Branched, dendrimeric-type macromolecules composed essentially of a central nucleus and of a series of polyoxaalkyl chains that depart from said nucleus and spread into the surrounding space branching in a cascade fashion useful as carriers of drugs, contrast agents, etc.
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[ We claim:] [1.] Dendrimeric macromolecules of the formula: EQU A[G.sub.1-p ].sub.r ing r number of structures G.sub.(1.fwdarw.p) in the dendrimer per structure where:A is a polyfunctional/polyvalent central nucleus, or core, which is an aliphatic open chain, branched or unbranched, or an alicyclic
[ We claim:] [1.] Dendrimeric macromolecules of the formula: EQU A[G.sub.1-p ].sub.r ing r number of structures G.sub.(1.fwdarw.p) in the dendrimer per structure where:A is a polyfunctional/polyvalent central nucleus, or core, which is an aliphatic open chain, branched or unbranched, or an alicyclic, or a heterocyclic group containing N, O and/or S, or an aromatic or a heteroaromatic group and which contains terminal group to which polyoxaalkylene chains of a first generation shell are attached;r is an integer from 2 to 10 representing the functionality of the core A and, as a consequence, also the total number of dendra, in whichG.sub.(1.fwdarw.p) is a single dendron linked to A,[G.sub.(1.fwdarw.p) ].sub.r represents the branched structure of the macromolecule comprising p levels of generation shells from the first one g.sub.(1) to the last one g.sub.(p), in which the total number of said generation shells p can range from 1 to 20 and in which the different generation shells may contain the same repetition units, and in which:(a) each generation g.sub.(i), except for the last g.sub.(p), comprises repeating units, which are represented by a functional group of formula EQU --B--M-- re:B is a polyoxaethylene or polyoxapropylene chain of formula: [ STR 32 ] in which n can range from 0 to 25 and may differ from generation to generation and in which in at least one generation shell of the macromolecule, n is other than 0,M represents a branching point which is a polyvalent aliphatic group comprising m reactive functional groups for the linking of the polyoxaalkylene chains of the next generation shell, in whichm in an integer ranging from 2 to 5 and m may differ from one generation shell to another;(b) the last generation shell g.sub.(p) comprises functional groups of formula: EQU --B.sub.(p) --M.sub.(p) [T].sub.m(p)where B.sub.(p), M.sub.(p), m.sub.(p) defined analogously to B, M, and m, with all the m.sub.(p) reactive groups of M.sub.(p) connected to groups T, in whichT is a terminal group that is either H or halo, hydroxyl, amino, thiol, --O-tosyl, --O-mesyl, --O-tresyl, --O-brosyl, trifluoromethanesulfonyl, aldehydo, carboxy or an amido group, said terminal group T being free, either dissociated or undissociated, or protected by a protective group, orM.sub.(p) is a single bond, no branching exists and the last generation shell g.sub.(p) is formed by groups of formula: EQU --B.sub.(p) --Twhere B.sub.(p), and T are as above defined, and(c) when p=1 the macromolecule contains only one generation shell, g.sub.(p) which corresponds to g.sub.(i) and has the formula: EQU --B.sub.(1) --M.sub.(1) [T]m.sub.(1)where B.sub.(1), M.sub.(1), m.sub.(1) and T are defined analogously to B.sub.(p), M.sub.(p), m.sub.