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Water-soluble prodrugs positively charged with 1H-imidazo [4,5-c] quinolin-4-amines and compounds related to very high skin penetration rats
专利权人:
Chongxi;Yu
发明人:
Yu, Chongxi
申请号:
ES07705747
公开号:
ES2607901T3
申请日:
2007.01.31
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound having a general formula of Structure 1 or Structure 2, in which, R represents a branched or straight chain, - (CH2) n-, in which n>; = 0, 5 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, in - (CH2) n-, any CH2 can be replaced with O, S, CH>; = CH, C≡C, or CR11R12; R1 and R2 are independently selected from the group consisting of H, alkyl having 1 to 15 carbon atoms, alkyloxy, having 1 to 15 carbon atoms, alkenyl having up to 15 carbon atoms, perfluoroalkyl having 1 to 15 atoms carbon, alkyl halide having 1 to 15 carbon atoms, alkynyl having up to 15 carbon atoms, aryl, and parts of heteroaryl, or taken together at - (CH2) m-, where m>; = 2, 3 , 4, 5, 6, 7, 8, 9, 10, and any CH2 can be replaced with O, S, CH>; = CH, C≡C; R3 is selected from the group consisting of H, alkyl having 1 to 15 carbon atoms, alkyloxy having 1 to 15 carbon atoms, alkenyl having up to 15 carbon atoms, perfluoroalkyl having 1 to 15 carbon atoms, alkyl halide having 1 to 15 carbon atoms, alkynyl having up to 15 carbon atoms, aryl and parts of heteroaryl, in which, any CH2 can be replaced with O, S, CH>; = CH, C≡C, or CR11R12; X represents O, NH, or S; Y represents C, S>; = O, or P-OR11; R4 is selected from the group consisting of alkyl of 1 to 10 carbon atoms, hydroxylalkyl of 1 to 10 carbon atoms, acyloxyalkyl in which the part of alkoxy is alkanoyloxy of 2 to 5 carbon atoms or benzoyloxy, and the part of alkyl contains 1 to 8 carbon atoms, benzyl, (phenyl) ethyl and phenyl, said benzyl, (phenyl) ethyl or phenyl substituent which is optionally substituted on the benzene ring by 1 or 2 parts selected independently from the group consisting of C 1 -C 5 -alkyl, C 1 -C 5 -alkoxy and halogen, provided that if said benzene ring is replaced by 2 of said parts, then said parts together contain no more than 8 carbon atoms ; R5 is selected from the group consisting of hydrogen, alkyl of 1 to 10 carbon atoms, benzyl, (phenyl) ethyl and phenyl, said benzyl, (phenyl) ethyl or phenyl substituent whi
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