Patent Evaluation: Calcium Channel Antagonists as Ocular Hypotensive Agents

Summary

Novelty: A therapeutic agent for the treatment of glaucoma, which comprizes the topical or systemic administration of 2-phenyl-3-oxo-2H-1,4-benzothiazine derivatives, is disclosed.

Biology: For evaluation of the effect of the compounds in the treatment of glaucoma the compounds were administered to rabbits having a high intraocular pressure provoked by chymotrypsin, according to the method of Sears et al. A typical compound lowered the intraocular pressure by 2.3 mmHg after 1h, by 3.1 mmHg after 2h and by 3.0 mmHg following administration of 3mg/kg of the compound.

Chemistry: No details of synthesis are given. Ten examples of formulations are presented. (+)-(R)-3,4-Dihydro-2-[5-methoxy-2-[-3-[N-methyl-N-[2-[(3,4-3,4-methylenedioxy)phenoxy]ethyl]amino]propoxy]phenyl]-4-methyl-3-oxo-2H-1,4 -benzothiazine is specifically claimed.