22-10-2015 дата публикации
Номер: US20150297662A1
Принадлежит:
BIOTRONIK AG
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)—(CH)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 (CH)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. 3. A method of treating (i) restenosis; (ii) wound healing; (iii) vascular injury; (iv) vascular inflammation; (v) transplantation rejection; (vi) proliferative ophthalmic diseases claim 1 , including wet age-related macular degeneration (AMD) and diabetic macular edema (DME); (vii) uveitis claim 1 , or (viii) cancer in a mammal claim 1 , by administering to the mammal claim 1 , a therapeutic amount of the rapamycin 40-O-cyclic hydrocarbon ester of .4. The method of claim 3 , for inhibiting restenosis at a vascular injury site claim 3 , wherein the rapamycin 40-O-cyclic hydrocarbon ester is administered from a drug-eluting stent placed at the vascular injury site.5. The method of claim 4 , wherein the drug-eluting stent has an expandable stent body formed of one or more filaments claim 4 , and carried thereon claim 4 , a coating containing between 20 and 100 weight percent of the rapamycin 40-O-cyclic hydrocarbon ester and between 0 and 80 weight percent of a polymer.6. The method of claim 5 , wherein the stent coating contains between 20 and 60 weight percent of the rapamycin 40-O-cyclic hydrocarbon ester and 40 and 80 weight percent of at least one polymer selected from the group consisting of polyanhydride claim 5 , poly(glycolic acid) claim 5 , poly(glycolide) claim 5 , poly(L-lactide) claim 5 , poly(d claim 5 ,l-lactide) claim 5 , poly(L-lactic acid) claim 5 , poly(d claim 5 ,l-lactic acid) claim 5 , poly(caprolactone) claim 5 , poly(trimethylene carbonate) claim 5 , polyester amide claim 5 , polyhydroxyalkanoate ...
Подробнее