摘要 |
The invention relates to a compound of general formula (I), wherein the moiety of formula (II), comprises one or more tertiary amines; R1 represents hydrogen, C1-4alkyl or aryl; A is an ester group (-O-C(O)-) or a carbonate group (-O-C(O)-O-); B represents poly-saccharide, poly-amino acid, poly-acrylate, poly-urea, poly-urethane, poly-vinyl pyrrolidone, poly-vinyl alcohol or -(CH2)m-[Y]n-(CH2)r-R, wherein R is C1-6alkyl, C3-6cycloalkyl, C2-6alkenyl, C2-6alkenyl, aryl, aralkyl, heteroaryl or non-aromatic hetorocyclic hydrocarbon, all of which are substituted with one or more substituents selected from the group consisting of amino, aminoalkyl, hydroxysulfonyloxy, dihydroxyphosphinoyl, dialkoxyphospinoyl, dihydroxyphosphinoyloxy, carboxy, sulfo, sulfamino, aminosulfonyl, aminocarbonyl, C1-4alkoxycarbonyl or aminoacylamino; R may also be (A), wherein q is an integer from 1 to 200, each R2 is independently hydrogen or methyl; and R3 is hydrogen or C1-4alkyl; Y is O or N(R4), wherein R4 is hydrogen or C1-4alkyl; m and r are independently an integer from 0 to 4; n is 0 or 1; Z is an anion such as chloride, bromide, iodide, sulphate, methanesulphate, p-toluenesulphonate or nitrate; and a salt thereof. The compounds are useful in increasing the solubility of compounds of formula (II).
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申请人 |
LEO PHARMACEUTICAL PRODUCTS LTD. A/S;BINDERUP, ERNST, TORNDAL;BJOERKLING, FREDRIK |
发明人 |
BINDERUP, ERNST, TORNDAL;BJOERKLING, FREDRIK |