Cell Permeability of Macrocycles Patents: Who Leads, Gaps 2026
- Concentrated at the top. The top 5 assignees hold 55.7% of all 106 records in scope, and the top 10 hold 79.2% — a small group set the boundaries most new filers have to design around.
- Filing has cooled since 2021. Filings ran 6 in 2021 down to 1 in 2024, an 83% drop over that span; 2023 was the peak year so far at 8, but publication lag means the last two years understate real activity.
- Medicinal chemistry dominates the claim space. A61K covers 80.2% of the 106 records, with peptide chemistry (C07K, 35.8%) and heterocyclics (C07D, 22.6%) the next densest classes — assay and analytical claims (G01N, C12Q) sit far thinner.
Filing growth compares 2021 (6 records) with 2024 (1) — a three-year span. 2024 is the most recent year we treat as complete: publication lags filing by roughly 18 months, so 2025 onwards are still filling in and any growth rate that ends there would understate the field. Top-5 share is the combined record count of the five largest assignees divided by all 106 records in scope (CR5), not by the ranked leaders only.
What this landscape covers
Macrocycle permeability sits at the intersection of medicinal chemistry and biophysics: patents in this set claim molecules, formulations or design methods that let large, often peptidic, ring structures cross cell membranes by passive diffusion rather than active transport. The search combines terms for the underlying mechanism — intramolecular hydrogen bonding, conformational shielding, chameleonic behavior — with the pharmacological metrics used to demonstrate it, such as polar surface area, efflux ratio and the solubility-permeability tradeoff. That pairing keeps the corpus focused on molecules and methods where permeability is the claimed inventive step, not an incidental property.
106 published records sit in scope from 2015 through the mid-2026 data cut-off. The assignee base is a mix of universities, research institutes and a handful of pharmaceutical filers, with receiving offices concentrated in the United States, WIPO/PCT and Europe.
Filing trend and technology composition
Two views of the same 106 records: how filing activity has moved year over year, and which IPC subclasses carry the claims.
Filing activity has thinned since its 2023 peak
Filings held near zero through 2017, then rose to a peak of 8 in 2023 before falling. The 2021-to-2024 span shows a drop from 6 to 1 filings, an 83% decline — but because publication typically lags filing by around 18 months, the 2025 and 2026 figures are still incomplete and should not be read as confirmation the field is slowing further.
A61K anchors the field; assay-side classes are thin
Medicinal preparations (A61K) appear in 80.2% of the 106 records, with therapeutic-activity claims (A61P, 36.8%) and peptide chemistry (C07K, 35.8%) close behind. Heterocyclic compounds (C07D) sit at 22.6%. Measurement and testing classes — C12Q, G01N — each cover under 10% of records, suggesting the assay-correlation side of the field is claimed far less densely than the molecule and formulation side.
Shares are the percentage of the 106 records in scope. A patent can carry several IPC classes, so the shares add up to more than 100%.
Go deeper on Cell Permeability of Macrocycles with Eureka
This page is one run against one query. Ask Eureka your own question about cell permeability of macrocycles and every answer comes back with the patent numbers behind it.
Try EurekaA representative claim on intramolecular hydrogen bonding
Amino acid having functional group capable of intermolecular hydrogen bonding, peptide compound containing same and method for production thereof
It has been found that the membrane permeability of peptide compounds can be improved by making at least one of amino acids constituting the peptide compound be an amino acid having a side chain capable of forming an intramolecular hydrogen bond.Filed by Chugai Seiyaku, published 2023-03-30 as US20230096766A1.
| # | Publication no. | Patent title | Citations |
|---|---|---|---|
| 1 | US8008088B2 | SMMR (small molecule metabolite reporters) for use as in vivo glucose biosensors | 879 |
| 2 | US8029765B2 | SMMR (small molecule metabolite reporters) for use as in vivo glucose biosensors | 706 |
| 3 | US8466286B2 | SMMR (small molecule metabolite reporters) for use as in vivo glucose biosensors | 648 |
| 4 | US20140127137A1 | SMMR (small molecule metabolite reporters) for use as in vivo glucose biosensors | 569 |
| 5 | US20040077540A1 | Compositions and methods for modulating physiology of epithelial junctional adhesion molecules for enhanced m… | 249 |
| 6 | US20040028613A1 | Dopamine agonist formulations for enhanced central nervous system delivery | 185 |
| 7 | US20040115135A1 | Compositions and methods for enhanced mucosal delivery of peptide YY and methods for treating and preventing … | 141 |
| 8 | US5672584A | Cyclic prodrugs of peptides and peptide nucleic acids having improved metabolic stability and cell membrane p… | 112 |
| 9 | US7166575B2 | Compositions and methods for enhanced mucosal delivery of peptide YY and methods for treating and preventing … | 90 |
| 10 | WO2003000018A2 | Dopamine agonist formulations for enhanced central nervous system delivery | 76 |
Citation counts favour older filings simply by virtue of time in the corpus; treat them as a measure of influence on later work, not of current commercial relevance.
Each row carries its publication number; clicking a row searches Eureka by that number.
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Three patterns stand out once the concentration figures and IPC composition are read together.
A small group set the boundaries
With the top 10 assignees accounting for 79.2% of all 106 records in scope, most of the foundational claim space around macrocycle permeability chemistry is already staked out. New entrants are more likely to find room in method-of-use, formulation or assay claims than in core molecule composition.
