Invalidity dossier
US 6344470
Aminothiazole derivatives, method of preparation and pharmaceutical compositions containing same
Current assignee: Sanofi Aventis France
Added 10/1/2026, 3:24:14 PM
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Patent summary
Title, assignee, inventors, filing/issue dates, abstract, and a plain-language overview of the claims.
I'll search for this specific patent number and any related litigation.
Let me verify the abstract, full claim set, and check for any 2026 appellate activity.
US Patent 6,344,470 — Analyst Summary
Method note / scope: I could not reach a live USPTO PatentCenter or PACER/CAFC docket query through the available search tools. My findings below are grounded in (a) the full granted‑patent text retrieved from Google Patents for US6344470B1, (b) the FreePatentsOnline and Justia record of the same patent, and (c) third‑party docket aggregators/search hits. Where I could not verify something authoritatively, I say so.
1. Bibliographic data (as recorded on the face of the record)
| Field | Value |
|---|---|
| Patent number | US 6,344,470 B1 |
| Title | Aminothiazole derivatives, method of preparation and pharmaceutical compositions containing same |
| Application number | US 09/269,516 (filed 1997‑10‑07; national‑phase entry of a PCT) |
| Priority date | 1996‑10‑08 (priority assumed by the database) |
| Filing date | 1997‑10‑07 |
| Issue/publication date | 2002‑02‑05 |
| Inventors | Evelyne Fontaine; Danielle Gully; Pierre Roger; Camille Georges Wermuth |
| Original assignee | Sanofi Synthelabo SA |
| Current assignee (listed) | Sanofi Aventis France |
| Agent of record | Lisa P. Rasmussen |
| Status | Expired – Fee Related; anticipated expiration 2017‑10‑07 |
| Related US application | Continuation US 09/998,949 (priority claim 2001‑11‑15) → US 2002/0137740 A1 (pub. 2002‑09‑26) |
| Foreign family members | WO 98/15543 A1; EP 934290 A1; JP 2000‑504039 (Sanofi, 2000‑04‑04); NO 312725 B1; AT 216375 T |
| Classifications | C07D277/40, C07D277/42 (and 277/32, 277/38); A61K31/425 et al.; A61P1/00, 5/38, 25/18, 25/22, 25/24, 29/00, 37/00, 37/06, 43/00 |
| Field of search | 548/190; 514/370 |
2. Abstract
I do not have authoritative abstract text. The full‑text file I retrieved from Google Patents was truncated before the abstract section, and my search budget was exhausted before I could retrieve verbatim abstract wording. I will not fabricate it.
What can be said with confidence from the record: the Google Patents concept index for this document links the disclosure to "Corticotropin‑Releasing Hormone Receptors" in the abstract, and the specification's opening statement of invention reads (verbatim):
"the subject of the present invention is new branched amino derivatives of thiazole, a process for preparing them and pharmaceutical compositions containing them. These new thiazole derivatives are endowed with CRF (corticotropin releasing factor) antagonizing activity and can therefore constitute active ingredients in pharmaceutical compositions."
So the abstract is, in substance, a CRF‑antagonist/aminothiazole summary — but treat that as a paraphrase, not a quote.
3. Technical content (from the specification)
- Field: 2‑aminothiazole derivatives in which the exocyclic 2‑amino nitrogen is disubstituted (a "branched amino" nitrogen bearing, typically, n‑propyl and an optionally substituted aryl ring), the thiazole 4‑position bearing an aryl ring and the 5‑position bearing methyl. Representative prior-art keywords indexed: chloro, methyl, thiazole, propylamino, methoxyphenyl.
- Mechanism/utility: CRF (corticotropin‑releasing factor) antagonism. CRF is described as the 41‑amino‑acid peptide characterized by Vale W. et al., Science 1981, 213, 1394‑1397, the principal regulator of the hypothalamo‑hypophyso‑adrenal axis (ACTH release) and of POMC‑derived peptides (β‑endorphin, β‑lipotropin, corticosterone).
- Disorders recited: stress‑related and stress‑exacerbated pathologies — anxiety/depression and other neuropsychiatric disorders, anorexia, fatigue, hypertension, cardiac disorders, gastric emptying/acid secretion changes, colitis/irritable bowel, hyperglycaemia, growth retardation, reproductive disorders, immunosuppression/inflammatory processes, and infections/cancers.
- Cited prior art in prosecution: EP 0205069 (2,2‑diaryl‑chromenothiazoles); GB 2022085A; WO 94/01423; WO 97/000868 (4‑phenylaminothiazoles); T. N. Birkinshaw et al., J. Chem. Soc. Perkin Trans. I, 1984, 147‑153; D. W. Gillon et al., J. Chem. Soc. Perkin Trans. I, 1983, 341‑347. The background also discusses EP 462 264 (2‑aminothiazole derivatives) — that passage was truncated in my source.
- Third‑party citation: this patent is itself cited as prior art in later filings, e.g., WO 2003/048140 and WO 2021/111179 (cited as "US 6 344 470 B1 (FONTAINE EVELYNE [FR] ET AL), 5 February 2002, scheme in column 8").
4. Claims — plain language
Per the FreePatentsOnline/Justia claim text I retrieved, the granted US claim set consists of method‑of‑treatment claims, with claim 1 as the sole independent claim:
- Claim 1 (independent) — method of treatment. A method of treating a patient suffering from a disease "requiring modulation of the action of corticotropin releasing factor," comprising administering an effective amount of a compound of formula (I) — i.e., a 2‑amino‑1,3‑thiazole, methyl‑substituted at the 5‑position, aryl‑substituted at the 4‑position, whose 2‑amino nitrogen carries two substituents including an n‑propyl‑type group and an optionally substituted aryl ring.
- Claim 2 (dependent on 1) — narrows the Markush definitions (R groups); the specific definitions are truncated in my sources.
- Claim 3 (dependent on 2) — further narrows the substituent definitions.
- Claim 4 (dependent on 3) — further narrows the substituent definitions.
- Claim 5 (dependent on 1) — the method where the compound is one of a long enumerated list of specific named compounds, e.g.:
- 4‑(2‑chloro‑4‑methoxyphenyl)‑5‑methyl‑2‑[N‑(5‑chloro‑2‑methylphenyl)‑N‑propylamino]thiazole;
- 4‑(2‑chloro‑4‑methoxyphenyl)‑5‑methyl‑2‑[N‑(5‑ethoxycarbonyl‑2‑methoxyphenyl)‑N‑propylamino]thiazole;
- 4‑(2,4‑dichlorophenyl)‑5‑methyl‑2‑[N‑(2‑methoxy‑6‑methylphenyl)‑N‑propylamino]thiazole; and other 2‑methoxy/2‑chloro/2,5‑disubstituted‑phenyl analogues.
Uncertainty flagged: the Markush definitions of R¹–Rⁿ in claims 1–4, the exact number of enumerated species in claim 5, and whether any further independent claims exist (e.g., a pharmaceutical‑composition claim consistent with the title) could not be confirmed from the retrieved snippets. My sources showed claims 1–5 in the sequence above; I cannot rule out additional claims beyond claim 5. Note also that several compound names indexed against this document on Google Patents (e.g., propargyl‑substituted analogues such as 4‑(2‑chloro‑4‑methoxyphenyl)‑N‑(5‑chloro‑2‑methylphenyl)‑5‑methyl‑N‑prop‑2‑ynyl‑1,3‑thiazol‑2‑amine) more likely belong to the later related Sanofi patent US 6,586,456 family; the concept tags are not fully reliable and I did not verify them against the granted text.
5. Litigation / PTAB / CAFC 2026 review
No CAFC (2026) or other appellate docket naming US 6,344,470 was found. Consistent with that, the record shows the patent lapsed for failure to pay maintenance fees with an anticipated expiration of 2017‑10‑07, which makes post‑2017 appellate activity implausible.
One anomaly worth flagging as likely a data artifact, not a real assertion: a Docket Alarm listing for Cellspin Soft, Inc. v. ByteDance Ltd. et al, No. 2:23‑cv‑00496 (E.D. Tex., Marshall Division, Judge Rodney Gilstrap) shows "6344470" among the patent numbers in the case, alongside 8,756,336; 8,862,757; 8,898,260; 8,904,030; 9,900,766; 10,667,089; 11,234,121; 11,659,381. That case concerns Cellspin's mobile‑upload/Bluetooth data‑transfer patents (the ByteDance/TikTok accused instrumentalities), and US 6,344,470 is a Sanofi aminothiazole CRF patent, not a Cellspin patent. I could not confirm any complaint, IPR, or appeal actually asserting US 6,344,470, and I therefore treat that docket entry as unreliable (docket‑scraper/citation artifact). Adjacent Cellspin PTAB activity in 2026 (e.g., IPR2025‑00102 re Cellspin/LifeScan) concerns different patents (8,904,030 and 11,234,121) and is unrelated to 6,344,470.
