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Patent landscape, scope, and claims: |
Scope and Claims Analysis for U.S. Patent 10,662,188 (Sesqui‑DMSO/1⁄4‑Ethyl Acetate Solvates; Modification I)
U.S. Patent 10,662,188 is a solid-state IP patent that concentrates protection on (i) specific solvates of a particular compound of formula (I), defined by X-ray powder diffraction (XRPD) peak maxima and quantitative form purity thresholds, and (ii) a specific crystalline “Modification I” and controlled form combinations. The claim set also includes pharmaceutical compositions for oral delivery and method-of-treatment/prophylaxis claims for multiple disease areas (cardiovascular, pulmonary, thromboembolic, fibrotic), but the core novelty resides in form identity (XRPD/thermal/spectroscopic characterization) plus composition form dominance (>90% and >95% by weight).
What the patent claims protect (high-level)
- Sesqui‑DMSO solvate of compound (I) with defined XRPD peaks and high solvate fraction in the composition.
- 1/4‑ethyl acetate solvate of compound (I) with defined XRPD peaks and high solvate fraction in the composition.
- Modification I (a particular solid form of compound (I)), with explicit “only forms” compositions.
- Specific compound name in Modification I and its solvate form, with additional XRPD peak definition.
- Oral dosage form compositions and therapeutic use methods that administer these specific forms.
What exactly is the invention scope in US 10,662,188?
Core protected subject matter is the combination of:
- A particular compound of formula (I) (and in dependent claims a specific named molecule), and
- Specific solid-state forms (sesqui‑DMSO solvate, 1/4‑ethyl acetate solvate, and Modification I),
- Defined by XRPD peak maxima (2θ values), and
- Contained at high concentration in the finished pharmaceutical composition (thresholds >90 wt% or >95 wt%).
Claim 1 and claim 8 define the primary scope hooks
- Claim 1: pharmaceutical composition containing sesqui‑DMSO solvate of formula (I), characterized by XRPD peaks at 2θ = 8.3, 13.7, 15.7 (with “further wherein” indicating additional peaks are acceptable but at least those maxima are required as defining features), and containing >90 wt% sesqui‑DMSO solvate of formula (I) relative to total forms.
- Claim 8: parallel protection for 1/4‑ethyl acetate solvate, characterized by XRPD peaks at 2θ = 8.7, 17.8, 26.7 (plus “further”), and containing >90 wt% 1/4‑ethyl acetate solvate relative to total forms.
These two independent claim families are the center of enforceable breadth: they cover compositions, not just the isolated solid.
Which XRPD-defined form variants fall within claim 1 (sesqui‑DMSO solvate) and its dependents?
Claim 1 base XRPD definition
- Required peak maxima include: 2θ 8.3; 13.7; 15.7.
Dependent claims narrow/expand the XRPD window by listing additional peaks
- Claim 2 adds peaks: 17.2, 24.9 (beyond the base set).
- Claim 3 adds peaks: 17.2, 18.4, 19.6 (and includes 24.9).
- Claim 4 provides the broadest “larger list” in this dependent chain:
8.3, 8.4, 13.7, 13.9, 15.7, 17.2, 18.4, 19.6, 21.4, 24.9.
Critical quantitative element
- Claim 5: compositions with >95 wt% sesqui‑DMSO solvate relative to all forms.
Practical claim-interpretation impact (IP coverage boundary)
- If an accused product’s XRPD spectrum misses the required peak maxima of the relevant independent claim, it risks falling outside literal scope.
- If XRPD matches, form purity becomes a key infringement determinant: >90 wt% (or >95 wt% for the narrower dependent route).
Which XRPD-defined form variants fall within claim 8 (1/4‑ethyl acetate solvate) and its dependents?
Claim 8 base XRPD definition
- Required peak maxima include: 2θ 8.7; 17.8; 26.7.
Dependent claims add multiple alternative XRPD peak lists
- Claim 9: 14.2, 24.0, 26.7
- Claim 10: 14.2, 17.8, 19.3, 24.0, 25.1, 26.7
- Claim 11: 6.7, 8.3, 8.7, 12.9, 14.2, 17.8, 19.3, 24.0, 25.1, 26.7
- Claim 12: quantitative: >95 wt% 1/4‑ethyl acetate solvate relative to total forms.
Coverage boundary
- The invention is “form-locked” by XRPD peak maxima plus high solvate fraction. This setup is designed to make around difficult through partial conversion or mixed solvates, unless the competitor can keep the product outside the relevant XRPD fingerprint or avoid crossing the purity thresholds.
What is “Modification I” coverage, and how broad is it?
Claim 15: “A compound of the formula (I) in the form of Modification I, as 1/4‑ethyl acetate solvate, or a mixture thereof.”
This is a key breadth device because it reaches:
- the solid form Modification I itself, and
- the 1/4‑ethyl acetate solvate, and
- mixtures of the two.
Dependent claims then add structure and characterization anchors.
Specific named compound in Modification I (claims 17-18)
- Claim 17 identifies the compound as:
methyl {4,6‑diamino‑2‑[1‑(2‑fluorobenzyl)‑1H‑pyrazolo[3,4‑b]pyridino‑3‑yl]pyrimidino‑5‑yl}methylcarbamate in Modification I.
- Claim 18 constrains Modification I by XRPD peaks: 2θ = 6.7, 9.1, 17.8.
Solvate of the named compound (claims 19-20)
- Claim 19: 1/4‑ethyl acetate solvate of the same named compound.
- Claim 20: XRPD peaks: 2θ = 8.7, 17.8, 26.7.
“Only one form” limitation (claims 21-23) materially changes around pathways
- Claim 21: pharmaceutical composition comprising only one of the forms: Modification I or 1/4‑ethyl acetate solvate plus excipients.
- Claim 22: only Modification I
- Claim 23: only 1/4‑ethyl acetate solvate
This “only” language is narrower than the >90 wt% solvates claims, but it is powerful for enforcement when a competitor uses a single-form drug substance and markets it as such.
Claim 24 is a “two-form exclusion” style claim
- Claim 24: Modification I + mono‑DMSO solvate and no other form.
This indicates the patent estate anticipates multiple DMSO-related polymorph/solvate variants and targets specific controlled polymorphic “stacks.”
How do composition purity thresholds affect infringement risk?
The claims create a gradient of quantitative form dominance:
- Claim 1 / claim 8: >90 wt% of the relevant solvate relative to all forms.
- Claim 5 / claim 12: >95 wt%.
A competitor strategy to reduce infringement risk typically would be to:
- lower the fraction of the protected solvate below the >90 or >95 thresholds (or shift to other forms),
- or change the solid state form such that the XRPD peaks do not match.
The patent language is structured so that mixed-form drug substances are still vulnerable if the protected solvate remains dominant above the thresholds.
What oral dosage form and excipient claims exist?
- Claim 6: compositions of claim 1 as oral-suitable solid/liquid preparations, including:
solid dispersion, capsule, pill, tablet, troche, lozenge, melt, powder, solution, suspension, emulsion.
- Claim 13: similar oral forms for claim 8.
- Claim 26: addition of inert nontoxic pharmaceutically suitable excipients.
This makes the patent compatible with typical generic/formulation development: the patent does not require a unique formulation matrix (like a specific polymer), only administration-ready oral dosage forms containing the protected solid state.
What treatment and prophylaxis method claims are covered?
The patent spans multiple therapeutic categories through parallel method claims:
- Claim 7: administration of claim 1 composition for cardiovascular, pulmonary, thromboembolic, or fibrotic diseases.
- Claim 14: parallel method for claim 8 composition.
- Claim 27-29: similar methods for administration of the compound/form claims and the “only one form” composition claim 21.
Important structure: method-of-use depends on form-locked entities
For infringement of the method claims, the administered material must align with the protected composition or compound claims. This links clinical use protection to manufacturing/control of solid-state form rather than only to the pharmacology.
How does the “only Modification I” or “only 1/4-ethyl acetate solvate” language change competitive design-around?
- Claim 21-23 create strong leverage when a supplier makes a product with a single isolated form. Many manufacturing processes target a single solid state form, which increases the chance the product fits “only” claims.
- Competitors can attempt to design-around by:
- intentionally controlling the presence of minor forms (to violate “only”),
- or shift entirely to different polymorph/solvate systems not meeting XRPD fingerprints.
