SGLT2 inhibitor polymorph

This invention

This invention is a specific crystalline (solid) form of a C-aryl glucoside molecule that carries a tetrahydrofuran group, developed as an oral treatment for type 2 diabetes mellitus. The crystalline form aims to improve two things at once: how well the body absorbs the drug (bioavailability) and how stable it stays as a solid (shelf-life and handling). It sits in medicinal chemistry and pharmaceutical solid-state science — specifically SGLT2-inhibitor antidiabetic compounds and their polymorphic forms.

Where it fits

Your invention lands in a well-developed corner of antidiabetic drug chemistry. The results cluster in Therapeutic Drug Activity (A61P) and Heterocyclic Compounds (C07D), and especially in Sugars & Nucleic Acids (C07H) — about 117× the corpus average, which simply reflects how focused this glucoside-chemistry niche is. Filings run from 2001 through 2023, a sign that this is a steady, actively pursued direction. Several groups have been busy nearby: Bristol-Myers Squibb and Boehringer Ingelheim International most prominently, alongside Astellas Pharma, AstraZeneca, Takeda, and Merck & Co. The field also reaches into Crystal Growth (C30B) and catalysis-related chemistry, which these results touch less.

Closest related work

US-7713938-B2 — Crystalline form of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene (Boehringer Ingelheim International GmbH · 94 citations · 51-member family)

This patent is strikingly close to your concept. It describes a crystalline form of a C-aryl glucoside bearing a tetrahydrofuran group, methods to prepare it, and its use in medicaments. Reading it shows how Boehringer Ingelheim approached the exact challenge of capturing a defined solid-state form of a tetrahydrofuran-containing glucoside for diabetes. The large family signals significant investment in this molecule and makes it an excellent reference for how crystalline forms in this chemical class are characterized and claimed.

US-7723309-B2 — Crystalline forms of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((R)-tetrahydrofuran-3-yloxy)-benzyl]-benzene (Boehringer Ingelheim International GmbH · 73 citations · 10-member family)

A companion to the patent above, this one covers crystalline forms of the (R)-enantiomer of the same tetrahydrofuran-glucoside scaffold. It illustrates how stereochemistry (R vs. S) produces distinct solid forms worth protecting separately. It also demonstrates the analytical approach to describing crystalline forms in this family — useful context for how subtle structural variations translate into different solid-state properties and stability.

US-6774112-B2 — Amino acid complexes of C-aryl glucosides for treatment of diabetes and method (Bristol-Myers Squibb Company · 222 citations · 16-member family)

This widely cited patent describes crystalline complexes formed between C-aryl glucosides and natural amino acids to improve their solid-state properties. It shows how Bristol-Myers Squibb tackled the same underlying problem — turning a difficult-to-crystallize glucoside into a stable, well-defined solid — by co-crystallizing with amino acids rather than isolating a single polymorph. It's a valuable lens on alternative routes to bioavailability and stability in this exact compound class.

US-8551957-B2 — Pharmaceutical composition comprising a glucopyranosyl-substituted benzene derivative (Boehringer Ingelheim International GmbH · 48 citations · 63-member family, filed 2013)

This more recent filing moves from the molecule to the finished product, pairing a glucopyranosyl-substituted benzene SGLT2 inhibitor with a DPP-IV inhibitor for treating type 2 diabetes. It's a helpful read for seeing how the crystalline drug substance is ultimately formulated and combined with other agents — context for where a defined crystalline form fits within a complete therapeutic product.

What you can do next

• Explore & build on it. Browse the related work above — new, differentiated