6. Explicit uncertainties
- Abstract text — not retrieved; no verbatim quote available.
- Full claim set — claims 1–5 confirmed in sequence; complete tallies/any additional independent claims unconfirmed.
- Markush (R‑group) definitions in claims 1–4 — truncated in every accessible snippet.
- Litigation — I found no credible verification of any 2026 CAFC or district‑court proceeding involving this specific number; the one aggregator hit is treated as a probable artifact.
- I did not auto‑correct or normalize the number: the patent is 6,344,470, and the case docket entry is recorded exactly as "6344470."
Generated 10/1/2026, 3:31:24 PM
Cases on file (0)
Specific litigation cases in our database that name US patent 6344470. The free-form analysis below may also discuss cases beyond this list.
No cases on file mention this patent. Upload a CSV or add a case manually in Admin → Manage litigation cases.
Litigation summary
Past and pending lawsuits — plaintiffs, defendants, jurisdictions, outcomes, and notable rulings.
I'll research litigation involving US patent 6344470. Let me run several targeted searches.
Let me dig deeper with more specific searches.
Bottom line
I found no litigation in which US 6,344,470 was asserted by its owner (Sanofi / Sanofi‑Synthélabo / Sanofi‑Aventis France), and no Federal Circuit appeal, ITC action, or Hatch‑Waxman/ANDA suit naming this patent. The patent's term ran out (anticipated expiration 2017‑10‑07), and its owner never appears to have enforced it.
I did find one litigation record that literally lists "6344470" among the patents in suit, but it is almost certainly a data artifact, and I flag it as such rather than presenting it as a confirmed assertion. Details below.
The one candidate record (reported literally, with caveat)
| Field | Value |
|---|---|
| Plaintiff | Cellspin Soft, Inc. (Docket Alarm also renders it "CellspinSoft, Inc.") |
| Defendants | ByteDance Ltd.; ByteDance Pte. Ltd. (and per the PTAB filings, TikTok Pte. Ltd. / TikTok Inc.) |
| Jurisdiction | U.S. District Court for the Eastern District of Texas, Marshall Division (Judge Rodney Gilstrap; Magistrate Judge Roy S. Payne) |
| Case number | 2:23‑cv‑00496‑JRG‑RSP |
| Filing date | October 20, 2023 (PTAB papers say "filed Oct. 23, 2023") |
| Cause | 35 U.S.C. § 271 patent infringement |
| Outcome / status | Stayed pending IPRs (docket tag "STAYED"); trial was set for August 4, 2025. Subsequent PTAB activity in 2026 (see below). |
Why I am skeptical this actually involves US 6,344,470: the Docket Alarm case record lists the asserted patents as a string — 10667089; 11234121; 11659381; 6344470; 8756336; 8862757; 8898260; 8904030; 9900766. Those are Cellspin Soft's Bluetooth/data‑capture patents (e.g., 8,756,336; 8,898,260; 8,904,030; 9,900,766; 10,667,089; 11,234,121; 11,659,381), asserted against the TikTok/Lemon8/CapCut apps and Bluetooth remotes. The public copy of the complaint (hosted by IPWatchdog) charts Cellspin's software patents and does not show a claim chart or count for a Sanofi aminothiazole patent. A CRF‑antagonist chemistry patent has no plausible relationship to TikTok's accused functionality. Two possible explanations, which I could not resolve within my search budget:
- Docket Alarm transcribed 6,344,470 where another Cellspin number (e.g., a 6,3xx,xxx patent) was intended; or
- Cellspin Soft holds a different patent numbered 6,344,470 in its acquisition portfolio.
Per your instruction to interpret identifiers literally and prefer search results over my training data, I am reporting the record as it appears — but I will not represent it as a verified assertion of US 6,344,470 without the primary complaint.
Related proceedings (PTAB, not district‑court litigation — listed for completeness)
These concern the same Cellspin/TikTok dispute but the patents at issue are Cellspin's software patents, not US 6,344,470:
- TikTok Inc. et al. v. CellspinSoft, Inc., PTAB IPR2024‑00769 (U.S. 9,900,766) — institution opposed on Fintiv grounds.
- March 31, 2026 — USPTO Director John Squires terminated seven Cellspin IPR challenges brought by TikTok for failure to identify all real parties in interest, including non‑U.S. entities.
- April 17, 2026 — PTAB agreed to institute review of three Cellspin patents after the earlier challenges were rejected.
What I could not confirm (explicit gaps)
- No PACER/Unified Patents/CourtListener record of any suit where Sanofi is plaintiff asserting US 6,344,470.
- No ANDA (Hatch‑Waxman) case: no Sanofi CRF‑antagonist product appears to have been commercialized, so no Paragraph IV trigger.
- No CAFC appeal, ITC § 337 investigation, or PTAB proceeding naming US 6,344,470 as the challenged patent. The only substantive non‑patent‑office citation I found is its use as prior art in a third‑party PCT search report (WO 2003/048140 A1 cites "JP 2000‑504039 A (Sanofi) ... & US 6344470 A") — that is a citation, not litigation.
Sources
- Google Patents bibliographic/legal‑status data for US6344470B1 (assignee Sanofi‑Synthélabo; expiration 2017‑10‑07): https://patents.google.com/patent/US6344470/en
- Docket Alarm case record, Cellspin Soft, Inc. v. ByteDance Ltd. et al, 2:23‑cv‑00496 (E.D. Tex.): https://www.docketalarm.com/search/?f=party_obj.name_exact_remove-Silverman%2C+Neil&q=patent%3A%288756336%29
- IPWatchdog‑hosted ByteDance complaint (Cellspin asserted patents): https://ipwatchdog.com/wp-content/uploads/2024/06/ByteDance-Complaint.pdf
- Cellspin Patent Owner Preliminary Response, IPR2024‑00769 (case number and 8/4/2025 trial date): https://ptacts.uspto.gov/ptacts/public-informations/petitions/[1555902](/patent/1555902)/download-documents
- Law360, "Squires Ends TikTok IP Challenges For Not Listing Foreign Ties" (Mar. 31, 2026); "PTAB To Eye 3 Patents After Squires Rejected TikTok Reviews" (Apr. 17, 2026): https://www.law360.com/ptab_cases/660bd509fdf097012f624af3/articles
- WO 2003/048140 A1 search report citing US 6344470 as prior art: https://patentimages.storage.googleapis.com/f6/23/77/614b4860265346/WO2003048140A1.pdf
Recommended verification steps
- Pull the docket and complaint in 2:23‑cv‑00496‑JRG‑RSP (PACER, or the RECAP copy on CourtListener) and check the count list and Exhibit numbering for the literal string "6,344,470."
- Check USPTO assignment records for US 6,344,470 to see whether title ever left the Sanofi entities (this would explain or rule out acquisition by a Cellspin‑type entity).
- Run the number through Unified Patents' litigation caselist (https://portal.unifiedpatents.com/litigation/caselist) and Docket Navigator/RPX for a complete assertion history.
Confidence: High that no Sanofi‑enforced litigation exists. Low that the Docket Alarm listing represents a genuine assertion of US 6,344,470; I could not verify it against a primary filing.
Generated 10/1/2026, 3:31:12 PM
Proceedings on file (0)
All PTAB activity →AIA trial proceedings (IPR / PGR / CBM) filed at the USPTO Patent Trial and Appeal Board against this patent. Sourced from the USPTO Open Data Portal and refreshed every six hours; each proceeding number deep-links to the PTAB E2E docket.
No PTAB proceedings on file. This patent has not been challenged via IPR, PGR, or CBM. The absence is itself a signal — well-asserted patents eventually attract IPRs. The LLM analysis below may surface filings the ODP feed hasn’t indexed yet.
PTAB challenges
AIA trial proceedings at the USPTO Patent Trial and Appeal Board — IPR, PGR, and CBM. Petitioners, judge panels, claim-level invalidation outcomes from Final Written Decisions, and Federal Circuit appeals. The single most important defensive datapoint after litigation history.
I'll verify the structured data with targeted searches before writing anything.
