Crystalline form of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments

This patent claims a specific crystalline (polymorphic) form of the compound 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene — the SGLT2 inhibitor that became known as empagliflozin (marketed as Jardiance). Rather than claiming the molecule itself, claim 1 covers a particular solid-state crystal form fingerprinted by its X-ray powder diffraction pattern: characteristic peaks at 18.84, 20.36 and 25.21 degrees 2θ (±0.05°) measured with CuKα1 radiation. Dependent claims tighten this to additional diffraction peaks (claim 2), to material that is at least 50% in this crystalline form (claim 3), and to a pharmaceutical composition containing it (claim 4). The practical purpose of such a patent is to lock down the defined, manufacturable solid form actually used in the drug product — a polymorph with predictable stability, processability and dissolution behavior — which is distinct from the broader compound and method-of-use patents.

The patent is assigned to Boehringer Ingelheim International GmbH and names five inventors — Frank Himmelsbach, Sandra Schmid, Martin Schuehle, Hans-Juergen Martin and Matthias Eckhardt. It was granted in 2010. The family is large — 51 members across 32 countries — signaling aggressive worldwide prosecution consistent with a form patent protecting a flagship commercial product across all major markets. Its 94 forward citations are substantial for a polymorph claim and reflect heavy downstream interest from generic and competing innovators tracking the empagliflozin solid form. The classification spread (C07H sugars/nucleic acids, C07D heterocycles, A61K pharmaceutical preparations, A61P therapeutic activity) places it squarely in the small-molecule antidiabetic chemistry space.

Where this patent stands: This is a product-protecting polymorph filing within a tightly coordinated portfolio, not a foundational discovery patent. The anchor invention — the empagliflozin compound genus and the SGLT2-inhibitor scaffold — sits in earlier Boehringer filings such as US-7579449-B2 (184 citations). This patent's role is to fence the specific crystalline form used in the marketed product, extending and reinforcing the franchise's protection beyond compound expiry and raising the bar for generic formulation. It plainly underpins a major commercial product (Jardiance) and is one node in a dense Boehringer cluster of compound, process, composition and crystal-form patents that collectively wall off the SGLT2 program.

The surrounding space is densely clustered and overwhelmingly dominated by a single owner: Boehringer Ingelheim, which holds 19 of the patents in this set with 1,169 citations — and a near-complete sweep of the nearest patents to the subject. Of the top 20 most-relevant patents, the large majority are Boehringer filings; the only non-Boehringer near neighbors are crystalline-form patents from Japanese SGLT2 players (Mitsubishi Tanabe, Kissei) and a recent Lek Pharmaceuticals hydrate. The other names on the citation chart (OSI, Novartis, Theravance, Bayer, Vertex, Takeda) appear with one or three patents each and reflect adjacent small-molecule chemistry rather than direct competition in this specific scaffold. This is effectively a proprietary thicket built around one company's SGLT2 program.

Closest related patents:

• US-7723309-B2 — Crystalline forms of the (R)-tetrahydrofuran-3-yloxy stereoisomer (Boehringer Ingelheim · 73 citations · 10-member family). The direct stereochemical counterpart to the subject patent, claiming crystalline forms of the (R)-isomer versus the subject's (S)-isomer — companion coverage within the same chemical series.
• US-8802842-B2 — Method for the preparation of a crystalline form (Boehringer Ingelheim · 25 citations · 32-member family). A process patent covering preparation of the crystalline form, extending protection from the form itself to how it is made.
• US-7579449-B2 — Glucopyranosyl-substituted phenyl derivatives (Boehringer Ingelheim · 184 citations · 82-member family). The most-cited and broadest filing in the set — the foundational compound-genus patent that the subject crystalline-form claim sits beneath.
• US-7943582-B2 — Crystalline form of a glucopyranosyl thienylmethyl benzene hemihydrate (Mitsubishi Tanabe · 30 citations · 62-member family). A competing innovator's crystalline-form patent on a different SGLT2 inhibitor (canagliflozin scaffold), illustrating that polymorph claiming is the standard defensive move across this drug class.
• US-10323056-B2 — Crystalline hydrates of a glucopyranosyl benzene (Lek Pharmaceuticals · 0 citations · 11-member family). A 2019 generic-affiliate filing on crystalline hydrate forms — recent, on-point, lightly-cited strategic IP the citation-weighted score under-rewards, signaling generic-side activity around solid forms.

The technology concentration confirms how tight this cluster is: Sugars & Nucleic Acids (C07H) runs at **161.7× the corpus