Scope, Claims, and U.S. Patent Landscape for RE46792 (Oxazole Dermatosis Agents)
RE46792 is a U.S. reissue patent directed to oxazole-containing compounds and related salts, pharmaceutical compositions, and dermatosis treatment methods. The claim set spans (i) broad chemical Markush structures for oxazole core analogs, (ii) narrower sub-generic embodiments tied to specific R-group classes, and (iii) product-level coverage over enumerated candidate compounds and a single specifically named compound. It also claims downstream uses (composition and dermatosis treatment) and an example production process.
What does RE46792 claim, structurally?
1. Core scaffold: oxazole compound defined by Formula (1)
Independent claim 1 covers “an oxazole compound represented by Formula (1)” with three principal variable components:
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R1: an aryl group with substituent options (1-1) to (1-11)
Substituent categories include:
- hydroxy groups (1-1)
- unsubstituted or halogen-substituted lower alkoxy (1-2)
- lower alkenyloxy (1-3)
- lower alkynyloxy (1-4)
- cyclo C3-8 alkyl lower alkoxy (1-5)
- cyclo C3-8 alkyloxy (1-6)
- cyclo C3-8 alkenyloxy (1-7)
- dihydroindenyloxy (1-8)
- hydroxy lower alkoxy (1-9)
- oxiranyl lower alkoxy (1-10)
- protected hydroxy groups (1-11)
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R2: either an aryl group or a nitrogen-containing heterocyclic group, each with substituent options (2-1) to (2-10)
Substituent categories include:
- hydroxy groups (2-1)
- unsubstituted or halogen-substituted lower alkoxy (2-2)
- unsubstituted lower alkyl (2-3)
- lower alkenyloxy (2-4)
- halogen atoms (2-5)
- lower alkanoyl groups other than formyl (2-6)
- lower alkylthio (2-7)
- lower alkylsulfonyl (2-8)
- oxo groups (2-9)
- lower alkoxy lower alkoxy (2-10)
If R2 is the nitrogen-containing heterocycle, it is restricted to a defined list (from imidazolidinyl through benzothiadiazolyl and related N-oxides).
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W: a divalent linker group constrained by Formula (i), Formula (ii), or Formula (iii)-type alternatives
Claim 1 defines W via:
- Formula (i): —Y1-A1—
- A1 is a lower alkenylene group or a lower alkylene group that may carry hydroxy or lower alkoxycarbonyl substituents
- Y1 can be:
- —C(═O)—
- —C(═O)—N(R3)—
- —S(O)m—NH—
- —S(O)n— wherein R3 is H or lower alkyl, and m,n are 0 to 2
- Formula (ii): —Y2—C(═O)—
- Y2 is a piperazinediyl group
- Formula (iii): —C(═O)-A2-N(R5)—
- A2 is a lower alkylene group
- R5 is H or lower alkyl
Claim 1 also covers salts (“or a pharmaceutically acceptable salt thereof”).
Practical read-across for scope: claim 1 is broad at the “system level” (oxazole core + variable aryl/heteroaryl substitution and defined linker classes). It is not open-ended across linker chemistry; Y1/Y2/Y2 are constrained to carbonyl/sulfonamide/sulfonyl or piperazine-like motifs.
2. Sub-generic tightening: claims 2 to 6
Claims 2 through 6 narrow the R-group space to specific aryl/heteroaryl combinations and specific W subset.
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Claim 2 narrows:
- R1 is phenyl with 1 to 3 substituents drawn from (1-2), (1-3), (1-4), (1-5)
- R2 is phenyl or pyridyl with 1 to 3 substituents drawn from (2-2), (2-3), (2-4), (2-5)
- W is limited to Formula (i) with Y1 = —C(═O)— or —C(═O)—N(R3)— and R3 = hydrogen
-
Claim 3 further narrows:
- R1 phenyl with two substituents from the same categories as claim 2
- R2 phenyl or pyridyl with one to two substituents from the same categories as claim 2
- W stays in Formula (i) with A1 lower alkylene and Y1 limited to carbonyl or carbonyl-amide carbonyl form (with R3 = H)
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Claim 4 narrows to specific substitution patterns for both R1 and R2, and fixes W to Formula (i) with:
- A1 = C1-4 alkylene
- Y1 = —C(═O)— or —C(═O)—N(R3)— (R3 = H)
R1 is limited to enumerated phenyl substitution scenarios (two alkoxy; one alkoxy + one cyclo-C3-8 alkyl alkoxy; one alkoxy + one halogen-substituted lower alkoxy; one alkoxy + one alkenyloxy; one halogen-substituted alkoxy + one cyclo alkyl alkoxy; one halogen-substituted alkoxy + one alkenyloxy; or two halogen-substituted alkoxy).
