A facile stereocontrolled synthesis of taxol CD rings

The crucial highly functionalized CD substructure of taxol has been synthesized featuring a stereocontrolled Boord reaction and stereoselective Sharpless allylic oxidation sequence leading to oxetane formation

First and stereocontrolled entry to C-7 hydroxy functionality of taxanes employing Boord reaction

Synthesis of a highly functionalized taxol skeleton core making use of Diels-Alder and a novel oxygen bridge opening strategies leading to functionalized C-ring is described

Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma

The structure of LX7101, a dual LIM-kinase and ROCK inhibitor for the treatment of ocular hypertension and associated glaucoma, is disclosed. Previously reported LIM kinase inhibitors suffered from poor aqueous stability due to solvolysis of the central urea. Replacement of the urea with a hindered amide resulted in aqueous stable compounds, and addition of solubilizing groups resulted in a set of compounds with good properties for topical dosing in the eye and good efficacy in a mouse model of ocular hypertension. LX7101 was selected as a clinical candidate from this group based on superior efficacy in lowering intraocular pressure and a good safety profile. LX7101 completed IND enabling studies and was tested in a Phase 1 clinical trial in glaucoma patients, where it showed efficacy in lowering intraocular pressure