The patent application No. 1430/DELNP/2011 entitled “DIOXA-BICYCLO[3.2.1.]OCTANE-2,3,4-TRIOL DERIVATIVES” has been granted to Pfizer Inc. by the Indian Patent Office. A pre-grant opposition u/S 25(1) with regard to this application was filed by Mr. Antony David on 20/08/2018. A hearing was held in the matter on 05/11/2019.

The compound claimed in the present application is (1S,2S,3S,4R,5S)-5-[4-chloro-3-(4-ethoxy-benzyl)-phenyl]-1-hydroxymethyl-6,8-dioxa-bicyclo[3.2.1]octane-2,3,4-triol and its crystalline form particularly with L-proline and L-pyroglutamic acid. The compound has therapeutic application as sodium-glucose transporter inhibitor, particularly SGLT2 inhibitor (INN: Ertugliflozin, WHO 27(1), 2013).

With regard to the objection of obviousness various prior art documents were relied. Some documents were relied to demonstrate the structural aspect of the compound, whereas some were relied to illustrate that to form crystalline polymorph of the compound was well known in art. The structural differences between the compound disclosed in the prior art and compound of present invention along with the stereochemistry orientations and other key difference were highlighted by the Applicant.

The Applicant also relied on the IC50 values that clearly demonstrated the clinical efficacy of the claimed compound. The compound of the present application ≈ 2000 times more selective to SGLT2 as compared to SGLT1..

Further, as the specification provided all the required information relating to the method of preparation, the biological activity, the aforementioned specification was considered sufficient by the Controller and opposition was dismissed.