(p) and T, said macromolecule optionally labeled with an isotope. [6.] A dendrimeric type macromolecule which is a member selected from the group consisting ofa) BI: 1,4,7,11,14,17-hexaoxa-1,17-bis(oxan-2-yl)-9,9-bis[2,5,8-trioxa-8-oxan-2-y l)octyl]heptadecane;b) BII,III: 1,4,7,10,14,17,20,23-octaoxa-1,23-bis(oxan-2-yl)-12,12-bis[2,5,8,11-tetrao xa-11-(oxan-2-yl) undecyl]tricosane;c) BIV,V: 1,4,7,10,13,17,20,23,26,29-decaoxa-1,29-bis(oxan-2-yl)-15,15-bis[2,5,8,11, 14-pentaoxa-14-(oxan-2-yl)tetradecyl]nonacosane;d) CI: 3,6,10,13-tetraoxa-8,8-bis-(2,5-dioxa-7-hydroxyheptyl)pentadecan-1,15-diole) CII: 3,6,10,13,16,19-hexaoxa-11,11-bis(2,5,8-trioxa-10-hydroxydecyl)enicosan-1, 21-diol;f) CIII: 14,14-bis(2,5,8,11-tetraoxa-13-hydroxydecyl)-3,6,9,12,16,19,22,25-octaoxah eptacosan-1,27-diol;g) GI: 3,6,10,13-tetraoxa-8,8-bis(2,5-dioxa-7-bromoheptyl)pentadecan-1,15-dibromi de;h) DI: 1,4,7,11,14,17-hexaoxa-1,17-bis(p-toluensulfonyl)-9,9-bis[2,5,8-trioxa-8-( p-toluenesulfonyl)octyl]heptadecane;i) DII: 1,4,7,10,14,17,20,23-octaoxa-1,23-bis(p-toluenesulfonyl)-12,12-bis[2,5,8,1 1-tetraoxa-11-(p-toluenesulfonyl)undecil]tricosane;j) DIII: 15,15-bis[2,5,8,11,14-pentaoxa-14-(p-toluenesulfonyl)tetradecyl]-1,29-bis( p-toluensulfonyl)-1,4,7,10,13,17,20,23, 26,29-decaosanonacosane;k) EI: 3,6,10,13-tetraoxa-1,15-bis(phthalimido)-8,8-bis[2,5-dioxa-7-(phthalimido) heptyl] pentadecane;l) EII: 3,6,9,13,16,19-hexaoxa-1,21-bis(phthalimido)-11,11-bis[2,5,8-trioxa-10-(ph thalimido) decyl]enicosane;m) FI: 3,6,10,13-tetraoxa-8,8-bis(2,5-dioxa-7-aminoheptyl)pentadecan-1,15-diamine ;n) HI: 4,7,10,14,17,20-hexaoxa-2,2,22,22-tetra(hydroxymethyl)-12,12-bis[2,5,8-tri oxa-10,10-bis(hydroxymethyl)-11-hydroxyundecyl]tricosan-1,23-diol;o) HII: 18,18-bis[2,5,8,11,14-pentaoxa-16,16-bis(hydroxymethyl)-17-hydroxyheptadec yl]-2,2,34,34-tetra(hydroxymethyl)-4,7,10,13,16,20,23,26,29,32-decaoxapenta triacontan-1,35-diol;p) LI: 1,23-di(p-toluenesulfonyloxy)-12,12-bis[11-(p-toluenesulfonyloxy)-10,10-bi s(p-toluenesulfonyloxymethyl)-2,5,8-trioxaundecyl]-2,2,22,22-tetra(p-toluen esulfonyloxymethyl)-4,7,10,14,17,20-hexaoxatricosane;q) MI: 1,23-dibromo-12,12-bis[11-bromo-10,10-bis(dibromomethyl)-2,5,8-trioxaundec yl]-2,2,22,22-tetrabromomethyl-4,7,10,14,17,20-exaoxatricosane;r) NI: 1,35-di(oxan-2-yl-oxy)-18,18-bis[17-(oxan-2-yl-oxy)-10,10-bis(7-(oxan-2-yl -oxy)-2,5-dioxaheptyl)-2,5,8,12,15-pentaoxaheptadecyl]-8,8,28,28-tetra[(7-o xan-2-yl-oxy)-2,5-dioxaheptyl]-3,6,10,13,16,20,23,26,30,33-decaoxapentatric ontane. [8.] A dendrimeric macromolecule consisting of a core, and at least two cascade branched chains linked to said core, wherein said core is a polyvalent organic molecule and said branched chains comprise a plurality of repeating units, said units being the same or different from one generation shell to another, each of said units consisting of(a) a polyoxaalkylene chain, and(b) a polyvalent branched aliphatic group having further branching points attached to it; d dendrimeric macromolecule having at the most 20 generation shells of said repeating units, the last of said generation shells having mono- or polyvalent functional terminal groups; and said polyoxaalkylene chain consists of n oxyalkylene group wherein n is an integer ranging from 0 to 25 and is the same or different from one generation shell to another and at least in one of said generation shells is other than 0.
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이 특허에 인용된 특허 (3)
Tomalia Donald A. (Midland MI), Bridged dense star polymers.
Orlicki, Joshua A.; Jensen, Robert E.; Bratcher, Matthew S.; McKnight, Steven H., Interface-directed branched polymer transports and methods for producing same.
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