[EN] OCULAR INSERTS COMPRISING A COVALENTLY LINKED STEROID DIMER<br/>[FR] INSERTS OCULAIRES COMPRENANT UN DIMÈRE STÉROÏDIEN LIÉ DE MANIÈRE COVALENTE
申请人:INTERFACE BIOLOGICS INC
公开号:WO2019148291A1
公开(公告)日:2019-08-08
The disclosure features ocular inserts for the sustained release of steroids in the treatment ocular conditions. Said ocular inserts are articles formed from a compound of formula D1-L-D2 (A-I), wherein D1 and D2 are steroid radicals selected from the group consisting of an antibiotic steroid, a glucocorticoid steroid, an anti-angiogenic steroid, an intraocular pressure lowering steroid, and a corticosteroid; and L is a linker covalently linking D1 to D2. The article is a fiber, fiber mesh, woven fabric, non- woven fabric, pellet, cylinder, microparticle, nanoparticle, or shaped article. Also disclosed are carbonate and carbonate ester linked dimers of corticosteroids linked at the 3-hydroxyl, the 11-hydroxyl, the 17-hydroxyl, or the 21-hydroxyl positions of the steroid.
该披露涉及眼用插入物,用于缓释类固醇治疗眼部疾病。所述眼用插入物是由化合物D1-L-D2(A-I)形成的物品,其中D1和D2是类固醇基团,所选自抗生素类固醇、糖皮质激素类固醇、抗血管生成类固醇、降低眼内压力类固醇和皮质类固醇;而L是将D1与D2共价连接的连接剂。该物品是纤维、纤维网、织物、非织造布、颗粒、圆柱体、微粒子、纳米粒子或成型物品。此外,还披露了碳酸盐和碳酸酯连接的皮质类固醇二聚体,连接在类固醇的3-羟基、11-羟基、17-羟基或21-羟基位置。