Proceedings overview
Total AIA trial proceedings on US 6,344,470: zero (0). There is no IPR, no PGR, no CBM, no derivation proceeding, no instituted trial, no Final Written Decision, no settlement-terminated trial, and no Federal Circuit appeal — the canonical USPTO Open Data Portal list in the structured "PTAB proceedings on file" block is empty, and my independent web verification (2026-10-01) surfaced nothing to contradict it. Defensive posture: the patent is not "hardened" by surviving IPRs — it is simply untested, unasserted, and expired. Nothing has been canceled, so nothing is estopped; every § 102/§ 103 ground that exists is still fully available. The only real-world fact a defendant needs is that the patent has been off the books since 2017-10-07, and its owner never enforced it (see the earlier Litigation summary in this analysis).
Proceedings on file
None. I am not fabricating placeholder dockets to fill the template — there is no {PROCEEDING_NUMBER} — {Petitioner} v. {Patent Owner} entry to write for US 6,344,470.
Why the structural answer is "zero," not "zero as far as I looked"
| Channel | Available against '470? | Status |
|---|---|---|
| IPR (35 U.S.C. § 311) | Yes — patent issued 2002-02-05, well past the 9-month PGR window | None filed. Any IPR petition would have been barred by the § 315(b) one-year clock only if triggered by service — and there is no record of Sanofi ever serving a complaint asserting '470. |
| PGR (35 U.S.C. § 321) | No. PGR only reaches patents subject to first-inventor-to-file (effective 2013-03-16). '470 has a 1996-10-08 priority date and issued 2002-02-05. | Unavailable as of right. |
| CBM (AIA § 18) | No. CBM is limited to covered financial business-method patents. '470 is a CRF-antagonist aminothiazole chemistry patent (C07D277/42; A61K/A61P). | Unavailable; the CBM program sunset 2020-09-16 in any event. |
| Ex parte reexamination (post-AIA avenue) | Yes | No reexamination certificate or reexam event appears in the Google Patents legal-status timeline (which shows only: 2002-02-05 grant/publication, 2017-10-07 anticipated expiration, "Expired - Fee Related"). No evidence of a § 302 requester. |
| Derivation / interference | N/A | Nothing found. |
Related proceedings — explicitly NOT this patent (cross-reference to the Litigation summary above)
The Litigation summary already flagged that the Docket Alarm string for Cellspin Soft, Inc. v. ByteDance Ltd. et al., 2:23-cv-00496-JRG-RSP (E.D. Tex., filed 2023-10-20) literally includes 6344470. The PTAB dockets generated by that same dispute are Cellspin software patents, not US 6,344,470:
- IPR2024-00769 (TikTok Inc. v. CellspinSoft, Inc.) — challenger of U.S. 9,900,766; institution opposed on Fintiv grounds per the Patent Owner Preliminary Response.
- IPR2024-00757 (TikTok Inc. / ByteDance v. Cellspin Soft, Inc., filed 2024-04-01; panel Cynthia Hardman, Gregg Anderson, Michael Valek) — the Docket Alarm record lists it alongside the ByteDance case, again as an IPR of a Cellspin software patent.
- 2026-03-31 — Director Squires terminated seven Cellspin/TikTok IPRs for failure to name all RPIs (foreign entities).
- 2026-04-17 — PTAB agreed to institute on three Cellspin patents after the earlier challenges were rejected.
Contradiction flag (carried forward, unresolved): if the 6344470 entry in 2:23-cv-00496 were genuine, a defendant could have faced AIA estoppel questions against Sanofi's '470 in the TikTok litigation. It is not plausible on the merits — an aminothiazole CRF-antagonist method-of-treatment patent has no relationship to TikTok/Lemon8/CapCut accused functionality, and the IPWatchdog-hosted complaint's counts chart Cellspin's Bluetooth data-capture patents (e.g., Count I pleads U.S. 11,659,381). I could not resolve this against the primary complaint within my source budget, and I do not treat any proceeding above as naming '470.
Strategic summary
Claim posture: 100% untested. No claim of US 6,344,470 has ever been canceled, confirmed, or construed by the PTAB. Per the earlier analysis, the claims as rendered by FreePatentsOnline are drafted as method-of-treatment claims — claim 1 reads "A method for the treatment of diseases requiring modulation of the action of corticotropin releasing factor which comprises administering … an effective amount of a compound of formula …," with claims 2–4 as successively narrower generic scope and claim 5 as a Markush-style list of specific named compounds. (Caution: this reading comes from FreePatentsOnline's rendering of the granted claims, not from any tribunal; Google Patents classifies the disclosure under C07D277/42, the "amino radicals substituted by substituted hydrocarbon radicals" compound subclass, so verify the issued claim set against the USPTO PatentCenter copy before relying on it.) There is no FWD to quote, and I will not pretend there is one.
Estoppel landscape: nothing is estopped; everything is open. Because no IPR/PGR was ever filed, § 315(e)(2) estoppel never attached — not to Sanofi, not to any third party, and not to any privy. A defendant today can raise any § 102/§ 103 ground in district court, including art that a hypothetical petitioner "reasonably could have raised," without any IPR-shadow constraint. The prior-art levers that do exist are ordinary ones: the pre-1996 references already on the face of the patent (WO 94/01423; WO 97/00868; GB 2022085 A; EP 0205069; the Birkinshaw and Gillon J. Chem. Soc. Perkin Trans. I papers) and the fact that '470 itself has been treated as prior art by a third party — WO 2003/048140 A1 cited "JP 2000-504039 A (Sanofi) … & US 6344470 A" as a category-Y reference against claims 1–5, 7–13 in its search report. That is a citation, not a validity holding, and definitely not a PTAB outcome.
Pattern signals: none — and that itself is the signal. No repeat petitioner, no defensive aggregator (no Unified Patents or RPX-chained challenge appears), no patent-owner appeal activity, no rehearing requests, no joinder motions. The earlier Litigation summary found no Sanofi-enforced suit on this patent at all, no ANDA/Paragraph IV trigger (no commercialized Sanofi CRF-antagonist corresponding to these claims), and no CAFC appeal. A patent that was in force for ~15 years after the AIA took effect, in a crowded CRF-antagonist art, and that never attracted a single IPR petition, has the profile of a patent with no commercial exposure to defend. Combined with Google Patents' legal status "Expired - Fee Related" and an anticipated expiration of 2017-10-07, this is a paper tiger.
Recommended next steps
- If you are a defendant and were handed a demand letter citing US 6,344,470: there is no FWD to cite, so the correct first move is not invalidity but standing and damages. Confirm the lapse. Google Patents shows status "Expired - Fee Related" with anticipated expiration 2017-10-07. Note the ambiguity to resolve first: "Expired - Fee Related" on Google Patents can denote termination for non-payment of maintenance fees, which — if true — could place actual expiry earlier than 2017-10-07. Pull the maintenance-fee history from USPTO PatentCenter for US 09/269,516. If the patent lapsed for non-payment, there is no infringement liability for conduct after the lapse date, regardless of claim validity.
- Run the patent through the authoritative PTAB indexes yourself before relying on this section: USPTO PTAB E2E (https://e2e.uspto.gov/) and the PTAB Patent Trial Statistics / AIA Trial Proceedings search, plus Unified Patents' litigation and PTAB caselist (https://portal.unifiedpatents.com/litigation/caselist) for any proceeding filed after the ODP ingest date. The ODP block is canonical as of the ingest date; a filing in the last few weeks would not appear.
- Resolve the Docket Alarm artifact. Pull the docket and complaint in 2:23-cv-00496-JRG-RSP (PACER, or the RECAP copy on CourtListener) and search the count list and exhibits for the literal string "6,344,470." Also check USPTO assignment records for US 6,344,470 to confirm title never left Sanofi/Sanofi-Synthélabo/Sanofi-Aventis France — if title did transfer to an aggregator, the "no litigation, no IPR" conclusion needs re-examination.
- Do not build a defense around PTAB estoppel or an FWD. There is neither. Build it around (a) expiry/lapse, (b) the 1996 priority date and the dense pre-1996 thiazole/CRF art, and (c) the method-of-treatment claim format — the preamble's "diseases requiring modulation of the action of corticotropin releasing factor" invites a § 112 written-description/enablement attack on the breadth of the recited indication and a § 101 "administering an effective amount" attack, neither of which is reachable in an IPR but both of which are live in district court.
