Patent Evaluation: Bisphosphonic Acids as Effective Anti-Arthritic Drugs

Summary

Novelty: Acyclic bisphosphonates are disclosed and are claimed to be effective anti-arthritic agents. These compounds are said to display reduced side-effects compared to NSAIDs, because they do not inhibit cyclooxygenase.

Biology: No biological data are disclosed.

Chemistry: One hundred and six compounds are disclosed; the preparation of thirty-four are fully described and physical data are given for another forty-eight compounds. The majority of the compounds were prepared by condensation of (simple) bisphosphonates with appropriate reagents under basic contions. Ninety-three are explicitly claimed, including (+)[2,(3,4-dihydro-4-oxo-2-phenyl-2H-1-benzopyran-3-yl)ethylidene-bisphosphonic acid tetraethyl ester.

Structure: