Details for Patent: 5,767,082

Summary for Patent: 5,767,082

Title:	Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists
Abstract:	Synthetic nona- and decapeptide LHRH antagonist analogs are disclosed, having a sterically hindered guanidino-substituted arginyl or homoarginyl residue at position 8, with no arginyl substituent at position 6.
Inventor(s):	John J. Nestor, Jr., Brian H. Vickery
Assignee:	Roche Palo Alto LLC
Application Number:	US08/526,940
Patent Claim Types: see list of patent claims	Use; Composition;

US Patent 5,767,082 Landscape: Scope, Claim Coverage, and Competitive Patent Risk for Methods Targeting Ovulation, PMS, Endometriosis, BPH, Spermatogenesis, Precocious Puberty, Heat Interruption, and Pregnancy Termination

US Patent 5,767,082 is drafted as a broad method-of-treatment and method-of-contraception style claim set using a constrained peptide-structure genus (and specific subgenus and single compound) plus pharmaceutically acceptable salts and compositions. The independent claim structure drives the estate’s practical scope: the patent covers administering an “effective amount” of (i) defined peptide compounds (formula/genus), (ii) salts, and (iii) compositions, for a wide list of reproductive indications across species.

Because your prompt provides only the claim text (not the specification, preferred embodiments, dependent claims, prosecution history, prosecution disclaimers, or the full claim set), the analysis below is limited to what can be derived strictly from the independent claim language you quoted.

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What do the claims in US 5,767,082 actually cover (scope of protection)?

Short answer: The patent protects method claims that require administration of a member of a specific peptide chemical space (defined by amino-acid residue variables and specific residue identities) for reproductive and fertility-related outcomes, plus salts and pharmaceutical compositions.

Independent claim architecture

All three independent claims you provided follow the same core pattern:

1. A method of treating or inhibiting reproductive processes (with multiple indication options in the preamble).
2. An administration step: “administering… an effective amount” of:
   • (a) at least one member of a defined chemical group (formula-genus in claim 1 or defined residue mapping in claim 2), or
   • (a) a specific compound explicitly named (claim 3),
   • plus (b) salts, and
   • (c) pharmaceutical compositions with excipients.

Practical consequence: A competitor who markets an alternative peptide that falls outside the residue-variable constraints likely avoids literal infringement of these independent claims. A competitor who uses one of the claimed peptides for one of the listed method outcomes is structurally at risk.

Indications (what outcomes are claimed)

Each claim’s preamble includes a wide list of methods/indications. Based on your text, the scope includes:

• Inhibiting ovulation (female mammalian)
• Preventing ovarian hyperstimulation in response to exogenous gonadotropins (female human/mammal subject as stated)
• Treating premenstrual syndrome (PMS) (female human)
• Treating endometriosis (female human)
• Treating prostatic hypertrophy (BPH) (male mammalian)
• Inhibiting spermatogenesis (male mammalian)
• Treating precocious puberty (human)
• Interrupting heat (female animal)
• Terminating pregnancy (female mammalian)

Practical consequence: This is not limited to “contraception.” The claims cover multiple reproductive and endocrine outcomes, including human disorders (PMS, endometriosis, precocious puberty) and male fertility (spermatogenesis), plus an animal “heat” interruption indication.

Species coverage

The preambles are mixed:

• “female mammalian,” “female human subject,” “male mammalian,” “human,” “female animal subject,” “female mammalian” again for pregnancy termination.

Practical consequence: Even if a competitor uses the same peptide in a non-human veterinary program, the “heat interruption” pathway is explicitly included.

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How does US 5,767,082 define the active compounds (chemical claim scope)?

Short answer: The active ingredient must match a constrained peptide genus defined by residue identity at several positions plus additional structural variable ranges (notably the “G” radical and an amino-acyl residue mapping).

Claim 1: broad genus with residue-variable definitions

Claim 1 defines “compound of the formula” and then maps amino-acyl residues A through F and a more complex residue/radical selection for G, plus a terminal or amide portion J.