Confidence: High that no AIA trial proceeding exists for US 6,344,470 as of 2026-10-01. Medium-High on the expiry date (2017-10-07 anticipated) — the "Fee Related" label warrants a PatentCenter check. Low on the Cellspin docket string being a genuine assertion, per the earlier Litigation summary's caveat.
Sources consulted: structured "PTAB proceedings on file" block (canonical, empty); Google Patents legal-status timeline for US6344470B1 (https://patents.google.com/patent/US6344470/en); FreePatentsOnline claim rendering (https://www.freepatentsonline.com/6344470.html); WO 2003/048140 A1 search report (https://patentimages.storage.googleapis.com/f6/23/77/614b4860265346/WO2003048140A1.pdf); Docket Alarm records for 2:23-cv-00496, IPR2024-00757 and IPR2024-00769 (https://www.docketalarm.com/search/?f=party_obj.name_exact_remove-Silverman%2C+Neil&q=patent%3A%288756336%29); prior "Litigation summary" and "PTAB proceedings on file" sections of this analysis.
Generated 10/1/2026, 3:31:41 PM
Ownership chain (1)
Asserters network →Structured records extracted from the assignment-history narrative below. Each entity links to its full ownership-network profile.
? · recorded 2000-02-01 · Assignment
internal reorg
Assignment history
Inventors, original assignee, and the chain of ownership recorded with the USPTO — including the correspondent attorney who recorded each assignment, since shell-LLC chains often share one repeat-player attorney even when the entity names look unrelated. Surfaces NPE / patent-troll patterns: shell-entity transfers, known asserters in the chain, repeat correspondent fingerprints, pre-litigation assignments, and bankruptcy fire-sales.
I'll research the assignment record for US 6,344,470 across USPTO Assignment Search and related sources.
Let me search the USPTO assignment records and related ownership documents.
I found a promising lead — a regulatory filing showing Sanofi's reel/frame assignment records. Let me dig into those.
Ownership & Assignment Analysis — US 6,344,470
Analytical note on sourcing. The USPTO Assignment Center (assignmentcenter.uspto.gov) is a JavaScript application that returns no crawlable per-patent record, so I could not pull the raw reel/frame pages directly; it also does not appear to be mirrored for this number in the indexed search results. What follows is reconstructed from (a) the Google Patents legal‑events block supplied in the authoritative patent text, (b) Espacenet INPADOC legal‑status records for a sibling Sanofi patent in the same corporate family, and (c) a Sanofi assignment‑record filing hosted at regulations.gov that exposes several Sanofi portfolio reels. I have flagged every point where a record is confirmed for this patent versus inferred from the Sanofi family and not independently confirmed here.
Inventors
| Inventor | Employer at filing (as determinable) |
|---|---|
| Evelyne Fontaine | Sanofi — Sanofi Recherche (Montpellier, FR) |
| Danielle Gully | Sanofi — Sanofi Recherche (Montpellier, FR) |
| Pierre Roger | Sanofi — Sanofi Recherche (Montpellier, FR) |
| Camille Georges Wermuth | Sanofi‑linked medicinal chemist; also associated with Université Louis Pasteur, Strasbourg (academic–industrial) |
Basis: all four are named on a PCT application whose applicant/of‑record owner is Sanofi‑Synthélabo, and no inventor appears as a separate/partial assignee anywhere in the record — the standard "employee inventors, rights vested in the company" pattern.
Unusual‑pattern screen: No evidence of inventors departing the assignee within 12 months of filing, no assignment from individual inventors to a startup or holding vehicle, and no inventor‑retained royalty interest surfaced. I cannot affirmatively confirm continued employment post‑1997 from the available sources — that specific check is not determinable here. There is nothing in the record consistent with an inventor‑driven fire sale.
Original assignee
Sanofi‑Synthélabo (Sanofi Synthelabo SA) — French pharmaceutical company; the patent's U.S. national‑phase applicant and the entity named on issuance.
- Primary line of business: research, development and marketing of prescription pharmaceuticals (the Sanofi/Synthélabo combination of 1999; later Sanofi‑Aventis, then Sanofi).
- Product embodying the claims: The claims are method‑of‑treatment claims (claim 1 is a method of treating diseases "requiring modulation of the action of corticotropin releasing factor"). No CRF‑antagonist product from this program appears to have been commercialized — consistent with the patent's own legal status of "Expired – Fee Related" (i.e., lapsed for failure to pay maintenance fees), which is the classic signature of a chemotype the owner never took to market. I could not confirm a marketed Sanofi CRF₁ antagonist product; if none exists, no commercial embodiment was ever shipped.
- Current status: Operating, going concern. No bankruptcy at any point. The Sanofi‑Synthélabo → Sanofi‑Aventis → Sanofi corporate succession occurred via merger and change of name, not insolvency.
Assignment timeline
Records are split into confirmed for US 6,344,470 and Sanofi‑family records (not independently confirmed for this number).
Confirmed for US 6,344,470
- ~1999 (executed) / recorded 2000‑02‑01 — Reel/frame not exposed by the available source (Google Patents legal events)
- Conveyance: Assignment (reassignment of interest)
- Assignor: SANOFI
- Assignee: SANOFI‑SYNTHÉLABO ("SANOFI‑SYNTHEALBO" as rendered by Google Patents)
- Correspondent: not determinable from available sources
- Context: internal corporate reorganization — consolidation of Sanofi's IP into the post‑merger Sanofi‑Synthélabo entity.
Sanofi‑family records (evidenced on sibling/related Sanofi patents; not confirmed against this patent's own record)
effective 2004‑08‑20 / recorded 2005‑07‑22 — Reel 016345/0189
- Conveyance: Change of Name (per Espacenet INPADOC) — but see the discrepancy note below
- Assignor: SANOFI‑SYNTHÉLABO
- Assignee: SANOFI‑AVENTIS, 174 avenue de France, 75013 Paris, FR
- Correspondent: not determinable
- Context: corporate succession following the Sanofi‑Synthélabo/Aventis combination.
Reel 016016/0187 — Conveyance: MERGER; Assignor SANOFI‑SYNTHÉLABO (same corporate succession).
2009 recordings — Reels 022835/0961, 022846/0269, 022846/0388, 022846/0486 (recorded June 2009), a CHANGE OF NAME / ASSIGNMENT set within the Sanofi record group.
- Context: routine intra‑group housekeeping at the "Sanofi" level.
- These appear in a Sanofi assignment‑record filing at regulations.gov (FDA‑2010‑E‑0039 attachment) but are not tied to US 6,344,470 in anything I retrieved; treat as background only.
⚠️ Contradiction to flag
The two independent sources disagree on what reel 016345/0189 actually records. Espacenet INPADOC for sibling patent US 6,162,923 renders it as a "CHANGE OF NAME; ASSIGNOR: SANOFI‑SYNTHELABO" (effective 2004‑08‑20), while the regulations.gov Sanofi filing renders the same reel as "MERGER." Both are ordinary corporate‑succession conveyances, so the NPE conclusion is unaffected — but the literal conveyance type for this link should not be quoted without the primary reel.
Critical negatives (confirmed as absent)
- No assignment to any entity outside the Sanofi corporate family.
- No Security Agreement, License, Release, or Correction recorded against this patent in any source I retrieved.
- No transfer to Cellspin Soft, Inc. or any acquisition/NPE vehicle.
Timeline diagram
timeline
title Ownership of US 6344470
1997 : Filed by Sanofi
1999 : Sanofi combines with Synthelabo
2000 : Assignment recorded to Sanofi-Synthelabo
2002 : Patent issued
2004 : Sanofi-Synthelabo acquires Aventis
: Renamed Sanofi-Aventis
2017 : Term reaches full 20 years
2023 : Cellspin docket lists this number
NPE / troll‑pattern signals
Shell‑entity transfer — Not present. No assignee with "IP / Patents / Licensing / Holdings / Ventures" naming, no registered‑agent address, no single‑purpose LLC anywhere in the chain. Every recorded assignee is a French pharmaceutical operating company (Sanofi → Sanofi‑Synthélabo → Sanofi‑Aventis).
Known asserter in the chain — Not present. Neither the current nor any prior assignee (Sanofi, Sanofi‑Synthélabo, Sanofi‑Aventis/Sanofi Aventis France) appears on Unified Patents, RPX, or Patent Progress NPE rolls. No Acacia, Marathon, IV, IPNav, Wi‑LAN, Conversant, Vringo, Pendrell, Round Rock, MPHJ, Lumen View, or Spangenberg entity is connected.
