Processes for preparing pimecrolimus starting from ascomycin, exploiting the selectivity characteristics of the purified enzymatic systems particularly regarding the selective deprotection of the hydroxyl groups present in position 33 of ascomycin. Such method represents the first example of chemoenzymatic synthesis for preparing pimecrolimus.

PURPOSE: A composition containing an immunosuppressant and a transglutaminase 2 inhibitor as active ingredients for preventing and treating atopic dermatitis is provided to reduce the volume of the immunosuppressant and to enhance treatment and prevention effects. CONSTITUTION: A pharmaceutical composition for preventing or treating atopic dermatitis contains an immunosuppressant and a transglutaminase 2 inhibitor as active ingredients. The immunosuppressant is selected from the group consisting...

This invention is directed to methods of treating solid tumor cancers, particularly refractory cancers by administration of a drug capable of inhibiting mTOR and/or inhibiting an efflux pump and/or inhibiting HIF-1alpha and VEGF, the drug in particular being selected from the group consisting of sirolimus, everolimus, zotarolimus, tacrolimus, iolimus A9, deforolimus, AP23572, tacrolimus, temsirolimus, pimecrolimus, novolimus, 40-O-(3-hydroxypropyl), 40-O-[2-(2-hydroxy)ethoxy]ethyl-rapamycin and ...

This invention is directed to methods of treating solid tumor cancers particularly refractory cancers by administration of a drug capable of inhibiting mTOR and/or inhibiting an efflux pump and/or inhibiting HIF-1alpha and VEGF the drug in particular being selected from the group consisting of sirolimus everolimus zotarolimus tacrolimus iolimus A9 deforolimus AP23572 tacrolimus temsirolimus pimecrolimus novolimus 40-O-(3-hydroxypropyl) 40-O-[2-(2-hydroxy)ethoxy]ethyl-rapamycin and 40-O-tetrazoly...

Pharmaceutical foam compositions substantially free of ethanol and comprising pimecrolimus in a carrier vehicle comprising a mixture of oily solvents amounting to at least 40 % of the total weight of the composition and consisting of: i) hexylene glycol; ii) optionally oleyl alcohol; and iii) dimethylisosorbide and/or medium chain triglycerides; and additionally: iv) when oleyl alcohol is absent water in an amount of less than 25 %; v) at least one consistency agent; vi) at least one preservativ...

The disclosure relates to compounds and compositions for bone formation fracture treatment bone grafting bone fusion cartilage maintenance and repair and methods related thereto. In certain embodiments the disclosure relates to compositions comprising one or more compound(s) disclosed herein such as clotrimazole honokiol magnolol tacrolimus pimecrolimus sirolimus everolimus temsirolimus spironolactone fluticasone fluticasone propionate fluticasone furoate linezolid telmisartan chlorambucil retin...

Una composición farmacéutica de espuma esencialmente libre de etanol y que comprende pimecrolimus en un vehículo de transporte que comprende una mezcla de disolventes oleosos que equivale a al menos el 40% del peso total de la composición y que consiste en: i) hexilenglicol; ii) alcohol de oleílo; y iii) dimetilisosorbida y triglicéridos de cadena media; y adicionalmente: v) hidroxipropilcelulosa y/o alcohol de estearilo; vi) éster de ácido p-hidroxibenzoico con etilenglicolfeniléter; y vii) mon...