-geranyl; R5 represents hydrogen, hydroxy, C1-C4 alkyloxy, C2-C4 alkenyloxy, C1-C4 hydroxyalkyloxy, C1-C4 aminoalkyloxy or NR6R7; R6 represents hydrogen, hydroxy, C1-C4 alkyl, C2-C4 alkenyl, C1-C4 aminoalkyl, C1-C4 hydroxyalkyl, C1-C4 alkyloxy or C1-C4 alkylamino and R7 represents hydrogen, C1-C4 alkyl, C2-C4 alkenyl, C1-C4 aminoalkyl, C1-C4 hydroxyalkyl, C1-C4 alkyloxy or C1-C4 alkylamino, or wherein R6 and R7 together form a ring that includes morpholine, piperazine or piperidine; M is an organic or inorganic counterion that forms salt; R8 represents hydrogen or C1-C4 alkyl; and pharmaceutically acceptable salts and solvates thereof.Un antagonista de Ras representado por la fómula (I): R1-R2-R3-R4 (I) en el que: R1 representa CN, 5 C(>;=O)R5, S(>;=O)(>;=O)R5, CO2M, SO3M, o un tetrazol sustituido en N(R8); R2 representa un anillo heterocíclico de 5 miembros con uno o dos heteroátomos, R3 representa S, O, NH, SO, SO2, o Se; R4 representa farnesilo o geranilo-geranilo; R5 representa hidrógeno, hidroxilo, alquiloxi C1-C4, alqueniloxi C2-C4, hidroxialquiloxi C1-C4, aminoalquiloxi C1-C4 o NR6R7 ; R6 representa hidrógeno, hidroxilo, alquilo C1-C4, alquenilo C2-C4, aminoalquilo C1-C4, hidroxialquilo C1-C4, alquiloxi C1-C4 o alquilamino C1-C4 y R7 representa hidrógeno, alquilo C1-C4, alquenilo C2-C4, aminoalquilo C1-C4, hidroxialquilo C1-C4, alquiloxi C1-C4 o alquilamino C1-C4, o en el que R6 y R7 juntos forman un anillo que incluye morfolina, piperazina o piperidina; M es un contraión orgánico o inorgánico que forma sal; R8 representa hidrógeno o alquilo C1-C4; y sales y solvatos farmaceuticamente aceptables del mismo.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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