Patent: 10,759,793

Summary for Patent: 10,759,793

Title:	2-(pyrazolopyridin-3-yl)pyrimidine derivatives as JAK inhibitors
Abstract:	New 2-(pyrazolopyridin-3-yl)pyrimidine derivatives are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of Janus Kinases (JAK).
Inventor(s):	Esteve Trias; Cristina (Barcelona, ES), Taltavull Moll; Joan (Barcelona, ES), Gonzalez Rodriguez; Jacob (Barcelona, ES), Vidal Juan; Bernat (Barcelona, ES)
Assignee:	Almirall, S.A. (Barcelona, ES)
Application Number:	15/735,235
Patent Claims:	see list of patent claims

What is US Patent 10,759,793’s claim scope and where does it sit in the US landscape?

US Patent 10,759,793 is directed to 2-(pyrazolopyridin-3-yl)pyrimidine derivatives defined by a formula (I) scaffold with substantial genus-level latitude in substituents, salts/solvates/stereoisomers/deuterated forms, and with dependent claims that narrow to specific substitution patterns and specific enumerated compounds. The claims also extend into combination therapy coverage that pairs the claimed compounds with a broad menu of immunology and anti-inflammatory agents and other therapeutic classes.

The net effect is a wide chemical genus in claim 1, followed by selectively narrow sub-genus and single-compound fallbacks in claims 2-12 and named exemplars in claim 8, then a combination-product claim in claim 13.

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What does claim 1 actually cover (and how broad is it)?

Core structure and claim form

Claim 1 covers:

• A “2-(pyrazolopyridin-3-yl)pyrimidine derivative”
• Defined as a compound of formula (I) (not reproduced in the text here beyond variable definitions)
• Plus all pharmaceutically acceptable salts
• Plus solvates, N-oxides
• Plus stereoisomers
• Plus deuterated derivatives

This is an “umbrella” claim that, in US practice, typically creates both:

• Direct infringement exposure for the specific defined structures, and
• Design-around pressure because alternatives that retain the same formula variable assignment space often remain within the claim.

Variable-field breadth (formula (I) knobs that expand coverage)

Claim 1 uses four main “substitution knobs” and multiple defined substituent sets:

1. X is --NR³--
2. R¹ and R² are independently selected from:

• hydrogen
• halogen
• C1-4 alkyl
• C1-4 alkoxy
• --CN

3. R³ is selected from:

• hydrogen
• C1-4 alkyl
• (CH2)1-3NR’R’’
• (CH2)1-3-pyrrolidine

4. G¹ is --O--R⁶

5. Q is chosen from Qa, Qb, or Qc, each with additional sub-variables:

• R⁴ is chosen from:
  • --CO(CH2)1-2--OH
  • --CO(CH2)1-2--CN
• R⁵ is chosen from:
  • --(CH2)m--CN
  • --(CH2)m--OH
• G² is chosen from:
  • phenyl group, pyrimidine group, or pyridine group
    Each of these aromatic groups is unsubstituted or substituted by:
  • halogen
  • C1-4 alkyl
  • hydroxyl
  • --CN
• R⁶ is chosen from:
  • linear or branched (C1-6 alkoxy)-(C1-6 alkyl)
  • linear or branched C1-6 alkyl, which itself can be substituted by:
    • halogen
    • hydroxyl
• m is independently 0, 1, 2, or 3

What this means in practice

Claim 1 is not “one compound family.” It is a multi-parameter genus that can cover:

• Multiple choices at the aryl/pseudoring elements (G², Q variants),
• Multiple polarity and functionality patterns at R⁴/R⁵ (hydroxy vs nitrile vs carboxy-functional patterns),
• Multiple substituent sizes at R¹/R² (including halogen, alkyl, alkoxy, CN),
• Multiple linker/amine motifs at R³ (including pyrrolidine-bearing tails),
• Multiple ether substituent patterns at G¹ and R⁶.

Taken together, the genus is chemically broad and includes both:

• “Smoother” substituent sets (H, halogen, alkyl, alkoxy)
• and “functionally sharp” sets (nitrile groups, carboxy-hydroxymethyl fragments, hydroxylated side chains).

That breadth is reinforced by the claim’s treatment of salts/solvates/stereochemistry/deuteration, which typically makes infringement arguments easier for a competitor using the same chemical entity in variant physical forms.

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What do dependent claims 2–7 narrow (and where do they still leave design space)?

Claims 2–4: constrained halogen/alkyl patterns

• Claim 2: R¹ ∈ {H, F, Cl, methyl}
• Claim 3: R² ∈ {H, F}
• Claim 4: R³ = hydrogen

These reduce the genus by restricting:

• the substitution pattern on the pyrimidine (R¹/R²),
• and the amine substitution at R³ (to H).