Filing pace has cooled from its 2023 peak
Activity rose to a peak of 8 filings in 2023 after several thin years, then fell sharply through 2024. Because publication lags filing by roughly 18 months, the apparent drop in 2025-2026 data should be read cautiously rather than as evidence the field has gone quiet.
Medicinal-preparation claims dominate
Four in five records touch A61K, and peptide chemistry (C07K) and heterocyclics (C07D) are the next-heaviest classes. Measurement and testing classes remain comparatively open, which matters for filers building assay-correlation or permeability-prediction tools rather than new molecules.
Eureka can read the same corpus for gaps instead of for coverage: under-claimed branches adjacent to cell permeability of macrocycles, with the prior art for and against each one.
Who holds the claims, and where the gaps sit
The ranked assignee list covers 52 companies and institutions across the 106 records in scope — a mix of universities, research institutes and pharmaceutical filers, with activity heavily weighted toward a handful of leaders.
One filer sits well ahead of the field
The leading assignee holds 27 of the 106 records in scope, more than three times the fifth-place count of 7. That gap is unusual for a field this size and signals a filer who has built a sustained, multi-year programme rather than a single flagship patent family.
Most filers appear once or twice
Below the top 10, filing counts drop quickly toward single-digit and single-record entries. That long tail is typical of an academically-seeded field where individual labs file once around a discovery rather than building a portfolio.
Collaboration is limited but concentrated
Only 10 co-assignee pairs appear across the dataset, and the strongest pairing recurs across multiple records — a university and an affiliated virology-focused filer working jointly. Most other assignees file independently.
| Assignee | Recent year | YoY |
|---|---|---|
| Nastech Pharmaceutical | 0 | — |
| Cornell University | 0 | — |
| SODERSTROM KARL PETTER | 0 | — |
| The Chancellor, Masters and Scholars of the University of Oxford | 0 | — |
| University of Kansas | 0 | — |
| Unither Virology | 0 | — |
| The Regents of the University of California | 0 | — |
| Chugai Seiyaku Kabushiki Kaisha | 0 | — |
Where to take this analysis
The dataset points to a field with concentrated core claims and thinner activity on the measurement and prediction side.
Map freedom-to-operate against the top 10
With 79.2% of records held by 10 assignees, any new molecule or formulation claim should be checked against that group's portfolios before drafting.
Explore assignee portfolios in EurekaProbe the assay-correlation white space
C12Q and G01N each cover under 10% of the 106 records, well below the molecule-side classes — a candidate area for permeability-prediction or assay-standardisation claims.
Run a white-space search in EurekaCommon questions on macrocycle permeability patents
In this dataset, it is a filing that claims a macrocyclic or peptidic compound, formulation or design method where cell membrane permeability is the demonstrated inventive step, evidenced through metrics such as polar surface area, efflux ratio or passive diffusion assays. The search deliberately combines mechanism terms like intramolecular hydrogen bonding and conformational shielding with these measurement terms, so records where permeability is incidental rather than claimed are excluded. This keeps the corpus focused on molecules and methods purpose-built to cross membranes without active transport.
The ranking covers 52 assignees across 106 records, and it is top-heavy: the leading assignee alone holds 27 records, well ahead of the fifth-place holder at 7 and tenth place at 4. The top 5 assignees combined account for 55.7% of all records in scope, and the top 10 account for 79.2%. Most other filers in the ranking appear with only a handful of records each, typical of a field seeded largely by academic and research-institute filings.
Filings peaked at 8 in 2023 after several thin years, then fell to 1 by 2024 — an 83% decline over the 2021-to-2024 span. That said, publication typically lags actual filing by around 18 months, so the 2025 and 2026 figures in any such dataset are still filling in and should not yet be read as a continued slowdown. The more reliable read is that 2023 marked a filing peak and 2024 shows a genuine pullback from it.
Measurement and testing classes are comparatively thin: C12Q (enzyme and DNA-based testing) and G01N (material analysis and testing) each cover under 10% of the 106 records, versus 80.2% for medicinal preparations (A61K) and 35.8% for peptide chemistry (C07K). That gap suggests permeability-prediction algorithms, efflux-ratio measurement standardisation and assay-correlation methods are less densely claimed than the underlying molecules and formulations themselves, making them a plausible area to explore for new filings.
It is concentrated: the top 5 assignees hold 55.7% of the 106 records in scope, and the top 10 hold 79.2%. For a new entrant, that means core molecule and formulation composition claims around macrocycle permeability chemistry are largely occupied by a small group of long-standing filers. Freedom-to-operate work should prioritise checking those portfolios directly, while filing strategy may find more open ground in the thinner assay and prediction-method classes rather than in core compound claims.
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Disclaimer. This page is generated from Patsnap Eureka data drawn from a limited snapshot of global patent and scientific-literature records, and is provided for general information and reference only.
Patent data carries inherent limitations: recent filings (typically the most recent 18–24 months) are under-counted due to standard publication lag; counts may be reported at either a patent-family or a patent-record basis and are not always directly comparable; classification, applicant-name, and citation data may contain errors, duplicates, or omissions; and the underlying search query defines and constrains the scope shown. As a result, the analysis may be incomplete or inaccurate and may not reflect the full technology landscape.
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Machine translation. Assignee and organisation names originally recorded in Chinese, Japanese or Korean have been rendered into English by an AI translation step so that the tables stay readable. These renderings are best-effort and may not match a company’s registered English name; the original name is what the underlying patent record carries, and it is what any Eureka query launched from this page uses.