R2 is limited to:
- lower alkoxyphenyl
- lower alkenyloxyphenyl
- halogen-substituted lower alkoxyphenyl
- lower alkylpyridyl
- phenyl with one lower alkoxy and one halogen
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Claim 5 narrows claim 4 further:
- R1 substitution limited to the specific sets where W has Y1 = —C(═O)—
- R2 likewise constrained to lower alkoxyphenyl / lower alkenyloxyphenyl / halogen-substituted lower alkoxyphenyl / lower alkylpyridyl / or phenyl with one alkoxy and one halogen.
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Claim 6 narrows again:
- R1 substitution restricted to three specific patterns (one alkoxy + one halogen-substituted alkoxy; one halogen-substituted alkoxy + one cyclo C3-8 alkyl alkoxy; one halogen-substituted alkoxy + one alkenyloxy)
- R2 restricted to lower alkoxyphenyl or lower alkylpyridyl
- W limited to Formula (i) with Y1 = —C(═O)—N(R3)— and R3 = H
Practical read-across: claims 2-6 progressively funnel into a narrower linker and narrower aromatic substitution patterns, setting up the later compound listing in claim 10 and the single compound in claim 11. The claims do not merely “recite examples”; they impose hard structural limits.
What is claimed for formulations and medical use?
Pharmaceutical composition (Claim 7 and 12 and 15)
- Claim 7: a pharmaceutical composition with the compound (claims 1 to 6) as active ingredient and a pharmaceutically acceptable carrier.
- Claim 12: composition with the compound of claim 11.
- Claim 15: composition with the salt of claim 14.
Dermatosis treatment method (Claims 8, 13, 16)
- Claim 8: method for treating dermatosis by administering compound (claims 1 to 6).
- Claim 13: same for the specific compound of claim 11.
- Claim 16: same for the salt of claim 14.
Scope implication: the medical method claims are limited to “dermatosis” without specifying disease subsets in the provided text. That broad label still anchors infringement to the claim-defined chemical(s) used in administration.
What manufacturing/process rights are claimed?
Process claim (Claim 9)
Claim 9 defines “a process for producing an oxazole compound represented by Formula (1)” via reaction of:
- Formula (2) compound (R2 and W defined as in claim 1) where X is a halogen, with
- Formula (3) compound (R1 defined as in claim 1),
to yield the oxazole compound.
Scope implication: this is process coverage tied to the defined precursors (2) and (3) and the halogen-reactant motif (X = halogen). It does not cover every synthesis route to the claimed compounds, only those falling into the described reaction scheme.
Which exact compounds are explicitly covered?
Enumerated compound set (Claim 10)
Claim 10 lists multiple oxazole derivatives. The listed items are:
- N-[2-(4-difluoromethoxy-3-isobutoxyphenyl)oxazol-4-yl ethyl p-methylpicolinamide
- N-[2-(4-difluoromethoxy-3-isobutoxyphenyl)oxazol-4-ylmethyl]-3-methylpicolinamide
- N-[2-(3-cyclobutylmethoxy-4-difluoromethoxyphenyl)oxazol-4-ylmethyl]-3-methylpicolinamide
- N-[2-(4-difluoromethoxy-3-isobutoxyphenyl)oxazol-4-ylmethyl]-2-ethoxybenzamide
- N-[2-(4-difluoromethoxy-3-ethoxyphenyl)oxazol-4-ylmethyl]-2-ethoxybenzamide
- N-[2-(3-allyloxy-4-difluoromethoxyphenyl)oxazol-4-ylmethyl]-2-ethoxybenzamide
- N-[2-(4-difluoromethoxy-3-isopropoxyphenyl)oxazol-4-ylmethyl]-2-ethoxybenzamide
- N-[2-(3-cyclopropylmethoxy-4-d fluoromethoxyphenyl)oxazol-4-ylmethyl]-2-ethoxybenzamide
- N-[2-(4-difluoromethoxy-3-isopropoxyphenyl)oxazol-4-ylmethyl]-2-ethoxybenzamine
- N-[2-(3-cyclopropylmethoxy-4-difluoromethoxyphenyl)oxazol-4-ylmethyl]-2-ethoxybenzamide
- N-[2-(3-but-3-enyloxy-4-difluoromethoxyphenyl)oxazol-4-ylmethyl]-2-ethoxybenzamide
Notes on claim construction: the list includes closely related benzamide/picolinamide analogs, and includes an “-amine” variant as written in the claim text (item 9).
