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US 7,678,782 B2Granted
Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
AssigneeXenoPort, Inc.
InventorsMark A. Gallop, Kenneth C. Cundy
Life of this patent
Estimating the term…
Abstract
Disclosed are methods for providing enhanced systemic blood concentrations of orally delivered drugs that are incompletely translocated across the intestinal wall of an animal. Also disclosed are methods for the sustained release of drugs, whether poorly or readily bioavailable via oral delivery to animals. Still further, disclosed are compounds and pharmaceutical compositions that are used in such methods.
Claims4
A compound represented by formula (vii)
- wherein
- —N-D is a drug containing at least one primary or secondary amine;
- N is derived from the amine moiety of the drug;
- Q is O;
- V and V* are independently NR7, O, S or CR8R9;
- R10 is R8 or (CR8R9)rZ′;
- Z′ is selected from the group consisting of CO2H, SO3H, OSO3H, SO2H, P(O)(OR6)(OH), OP(O)(OR6)(OH) and pharmaceutically acceptable salts thereof;
- m is 0 or 1;
- n is 0, 1, 2, 3 or 4;
- p is 0, 1 or 2, providing that when m is 0, p is not 0;
- each q is independently 1, 2, 3 or 4;
- r is 0 or 1;
- R1 is selected from the group consisting of hydrogen and OH;
- R2 is selected from the group consisting of hydrogen and OH;
- R6 is selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl;
- and
- each R7, R8 and R9 is independently hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocycle, substituted heterocycle, aryl, substituted aryl, heteroaryl, substituted heteroaryl or R8 and R9 together with the atoms to which they are attached form a cycloalkyl, substituted cycloalkyl, heterocycle or substituted heterocyclic ring, or, when R7 and R9 are present and attached to adjacent atoms, then R7 and R9 together with the atoms to which they are attached form a cycloalkyl, substituted cycloalkyl, heterocycle or substituted heterocyclic ring.
14 more elements
A compound represented by formula (vii):
- wherein
- —N-D is a drug containing at least one primary or secondary amine;
- N is derived from the amine moiety of the drug;
- Q is CH2;
- V is O, S or CR8R9;
- V+ is NR7, O, S or CR8R9;
- R10 is R8 or (CR8R9)rZ′;
- Z′ is selected from the group consisting of CO2H, SO3H, OSO3H, SO2H, P(O)(OR6)(OH), OP(O)(OR6)(OH) and pharmaceutically acceptable salts thereof;
- m is 0 or 1;
- n is 0, 1, 2, 3 or 4;
- p is 0, 1 or 2, providing that when m is 0, p is not 0;
- each q is independently 1, 2, 3 or 4;
- r is 0 or 1;
- R1 is selected from the group consisting of hydrogen and OH;
- R2 is selected from the group consisting of hydrogen and OH;
- R6 is selected from the group consisting of alkyl, substituted alkyl, aryl and substituted aryl;
- and
- each R7, R8 and R9 is independently hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocycle, substituted heterocycle, aryl, substituted aryl, heteroaryl, substituted heteroaryl or R8 and R9 together with the atoms to which they are alt ached form a cycloalkyl, substituted cycloalkyl, heterocycle or substituted heterocyclic ring, or, when R7 and R9 are present and attached to adjacent atoms, then R7 and R9 together with the atoms to which they are attached form a cycloalkyl, substituted cycloalkyl, heterocycle or substituted heterocyclic ring.
15 more elements
Dependencies are inferred from the claim text.