Claims
- 1. A compound of general formula I:
- 2. A compound according to claim 1, in which D is a drug, peptide, protein, nucleic acid, mono- or oligosaccharide, sugar-amino conjugate, sugar-peptide conjugate, pro-drug or drug-like molecule.
- 3. A compound according to claim 1, in which D is a biological molecule.
- 4. A compound according to claim 1, in which the linker X is attached to the mono- or oligosaccharide S through the glycosidic position.
- 5. A compound according to claim 1, in which the linker X is attached to the mono- or oligosaccharide S via an O-glycoside, C-glycoside, N-glycoside, S-glycoside, amide, urea, thiourea, carbamate, thiocarbamate, carbonate, ether or ester bond.
- 6. A compound according to claim 1, in which the linker X is attached to the mono- or oligosaccharide S through a position other than the glycosidic position via an amide, urea, thiourea, carbamate, thiocarbamate, carbonate, ether or ester bond.
- 7. A compound according to claim 1, in which the linker X is attached to the lipidic moiety L via an amide, ester, ether, imine, carbamate, urea, thiourea, or carbonate linkage.
- 8. A compound according to claim 1, in which W is substituted with one or more functional groups selected from an amidine, guanidinium, carboxylate, tetrazole, hydroxamic acid, hydrazide, amine, sulfate, phosphonate, phosphate and a sulfonate group.
- 9. A compound according to claim 1, in which the lipidic moiety L is composed of:
(a) any combination of 1 to 4 lipoamino acids and/or lipoamino alcohols, of general formula IIa or IIb 14in which each of R1 and R2 may independently be: (i) hydrogen, or (ii) a linear or branched chain alkyl or alkenyl group having 4 to 24 carbon atoms, which may optionally be substituted, provided that the substituents do not significantly adversely affect the lipophilic nature of the group, with the proviso that both R1 and R2 cannot be hydrogen at the same time; (b) a glycerol-based lipid of general formula IIIa or 111b 15in which R1 and R2 are as defined in general formula IIa, and X is a linker group, as defined in general formula I; or (c) a trishydroxymethylmethylamine-based lipid of general formula IVa or IVb 16in which R1′,R2′ and R3′ are independently hydrogen or a linear or branched chain alkyl or alkenyl group having 4 to 24 carbon atoms, or an aryl or arylalkyl group having 6 to 24 carbon atoms, said alkyl, alkenyl, aryl or arylalkyl groups may optionally be substituted, provided that the substituents do not significantly adversely affect the lipophilic nature of the group, and X is as defined in general formula I; with the proviso that at least one of R1′, R2′ and R3′ must not be hydrogen.
- 10. A compound according to claim 8, in which the lipidic moiety L contains one or more charged functional groups.
- 11. A compound according to claim 10, in which the one or more charged functional groups are selected from the group consisting of amidine, guanidinium, carboxylate, tetrazole, hydroxamic acid, hydrazide, amine, sulfate, phosphonate, phosphate, and sulfonate.
- 12. A compound according to claim 1, in which the mono- or oligosaccharide S is a mono-, di- or tri-saccharide, and the lipidic moiety is one to three lipoaminoacids of general formula IIa or IIb:
- 13. A compound according to claim 1, in which r is greater than p.
- 14. A compound according to claim 13, in which D is a drug, peptide, protein, nucleic acid, mono- or oligosaccharide, sugar-amino conjugate, sugar-peptide conjugate, pro-drug or drug-like molecule.
- 15. A compound according to claim 13, in which D is a biological molecule.
- 16. A compound according to claim 1, in which D is a sulfated oligosaccharide, charged oligosaccharide, sulfated antithrombotic or an aminoglycoside.
- 17. A compound according to claim 13, in which D is a sulfated oligosaccharide, charged oligosaccharide, sulfated antithrombotic or an aminoglycoside.
- 18. A method of preparing a compound according to claim 1, comprising the step of forming a covalent bond between the mono- or oligosaccharide S and the linker X or the lipid L, in which the bond between S and X is an O-glycoside, C-glycoside, N-glycoside, S-glycosides, amide, urea, thiourea, carbamate, thiocarbamate, carbonate, ether or ester bond, and the bond between X and L is an amide, ester, ether, imine, carbamate, urea, thiourea, or carbonate bond.
- 19. A composition comprising a compound according to claim 1, together with a pharmaceutically-acceptable carrier.
- 20. A method of preparation of a compound according to claim 1, comprising the step of mixing a drug molecule D with [Wq—S—X-L](my) in which W, q, S, X, L, m and y are as defined in claim 1 in solution, followed by removal of the solvent(s) to provide a homogeneous mixed salt.
- 21. A method of delivery of a therapeutically useful molecule, comprising the step of administering the molecule to a subject in need of such treatment in the form of a compound according to claim 1.
- 22. A method according to claim 21, in which the administration is by the oral route.
- 23. A method of treating or preventing a pathological condition, comprising the step of administering a suitable compound according to claim 1 to a subject in need of such treatment.
Priority Claims (1)
Number |
Date |
Country |
Kind |
0100115.5 |
Jan 2001 |
GB |
|
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is a continuation-in-part of International Application No. PCT/AU02/00005, filed Jan. 3, 2002, designating the United States; which claims the priority of British Application No. 0100115.5, filed Jan. 4, 2001. The entire contents of these two applications are incorporated into this application by reference.
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
PCT/AU02/00005 |
Jan 2002 |
US |
Child |
10676436 |
Jun 2003 |
US |