Last Updated: June 24, 2026

Details for Patent: RE41783


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Which drugs does patent RE41783 protect, and when does it expire?

Patent RE41783 protects XELJANZ and XELJANZ XR and is included in three NDAs.

Protection for XELJANZ has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has seventy-five patent family members in fifty-two countries.

Summary for Patent: RE41783
Title:Pyrrolo[2,3-D]pyrimidine compounds
Abstract:A compound of the formula wherein R1, R2 and R3 are as defined above, which are inhibitors of the enzyme protein kinases such as Janus Kinase 3 and as such are useful therapy as immunosuppressive agents for organ transplants, xeno transplation, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases.
Inventor(s):Todd A. Blumenkopf, Mark E. Flanagan, Michael J. Munchhof
Assignee: Pfizer Corp SRL
Application Number:US12/577,790
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent RE41783
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

RE41783 Scope and Claims Analysis: What It Covers for US Compound Claims, Salts, and Specific Examples

United States RE41783 is a reissue patent with broad genus-style chemical coverage: it claims “a compound of the formula or a pharmaceutically acceptable salt thereof,” with large combinatorial scope driven by substituent variables (notably R1, R4, R5, R6-R11, and R12). Claim 3 and Claim 4 anchor the broad genus to a set of named (and one explicitly singled-out) embodiments, tightening enforceability for particular structures within the broader chemical space.

Below is a structured breakdown of (1) claim scope, (2) what the claim language does to claim breadth, (3) claim architecture and likely claim construction fault lines, and (4) what matters for infringement and freedom-to-operate (FTO) risk when targeting a US competitor pathway.


What does US RE41783 claim, and how broad is the genus coverage?

Answer (scope headline): RE41783 claims a chemical genus of compounds (plus pharmaceutically acceptable salts) defined by a complex core scaffold with multiple substituent variables. The genus scope is broad enough to cover many analogs differing in ring substitutions and heteroatom-containing side chains, while still being tethered to a specific underlying scaffold and connectivity pattern.

Core claim structure: “compound of the formula or a salt”

All independent claim sets you provided use the same opening premise:

  • “A compound of the formula or a pharmaceutically acceptable salt thereof”
  • with variable definitions controlling substituents and substitution patterns

This creates two immediate enforcement hooks:

  1. Direct product infringement by making/using/selling a covered compound.
  2. Salt infringement if the salt form is pharmaceutically acceptable and falls within the claimed compound structure.

Exclusionary effect of “R2 and R3 are each hydrogen”

Across claim 1 and claim 2 you provided, R2 and R3 are constrained to H. That narrows the claim by excluding analogs where those positions are substituted. For any competitor design, those two positions are high-priority claim-mapping targets.


How do the R-group variables drive the chemical space protected by RE41783?

R1: The main structural “gate”

Claim 1 and claim 2 define R1 as a substituted group with an internal formula and a parameter y.

  • In claim 1: y is 0, 1 or 2
  • In claim 2: y is 0

This means:

  • Claim 1 covers a larger R1 subspace than claim 2.
  • If a competitor’s scaffold corresponds only to one y-value, it may still fall under claim 1; but claim 2 is narrower and can be used to isolate a subset.

R4: Two major classes of substituents

Claim 1 gives two alternative R4 regimes:

  1. Alkyl / alkylsulfonyl / alkenyl / alkynyl (C1-C6 alkyl, etc.), optionally substituted by a list including deuterium, OH, amino, CF3, alkoxy, cyano, nitro, and acylamino-type groups.
  2. Cycloalkyl (C3-C10) optionally substituted by many of the same groups, including nitro and CF3-containing substituents.

This is broad in two ways:

  • R4 type diversity (acyclic vs cycloalkyl)
  • Functional group diversity (electron-withdrawing and polar groups are allowed, including CF3 and nitriles)

Claim 2 tightens R4 to:

  • R4 is (C1-C6)alkyl only.

So claim 1 is the workhorse for breadth, claim 2 is the narrower fallback.

R5: Piperidinyl substituted by 1 to 5 groups

Claim 1 and claim 2 both define R5 as:

  • piperidinyl substituted by one to five” substituents chosen from a long list, including:
    • carboxy
    • cyano
    • amino
    • deuterium
    • hydroxy
    • (C1-C6)alkyl / alkoxy
    • halo
    • (C1-C6)acyl
    • alkylamino and substituted amino variants
    • multiple acyloxy/acylamino and sulfonyl-containing motifs are also present via R15/R16/S(O)m patterns

This is where RE41783’s genus breadth becomes practically meaningful for competitors:

  • A piperidine ring that tolerates up to five substituents makes many “late-stage derivative” programs land in-coverage if they keep the same core and satisfy the other constrained variables.

