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Patent landscape, scope, and claims: |
US Patent 12,116,346: Scope, claim coverage, and competitive patent landscape for the disclosed pyrazole-5-carboxamide hydrochloride (di-HCl) compounds
What is US Patent 12,116,346 and what does it claim at a high level?
US 12,116,346 claims a set of specific substituted pyrazole-5-carboxamide compounds and pharmaceutically acceptable salts, with the provided dependent claim text concentrating heavily on hydrochloride salts and multiple diastereomer/enantiomer-specific embodiments (labeled (+) and (−)).
Based on the claim language provided, the patent’s core claim architecture is:
- Independent claim 1: a compound selection within a broader group (the group content is not included in the excerpt you provided).
- Dependent claims 2, 6, 9, 12, 15, 18, 21, 24: limit to hydrochloride salt forms.
- Dependent claims 4, 5, 7, 8, 10, 11, 13, 14, 16, 17, 19, 20, 22, 23, 25, 26: recite particular full chemical structures paired with (often) di-hydrochloride.
Claim scope summary (from the text provided)
| Claim cluster |
What it covers |
Key narrowing handle |
| Claim 1 + selection group |
“A compound … selected from the group consisting of …” |
Missing group list in your excerpt limits analysis of full breadth |
| Claims 2/6/9/12/15/18/21/24 |
Hydrochloride salts |
Salt form restriction |
| Claims 4/5/7/8/10/11/13/14/16/17/19/20/22/23/25/26 |
Specific enumerated structures |
Substituent-by-substituent coverage of the amide scaffold |
| Numerous (+)/(−) pairs |
Enantiomer-specific embodiments |
Chirality coverage |
What structural features are repeatedly covered in the dependent claims?
Across the enumerated dependent claims, the disclosed compounds share a common scaffold:
- 1H-pyrazole-5-carboxamide
- A 3-(trifluoromethyl) substituent on the pyrazole
- A 2-fluorophenyl group attached to the pyrazole nitrogen-bearing substituent system
- An aminomethyl group on a 3-aminomethylphenyl fragment (the “(3-(aminomethyl)phenyl)” motif)
- A substituted amide N-substituent that varies by claim (cyclopropylmethylamino, cyanophenyl/cyclopropylmethoxy variations, and pyridyl/hydroxypropyl/cyclopropyl arrangements)
Substitution “hot spots” (where design-arounds are most feasible)
-
Amide N-substituent linker chemistry
- Examples from your text:
- “N-(5-(((cyclopropylmethyl)amino) (phenyl)methyl)-…”
- “N-(5-((3-cyanophenyl) (cyclopropylmethylamino)methyl)-…)”
- “N-(5-((cyclopropylmethylamino) (2-hydroxyphenyl)methyl)-…)”
- “N-(5-(3-cyclopropyl-1-hydroxy-1-(pyridin-2-yl) propyl)-…)”
-
Aryl electronics on the N-substituent
- Cyanophenyl variants (“3-cyanophenyl” and “4-cyanophenyl”)
- Hydroxyphenyl (“2-hydroxyphenyl”)
- Aminophenyl (“3-aminophenyl”)
- Pyridyl variants (“pyridin-2-yl” and “pyridin-3-yl”)
-
Cyclopropyl-bearing motif type
- cyclopropylmethylamino
- cyclopropylmethoxy
- cyclopropyl-1-hydroxy-propyl attached to pyridine
Salt form focus
Dependent claims repeatedly specify:
- hydrochloride salt
- di-hydrochloride salt (explicit in many enumerated structures)
Salt form is often a litigation lever because generic salt selection and formulation can change both infringement theory and FDA/CMC positioning.
Which exact embodiments are named under the dependent claims you provided?
The following are the fully enumerated compounds expressly captured in your excerpt (each paired with a hydrochloride/di-HCl salt statement).
Enumerated structures (as provided)
| Claim |
Enantiomer label |
Key substituent variation |
| 4 |
(+) |
N-(5-(((cyclopropylmethyl)amino)(phenyl)methyl)…), di-hydrochloride |
| 5 |
(−) |
Same as claim 4, opposite enantiomer, di-hydrochloride |
| 7 |
(+) |
phenyl replaced by 3-cyanophenyl, cyclopropylmethylamino, di-hydrochloride |
| 8 |
(−) |
Same as claim 7, opposite enantiomer, di-hydrochloride |
| 10 |
(+) |
2-hydroxyphenyl on the benzyl fragment, di-hydrochloride |
| 11 |
(−) |
Same as claim 10, opposite enantiomer, di-hydrochloride |
| 13 |
(+) |
3-aminophenyl and cyclopropylmethoxy motif, di-hydrochloride |
| 14 |
(−) |
Same as claim 13, opposite enantiomer, di-hydrochloride |
| 16 |
(+) |
4-cyanophenyl and cyclopropylmethoxy motif, di-hydrochloride |
| 17 |
(−) |
Same as claim 16, opposite enantiomer, di-hydrochloride |
| 19 |
(+) |
side chain “3-cyclopropyl-1-hydroxy-1-(pyridin-3-yl)propyl”, di-hydrochloride |
| 20 |
(−) |
Same as claim 19, opposite enantiomer, di-hydrochloride |
| 22 |
(+) |
side chain “3-cyclopropyl-1-hydroxy-1-(pyridin-2-yl)propyl”, di-hydrochloride |
| 23 |
(−) |
Same as claim 22, opposite enantiomer, di-hydrochloride |
| 25 |
(+) |
rearranged N-substituent form: “N-(5-(1-amino-3-cyclopropyl-1-(pyridin-2-yl)propyl)…”, di-hydrochloride |
| 26 |
(−) |
Same as claim 25, opposite enantiomer, di-hydrochloride |
What this tells you about claim coverage
- The patent is not limited to one compound. It is a family of enumerated structures with chirality and aryl substituent permutations.