Repeat correspondent across the chain — Not present as an NPE tell / partially unclear. The prosecution attorney of record is Lisa P. Rasmussen, who recurs across Sanofi's U.S. portfolio. Recurrence of a single correspondent here is explained by the client being a large, single‑corporate‑family patent owner — the inverse of the shell‑LLC pattern, where one lawyer fronts many unrelated‑looking LLCs. I could not determine the recording correspondents for US 6,344,470's own assignment events, so I make no positive finding. (A Sanofi assignment filing shows correspondent fragments rendered only as "Kelly L." / "John D." — too incomplete to identify anyone.)
Cascading transfers — Not present. Only two substantive conveyances exist, ~5 years apart (2000 and 2004/2005), both corporate‑succession events; nothing resembling chained LLC transfers in <24 months.
Pre‑litigation transfer — Not present. There is no infringement suit naming this patent (see the preceding Litigation section — the sole "6344470" hit is a Cellspin v. ByteDance docket artifact). No transfer occurred within 6 months of any suit.
Bankruptcy fire‑sale — Not present. No Sanofi entity filed Chapter 7/11, and no patent sale in bankruptcy proceedings is recorded.
Privateering — Not present. Sanofi retained title throughout and never transferred to an NPE to assert on its behalf.
Defensive aggregator (anti‑NPE) — Not present as defined (the chain does not terminate at RPX, AST, LOT, Unified Patents, or OIN). However, the inverse signal in this item is satisfied in substance: the patent has been neutralized — never asserted and allowed to lapse for non‑payment of maintenance fees ("Expired – Fee Related," per Google Patents).
Verdict
Defensive / non-asserting.
The chain never leaves Sanofi's corporate family: the only substantive conveyances are the 2000‑02‑01 record from SANOFI to SANOFI‑SYNTHÉLABO and the 2004/2005 merger/change‑of‑name succession to Sanofi‑Aventis (reel 016345/0189 and reel 016016/0187, evidenced on sibling patent US 6,162,923). There is no NPE, no shell LLC, no cascading transfer, and no assertion. I explicitly note that this verdict deviates from the literal definition of the category — the chain terminates at an operating pharmaceutical company, not at a defensive aggregator — but the patent is unambiguously non‑asserting and has been effectively neutralized by expiration/fee‑abandonment.
Reconciling with the Litigation section: this reconstruction supports the earlier "data artifact" hypothesis. A U.S. patent number is unique — only one patent can be numbered 6,344,470 — and that patent is Sanofi's, was never assigned outside the Sanofi family, and reached full term in October 2017, roughly six years before the October 2023 Cellspin/ByteDance complaint. Title never left Sanofi, so Cellspin could not have asserted this number. The Docket Alarm listing of "6344470" in Cellspin Soft, Inc. v. ByteDance Ltd. (2:23‑cv‑00496‑JRG‑RSP) should be treated as a citation/transcription error, not an assertion of this patent.
Verify at: USPTO Assignment Center — https://assignmentcenter.uspto.gov/ (search patent number 6344470); legacy interface — https://assignment.uspto.gov/patent/index.html
Confidence: High that the patent remained Sanofi‑owned and was never NPE‑acquired. Moderate on the exact reel/frame and conveyance‑type of the Sanofi‑Aventis succession as applied to this patent, because that link is confirmed only on a sibling patent and the two secondary sources conflict on whether reel 016345/0189 is a "merger" or a "change of name." Medium on the negative product finding (no marketed Sanofi CRF₁ antagonist embodying the claims) — I could not exhaustively confirm the absence of a commercial product.
Generated 10/1/2026, 3:32:18 PM
Prior art
Earlier patents, publications, and products that may anticipate or render the claims unpatentable.
I'll research the prior-art references cited against US 6,344,470. Let me run targeted searches.
I have the core citation list for the WO family member. Let me gather details on each cited reference.
Prior-Art Analysis for US 6,344,470 B1
Scope note first. I could not open USPTO PatentCenter/PAIR or the USPTO full-text search directly through the available tools; the citation data below is taken from the front-page reference lists as reproduced by Google Patents (https://patents.google.com/patent/US6344470/en), the FreePatentsOnline record (https://www.freepatentsonline.com/[6344470](/patent/6344470).html), the WO sibling WO1998015543A1 (which prints the same search-report citations), and PubChem/EPO publication-server records for the individual references. I did not auto-correct any number: the target is 6,344,470 only, and every reference below is reported as it is printed.
Important structural point that governs the whole § 102 analysis (carried over from the earlier sections): the granted US claim set is a method-of-treatment set — claim 1 is the sole independent claim and reads "[a] method for the treatment of diseases requiring modulation of the action of corticotropin releasing factor which comprises administering … a compound of formula [I]," with claims 2–4 narrowing the Markush and claim 5 reciting specific named species. Because claim 1 is a use claim, a reference can only anticipate under § 102 if it discloses both (a) a compound within formula (I) and (b) the administration of that compound to treat a CRF-modulated disease. A chemistry reference that discloses the scaffold but a non-CRF utility is at best § 103 art. That distinction drives everything below.
1. The two citation sets (they are not identical — flagged per instructions)
| Source | References listed |
|---|---|
| US front page (Foreign References, via FPO) | EP 0 205 069; GB 2 022 085 A; WO 94/01423 A1; WO 97/00868 A1 |
| WO 98/15543 search report (Google Patents, "Patent Citations (6)") | EP 0 283 390 A2; WO 91/09857 A1; EP 0 576 350 A1; WO 94/01423 A1; EP 0 659 747 A1; WO 97/00868 A1 |
| Background discussion in the specification (given full text + siblings) | EP 0 462 264; GB 2 022 285; EP 0 432 040; JP 01‑75475; EP 0 205 069; EP 0 283 390; WO 91/09857; plus the two journal papers |
| Non-patent literature cited | Birkinshaw et al. (1984); Gillon et al. (1983) |
Flag: The US and PCT citation lists overlap but differ. EP 0 576 350 and EP 0 659 747 appear on the WO search report but were not visible on the truncated US front page, while EP 0 205 069 and GB 2 022 085 A appear on the US page. All are, however, discussed in the specification's background, so the substance is the same. Treat the merged list below as the operative prior-art universe; my earlier summary's reference list was consistent with this (EP 0205069, GB 2022085A, WO 94/01423, WO 97/00868, Birkinshaw, Gillon) — I add EP 0 283 390, WO 91/09857, EP 0 576 350, EP 0 659 747, EP 0 462 264, EP 0 432 040 and JP 01‑75475 from the search report/background.
Pre-AIA § 102 governs (filed 1997‑10‑07, priority 1996‑10‑08), so the § 102(b) critical date is 1996‑10‑07 (one year before the US filing date).
2. Reference-by-reference analysis
A. CRF-active aminothiazoles — the only references that can touch § 102
(1) EP 0 576 350 A1 — Sanofi
- Full citation: EP 0 576 350 A1, "Branched alkylamino thiazole derivatives, process for their preparation and pharmaceutical compositions containing them," Sanofi SA. Priority 1992‑06‑24 (FR 92 07810 family); filed 1993‑06‑22; published 1993‑12‑29; granted EP 0 576 350 B1 on 1997‑10‑29.
- Description: 2‑Aminothiazoles whose 2‑amino group is a tertiary amine bearing a branched alkyl/aralkyl substituent; described as having affinity for CRF receptors. Inventors overlap directly with the target (Roger, Gully, Wermuth, Courtemanche, Gautier, Valette).
- § 102 potential: A § 102(b) printed publication (published ~3 years before the critical date) that shares the CRF utility. However, the reference's amine nitrogen carries a branched alkyl/aralkyl group, not the optionally-substituted phenyl + n‑propyl combination exemplified in claim 5 of US 6,344,470 (the later Sanofi patent US 6,586,456 states expressly that the EP 576 350 / EP 659 747 compounds "do[] not carr[y] a substituted phenyl as a substituent of the tertiary amine in position 2"). Conclusion: it does not anticipate claims 1–5; it is the principal § 103 starting point.
(2) EP 0 659 747 A1 — Sanofi
- Full citation: EP 0 659 747 A1, "Branched aminothiazole derivatives, process for their preparation and pharmaceutical compositions containing them," Sanofi SA. Priority 1993‑12‑21 (FR 93 15386); filed 1994‑12‑20; published 1995‑06‑28. (RU 2107063 C1 is a family member.)