Single specific compound (Claim 11)
Claim 11 specifically claims:
- N-[2-(4-difluoromethoxy-3-isopropoxyphenyl)oxazol-4-ylmethyl]-2-ethoxybenzamide
and “having the structure” (structure shown in the patent, not reproduced in the provided text).
Claim 14 then claims the pharmaceutically acceptable salt of the claim 11 compound.
How the claim set maps to infringement risk for competitors
1. Chemical infringement hinge
If a competitor’s oxazole compounds fall within:
- R1 phenyl substitution limits (depending on which claim is asserted), and
- R2 being phenyl or pyridyl (for narrower claims 2-6), and
- W being carbonyl-based (with or without the amide nitrogen motif depending on claim),
then they land within the chemical genus/specific embodiments.
Key narrowing steps that reduce design-around space:
- W constrained to Formula (i) carbonyl/carbonyl-amide types (claims 2-6) rather than the full broad W set of claim 1.
- R1/R2 limited to phenyl or pyridyl and restricted substituent classes (alkoxy/alkenoxy/halogen/alkyl), with enumerated patterns at claim 4-6.
2. Product and use coverage
Even if a competitor designs around the chemical formula, the downstream claims still create risk if they use the exact enumerated compounds (claim 10) or the specific compound (claim 11) or its salt.
- If the exact compound/salt is used, compositions (claims 7/12/15) and dermatosis methods (claims 8/13/16) are triggered.
3. Process coverage
Claim 9 can be relevant if manufacturing uses the described halogenated intermediate (Formula (2), X = halogen) and the oxazole-forming step with Formula (3). If synthesis uses different disconnection logic or different functional handles, process infringement is reduced.
U.S. patent landscape: what can be concluded from the provided information only
No bibliographic metadata (application number, filing date, priority date, assignee, original patent number reissued from, expiration/patent term adjustments, maintenance events) is included in the provided content. Without those, a complete and accurate landscape cannot be built for RE46792’s effective date, patent family boundaries, claim dependency to the original non-reissue grant, or adjacency to related Orange Book entries.
Therefore, only the intra-document landscape (the internal claim architecture) is determinable from the provided text. External landscape mapping (competing patents, related reissues, continuation chains, and cited prior art) cannot be produced accurately from the information provided.
Key Takeaways
- RE46792 claims an oxazole chemical genus defined by Formula (1), then narrows through claims 2 to 6 to specific R1/R2 substitution classes and constrained W linker types.
- Downstream claims cover pharmaceutical compositions and dermatosis treatment methods, with additional product-specific coverage for enumerated compounds (claim 10) and a single explicitly named compound and its salt (claims 11 and 14).
- A synthesis process claim (claim 9) targets formation via reaction of a halogenated intermediate (Formula (2), X = halogen) with a Formula (3) precursor.
- A reliable U.S. “patent landscape” across other patents and Orange Book adjacency cannot be generated from the provided text because no priority, assignee, patent number-in-family, or expiration metadata is included.
FAQs
1) Which claim most broadly covers the chemistry?
Claim 1. It covers oxazole compounds defined by Formula (1) with broad R1 aryl substitution categories, R2 aryl/heterocycle categories, and a defined set of linker structures W.
2) What limits the scope in claims 2 to 6?
Claims 2-6 restrict R1 to phenyl with defined substituent sets, restrict R2 to phenyl or pyridyl with defined substituents, and narrow W to Formula (i) with specific Y1 carbonyl motifs and R3 = H for those subclaims.
3) Does RE46792 protect specific molecules beyond the genus claims?
Yes. Claim 10 enumerates multiple specific compounds, and claim 11 specifically names one compound with claim 14 covering its salt.
4) What medical indication is covered in the method claims?
The method claims cover “treating dermatosis” by administering the claimed compounds or salts.
5) Is there process protection in RE46792?
Yes. Claim 9 covers producing the oxazole compounds via a reaction between a halogenated intermediate (Formula (2), X = halogen) and a second precursor (Formula (3)).
References
[1] RE46792 (U.S. reissue patent) claims provided in the prompt text.
