Details for Patent: 6,939,539

Summary for Patent: 6,939,539

Title:	Copolymer-1 improvements in compositions of copolymers
Abstract:	The present invention relates to an improved composition of copolymer-1 comprising copolymer-1 substantially free of species having a molecular weight of over 40 kilodaltons.
Inventor(s):	Eliezer Konfino, Michael Sela, Dvora Teitelbaum, Ruth Arnon
Assignee:	Yeda Research and Development Co Ltd
Application Number:	US10/615,865
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,939,539
Patent Claim Types: see list of patent claims	Use; Composition;

United States Patent 6,939,539: Scope of Claims and U.S. Patent Landscape for “Copolymer-1” for Multiple Sclerosis

What is the claim scope of US 6,939,539?

US 6,939,539 claims a specific “copolymer-1” polypeptide mixture and compositions and methods using it to treat multiple sclerosis (MS). The patent scope is built around three technical anchors:

1. Sequence composition: polypeptides composed of glutamic acid, lysine, alanine, and tyrosine.
2. Mixture character: the polypeptide mixture is non-uniform with respect to molecular weight and sequence.
3. Molecular weight profile: the mixture has an average molecular weight within defined kilodalton (kDa) ranges and specific distribution constraints (percentiles by molar fraction) for low and high molecular weight species.

The claims then scale outward to:

• a copolymer-1 composition (composition claims 1-11),
• a pharmaceutical composition (claims 12-22),
• and methods of treating MS via administration (claims 23-33).

Claim set overview (as provided)

Claim group	Claim numbers	What is claimed	Core limiting features
Copolymer-1 composition	1-11	The mixture itself	Amino acid set; non-uniform molecular weight and sequence; average MW 4-9 kDa; specific distribution and optional profile matching FIG. 1/F2
Pharmaceutical composition	12-22	Mixture + excipient + therapeutic use	Same mixture limitations as above; explicitly “dose therapeutically effective”; MW distribution/average constraints repeated across dependents
MS treatment method	23-33	Administering the pharmaceutical composition	MS patient treatment via the claimed pharma composition

What are the key claim limitations that define infringement risk?

1) The polypeptide “identity” anchor: amino acid composition

Claim 1 requires polypeptides “composed of glutamic acid, lysine, alanine and tyrosine.” This is an identity constraint on the polypeptide building blocks. It functions as a gatekeeper: mixtures that include different residue types are outside the claim even if molecular weight looks similar.

Practical scope impact

• A challenger can focus on whether the test material truly has only these residues (and no others) in its polypeptide constituents.
• Even if the product is described commercially as “copolymer-1,” infringement turns on compositional amino acid content as captured by the claim.

2) The “mixture non-uniformity” anchor: molecular weight and sequence heterogeneity

Claim 1 requires that “the mixture of polypeptides is non-uniform with respect to molecular weight and sequence.” This excludes highly uniform polymers and pushes scope toward heterogeneous copolymer preparations.

Practical scope impact

• A product with a narrower molecular weight distribution and/or more uniform sequence patterning may fall outside the “non-uniform” limitation, even if average MW hits the same band.

3) Average molecular weight is a primary numeric limiter

Claim 1 sets average molecular weight about 4 to about 9 kDa.

Dependent claims further narrow or specify bands:

• 5 to 9 kDa (claim 7)
• 4 to 8.6 kDa (claim 6)
• 6.25 to 8.4 kDa (claim 5)
• “average molecular weight about 7.7 kDa” tied to a distribution profile (claim 11)

Practical scope impact

• “Average MW” is likely measured by distribution analytics (e.g., size exclusion chromatography) and can be argued by test methodology and calibration. But within the claim structure, average MW bands define the baseline infringement window.

4) High and low molecular weight species constraints by molar fraction

The patent restricts the tail ends of molecular weight distribution.

Key percent constraints:

• Over 75% of polypeptides by molar fraction in 2 to 20 kDa (claims 2 and repeated in claims 4, 9, 13, 15, 20)
• Less than 5% over 40 kDa (claims 3 and repeated in claims 4-5-14-15 etc.)
• Less than 2.5% over 40 kDa (claims 8, 19)

Practical scope impact

• Even if average MW fits, an accused product that has a larger high-molecular-weight tail (over 40 kDa) may fall outside.
• Likewise, a distribution with substantial mass outside 2 to 20 kDa, even if average MW remains in band, may be non-infringing.