- Description: Same series as (1); 2‑aminothiazoles with a tertiary 2‑amino bearing a branched alkyl/aralkyl; the abstract states the compounds "find their application in the treatment of all pathologies involving CRF."
- § 102 potential: § 102(b) publication (published ~16 months before the critical date) and, unlike the purely chemical references, it discloses the CRF-treatment use that claim 1 requires. Anticipation therefore turns entirely on whether its Markush overlaps the formula (I) genus of claim 1 / the aryl-on-amine species of claim 5. On the record I have, the amine substituents are branched alkyl/aralkyl rather than the substituted phenyl + n‑propyl of claim 5, so no clear anticipation of the species claims; it is the closest § 103 art (same scaffold, same use, same inventors/assignee). Caveat: the exact R‑group definitions of US claim 1's formula (I) are still unverified (carried over limitation), so a definitive § 102 verdict on the genus claim cannot be given.
(3) WO 97/00868 A1 — Sanofi (cited on the US front page)
- Full citation: WO 97/00868 A1, "4‑Phenylaminothiazole derivatives, method for preparing same, and pharmaceutical compositions containing said derivatives," Sanofi. Priority 1995‑06‑21; PCT/FR96/00941 filed 1996‑06‑18; published 1997‑01‑09. US counterpart US 5,880,135 (granted 1999‑03‑09).
- Description: Substituted 4‑phenylaminothiazoles disclosed as CRF (corticotropin-releasing-hormone) antagonists. The 4‑position is an amino-aryl, not the C-linked aryl of formula (I).
- § 102 potential: Discloses CRF antagonism (i.e., the claim‑1 use), but the core substitution pattern is different (4‑amino vs. 4‑aryl), so it does not anticipate. Timing is also problematic for the office: it published after the 1996‑10‑08 priority and less than one year before the 1997‑10‑07 US filing, so it is not § 102(b). As a PCT published in French, its eligibility as § 102(e) art as of the international filing date (1996‑06‑18) under the pre‑2000 text of § 102(e) is doubtful (that provision required English-language publication). Best characterized as § 103 art, not an anticipatory reference.
B. Thiazole-chemistry / non-CRF references (cannot anticipate the method claim)
(4) EP 0 205 069 A1 — on the US front page. "2,2‑Diaryl‑chromenothiazoles, their preparation and their use as recording materials." Published 1986‑12‑17 (well before the critical date; § 102(b)). The specification cites it only for 2‑amino‑4‑(4‑hydroxyphenyl)thiazole intermediates. No CRF use disclosed → no § 102 anticipation of claims 1–5; § 103 background only.
(5) GB 2 022 085 A — on the US front page. Thiazole derivatives substituted at the 2‑position with secondary amino groups, described as immune-response regulators with anti-inflammatory properties. Published 1979‑12‑12 (§ 102(b)). Secondary (not tertiary) 2‑amino and a non-CRF utility. No anticipation; § 103 background.
(6) WO 94/01423 A1 — Nippon Soda Co., Ltd. "Thiazole derivative." Published 1994‑01‑20 (§ 102(b)). Listed on both citation sets; no CRF utility is disclosed. No anticipation; at most § 103 scaffolding.
(7) EP 0 283 390 A2 — Elf Sanofi. Thiazole derivatives active on the cholinergic system (2‑[N‑alkyl‑N‑pyridylalkylamino]thiazoles; muscarinic agonists for memory disorders/senile dementia). Published 1988‑09‑21 (§ 102(b)). Different N‑substitution and a cholinergic — not CRF — utility. No anticipation; § 103 background.
(8) WO 91/09857 A1 — Sanofi. "Heterocyclic derivatives, method for preparing same, and their therapeutic applications" — the PAF‑antagonist series. Published 1991‑07‑11 (§ 102(b)). Non-CRF utility. No anticipation.
(9) EP 0 462 264 A1/B1 — Sanofi (discussed in the specification; the given text is truncated mid-sentence at "EP 462 264 describes 2‑aminothiazole derivatives whose t…"). Heterocyclic PAF‑acether antagonists (Bernat, Herbert, Valette; priority 1989‑12‑29; published 1991‑12‑27). It is the reference the applicants characterize as showing 2‑aminothiazoles whose tertiary 2‑amino "comprises two substituents each having at least one heteroatom." § 102(b) publication, but PAF utility, not CRF. No anticipation; § 103 background.
(10) EP 0 432 040 A1 (background only). Heterocyclic 2‑acylaminothiazoles described as cholecystokinin and gastrin antagonists (published 1991). Non-CRF, 2‑acylamino (not 2‑tertiary-amino). No anticipation.
(11) JP 01‑75475 (background only). 2‑Amino‑4,5‑diphenylthiazoles with anti-inflammatory properties. No CRF use → no anticipation.
C. Non-patent literature (the two journal citations on the US face page)
(12) T. N. Birkinshaw et al., "2‑(N,N‑Disubstituted Amino)thiazoles with Electron-withdrawing Groups at Position 5: Preparation and Investigation of Structural Features," J. Chem. Soc. Perkin Trans. I, 1984, 2, 147–153. § 102(b) printed publication. Description: synthetic/structural study of N,N‑disubstituted 2‑aminothiazoles bearing electron‑withdrawing groups at C‑5 — i.e., it teaches the 2‑(N,N‑disubstituted amino)thiazole core. § 102 potential: It is chemistry only — no pharmaceutical use, no CRF — and it teaches electron‑withdrawing C‑5 groups rather than the methyl/aryl-amine combination of the claims. Cannot anticipate the method claim; evidentiary § 103 art for the scaffold.
(13) D. W. Gillon et al., "N,N‑Disubstituted 2‑Aminothiazole‑5‑carbaldehydes…," J. Chem. Soc. Perkin Trans. I, 1983, 2, 341–347. § 102(b) printed publication. Description: preparation of N,N‑disubstituted 2‑aminothiazole‑5‑carbaldehydes. § 102 potential: same as (12) — pure chemistry, no CRF use, different C‑5 substituent. No anticipation; § 103 background.
3. Bottom line on § 102
| Reference | Date vs. critical date (1996‑10‑07) | Discloses formula (I)-type compound? | Discloses CRF treatment? | § 102 anticipation of US 6,344,470? |
|---|---|---|---|---|
| EP 0 576 350 | 1993‑12‑29 (before) | Yes (scaffold) | Yes | No — amine substituent differs (branched alkyl/aralkyl, not aryl) |
| EP 0 659 747 | 1995‑06‑28 (before) | Yes (scaffold) | Yes | No (probable) — same reasoning; closest § 103 art |
| WO 97/00868 | 1997‑01‑09 (after priority; <1 yr pre-filing) | Different core (4‑amino) | Yes | No; § 102(e) status doubtful (French-language PCT) |
| EP 0 205 069 | 1986‑12‑17 | Partly (intermediates) | No | No |
| GB 2 022 085 A | 1979‑12‑12 | Secondary amine | No | No |
| WO 94/01423 | 1994‑01‑20 | Thiazole (unrelated utility) | No | No |
| EP 0 283 390 | 1988‑09‑21 | Cholinergic series | No | No |
| WO 91/09857 | 1991‑07‑11 | PAF series | No | No |
| EP 0 462 264 | 1991‑12‑27 | 2‑aminothiazoles (PAF) | No | No |
| EP 0 432 040 | 1991 | 2‑acylaminothiazoles | No | No |
| JP 01‑75475 | pre‑1996 | 2‑amino‑4,5‑diphenyl | No | No |
| Birkinshaw 1984 | 1984 | 2‑(N,N‑disubst. amino)thiazole core | No | No |
| Gillon 1983 | 1983 | 2‑aminothiazole‑5‑carbaldehydes | No | No |
No cited reference anticipates any claim of US 6,344,470 under § 102. The method-of-treatment format of claim 1, combined with the fact that the CRF-active references (EP 0 576 350, EP 0 659 747, WO 97/00868) each lack the optionally-substituted-phenyl/n‑propyl substitution on the 2‑amino nitrogen that characterizes the claim‑5 species, defeats anticipation. The prior art instead supports a § 103 case built on EP 0 576 350 or EP 0 659 747 (same scaffold, same CRF utility, same inventors) optionally combined with the Birkinshaw/Gillon papers on 2‑(N,N‑disubstituted amino)thiazole chemistry.
4. Explicit uncertainties / things I could not verify
- Markush scope of claims 1–4 of US 6,344,470 is still unverified (carried-over limitation). Without the verbatim formula (I) definitions, I cannot give a definitive § 102 verdict on the genus claim 1 — only on the named claim‑5 species, where the analysis above holds. This is the single biggest caveat.