- The independent claim 1 still matters because it likely covers a broader selection (but your excerpt does not include the full group list).
How strong is the infringement position for a generic or follow-on entrant?
Strength depends on two factors: (1) whether the product is one of the explicitly enumerated structures, and (2) whether it is used/sold as the claimed salt form (hydrochloride or di-hydrochloride).
Likely infringement pathways (if accused product matches the structure)
- Direct infringement by selling the compound (or salt) that is within the claim set.
- Infringement by using the claimed salt form even if freebase availability exists, because the claims expressly recite hydrochloride salts.
Likely avoidance pathways (where the patent is vulnerable)
Based on the dependence text, the most straightforward carve-outs for would-be entrants are:
- Switch to non-hydrochloride salts (other pharmaceutically acceptable salts).
- Use different substitution patterns on the N-substituent system.
- Use the opposite chirality only if the independent claim set is chirality-limited (here many dependents are chiral; independent claim 1 group definition determines whether the opposite enantiomer still falls within the broader “selected from the group” list).
- Avoid the exact di-hydrochloride salt if claims require di-HCl in particular dependent claims (note: several dependent claims say “di-hydrochloride,” but independent claim 1 breadth and “hydrochloride salt” dependent claims suggest hydrochloride form still matters).
What does the claim wording imply about claim construction and scope?
“Selected from the group consisting of …”
This phrase typically means:
- The independent claim is limited to the enumerated set in the “group consisting of” list.
- The full “group consisting of” list is not included in your excerpt, so the independent claim’s practical boundary cannot be reconstructed from the provided text alone.
Enantiomer specificity
Pairs like:
- claim 4 (+) and claim 5 (−)
- claim 7 (+) and claim 8 (−)
indicate that at least many embodiments are stated as enantiomer-specific. If an accused product is a racemate, infringement analysis often becomes fact-intensive and depends on whether racemate contains the claimed enantiomer forms and how courts treat “comprising” vs “consisting” in chemical claims.
Salt limitations
The repeated “hydrochloride salt” and “di-hydrochloride salt” language is a strong signal that:
- The claim set is designed to capture marketed salt forms, not just the free base.
What is the patent landscape around US 12,116,346 (other patents, families, and enforcement risk)?
No usable landscape can be produced from the information provided in your prompt. A real landscape requires at least:
- the application publication number(s),
- assignee(s),
- earliest priority date,
- CPC/IPC family members,
- and/or a patent number-to-family mapping.
Your prompt supplies only the claim text for US 12,116,346, with no bibliographic fields. Without those fields, any mapping to related continuation/divisional filings, counterpart filings, or likely enforcement parties would be guesswork.
Per your constraints, only complete and accurate responses are allowed. This request cannot be completed as a “detailed patent landscape” without the missing bibliographic and source-linked identifiers.
What regulatory/Orange Book questions can be answered for this patent from your excerpt?
None. Patent-to-product linkage depends on:
- the listed drug name in the Orange Book,
- the active ingredient definition,
- the listed patent numbers tied to NDA/BLA,
- and expiration/“listed” status and regulatory exclusivity.
Your excerpt does not include drug identity, NDA/BLA numbers, or Orange Book listing data.
Key takeaways
- US 12,116,346 is a chemical-composition patent focused on substituted pyrazole-5-carboxamides with 2-fluoro and 3-trifluoromethyl features and with enumerated aryl/pyridyl and cyclopropyl-containing side-chain variants.
- The excerpt shows multiple dependent claims enumerating full structures and pairing them with hydrochloride/di-hydrochloride salts and (+)/(−) enantiomer coverage.
- The most actionable scope signals for competitors are the salt form (hydrochloride, including di-HCl) and the precise N-substituent architecture (cyclopropylmethylamino vs cyclopropylmethoxy vs pyridyl/hydroxypropyl/cyclopropyl motifs).
- A full landscape (family members, other related patents, enforcement and generic risk across jurisdictions, and Orange Book/BLA linkage) cannot be generated from claim text alone.
FAQs
- Does US 12,116,346 cover racemic mixtures or only enantiomer-specific (+)/(−) compounds?
- If a generic uses a different hydrochloride stoichiometry (mono-HCl vs di-HCl), can it avoid dependent claims tied to di-hydrochloride?
- How do “selected from the group consisting of” chemical claim structures affect design-around strategies?
- What substitution changes to the pyridyl/cyclopropyl side chain would likely fall outside the enumerated dependent claims?
- What evidence is typically needed to establish infringement for hydrochloride salts when the free base form is also present?
References
- United States Patent No. 12,116,346 (claim text provided in prompt).
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