Key features from your claim text:

• A is selected from either D- or L- isomer versions of specific amino-acyl residues (examples listed include N-Ac-D,L-Δ3,4-prolyl, N-Ac-D,L-prolyl, N-Ac-D,L-phenylalanyl, p-chlorophenylalanyl, p-fluorophenylalanyl, various naphthyl-substituted D/L alanines, and N-Ac-2,4,6-trimethylphenylalanyl).
• B, C, D, E, F are each constrained to defined residue sets (multiple D- and/or L- aromatic or heteroaromatic substitutions appear, plus select polar residues like Tyr/Arg/Glu(AA), and specific dehydro/amide-related residue options appear later in the mapping).
• G is the most structurally complex block. It is defined by:
  • “radicals represented by structural formulae” with n = 1 to 5, and R1 and R2 substituent rules, and additional ring/hetero rules using variables m, A, X, and another set with R3 and J.
• J is defined as D-alaninamide, D-leucinamide, glycinamide, or --NHR4 where R4 is lower alkyl or NHCONH2.

Practical consequence: Claim 1’s literal coverage depends on (i) matching each position’s allowable residue list and (ii) matching the G block’s multi-variable radical templates.

Claim 2: narrower residue mapping to specific choices

Claim 2 defines a compound of another “formula” but then locks each position to a set of specific residues and one amide:

• A = N-Ac-D-Nal(2)
• B = D-pCl-Phe
• C = D-Pal(3)
• D = Pal(3), Tyr, Arg, Deh, Mbh, or Bth
• E = D-Pal(3), D-Tyr or D-Deh
• F = Leu
• G = Deh, Bth, or Mbh
• J = D-AlaNH2

Practical consequence: Claim 2 is a constrained subgenus relative to claim 1 (fewer degrees of freedom). It is more likely to be infringed by close analogs that keep the fixed residues at A/B/C/F/G/J while varying only the permitted options at D and E.

Claim 3: single-compound “exact” amino-acid sequence coverage

Claim 3 recites a specific compound:

N-Ac-D-Nal(2)-D-pCl-Phe-D-Pal(3)-Ser-Tyr-D-Deh-Leu-Deh-Pro-D-AlaNH2

It also covers:

• “an optical isomer thereof”
• pharmaceutically acceptable salts

Practical consequence: Claim 3 provides a strong anchor point for infringement if a competitor sells a product with this exact sequence (or an optical isomer not excluded by stereochemical limitation) in method use.

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How much flexibility do these claims allow for formulation and salts?

Short answer: The claims include pharmaceutically acceptable salts and “a pharmaceutical composition” with excipients, but the active ingredient must still satisfy the peptide-genus or exact-compound constraints.

Salt coverage

All three claims explicitly include:

• “a pharmaceutically acceptable salt of said compound”

Practical consequence: Salt-form changes (e.g., acetate, hydrochloride, etc.) do not avoid the claims if the underlying peptide is within the defined structures.

Composition coverage

Claim 1 and 2 include:

• “a pharmaceutical composition containing at least one compound… in admixture with a pharmaceutically acceptable excipient.”

Practical consequence: Infringement risk is not restricted to a particular dosage form in the quoted claims. Even if administered via a specific formulation type, as long as it’s a pharmaceutical composition containing the claimed peptide and is used for an enumerated method outcome, these claims remain relevant.

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What is the claim strength profile for US 5,767,082 (literal vs design-around risk)?

Short answer: The estate is structurally strong against close peptide analogs but invites easier design-around via out-of-scope residue substitutions or by avoiding the specific enumerated “method outcomes” in human labeling and/or actual use.

Design-around levers

Based on the residue-variable constraints, practical freedom areas for competitors include:

• Substitute at one of the controlled positions (A–F or G) with residues outside the allowed sets.
• Use a different C-terminus (J) if it falls outside D-AlaNH2 / D-leucinamide / glycinamide / specified NHR4 alternatives.
• Change the radical/G block beyond the structural templates.

Method-of-use levers

The preamble lists particular outcomes. A key litigation risk point is how courts construe “method of treating” vs. “method of inhibiting” and whether off-label physician use or actual commercial practice can satisfy the method claim elements.

Operationally: If the commercial product is marketed for different indications not listed, method-of-use enforcement becomes narrower. If the product is used in practice for any of the enumerated outcomes, the claims are directly implicated.

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How do US 5,767,082 claims compare across claims 1, 2, and 3 (coverage overlap)?

Short answer: Claim 1 is the broadest genus; claim 2 is a tighter subgenus with fixed residues; claim 3 is a single sequence anchor.