- EP 0 659 747's full R‑group definitions were not retrieved in machine-readable form (the RU 2107063 abstract suggests R5 may include "optionally substituted phenyl," which, if correct, would move EP 0 659 747 closer to the claim‑1 genus and warrants a direct reading of the EP 0 659 747 claims). Flagged as unverified.
- § 102(e) status of WO 97/00868 turns on the pre‑2000 statutory English-language-publication requirement for international applications; I applied the rule as written but did not pull the statute text to confirm.
- The US vs. WO citation lists differ (see § 1); I merged them. If a strict "face-of-the-US-patent only" answer is required, the operative US list is EP 0 205 069, GB 2 022 085 A, WO 94/01423 A1, WO 97/00868 A1 (the FPO list as retrieved), while the remainder belong to the WO search report/background.
Sources: https://patents.google.com/patent/US6344470/en (front page + concepts); https://www.freepatentsonline.com/6344470.html (foreign references + NPL citations); https://patents.google.com/patent/WO1998015543A1/en (search-report citations); https://pubchem.ncbi.nlm.nih.gov/patent/EP-0576350-B1 and https://pubchem.ncbi.nlm.nih.gov/patent/EP-0659747-A1 (dates/abstracts); https://patents.justia.com/patent/[6586456](/patent/6586456) (statement that EP 576 350 / EP 659 747 compounds lack a substituted phenyl on the 2‑amino nitrogen); https://patentimages.storage.googleapis.com/7a/b9/b1/046e10714bcf5a/US5880135.pdf (US counterpart of WO 97/00868, PCT/FR96/00941 filed 1996‑06‑18).
Generated 10/1/2026, 3:32:33 PM
Obviousness
Combinations of prior art that suggest the claimed invention would have been obvious under 35 U.S.C. § 103.
I'll ground this analysis in the actual prior-art references cited on the face of US 6,344,470 and in the surrounding CRF-antagonist art. Let me pull the reference details first.
Good — the cited-art list is confirmed. Now let me pull the two CRF-specific 2-aminothiazole references (EP 576 350, EP 659 747), the Courtemanche/AU 41399/93 reference, and check whether the EP family member was opposed (which would give a real-world § 103 record).
Obviousness Analysis — US 6,344,470 B1 under 35 U.S.C. § 103
Scope note / honesty flag. This analysis is built on (a) the cited-art list on the face of US 6,344,470 (as returned by FreePatentsOnline for that number), (b) the admission section of the specification itself, and (c) the surrounding CRF-antagonist art that the specification expressly discusses. I was not able to retrieve the full Markush text of claims 1–4, the complete claim-5 list, or the full disclosure of several references (notably AU‑A‑41399/93) before my search budget ran out. Where I rely on a secondary characterization rather than the primary document, I say so. I am not auto-correcting any identifier.
1. The claim(s) to be tested
Claim 1 is a method-of-treatment claim: treating a disease requiring modulation of CRF action by administering an "effective amount" of a compound of formula (I). Claims 2–4 narrow R-groups; claim 5 recites ~40 named species. Every species visible on the face of the record is a 4-(substituted phenyl)‑5‑methyl‑2‑[N‑alkyl‑N‑(substituted phenyl)amino]‑1,3‑thiazole — e.g. 4‑(2‑chloro‑4‑methoxyphenyl)‑5‑methyl‑2‑[N‑(5‑chloro‑2‑methylphenyl)‑N‑propylamino]thiazole. Because claim 1 is a method claim covering a broad genus, validity turns on (i) whether the genus of administered compounds would have been obvious, and (ii) whether the CRF-modulating use would have been obvious.
PHOSITA: a medicinal chemist (Ph.D. or M.S.) with ~2–5 years in small-molecule CNS/peptide-GPCR drug discovery, conversant with the thiazole literature, CRF pharmacology, and routine analogue synthesis plus radioligand binding assays.
2. The prior art actually available as of the 1996‑10‑08 priority date
| Ref. (as it appears on the record) | Date | Teaching relied on |
|---|---|---|
| EP 462 264 (discussed in spec.) | ~1991/92 | 2‑Aminothiazoles whose 2‑position tertiary amine bears two substituents; PAF‑acether antagonists |
| GB 2022085A (record) / "GB 2 022 285" (spec.) | 1979‑12‑12 | Thiazoles substituted at 2 by secondary amine groups; immunoregulatory / anti‑inflammatory |
| EP 0205069 / EP 205 069 | 1986‑12‑17 | 2,2‑Diaryl‑chromenothiazoles; 2‑amino‑4‑(4‑hydroxyphenyl)thiazole intermediates |
| WO 94/01423 | 1994‑01‑20 | 2‑Aminothiazoles in which the 2‑amine nitrogen carries an alkyl and a substituted phenyl; used as insecticides; no substitution at the thiazole 5‑position |
| EP 576 350 and EP 659 747 (discussed in spec.) | ~1993 / ~1995 | 2‑Aminothiazoles whose 2‑amine is a tertiary amine bearing a branched alkyl or aralkyl, stated to have affinity for CRF receptors |
| Birkinshaw et al., J. Chem. Soc. Perkin Trans. I, 1984, 147‑153; Gillon et al., ibid. 1983, 341‑347 | 1983/84 | Preparation and structural investigation of 2‑(N,N‑disubstituted amino)thiazoles bearing electron‑withdrawing groups at the 5‑position; N,N‑disubstituted 2‑aminothiazole‑5‑carbaldehydes |
| US 5,063,245 (Abreu) (cited in the art) | 1991 | Substituted pyrazolines as small-molecule (non-peptide) CRF antagonists |
| AU‑A‑41399/93 (Courtemanche) | 1993 | Substituted 2‑aminothiazoles reported as CRF receptor antagonists (IC₅₀ ≈ 0.1–10 µM) — I know this only through the secondary citation in US 6,348,466 (Haddach et al.); I could not pull the primary document. |
| US 5,880,135 / WO 97/000868 (Sanofi; Gully/Roger/Wermuth) | WO pub. 1997‑01‑09; US app. §371 of PCT/FR96/00941 filed 1996‑06‑18 | 4‑Phenylaminothiazoles as CRF antagonists |
| WO 96/16650, EP 432 040, JP‑01 75 475, US 5,109,111/5,132,111/5,245,009, WO 92/22576, WO 96/19499 | pre‑1996 | Crowded 2‑aminothiazole/CRF art; peptide CRF antagonists |
Admissions in the specification. The '470 specification itself recites that (i) "a large number of 2‑aminothiazole derivatives are already known"; (ii) WO 94/01423 teaches the N‑alkyl/N‑substituted‑phenyl 2‑aminothiazole; (iii) EP 576 350 and EP 659 747 teach 2‑aminothiazoles "having affinity for the CRF receptors"; and (iv) the only feature it asserts as absent there is "a substituted phenyl as substituent of the tertiary amine at the 2‑position." An applicant's own characterization of the art is usable as a § 103 admission (In re Fout; Constant v. Advanced Micro‑Devices).
Date caveats the challenger must clear. (1) WO 97/000868 published 1997‑01‑09 — after the 1996‑10‑08 priority date — so it is not § 102(a)/(b) art; only its US counterpart US 5,880,135 could serve, and then only under pre‑AIA § 102(e) (which for a pre‑29‑Nov‑2000 PCT runs from § 371(c) compliance, not the international filing date). (2) Because the Sanofi entities commonly owned that work, pre‑AIA § 103(c) would disqualify 102(e)‑only art for obviousness. The '470 claim set therefore most plausibly rises or falls on the third‑party art: WO 94/01423, EP 576 350/659 747, EP 462 264, Birkinshaw/Gillon, Abreu, and (if verified) AU 41399/93.
3. Combination 1 — WO 94/01423 + EP 576 350 (or EP 659 747) [± Birkinshaw/Gillon]
This is the strongest and cleanest prima facie case, and it maps element-by-element onto formula (I):
- N‑alkyl + N‑(substituted phenyl) on a 2‑aminothiazole → taught literally by WO 94/01423 ("R₁ₐ pouvant représenter un alkyle et R₂ₐ un phényle substitué"). This is the single most distinctive element of the claim, and it is old.
- CRF receptor affinity of 2‑aminothiazoles → taught by EP 576 350 / EP 659 747. This supplies both the utility and the motivation: a PHOSITA reading these documents would look to 2‑aminothiazoles as a CRF‑antagonist chemotype.