R6–R11: Terminal scaffold substituents

Claim 1 contains:

  • R6, R7, R8, R9, R10 and R11 each is hydrogen or (C1-C6)alkyl optionally substituted by the allowed polar/halogen/CF3/cyano/acylamino set.

This supports analog substitution patterns where:

  • the scaffold can be “alkyl-substituted then further functionalized” while remaining inside the genus.
  • competitors modifying only methyl/ethyl and installing CF3/OH/NH2 equivalents remain at risk.

R12: the big electronic/functional latitude

Claim 1:

  • R12 is chosen from an extensive list including carboxy, cyano, amino, oxo, deuterium, hydroxy, CF3, alkyl, alkoxy, halo, acyl, alkylamino, alkenyl, alkynyl, and multiple acyloxy/acylamino variants plus R15/R16 and sulfonyl-related moieties.

Claim 2 narrows R12 to:

  • cyano, CF3 (and CF3-alkyl), alkyl, alkylamino, dialkylamino, alkynyl, cyano-alkyl, and alkyl-S(O)m (m 0–2)

Net effect:

  • Claim 1 is broader on R12 than claim 2.

What does “R15R16N—CO—O—” and the sulfonyl fragments mean for claim construction?

Your claims include two additional motif families that can act as literal infringement anchors:

  1. Urea/amide-ester-like carbonyl-oxygen patterns

    • e.g., “R15R16N—CO—O—”, “R15R16N—CO—(C1-C6)alkyl”, and similar N-acyl and carbamate-like fragments
  2. Sulfur oxidation state substituents

    • e.g., “(C1-C6)alkyl-S(O)m”, “R15R16NS(O)m…”, “R15S(O)mR16N…”
    • with m is 0, 1, or 2

Why this matters: when competitors swap sulfonyl vs sulfoxide vs sulfide, or switch between N-acyl and related carbonyl-oxygen groups, they often assume “equivalence.” The claim text here is explicitly enumerating sulfur oxidation states and multiple connected functional group variants, which reduces the ability to design around by minor oxidation-state changes.


Which specific compounds are enumerated in claim 3, and what does that do to enforceability?

Claim 3 lists a set of explicit embodiments:

  1. Methyl-[4-methyl-1-(propane-1-sulfonyl)-piperidin-3-yl]-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amine
  2. 4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidine-1-carboxylic acid methyl ester
  3. 3,3,3-Trifluoro-1-{4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-propan-1-one
  4. 4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidine-1-carboxylic acid dimethylamide
  5. 3-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile
  6. 3,3,3-Trifluoro-1-{4-methyl-3-[methyl-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-propan-1-one
  7. 1-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-but-3-yn-1-one
  8. 1-{3-[(5-Chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-methyl-amino]-4-methyl-piperidin-1-yl}-propan-1-one
  9. 1-{3-[(5-Fluoro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-methyl-amino]-4-methyl-piperidin-1-yl}-propan-1-one

Enforceability effect: enumeration in claim 3 helps because it:

  • demonstrates concrete coverage within the genus
  • makes design-around risk assessment more direct for known development candidates
  • supports argument that those specific embodiments are unambiguously within the claim’s structure limits (less reliance on “edge” reading of variable definitions)

Claim 4: single out a “core” embodiment

Claim 4 narrows to:

  • 3-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile (or salt)

That singled-out member is a litigation-grade target: if a competitor reproduces that exact structure (or a pharmaceutically acceptable salt), it hits the narrower claim even if some broader genus permutations are contested.


What patent landscape insights can be derived from the claim text alone?

You asked for “Detailed analysis of the scope and claims and patent landscape for United States Drug Patent RE41783.” Based strictly on the claim language you provided:

1) The landscape is likely crowded around a shared scaffold

The explicit pyrrolo[2,3-d]pyrimidin-4-yl and piperidine substitution patterns suggest:

  • a sustained medicinal chemistry program around this core.
  • multiple follow-on patents likely exist on:
    • alternative R4/R5 substitutions
    • salts
    • crystalline forms
    • method-of-use and dosing regimens (often separate from compound claims)

This is not a sourced statement about specific patents, but it is a direct inference from the breadth and the number of enumerated embodiments in claim 3.

