Novel pharmaceutical agents containing carbohydrate moieties and methods of their preparation and use
OwnerSamuel T. Christianinventor
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Abstract
Hydrophilic N-linked pharmaceutical compositions, methods of their preparation and use in neuraxial drug delivery comprising a glycosyl CNS acting prodrug compound covalently N-linked with a saccharide through an amide or an amine bond and a formulary consisting of an additive, a stabilizer, a carrier, a binder, a buffer, an excipient, an emollient, a disintegrant, a lubricating agent, an antimicrobial agent or a preservative, with the proviso that the saccharide moiety is not a cyclodextrin or a glucuronide.
Claims42
A pharmaceutical composition for neuraxial delivery comprising both a hydrophilic N-linked glycosyl prodrug compound and a formulary, wherein said hydrophilic N-linked glycosyl prodrug compound comprises a CNS acting prodrug compound covalently linked with a saccharide through an amide or an amine bond and said formulary comprises an agent selected from the group consisting of an additive, a stabilizer, a carrier, a binder, a buffer, an excipient, an emollient, a disintegrant, a lubricating agent, an antimicrobial agent and a preservative,
- with the proviso that said saccharide moiety is not a cyclodextrin or a glucuronide.
A process for preparing a hydrophilic N-linked glycosyl prodrug compound for neuraxial delivery, comprising the step of N-linking a CNS acting prodrug compound with a saccharide moiety under conditions suitable for formation of an amide or amine bond between said CNS acting prodrug compound and said saccharide moiety.
A process for preparing a pharmaceutical composition comprising hydrophilic N-linked glycosyl prodrug compound for neuraxial delivery, comprising the steps of N-linking a CNS acting prodrug compound with a saccharide moiety under conditions suitable for formation of an amide or amine bond between said CNS acting prodrug compound and said saccharide moiety;
- and formulating said N-linked glycosyl prodrug compound into said pharmaceutical composition by addition of an agent selected from the group consisting of an additive, a stabilizer, a carrier, a binder, a buffer, an excipient, an emollient, a disintegrant, a lubricating agent, an antimicrobial agent and a preservative.
A method for treating a neurological dysfunction in a subject in need thereof comprising the step of administering to the subject a pharmaceutical composition comprising a compound according to FORMULA I:
- A-B-D-E Formula I
- wherein, each of “—” comprises a single bond;
- A, comprises a CNS-acting prodrug;
- B, comprises a lower alkyl;
- D, comprises a nitrogen linker amine or amide;
- and, E comprises a saccharide, with the proviso that E is not a cyclodextrin.
A method for improving the aqueous solubility and blood brain barrier penetrability of a drug, comprising the step of forming a covalent chemical bond between the drug and a sugar or oligosaccharide, wherein said drug comprises an amide or amine group and said drug bonded to said sugar or oligosaccharide comprises a compound according to FORMULA I:
- A-B-D-E Formula I
- wherein, each of “—” comprises a single bond;
- A, comprises a CNS-acting prodrug;
- B, comprises a lower alkyl;
- D, comprises a nitrogen linker amine or amide;
- and, E comprises a saccharide, with the proviso that E is not a cyclodextrin.
A method of treating a subject in need thereof to effect a metabolic replacement therapy, comprising the step of administering to said subject a therapeutic compound, wherein said therapeutic compound comprises a hydrophilic compound transportable intact by an intestinal glucose transporter, transportable intact in blood, transportable intact by endothelial cells at a blood brain barrier and metabolizable by a neuronal cell, wherein said therapeutic compound further comprises a compound binding to a dopamine receptor and metabolizable in said neuronal cell to effect said metabolic replacement therapy and said subject comprises a patient with a neurological dysfunction, a Parkinson's disease or a Parkinson's related disease.
Dependencies are inferred from the claim text.