Details for Patent: 6,071,970

Summary for Patent: 6,071,970

Title:	Compounds active at a novel site on receptor-operated calcium channels useful for treatment of neurological disorders and diseases
Abstract:	Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, epilepsy, anxiety, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).
Inventor(s):	Alan L. Mueller, Manuel F. Balandrin, Bradford C. VanWagenen, Eric G. DelMar, Scott T. Moe, Linda D. Artman, Robert M. Barmore
Assignee:	Shire NPS Pharmaceuticals Inc
Application Number:	US08/485,038
Patent Claim Types: see list of patent claims	Use; Composition;

United States Patent 6,071,970: Scope, Claim Map, and Competitive Patent Landscape (Neuroprotection and Neurological Disease Methods)

What is US 6,071,970 claiming at a high level?

US 6,071,970 claims a family of substituted chemical compounds (core “Formula I/IV/V/VI/VII”-type scaffolds) and a broad set of pharmaceutical product and method claims oriented to neurological diseases. The claims fall into four enforceable layers:

1. Product (compound) claims: composition of matter covering a structurally defined compound genus with multiple variable groups.
2. Product (pharmaceutical composition) claims: formulations comprising the claimed genus, in pharmaceutically acceptable carriers, including broad salt coverage.
3. Product (specific compound selections): claim sets that narrow to explicit structures (where the patent includes enumerated selections).
4. Use claims (methods): administering the compounds for neurological indications, including stroke and a long list of neurodegenerative/psychiatric disorders, plus “neuroprotection” framing.

The claim set is designed for genus-level coverage (large chemical space) plus indication-level coverage (broad clinical endpoints and subtypes) plus salt/form/complextreatment coverage.

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How broad is the chemical genus in the compound claims (Claims 1–3 and related)?

Core structural variables

Across the compound claims (e.g., Claim 1 and Claim 2), the patent uses repeating variable definitions to expand the genus:

• Aromatic substituent positions (“each X”):
  • X is independently selected from: meta-fluoro, meta-chloro, ortho-methoxy, ortho-methyl
• R1/R2 patterns (alkyl/H or linked methylene chain):
  • R1/R2 configurations include:
  • R1 = methyl, R2 = H
  • both are H
  • R2 = methyl, R1 = H
  • R1 and R2 together = --(CH2)n-- where n = 1 to 6
• R3 (independent toggle):
  • R3 is either H or methyl
• Exclusion carve-outs in Claim 1:
  • Excludes cases where:
  • R3 = H and each X is all meta-chloro, or all meta-fluoro, or one meta-fluoro and one meta-chloro.

Claim 1 versus Claim 2

• Claim 1 uses the X set limited to meta-fluoro, meta-chloro, ortho-methoxy, ortho-methyl, and includes a negative limitation excluding specific X/R3 combinations.
• Claim 2 uses essentially the same variable framework but does not include the Claim 1 exclusion language (it is framed as “wherein … and R3 is either --H or methyl; and n is an integer …” without the excluded subset language).

Business implication: Claim 1 narrows the genus by excluding select halogen/position patterns, while Claim 2 preserves those patterns, improving coverage for design-arounds that only partially shift substitution patterns.

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What exactly are the enforceable product claims?

Pharmaceutical compositions with broad “neurological disease” use language (Claims 12–19, 23–29, 30–32)

A central composition claim is Claim 12, which ties the chemical genus to formulations:

• Claim 12: pharmaceutical composition “adapted for the treatment of a neurological disease or disorder” comprising a compound of a formula where:
  • R1 and R5: each independently from H, alkyl, hydroxyalkyl, OH, O-alkyl, O-acyl
  • R2 and R6: each independently from H, alkyl, hydroxyalkyl
  • R1/R2 may be connected: together are --(CH2)n--
  • R3: from H, alkyl, 2-hydroxyethyl
  • X positions: meta- or ortho- independently from H, Br, Cl, F, CF3, alkyl, OH, O-alkyl, O-acyl
  • m: 0 to 5
  • includes pharmaceutically acceptable salts in pharmaceutically acceptable carrier

Claim 13 expands coverage to:

• “pharmaceutically acceptable complex” (composition claim with additional product form).

Claims 15–17 and 23: additional formula-specific pharmaceutical composition claim sets derived from the same core chemotype, but with additional restrictions (e.g., choice sets for X, R3, m, and defined structural formula illustrations).

“Selected compound” compositions (Claims 19–22, 25–29)

• Claim 19: pharmaceutical composition comprising a compound selected from enumerated structure drawings (and salts).
• Claims 20–22: further narrow those selections.
• Claims 25–29: multiple compositions each keyed to additional explicit structural drawings.

Salt breadth (Claim 32)

• Claim 32 explicitly lists a large pharmaceutically acceptable salt portfolio, including:
  • common organic/inorganic salts (acetate, citrate, fumarate, malate, succinate, sulfate, etc.)
  • many specialty salts (camsylate, edisylate, besylate, gluceptate, etc.)
  • includes salts such as hydrochloride via separate dependent claims (e.g., Claims 18, 22, 56).