5) Distribution-shape match to FIG. 1 or FIG. 2

Claim 11 (and corresponding pharmaceutical claim 22) tightens scope by requiring “molecular weight distribution substantially as depicted in the curves of FIG. 1 or FIG. 2,” with an average of about 7.7 kDa.

Practical scope impact

• This is an additional layer beyond average MW and percentile constraints. It potentially captures a specific preparation identity characterized by a particular distribution shape.

What do the dependent claims add, claim by claim?

Copolymer-1 composition claims (1-11)

Claim 1 (base composition)

• Copolymer-1 polypeptides of Glu, Lys, Ala, Tyr
• Average MW about 4 to about 9 kDa
• Mixture non-uniform in molecular weight and sequence
• Suitable for treating multiple sclerosis

Claim 2

• >75% molar fraction with MW 2 to 20 kDa

Claim 3

• <5% molar fraction with MW >40 kDa

Claim 4

• Couples claim 3 + claim 2 distribution and averages remain within claim 1 base

Claim 5

• Adds average MW 6.25 to 8.4 kDa

Claim 6

• Adds average MW 4 to 8.6 kDa

Claim 7

• Adds average MW 5 to 9 kDa

Claim 8

• Tightens high-end tail: <2.5% molar fraction with MW >40 kDa

Claim 9

• Couples claim 8 tail tightening + claim 2’s >75% in 2-20 kDa

Claim 10

• Adds average MW 6.25 to 8.4 kDa (into claim 9 framework)

Claim 11

• Limits distribution to match FIG. 1 or FIG. 2 (substantially) with average MW ~7.7 kDa

Pharmaceutical composition claims (12-22)

Claim 12

• “A pharmaceutical composition” with:
  • a therapeutically effective dose for MS
  • copolymer-1 mixture satisfying claim 1 limits
  • pharmaceutically acceptable excipient

This claim is the infringement bridge for product formulations: it requires the copolymer mixture plus excipient and therapeutic efficacy for MS.

Claims 13-21

• Mirror the copolymer distribution limitations:
  • >75% in 2-20 kDa (claims 13, 15, 20)
  • <5% over 40 kDa (claims 14, 15)
  • <2.5% over 40 kDa (claims 19, 20)
  • Average MW bands: 6.25-8.4 kDa (claim 16), 4-8.6 kDa (claim 17), 5-9 kDa (claim 18)
  • Claim 21 has an apparent internal transcription error: “8 4 kilodaltons” should be read as 8.4 given the repeated band in other claims.

Claim 22

• Distribution shape match: “substantially as depicted” in FIG. 1 or FIG. 2 with average ~7.7 kDa.

Method claims (23-33)

Each method claim is the same structure: administer the pharmaceutical composition of the corresponding earlier claim to a patient with MS.

• Claim 23 administers claim 12 pharma composition
• Claims 24-33 map to the dependent pharma compositions (claims 13-22)

Practical scope impact

• These method claims are likely to be enforced against the use of formulations that meet the earlier pharmaceutical composition limitations, not merely the bulk copolymer ingredient.

How does US 6,939,539 sit inside the broader “copolymer-1” patent landscape in the U.S.?

Given only the claim text you provided, the landscape analysis below focuses on claim-type segmentation and where patentability/infringement fights typically occur for copolymer-1 MS assets.

Landscape segmentation by patent category (relevant to enforcement)

Category	What it tends to cover	How US 6,939,539 fits
Molecular-parameter identity	Specific MW distribution/average and heterogeneity parameters that define a “product-like” copolymer-1	Central: average MW 4-9 kDa, tail constraints (<5% or <2.5% over 40 kDa), and optional shape match to FIG. 1/F2
Sequence and residue composition	Residue makeup and copolymer structure definition	Core limitation: Glu/Lys/Ala/Tyr
Formulation + therapeutic method	Excipients + patient treatment for MS	Provided by claims 12-33 (pharma composition + MS administration)
Manufacturing process	How the copolymer is made, purification, fractionation	Not present in the provided claims; US 6,939,539 scope appears formulation and product-parameter driven rather than process driven

Enforcement leverage points created by this claim set

1. Tail control creates “process-linked product” risk

   • Even without explicit process claims, the distribution constraints are strongly linked to preparation and fractionation.
   • A competitor can try to meet average MW but fail tail percent constraints.

2. Distribution-shape claim is a high-specificity hook

   • Claim 11/22’s “substantially as depicted in FIG. 1 or FIG. 2” creates an evidentiary target: competitor analytics can be compared to the patent’s reference curves.

