发明名称 QUARTERNARY PROFORMS OF TERTIARY AMINE CONTAINING COMPOUNDS
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).
申请公布号 WO0242276(A1) 申请公布日期 2002.05.30
申请号 WO2001DK00770 申请日期 2001.11.20
申请人 LEO PHARMACEUTICAL PRODUCTS LTD. A/S;BINDERUP, ERNST, TORNDAL;BJOERKLING, FREDRIK 发明人 BINDERUP, ERNST, TORNDAL;BJOERKLING, FREDRIK
分类号 A61K31/196;A61K31/198;A61K31/282;A61K31/337;A61K31/4422;A61K31/4425;A61K31/475;A61K31/513;A61K31/675;A61K31/704;A61K31/7048;A61K31/7068;A61K45/00;A61P35/00;A61P35/02;A61P43/00;C07D211/84;C07D213/50;C07D213/74;C07D213/75;C07D217/22;(IPC1-7):C07D213/75;A61K31/442;A61K31/472 主分类号 A61K31/196
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