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NANO-SYSTEMS FOR THERAPY AND/OR DIAGNOSIS AND/OR THERAPY MONITORING AND/OR THERANOSTICS OF DISEASECM Patents

Índice de la ficha

Updated at
24/07/2026
Numero publicacion
EP.3452091.A1
Fecha publicacion
13/03/2019
Numero solicitud
EP20170725872
Fecha presentacion
03/05/2017

En detalle

Resumen

[0001] There is disclosed a composition comprising self-assembled nano-particles, the nano-particles comprising dendrimers having a phthalocyanine covalently bound to the periphery thereof. The composition is useful in the therapy and/or diagnosis and/or therapy monitoring and/or theranostics of a lesion of a tissue.

Reivindicaciones

Claims 1. A composition comprising self-assembled nano-particles, the nano-particles comprising dendrimers having a phthalocyanine covalently bound to the periphery thereof. 2. A composition as claimed in Claim 1, wherein the dendrimers are selected from the group consisting of polyamidoamine (PAMAM) dendrimers, polypropyleneimine (PPI) dendrimers, poly-lysine dendrimers, phosphorus dendrimers and polyester dendrimers, most preferably PAMAM dendrimers. 3. A composition as claimed in any preceding claim, wherein the dendrimers are dendrimers of the first generation or higher, or the dendrimers are dendrimers of the third generation or higher. 4. A composition as claimed in any preceding claim, wherein the periphery of the dendrimer is functionalised with one or more surface chemical groups selected from the group consisting of amine, amide, carboxybetaine, sulfobetaine, triazoliumcarboxylate, phosphorylcholine, pyrrolidone, 2-amino-2-hydroxymethyl-propane-l,3-diol, hydroxyl, carboxyl, methoxy, ethoxy, 4-carbomethoxy pyrrolidone, poly(ethylene glycol), and any combination thereof. 5. A composition as claimed in any preceding claim, wherein the phthalocyanine is a peripherally- sub stituted phthalocyanine . 6. A composition as claimed in any preceding claim, wherein the phthalocyanine is a zinc phthalocyanine. 7. A composition as claimed in Claim 6, wherein the phthalocyanine is a compound of the formula: <img class="EMIRef" id="509579181-imgf000065-0001" /> wherein Ri and R<2>are independently selected from the group consisting of — H — COOH — ^^COOH ^COOH / and R<3>, R<4>, R5 and R<6>groups are independently H, an alkyl group having from 1 to 12 carbon atoms, -OR7, -SR7 or -NR7R8, in which R7 and Rs independently represent H, an alkyl group having from 1 to 12 carbon atoms, or a phenyl group optionally substituted by one or more R9 groups independently selected from the group consisting of an alkyl group having from 1 to 12 carbon atoms, -OR10, -SR10, and -NRnRi<2>, wherein Rio, R11 and Ri<2>each independently represent H or an alkyl group having from 1 to 12 carbon atoms. A composition as claimed in Claim 7, wherein the phthalocyanine is a compound of <img class="EMIRef" id="509579181-imgf000066-0001" /> its regioisomers and mixtures thereof, more particularly wherein the phthalocyanine is a compound selected from the group of regioisomers consisting of: 9,16,23-tri-ier^utyl-2-carboxy-5,28: 14,19-diimino-7,12:21,26-dinitrilo- tetrabenzo[c,h,m,r][ 1,6,1 l,16]tetraazacycloeicosinato-(2<">)-N<29>,N<30>,N<31>,N<32>zinc (II); 9,16,24-tri-ier^utyl-2-carboxy-5,28: 14,19-diimino-7,12:21,26-dinitrilo- tetrabenzo[c,h,m,r][ 1,6,1 l,16]tetraazacycloeicosinato-(2<">)-N<29>,N<30>,N<31>,N<32>zinc (II); 9.17.23- tri-ier^utyl-2-carboxy-5,28: 14,19-diimino-7,12:21,26-dinitrilo- tetrabenzo[c,h,m,r][l,6,l l,16]tetraazacycloeicosinato-(2<">)-N<29>,N<30>,N<31>,N<32>zinc (II); 9.17.24- tri-ier^utyl-2-carboxy-5,28: 14,19-diimino-7,12:21,26-dinitrilo- tetrabenzo[c,h,m,r][ 1,6,1 l,16]tetraazacycloeicosinato-(2<">)-N<29>,N<30>,N<31>,N<32>zinc (II); 10.16.23- tri-ier^utyl-2-carboxy-5,28: 14,19-diimino-7,12:21,26-dinitrilo- tetrabenzo[c,h,m,r][ 1,6,1 l,16]tetraazacycloeicosinato-(2<">)-N<29>,N<30>,N<31>,N<32>zinc (II); 10,16,24-tri-ier^utyl-2-carboxy-5,28: 14,19-diimino-7,12:21,26-dinitrilo- tetrabenzo[c,h,m,r][ 1,6,1 l,16]tetraazacycloeicosinato-(2<">)-N<29>,N<30>,N<31>,N<32>zinc (II); 10, 17, 23-tri-ier^utyl-2-carboxy-5,28: 14,19-diimino-7,12:21,26-dinitrilo- tetrabenzo[c,h,m,r][l, 6, 11, 16]tetraazacycloeicosinato-(2<~>)-N<29>, N<30>, N<31>, N<32>zinc (II); 10.17.24- tri-ier^utyl-2-carboxy-5,28: 14,19-diimino-7,12:21,26-dinitrilo- tetrabenzo[c,h,m,r][ 1,6,1 l,16]tetraazacycloeicosinato-(2<">)-N<29>,N<30>,N<31>,N<32>zinc (II); and mixtures thereof, and most particularly wherein the phthalocyanine is a compound comprising a mixture of regioisomers 9(10), 16(17), 23(24)-tri-iert-butyl-2-carboxy-5,28: 14,19-diimino- 7,12:21 ,26-dinitrilo-tetra-benzo[c,h,m,r] [1,6,11,16] tetraazacycloeicosinato-(2<">)-N<29>,N<30>,N<31>,N<32>zinc (II). 9. A composition as claimed in any preceding claim, which is polydisperse, comprising a mixture of assemblies of dendrimer dimers, trimers and/or higher multimers, the self-assembled nano-particles having a mean hydrodynamic size in the range 20 to 200nm. 10. A composition as claimed in any preceding claim, wherein the nano-particles are at least 5nm in size. 11. A composition as claimed in any preceding claim, further comprising a phthalocyanine non-covalently associated with the self-assembled nano-particles. 12. A composition as claimed in any preceding claim, wherein the nano-particles are not conjugated to tissue/cell-targeting moieties. 13. A composition as claimed in any preceding claim, wherein the self-assembled nano-particles, following exposure to electromagnetic radiation, produce one or more of fluorescence, reactive oxygen species, heat, an optical signal and an acoustic signal. 14. A composition as claimed in any preceding claim, in a form suitable for injection, such as a solution or dispersion of the self-assembled nano-particles in an aqueous medium, or a lyophilised material, or a form suitable for topical administration, such as a gel, cream or ointment, or a form suitable for oral administration, such as a tablet or capsule, or a form suitable for direct administration to a lesion of a tissue. 15. A composition as claimed in any preceding claim, for use in therapy and/or diagnosis and/or therapy monitoring and/or theranostics of a lesion of a tissue, for example an atherosclerotic plaque, an inflammatory lesion, or a tumour.

Etiquetas

Inventores
Trohopoulos PanagiotisChristensen Jørn BolstadTorres-Cebada TomásMoghimi Seyed MoeinYlä-Herttuala Seppo Pasi AnteroFicker MarioWu LinpingMedel González MaríaMäkinen Petri Ilmari
Solicitantes
Cosmophos LtdUniversidad Autónoma de MadridUniv CopenhagenKøbenhavns UniversitetUniversity of Eastern FinlandKøbenhavns Univ
Clasificacion ipc
A61K 41/ 00 A IA61K 49/ 00 A IA61P 9/ 10 A IA61P 35/ 00 A I
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