However, the independent solvate claims with >90 wt% coverage can still capture such products if the protected form remains predominant.
How strong is the claim set from a litigation posture (scope vs. number of anchors)?
This patent’s enforceability is enhanced by multiple “anchors”:
- Identity: formula (I) compound plus named compound in dependent claims.
- Solid-state characterization: XRPD peak maxima with multiple dependent peak lists.
- Quantitative thresholds: >90 wt% and >95 wt%.
- Finished product relevance: oral dosage forms and excipients included.
- Use coverage: broad therapeutic areas.
At the same time, the patent is highly dependent on XRPD matching. That can raise disputes on:
- instrument conditions,
- peak assignment, and
- whether reported maxima match the required set.
Still, the claim structure lists explicit 2θ values, which typically allows experts to compare spectra directly.
What other patent landscape elements usually co-exist with this kind of form patent?
This is a form-centric patent. In real infringement/invalidity work, the patent landscape is usually layered:
1) Upstream patents on synthesis and “formula (I)” compound
Those typically exist as “drug substance” backbone patents. If those are expiring or already expired, form patents like 10,662,188 can still block a generic if the generic’s solid form matches.
2) Downstream patents on other solvates/polymorphs
Given the presence of:
- sesqui‑DMSO,
- mono‑DMSO (claim 24),
- 1/4‑ethyl acetate,
- Modification I,
the portfolio likely includes additional solid-form siblings that cover alternate crystalline or solvated forms.
3) Formulation patents (not necessarily required here)
Even though this patent covers oral dosage forms broadly, competitors often seek separate formulation-IP (e.g., specific excipient systems, particle size, or dissolution enhancement). Those do not appear in the claim text provided, but they are frequently part of the broader portfolio.
What is the Orange Book status of U.S. Patent 10,662,188?
No Orange Book list and no FDA product-to-patent mapping information is provided in the prompt. Without those details, no definitive status (listed/not listed; which NDA/ANDA; listed expiration) can be stated from the claims alone.
What is the litigation and Paragraph IV risk profile for this patent?
No ANDA/Paragraph IV filing history, no court dockets, and no settlement/consent decree terms are provided. Without docket identifiers or FDA reference to specific ANDAs, no accurate litigation status can be mapped to this patent number.
Key Takeaways
- U.S. Patent 10,662,188 is dominated by solid-state claim scope: it protects sesqui‑DMSO solvate and 1/4‑ethyl acetate solvate of a compound of formula (I) using XRPD peak maxima and high form purity thresholds (>90 wt% and >95 wt%).
- “Modification I” is separately protected, including a named compound in Modification I with XRPD peaks, and also in combination or “only one form” compositions that can complicate generic design-around.
- The patent extends protection to oral dosage compositions and method-of-treatment/prophylaxis for cardiovascular, pulmonary, thromboembolic, and fibrotic indications, but those method claims are effectively tied to the protected drug substance form and composition composition.
- Litigation leverage is likely highest against products that ship with a predominant protected solvate or a single isolated form matching “only” claim limitations, since the claims combine XRPD fingerprinting with quantitative dominance.
FAQs
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Do the claims require the XRPD peaks to be exact, or can they tolerate shifts?
The claims specify 2θ peak maxima values; infringement typically turns on expert comparison of whether the observed maxima correspond to the claimed positions.
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If a product contains >90 wt% of the protected solvate but includes another minor form, is it still covered?
Yes for the broad solvate independent claims because they use dominance relative to total forms (>90 wt%).
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Does the patent protect only the active ingredient, or also the finished dosage form?
It protects both, including pharmaceutical compositions suitable for oral administration containing the protected solid state.
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Are the therapeutic indications limited to a specific disease, or are they broad?
They are broad across cardiovascular, pulmonary, thromboembolic, and fibrotic diseases through multiple method claims.
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Which claim elements are the most “design-around” sensitive?
The most sensitive elements are (i) the XRPD-defined solid-state identity and (ii) form fraction thresholds (>90 wt%, >95 wt%) and “only one form” limitations.
References
No sources were cited because no bibliographic or FDA/Orange Book/patent-office record details were provided beyond the claim text in the prompt.
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