2) The highest infringement risk zones

For competitors designing around, the claim text highlights a few “do not touch” features:

  • maintain the pyrrolo[2,3-d]pyrimidin-4-yl core connectivity
  • preserve the piperidinyl linkage and its substitution latitude
  • keep the R2 and R3 positions at H
  • avoid substituting at constrained positions that map to the R2/R3 requirement
  • avoid altering the scaffold in a way that breaks the R1 formula constraints (especially y)

3) Salts expand commercial coverage

Even if a competitor uses a different counterion, if it remains a “pharmaceutically acceptable salt” of a claimed compound, it is still within the claims. For litigation strategy, salt form selection is often a weak design-around unless the underlying free base or stereochemical form is designed out.


How strong is the patent estate for competitors under the claim wording provided?

Strength indicators from claim architecture:

  • genus claims with many substituent options
  • explicit fallback narrow claim (claim 4)
  • enumerated embodiments (claim 3)
  • explicit inclusion of salts

Vulnerabilities:

  • claim scope depends on satisfaction of multiple nested variable definitions. If a competitor’s structure deviates so that key constraints (such as y value, R2/R3=H, or the R1 internal connectivity) cannot be met, it can fall outside literal scope.
  • functional group permutations are listed, but not every possible chemical alternative is covered. Particularly, if a competitor uses substitutions not in the enumerated sets or substitutes at positions not mapped by R-group variables, it may avoid coverage.

Key takeaways

  • RE41783 claims a broad genus of scaffolded compounds (and pharmaceutically acceptable salts) defined by extensive substituent variables, with meaningful narrowing via fixed constraints like R2=H and R3=H.
  • Claim 1 covers a wider R1/R4/R12 space than claim 2 (notably y = 0/1/2 in claim 1 vs y = 0 in claim 2; R4 broader in claim 1 than claim 2).
  • Claim 3 enumerates nine specific compounds, providing clear infringement targets within the broader genus.
  • Claim 4 singles out one embodiment, making it the most defensible “center of gravity” claim for enforcement.
  • For design-around: the most sensitive variables are the scaffold linkage and the constrained positions tied to the formula definitions, especially R2/R3 and the y-defined R1 subspace.

FAQs

1) Does RE41783 cover pharmaceutically acceptable salts even if the free base changes counterion?
Yes. The claims begin “compound of the formula or a pharmaceutically acceptable salt thereof,” which brings salts of covered compounds within scope.

2) Which variable is most important to distinguish claim 1 from claim 2?
The R1 parameter y and R4 category scope (claim 1 allows broader R4 classes; claim 2 limits R4 to (C1-C6)alkyl).

3) What is the most litigation-relevant embodiment in the claim set you provided?
Claim 4’s singled-out structure: 3-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile (or salt).

4) How does the piperidine substitution limit affect freedom-to-design?
R5 is a piperidinyl substituted by one to five groups selected from a broad list, making it hard to design out by simply adding common polar/halo/CF3 substituents within the specified set.

5) Which scaffold positions are explicitly fixed in the claims?
Across claim 1 and claim 2 as provided, R2 and R3 are each hydrogen, and the presence of multiple variable definitions for R1/R4/R5/R6–R11/R12 means competitors must map those positions precisely.


References (APA)

No external sources were provided or cited for RE41783, and no docket/Orange Book/FDA or prosecution history details were included in the prompt. Therefore, no reference list can be produced.

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Drugs Protected by US Patent RE41783

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Pfizer XELJANZ tofacitinib citrate SOLUTION;ORAL 213082-001 Sep 25, 2020 RX Yes Yes RE41783*PED ⤷  Start Trial Y ⤷  Start Trial
Pfizer XELJANZ XR tofacitinib citrate TABLET, EXTENDED RELEASE;ORAL 208246-001 Feb 23, 2016 AB RX Yes No RE41783*PED ⤷  Start Trial Y ⤷  Start Trial
Pfizer XELJANZ XR tofacitinib citrate TABLET, EXTENDED RELEASE;ORAL 208246-002 Dec 12, 2019 AB RX Yes Yes RE41783*PED ⤷  Start Trial Y ⤷  Start Trial
Pf Prism Cv XELJANZ tofacitinib citrate TABLET;ORAL 203214-001 Nov 6, 2012 AB RX Yes No RE41783*PED ⤷  Start Trial Y ⤷  Start Trial
Pf Prism Cv XELJANZ tofacitinib citrate TABLET;ORAL 203214-002 May 30, 2018 AB RX Yes Yes RE41783*PED ⤷  Start Trial Y ⤷  Start Trial
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

International Family Members for US Patent RE41783

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 1235830 ⤷  Start Trial C01235830/01 Switzerland ⤷  Start Trial
African Regional IP Organization (ARIPO) 1905 ⤷  Start Trial
Argentina 026534 ⤷  Start Trial
Austria 257157 ⤷  Start Trial
Austria 380031 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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