4-aminopyridine and a pharmaceutical composition for treatment of neuronal disorders
OwnerLandon Millerinventor
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Abstract
A composition is provided having the formula where R1 and R2 are each independently H or a C1-C4 hydrocarbon; R3 is H, and R4 is a moiety capable of crossing the blood brain barrier selected from the group consisting of: an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate. The composition includes 4-aminopyridine and a transporter species which allows for improved transport of the aminopyridine across the blood brain barrier thereby reducing systemic side effects of aminopyridine administration.
Claims34
A composition having the formula
- where R1 and R2 are each independently H or a C1-C4 hydrocarbon;
- R3 is H, and R4 is a moiety capable of crossing the blood brain barrier selected from the group consisting of:
- an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate.
A process for forming a conjugate compound having the formula
- where R1 and R2 are each independently H or a C1-C4 hydrocarbon;
- R3 is H, and R4 is a moiety capable of crossing the blood brain barrier selected from the group consisting of:
- an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate comprising:
- reacting a 4-aminopyridine and a moiety capable of crossing the blood brain barrier selected from the group consisting of:
- an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate with a coupling agent.
A composition having the formula
- where R1 and R2 are each independently H or a C1-C4 hydrocarbon;
- R3 and R5 are H, and R4 is H or a moiety capable of crossing the blood brain barrier selected from the group consisting of:
- an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate;
- and R6 is H or a moiety capable of crossing the blood brain barrier selected from the group consisting of:
- an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate, with the proviso that R4 and R6 are not both H.
A process for forming a conjugate compound having the formula
- where R1 and R2 are each independently H or a C1-C4 hydrocarbon;
- R3 and R5 are H, and R4 is H or a moiety capable of crossing the blood brain barrier selected from the group consisting of:
- an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate;
- and R6 is H or a moiety capable of crossing the blood brain barrier selected from the group consisting of:
- an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate, with the proviso that R4 and R6 are not both H comprising:
- reacting a 3,4-aminopyridine and a moiety capable of crossing the blood brain barrier selected from the group consisting of:
- an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate with a coupling agent.
Dependencies are inferred from the claim text.