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Blockers of sodium channels.
专利权人:
PARION SCIENCES; INC.
发明人:
JOHNSON, MICHAEL
申请号:
ES03742810
公开号:
ES2374130T3
申请日:
2003.02.19
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound represented by the formula: wherein X is hydrogen, halogen, trifluoromethyl, (C1-C8) alkyl, phenyl unsubstituted or substituted with halo, (C1-C8) alkyl-thio, phenyl-C1-C8 alkyl -thio, (C1-C8) alkyl sulfonyl, or phenyl (C1-C8) alkyl sulfonyl; Y is hydrogen, hydroxyl, mercapto, (C1-C8) alkoxy, (C1-C8) alkylthio, halogen, (C1-C8) alkyl, mononuclear aryl unsubstituted or substituted with halo or -N (R2) 2; R1 is hydrogen or (C1-C8) alkyl; each R2 is, independently, -R7, - (CH2) m-OR8, - (CH2) m-NR7R10, - (CH2) n (CHOR8) (CHOR8) n-CH2OR8, - (CH2CH2O) m-R8, - (CH2CH2O) m-CH2CH2NR7R10, - (CH2) nC (= O) NR7R10, - (CH2) n-Z8-R7, - (CH2) m-NR10-CH2 (CHOR8) (CHOR8) n-CH2OR8, - ( CH2) n-CO2R7, or R3 and R4 are each, independently, hydrogen, a group represented by the formula (A), (C1-C8) alkyl, hydroxy (C1-C8) alkyl, phenyl, phenyl-alkyl (C1-C8), (halophenyl) -C1-C8 alkyl, ((C1-C8) -phenyl alkyl), ((C1-C8) alkoxy-phenyl) -C1-C8 alkyl, naphthyl-alkyl ( C1-C8) or pyridyl-(C1-C8) alkyl, with the proviso that at least one of R3 and R4 is a group represented by the formula (A): in which each RL is, independently, -R7 , - (CH2) n-OR8, -O- (CH2) m-OR8, - (CH2) n-NR7R10, -O- (CH2) m-NR7R10, - (CH2) n (CHOR8) (CHOR8) n- CH2OR8, -O- (CH2) m (CHOR8) (CHOR8) n-CH2OR8, - (CH2CH20) m-R8, -O- (CH2CH2O) m-R8, - (CH2CH2O) m-CH2CH2NR7R10, -O- (CH2CH2O ) m-CH2CH2NR7R10, - (CH2) nC (= O) NR7R10, -O- (CH2) mC (= O) NR7R10, - (CH2) n- (Z) g-R7, -O- (CH2) m- (Z) g- R7, - (CH2) n-NR10-CH2 (CHOR8) (CHOR8) n-CH2OR8, -O- (CH2) m-NR10-CH2 (CHOR8) (CHOR8) n-CH2OR8, - (CH2) n-CO2R7, -O- (CH2) m-CO2R7, -OSO3H, -O-glucuronide, -O-glucose, or each or is, independently, an integer from 0 to 10; each p is an integer from 0 to 10; with the proviso that the sum of o and p in each adjacent chain varies from 1 to 10; each x is, independently, O, NR10, C (= O), CHOH, C (= N-R10), CHNR7R10, or represents a single bond; R5 is -O- (CH2) m-OR8, - (CH2) n-NR7R10, -O- (CH2) m-NR7R10, - (CH2) n (CHOR8) (CHOR8) n
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