Business implication: The salt list materially increases formulation freedom and reduces the impact of salt-based design-around.

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How does the patent frame “neuroprotection”?

The patent runs parallel product and method claim tracks using “neuroprotection” language.

Neuroprotection composition (Claims 45–50)

• Claim 45: pharmaceutical composition adapted to provide neuroprotection, comprising a compound having a defined formula with:

  • R1/R5, R2/R6 similar to Claim 12 style ranges
  • R3 either H, alkyl, or 2-hydroxyethyl
  • n = 1 to 6
  • X restricted with meta- or ortho- position emphasis (Claim text indicates “meta- or ortho-3position” with X options H, Br, Cl, F, CF3, alkyl, OH, O-alkyl, O-acyl)
  • m = 0 to 5
  • salts included

• Claim 50: neuroprotection composition comprising a compound selected from enumerated structures and salts.

Neuroprotection methods (Claims 158–185)

• Claim 158: method for providing neuroprotection to a patient by administering a compound with broad structural variables.
• Claims 172–184: dependent variants emphasizing:
  • R3 as NH2 or NH-methyl
  • (X)m limited to meta-/ortho- fluorine/chloro/methoxy/methyl set
  • and inclusion of specific neuroprotection compound selections.

Business implication: “Neuroprotection” framing is used to preserve enforcement even when the indication label changes (or is argued as disease-modifying rather than symptom controlling).

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What indications are covered in the methods and composition “adapted” language?

Stroke subtypes are explicitly covered

Multiple dependent claims call out stroke variants:

• Claims 33–34–35: composition adapted for:
  • stroke (Claim 33) with subtypes:
  • global ischemic (Claim 42)
  • hemorrhagic (Claim 43)
  • focal ischemic (Claim 44)
• Additional neurological indications in the list:
  • head trauma (Claim 34)
  • spinal cord injury (Claim 35)

Long indication list for “neurological disease or disorder”

From Claim 36–41 and Claim 93:

• epilepsy (Claim 36 / also in Claim 93 set)
• anxiety (Claim 37)
• Alzheimer’s disease (Claim 38)
• Huntington’s disease (Claim 39)
• Parkinson’s disease (Claim 40)
• amyotrophic lateral sclerosis (Claim 41)

Method claims mirror the same list.

• Claim 93: method covers stroke, head trauma, spinal cord injury, epilepsy, anxiety, Alzheimer’s, Huntington’s, Parkinson’s, ALS.

Business implication: The patent is built to support multiple label strategies and to catch competitors targeting different endpoints within the same chemotype.

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What are the method-of-treatment claim scopes?

General method for treating neurological disease (Claims 57–67, 72–79, 85–104, 99–105, etc.)

Key method scaffolding includes:

• Claim 57: administering a compound with an R3/NH2 or NH-methyl framing and X/m patterns and specific R1/R2 arrangements.

• Claims 59–67: strokes with:

  • global ischemic
  • focal ischemic
  • hemorrhagic

• Claim 63: neurological disease may be neurodegenerative disease (broadening).

• Claims 64 and 71: administering compounds having specific “structure of Formula IV/V/VI/VII” types with:

  • n = 1 to 6
  • X from H/Br/Cl/F/CF3/alkyl/OH/O-alkyl/O-acyl
  • R3 from H/alkyl
  • m = 0 to 5
  • salts included

• Claims 72–88: administering compounds selected from enumerated groups and specific formula subgroups; include complex formation dependent claims.

Alternative formula-based method claims (Claims 118–145)

The patent includes “Formula I” style methods:

• Claim 118: method administering “compound of Formula I” where:

  • R1 and R5 are independently from H, alkyl, hydroxyalkyl, OH, O-alkyl, O-acyl
  • R2 and R6 from H, alkyl, hydroxyalkyl
  • includes configurations where R1/R2 together are:
  • --(CH2)n--
  • or --(CH2)n--N(R3)--
  • R3 selected from H, alkyl, 2-hydroxyethyl
  • R4 selected from alkyl or cycloalkyl (plus enumerated structure portion in text)
  • X from Br/Cl/F/CF3/alkyl/OH/O-alkyl/O-acyl
  • m = 1 to 5
  • Y depends on the R1/R2 connection
  • salts included

• Dependent claims tie Formula I methods back to narrower “Formula III/VI/VII”-type structures (Claim 119 and Claim 122).

Business implication: enforcement can be pursued along multiple drafting routes: generic formula genus claims, sub-genus “selected structures,” and formula-figure-based method claims.

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What does the claim strategy reveal about likely infringement risk?

The claims combine:

1. Large chemical variable ranges

   • R1/R5 and R2/R6 are not limited to a narrow set; they include hydroxyalkyl and O-substitutions and O-acyl.
   • X includes H and multiple halogens and CF3 plus alkyl and oxygenated substituents.
   • m = 0 to 5 allows multiple substitution counts.