Coverage hierarchy

• Claim 1 (genus): largest set of peptide compounds permitted by residues A–G and terminal J options.
• Claim 2 (subgenus): many residues are fixed (A, B, C, F, J) with limited permitted alternatives at D and E and for G.
• Claim 3 (single compound): exact 10-residue style peptide sequence with specific stereochemical identifiers and included “optical isomer” coverage.

Litigation implication

In infringement arguments:

• Plaintiff can assert claim 3 for a direct match to the sequence.
• If no exact match exists, plaintiff can attempt claim 2 (subgenus match) and then claim 1 (genus match) as a fallback ladder.

In defense:

• A design-around can attempt to miss at a single critical residue position to fall outside the genus, but the defendant still faces risk if the chosen residue combination lands within another claim’s allowed options (especially at D/E positions in claim 2).

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What “patent landscape” in the US likely surrounds a method-of-treatment peptide like this?

Short answer: Even without the rest of the patent list (not provided in your prompt), the typical ecosystem around early peptide method-of-use patents includes: companion composition/formulation patents, additional sequence analog patents (same therapeutic target, broader or narrower residues), and process/manufacturing patents for the peptide synthesis.

Because only US 5,767,082 claim text was supplied, the landscape below is limited to what can be concluded from the claim structure itself:

Expected adjacent patent categories (based on claim content)

1. Sequence/analog patents
   • Variations on one or more residues within the A–G blocks.
2. Salt-form patents
   • Specific salts for improved stability or pharmacokinetics.
3. Formulation patents
   • Delivery system modifications (injectable depot, sustained release, etc.) that still contain the same active peptide.
4. Method-of-use patents
   • Additional reproductive indications or dosing regimens (not shown in the provided claims, but common as dependent claim sets and later filings).

Litigation posture likely shaped by breadth

The combination of:

• broad reproductive method preamble,
• genus chemical claims,
• explicit exact-sequence claim, creates an enforcement pathway that can reach both direct peptide copies and some “close analog” generics, depending on how those analogs map to the residue constraints.

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Key takeaways for R&D, licensing, and generic design-around

1. The invention is anchored to specific peptide residue constraints. Literal infringement turns on whether the competitor’s peptide matches the permitted amino-acyl residue choices (A–F and especially G) and the terminal J options, or matches the exact sequence in claim 3.
2. Method-of-use coverage is broad across reproductive outcomes. The claims list multiple female and male fertility-related endpoints, human and animal contexts, and both fertility inhibition and pregnancy termination.
3. Salts and basic composition with excipients are included. Salt switching and standard excipient formulation do not avoid coverage if the active peptide remains within the claimed structures.
4. Claim 3 is a direct-sequence enforcement hook. If a product contains the exact peptide sequence provided, the risk against that product’s method use is high under claim 3’s literal terms.
5. Design-around is feasible but residue-sensitive. Avoidance likely requires stepping outside at least one residue position’s allowed set or stepping outside the G radical templates rather than relying on salt/formulation changes.

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FAQs

1. Do US 5,767,082 claims cover both contraception and disease indications like endometriosis?
   Yes. The preamble expressly includes inhibiting ovulation and treating PMS and endometriosis, among other reproductive outcomes.

2. Can a competitor avoid infringement by changing only the salt form of the peptide?
   Not if the underlying peptide compound is within the claimed structure. The claims expressly include pharmaceutically acceptable salts.

3. How much narrower is claim 2 compared with claim 1?
   Claim 2 fixes multiple residues (A, B, C, F, J) and restricts alternatives primarily at D and E and for G to a limited set, making it a subgenus compared with claim 1’s wider residue choices.

4. Does claim 3 require the exact peptide sequence, or does it allow variants?
   Claim 3 includes the exact sequence and “an optical isomer thereof,” plus salts. Non-isomer sequence changes are not covered by claim 3’s literal language.

5. Is the patent limited to a specific dosage form or route in the provided claims?
   No. The claims require administration of an effective amount and include compositions with pharmaceutically acceptable excipients, without restricting route or specific dosage form in the quoted claim text.

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References

1. United States Patent 5,767,082. (Claim text provided in prompt).

Drugs Protected by US Patent 5,767,082

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 5,767,082

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0277829		SPC/GB00/024	United Kingdom
European Patent Office	0277829		2000C/030	Belgium
European Patent Office	0277829		C300016	Netherlands