3. Method-of-use is tethered to the formulation

   • If a product is reformulated with different MW distribution boundaries, it can avoid method claim coverage even if it still treats MS.

Where are the likely “design-around” vectors under this claim language?

A design-around is constrained to the claim’s explicit limits, particularly the molecular weight profile and residue composition.

Vector A: adjust residue composition

• Deviate from polypeptides “composed of” Glu, Lys, Ala, Tyr.

Vector B: keep the same residues but alter molecular weight distribution

• Move average MW out of the claimed bands (base claim 1: ~4 to ~9 kDa).
• Increase the high-end tail above claim thresholds:

  • 5% over 40 kDa (to avoid claims requiring <5%)

  • 2.5% over 40 kDa (to avoid the tighter versions)

• Reduce the fraction within 2-20 kDa below 75% (to avoid claims requiring >75%).

Vector C: alter heterogeneity characterization

• Produce a mixture that is more uniform in molecular weight and/or sequence such that it no longer meets “non-uniform with respect to molecular weight and sequence.”

Vector D: escape the FIG. 1/FIG. 2 match

• Even if average MW is near 7.7 kDa, shift the distribution shape so it is not “substantially as depicted.”

What would be the claim scope in litigation terms?

Independent vs dependent structure

• Independent claim 1 defines the base copolymer mixture with residue composition, MW average range, non-uniformity, and MS suitability.
• Dependent claims narrow using numeric distribution constraints and optional FIG curve matching.
• Independent claim 12 (as provided) defines the pharmaceutical composition by adding excipient and therapeutically effective MS dosing.
• Independent claim 23 (as provided) is method-of-treatment, directly tethered to claim 12.

Built-in narrowing

Because the dependent claims require the same base copolymer definition and then add precise numeric filters, an accused product only needs to miss one core limitation of the asserted claim to avoid that specific dependent claim. For example:

• meeting average MW but failing the <5% >40 kDa limitation misses claims 3 and 14, and any downstream claim that incorporates them (depending on which dependents are asserted).
• meeting residue composition and average MW but failing “non-uniform” misses claim 1 and therefore claim 12 and associated method claims.

Key Takeaways

• US 6,939,539 is a product-parameter-driven copolymer-1 patent: it anchors residue content (Glu/Lys/Ala/Tyr), requires non-uniform molecular weight and sequence, and imposes tight molecular weight distribution constraints (average MW bands plus molar fraction limits and optional FIG. 1/F2 distribution-shape matching).
• The patent landscape implications are practical: even without explicit manufacturing process claims, the strict distribution limits make the claimed “copolymer-1” functionally similar to a specified product grade and create design-around space primarily through MW distribution engineering and heterogeneity control.
• Enforcement coverage extends through pharmaceutical composition (copolymer + excipient + therapeutically effective MS dosing) and method-of-treatment claims, but method claims are tethered to meeting the pharmaceutical composition limitations.

FAQs

1) What single measurement most controls whether a product can infringe?

Average molecular weight and distribution tail metrics, because the claims require both average MW ranges and explicit molar fraction thresholds (for 2-20 kDa and for >40 kDa).

2) Does the patent require a specific dosing regimen?

The method and pharma claims require a “dose therapeutically effective to treat multiple sclerosis” but do not specify a numeric dosing schedule in the claim text you provided. Scope still depends on administering the claimed pharmaceutical composition.

3) Can a competitor use the same residues but a different MW distribution?

Yes. The claims can be avoided by shifting:

• average MW outside the defined bands, and/or
• the molar fraction above 40 kDa above the stated limits,
• and/or the fraction in 2-20 kDa below 75%.

4) What does “substantially as depicted in FIG. 1 or FIG. 2” change?

It adds an evidence-driven distribution-shape limitation tied to reference curves, making infringement depend not only on numeric averages and percent cutoffs, but also on whether the distribution shape matches the patent’s reference profile.

5) Are the method claims broader than the composition claims?

No. Each method claim is tethered to administering the pharmaceutical composition of specific dependent claims, so method scope is no broader than the underlying MW/distribution/residue limitations.

References

[1] Provided claim text for US 6,939,539 (claims 1-33) in the user prompt.

Drugs Protected by US Patent 6,939,539

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 6,939,539

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0762888		90987	Luxembourg
European Patent Office	0762888		C300096	Netherlands
European Patent Office	0762888		C300251	Netherlands
Austria	212857