Rapamycin 40-O-Cyclic Hydrocarbon Esters, Compositions and Methods
AssigneeBIOTRONIK SE & Co. KG
InventorsRonald E. Betts, John Dang Nguyen, Beatris Flores
Life of this patent
Estimating the term…
Abstract
A new class of rapamycin 40-O-cyclic hydrocarbon esters is disclosed. The 40-O position of the rapamycin ester has the form 40-O—R, where R is C(O)—(CH2)n—X, n is 0, 1 or 2, and X is a cyclic hydrocarbon having 3-8 carbons, optionally containing one or more unsaturated bonds, and one or more linear (CH2)n) and/or cyclic (X) carbon atoms may have an OH or halide group. Also disclosed are therapeutic compositions and methods that employ the novel analogs.
Claims8
A method of treating a disease selected from the group consisting of restenosis, wound healing, vascular injury, vascular inflammation, transplantation rejection, proliferative ophthalmic diseases (including wet age-related macular degeneration (AMD) and diabetic macular edema (DME)), uveitis and cancer in a mammal by administering an effective amount of a 40-O-cyclic hydrocarbon ester compound having the structure:
- where R is C(O)—(CH2)n—X, n is 0, 1 or 2, X is a cyclic hydrocarbon having 3-8 carbons, optionally containing one or more unsaturated bonds, one or more linear-chain or cyclic carbon atoms may contain an OH or halide substitution, and the rapamycin parent structure may contain substitutions at non-40 positions.
A method of treating uveitis comprising administering an effective amount of a 40-O-cyclic hydrocarbon ester compound having the structure:
- where R is C(O)—(CH2)n—X, n is 0, 1 or 2, X is a cyclic hydrocarbon having 3-8 carbons, optionally containing one or more unsaturated bonds, one or more linear-chain or cyclic carbon atoms may contain an OH or halide substitution, and the rapamycin parent structure may contain substitutions at non-40 positions, wherein the 40-O-cyclic hydrocarbon ester compound is combined with ethanol at a concentration range between at least 1 wt % and at least 60 wt %.
A method of treating cancer comprising administering an effective amount of a 40-O-cyclic hydrocarbon ester compound having the structure:
- where R is C(O)—(CH2)n—X, n is 0, 1 or 2, X is a cyclic hydrocarbon having 3-8 carbons, optionally containing one or more unsaturated bonds, one or more linear-chain or cyclic carbon atoms may contain an OH or halide substitution, and the rapamycin parent structure may contain substitutions at non-40 positions, wherein the 40-O-cyclic hydrocarbon ester compound is administered to an individual in need thereof at a dose range of the compound between about 0.1 nM to about 400 nM.
Dependencies are inferred from the claim text.