- 5‑methyl and 4‑aryl decoration → within the routine skill of the art. Birkinshaw 1984 and Gillon 1983 are specifically about 2‑(N,N‑disubstituted amino)thiazoles bearing 5‑substituents; installing a methyl (the archetypal small alkyl, used to block metabolism and tune sterics) at the one position the insecticidal WO 94/01423 compounds leave open is a predictable variation — structural homologation (In re Papesch; In re Dillon).
Motivation to combine (KSR/MPEP § 2143 rationales):
- Same field of endeavor / same problem: all three documents concern the medicinal chemistry of 2‑aminothiazoles; EP 576 350/659 747 target the very receptor the '470 claim recites.
- Obvious to try: after the 1993 cloning of the CRF₁ receptor and the demonstration of non-peptide CRF antagonism (Abreu '245; Courtemanche AU 41399/93), the art had a small, finite, identified set of chemotypes (thiazoles among them) and a routine screening assay — the very method the '470 specification itself invokes (E. B. De Souza radioligand binding).
- Known technique to improve a known compound: swapping an aralkyl N‑substituent (EP 576 350/659 747) for the N‑aryl group already disclosed in WO 94/01423 is a substitution of one known element for another with predictable effect.
- Reasonable expectation of success: the closest analogues were already reported CRF ligands, so retention/improvement of CRF binding was expected, not speculative.
4. Combination 2 — either of the above + WO 97/000868 / US 5,880,135
If the § 103(c) hurdle is not met by the patentee, US 5,880,135 adds a Sanofi‑authored CRF‑antagonist thiazole disclosure teaching both the aryl‑decorated thiazole core and the CRF utility, reinforcing the "same problem" motivation. (For the record, US 5,880,135 is 4‑phenylamino‑thiazole chemistry, so it is closer on utility than on structure; that structural gap is a fair rebuttal point.)
5. Combination 3 — + AU 41399/93 (Courtemanche)
If Courtemanche's substituted 2‑aminothiazoles are, as the secondary source states, CRF antagonists with 0.1–10 µM binding, then the "lead compound" analysis is nearly complete on its own: (1) a 2‑aminothiazole lead with known CRF activity; (2) obvious modifications = the N‑alkyl/N‑aryl pattern of WO 94/01423 plus a 5‑methyl; (3) reasonable expectation of success from the known CRF activity. I could not verify the primary disclosure, so this combination is asserted conditionally.
6. Combination 4 — + EP 462 264 / GB 2 022 285 / EP 0205069
These are secondary. EP 462 264 establishes that 2‑aminothiazoles with a fully substituted (tertiary) 2‑amino nitrogen are pharmacologically active; GB 2 022 285 establishes 2‑amino(thiazoles) generally; EP 0205069 supplies 2‑amino‑4‑arylthiazole intermediates. They are useful to show the genus was thoroughly explored and to rebut any argument of a "teaching away" from N,N‑disubstitution.
7. Claim-by-claim posture
- Claims 1 and 5: Claim 1 is broad enough that a single obvious species (e.g., the WO 94/01423 scaffold + 5‑methyl) supports a prima facie § 103 case for the method if the CRF utility is also suggested. Claim 5's species (2‑chloro‑4‑methoxyphenyl / 5‑methyl / N‑propyl / N‑(2‑substituted‑5‑substituted‑phenyl)) are all single, routine substituent selections (Cl, OMe, Me, CF₃) around the WO 94/01423 core. Under KSR, "a combination of familiar elements according to known methods is likely to be obvious when it does no more than yield predictable results."
- Claims 2–4: narrowing Markush claims. If the genus is obvious, dependent narrowing claims are a fortiori obvious absent a showing that the narrowed sub‑genus carries the patentable weight. I could not confirm the text of claims 2–4, so this is a framework conclusion only.
- § 103(c) and § 102(e) date analysis (above) is the patentee's best procedural defense against the WO 97/000868/US 5,880,135 leg.
8. Rebuttals the patentee would (properly) raise
- Unexpected results. The specification asserts that "compounds of similar structure… do not significantly displace this binding" and that the compounds are "surprising and unexpected," being "more active in vivo than compounds of similar structure," with sub‑10 µM displacement of CRF/urotensin/sauvagin binding. If supported by comparative data against the closest EP 576 350/659 747 compounds, this is classic non‑obviousness evidence.
- Teaching away / teaching direction. EP 576 350 and EP 659 747 teach branched alkyl or aralkyl on the 2‑amine and expressly do not carry a substituted phenyl; the art therefore pointed away from N‑aryl. The '470 family repeats this distinction verbatim in every member.
- WO 94/01423 is insecticidal, not pharmaceutical, and lacks 5‑substitution — a different field of use and a structural gap that the challenger must bridge with an explicit motivation.
- § 103(c) disqualification of the 102(e)‑only Sanofi reference.
- Commercial success / long‑felt need — the standard secondary considerations. I found no evidence of commercialization of a '470 compound, so this factor is likely unavailable on the current record.
9. Real-world § 103 signal (and its limits)
The only § 103‑flavored citation I could verify is the reverse direction: the WO 2003/048140 A1 search report cites "JP 2000‑504039 A (Sanofi) … & WO 98/15543 A1 & EP 934290 A1 & US 6344470 A" as a "Y" (inventive‑step) reference against claims 1‑5 and 7‑13 of that third‑party application. That shows the '470 disclosure is regarded as obviousness‑relevant art against others — it says nothing about whether '470 itself would have been held obvious.
I found no EPO opposition to EP 934290 B1 and no US IPR/PGR or § 103 holding on US 6,344,470, consistent with the prior sections' finding that the patent was never asserted and lapsed in 2017.
10. Confidence and gaps
| Proposition | Confidence |
|---|---|
| WO 94/01423 discloses an N‑alkyl/N‑(substituted phenyl)‑2‑aminothiazole | High (spec.'s own admission + family text) |
| EP 576 350 / EP 659 747 disclose 2‑aminothiazoles as CRF ligands | High (spec.'s own admission) |
| WO 97/000868 is not § 102(a)/(b) art (published after priority) | High |
| § 103(c) would disqualify US 5,880,135 as § 103 art | Medium‑High (assuming common ownership at invention) |
| Content of AU 41399/93 (Courtemanche) | Low — secondary source only |
| Full Markush of claims 1–4; total claim count | Low — text not retrieved |
| The "GB 2022085A" vs "GB 2 022 285" mismatch | Reported as it appears; not normalized |
Bottom line. The art supports a credible prima facie § 103 case against claims 1–5 along the line WO 94/01423 (N‑alkyl/N‑substituted‑phenyl 2‑aminothiazole) + EP 576 350 or EP 659 747 (CRF affinity of 2‑aminothiazoles) + Birkinshaw/Gillon (5‑position chemistry), optionally reinforced by Abreu US 5,063,245 and — if verified — Courtemanche AU 41399/93. The strongest patentee defenses are (i) the express teaching direction in EP 576 350/659 747 toward branched alkyl/aralkyl and away from N‑aryl, (ii) the asserted unexpected potency/solubility, and (iii) the pre‑AIA § 103(c) disqualification of the Sanofi 102(e) art. Resolving the case would require the primary disclosures of WO 94/01423 and AU 41399/93 and the full claim text — the gaps I have flagged rather than filled.
Sources. Google Patents record for US6344470B1 (assignee, dates, status): https://patents.google.com/patent/US6344470/en · FreePatentsOnline cited‑references list and claim 5 text: https://www.freepatentsonline.com/[6344470](/patent/6344470).html · Family background/admissions (CA2267154A1; FR2754258A1; US 2002/0137740; US 6,586,456): https://patents.google.com/patent/CA2267154A1/en · WO 2001005776A1 (WO 94/01423 characterized as insecticidal, no 5‑substitution): https://patents.google.com/patent/WO2001005776A1/en · US 5,880,135 (4‑phenylaminothiazoles, CRF): https://patents.justia.com/patent/[5880135](/patent/5880135) · US 6,348,466 (Abreu '245 and Courtemanche AU 41399/93 as CRF antagonists): https://patentimages.storage.googleapis.com/5b/ad/06/2802dd9cc26388/US6348466.pdf · WO 2003/048140 A1 search report citing US 6344470 as a "Y" reference: https://patentimages.storage.googleapis.com/f6/23/77/614b4860265346/WO2003048140A1.pdf
Generated 10/1/2026, 3:32:58 PM
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