2. Multiple independent R-parameter frameworks

   • There are several formula “families” (Claims 1–3 and multiple later method claims) that overlap in variable sets.

3. Indication clauses that reduce therapeutic narrowing

   • “adapted for the treatment” and method claims list multiple neurological disorders including stroke subtypes.
   • This makes design-around harder if competitors position the same compounds for different neurological therapeutic claims.

4. Formulation and salt fallback

   • complex and broad salt lists reduce the likelihood that a competitor can avoid infringement by changing only salt form.

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Where are the enforceability pressure points (claim narrowing and exclusions)?

Claim 1 exclusion (subset carve-out)

The strongest express chemical narrowing is in Claim 1’s exception:

• R3 = H and X is either:
  • all meta-chloro, or
  • all meta-fluoro, or
  • one meta-fluoro and one meta-chloro.

This exclusion is absent from Claim 2’s text (based on the claim language you provided), so Claim 2 likely covers the excluded patterns.

R3 variation split (H vs alkyl vs 2-hydroxyethyl vs NH-methyl)

The patent uses:

• R3 as methyl/H in some compound claims,
• R3 as 2-hydroxyethyl in composition/neuroprotection,
• R3 as NH2/NH-methyl in other sets.

That split suggests the drafter expected multiple analog series and built multiple claim lanes.

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Competitive patent landscape: what can be inferred from the claim architecture?

This section focuses on how competitors typically collide with patents like this, based on claim structure.

Primary infringement avenues for competitors

1. Compound selection inside the genus

   • If a competitor synthesizes a substituted analog using the same aromatic ring pattern set (meta-fluoro/meta-chloro/ortho-methoxy/ortho-methyl or broader X sets with Br/Cl/F/CF3/oxygenated substituents) and uses the same R1/R2 connected chain logic (including n 1–6), they are at high risk.

2. Using the compounds in neuroprotection or neurological disease methods

   • Even if a competitor argues disease is framed differently, the patent lists a wide set of neurological indications and subtypes, including stroke subtypes.
   • Dependent claims lock in subtypes (global ischemic, focal ischemic, hemorrhagic), reducing flexibility if the target market is stroke.

3. Salt/form/complex strategy

   • Broad salt claims (Claim 32) and explicit hydrochloride dependent claims widen coverage across common formulation practices.

Likely design-around themes that may or may not succeed

• Changing aromatic substitution set
  If a competitor uses different halogens or does not maintain the meta/ortho constraints and allowed X set, they may reduce literal overlap with X-defined formulas.

• Changing R3 functionality
  Moving away from NH2/NH-methyl where those dependent method claims anchor, or away from 2-hydroxyethyl in neuroprotection composition claims, may reduce fit with some narrower claim subgroups.

• Changing R1/R2 linkage Some claims require R1 and R2 to be connected as --(CH2)n-- (or --(CH2)n--N(R3)--). Competitors that remove that linkage could avoid certain formula-lane claims, but they may still land inside other independent claims unless they fully exit the genus.

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Key takeaways

• US 6,071,970 is a genus-driven chemical patent with broad substituent definitions (X, m, R1/R5 and R2/R6 oxygenated and alkyl/hydroxyalkyl ranges) and multiple independent claim lanes.
• The patent’s enforcement focus is not only “compound” but also pharmaceutical composition and method-of-use, including stroke subtypes and a broad neurological indication list.
• Neuroprotection is treated as a parallel claim track, expanding enforcement across disease-modifying positioning.
• Salt and complex coverage materially reduces formulation-based design-around options.
• The main internal narrowing is in Claim 1’s exclusion, but the patent includes other independent claims (e.g., Claim 2 and later method/formula claims) that likely preserve the excluded subset.

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FAQs

1) Does the patent cover both compounds and methods?

Yes. It includes product claims (compound genus and pharmaceutical compositions) and multiple method-of-treatment claims for neurological diseases and disorders, including stroke subtypes.

2) What are the most specific indications within the claim set?

Stroke subtypes are explicitly specified: global ischemic, focal ischemic, and hemorrhagic.

3) How is the chemical scope expanded?

Through variable definitions for aromatic substituents (X), oxygenated/alkyl options for R1/R2/R5/R6, chain length parameter n (1 to 6), and substitution count parameter m (0 to 5).

4) Can a competitor avoid infringement by switching salts?

The patent lists a very broad set of pharmaceutically acceptable salts (including hydrochloride explicitly). Salt switching alone is unlikely to move outside the claim coverage.

5) What does “neuroprotection” add to the landscape?

It creates separate composition and method claim lanes that can capture use arguments even when the indication is described under neuroprotective framing rather than a single labeled disease.

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References

[1] United States Patent No. 6,071,970. Claims and claim language as provided.

Drugs Protected by US Patent 6,071,970

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 6,071,970

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	200862
Austria	238782
Austria	346595