In infringement analysis, these dependent claims still act as fallback positions if the broad genus is challenged or if a court construes “formula (I)” narrowly.

Claim 5: selects Q

• Claim 5: Q = Qa

This is a direct narrowing by selecting a specific substructure class among Qa/Qb/Qc.

Claim 6: a composite narrowing to a specific sub-genus

Claim 6 ties together:

• R¹ ∈ {H, F, Cl, methyl}
• R² ∈ {H, F}
• X = --NR³-- (so X stays that)
• R³ = hydrogen
• Q = Qa
• R⁴ ∈ { --CO(CH2)1-2--OH, --CO(CH2)1-2--CN }
• G¹ = --O--R⁶
• R⁶ is constrained to:
  • (C1-6 alkoxy)-(C1-6 alkyl) OR C1-6 alkyl
  • and that C1-6 alkyl may carry halogen or hydroxyl

This claim is a “tightening” claim that preserves the broader functionality at the linker region (R⁴ and R⁶) while keeping the core substituent constraints.

Claim 7: a further constrained, more prescriptive scaffold

Claim 7 requires:

• X = --NR³--
• R¹ and R² each ∈ {H, F, methyl}
• R³ ∈ {H, methyl}
• G¹ = --O--R⁶
• R⁴ ∈ {--CO(CH2)-OH, --CO(CH2)--CN}
• R⁵ = --CH2CN
• G² ∈ {pyrimidine group, pyridine group}
  Each is unsubstituted or substituted with fluorine only
• R⁶ limited to a list of specific ether/alkyl substituents, including:
  • --(CH2)2OCH3
  • --(CH2)2OCH2CH3
  • --CH(CH3)CH2OCH3
  • methyl/ethyl/butyl
  • --CH2CF3, --CH2CHF2
  • isopropyl
  • --(CH2)2-3OH and related hydroxyalkyl stereochemical variants

Claim 7 is substantially narrower and functions like a sub-genus claim oriented to a particular medicinal-chemistry series.

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How do claim 8, 9, 10, 11, 12 function as hard “coverage anchors”?

Claim 8: enumerated compound list that effectively creates multiple single-compound fallbacks

Claim 8 lists multiple specific stereochemically defined compounds (several “Trans-4-” cyclohexylacetonitrile derivatives; multiple glycoloylpiperidine, methoxyethoxy, hydroxyethoxy analogs; and additional nitrile/oxoethanol variants). Each listed entity is coupled with catch-all language for:

• pharmaceutically acceptable salt
• N-oxide
• solvate
• stereoisomer
• deuterated derivative

This style matters: even if claim 1 is found invalid for indefiniteness or overbreadth, claim 8 can keep enforceable subject matter because the enumerated list ties to concrete structures.

Claim 9–12: single-compound claims

• Claim 9: a specific glycoloylpiperidinyl ether alcohol compound:
  “3-[(5-Fluoro-6-{[(3R)-1-glycoloylpiperidin-3-yl]amino}-2-pyrazolo[1,5-a]pyridin-3-ylpyrimidin-4-yl)oxy]propan-1-ol” plus variants.
• Claim 10: a specific “methoxy” analog:
  “2-{(3R)-3-[(5-Fluoro-6-methoxy-2-pyrazolo[1,5-a]pyridin-3-ylpyrimidin-4-yl)amino]piperidin-1-yl}-2-oxoethanol” plus variants.
• Claim 11: a specific “methoxyethoxy” analog:
  “3-((3R)-3-{[6-(2-Methoxyethoxy)-2-pyrazolo[1,5-a]pyridin-3-ylpyrimidin-4-yl]amino}piperidin-1-yl)-3-oxopropanenitrile” plus variants.
• Claim 12: a specific “hydroxyethoxy” analog:
  “3-((3R)-3-{[6-(2-Hydroxyethoxy)-2-pyrazolo[1,5-a]pyridin-3-ylpyrimidin-4-yl]amino}piperidin-1-yl)-3-oxopropanenitrile” plus variants.

These are strategically valuable as:

• Litigation fallback positions that map closely to likely exemplified lead candidates.
• Potentially easier prior art matching (because a single prior art compound can anticipate).

Claim 13: combination product claim with very broad partner space

Claim 13 covers a combination product comprising:

• (i) at least one claim 1 compound, and
• (ii) at least one additional active ingredient chosen from a long list spanning multiple therapeutic domains, including:
  • Corticoids and glucocorticoids
  • Dihydrofolate reductase inhibitors
  • DHODH inhibitors
  • Purine antagonists
  • Antimalarials
  • Calcineurin inhibitors
  • IMPDH inhibitors
  • Fumaric acid esters
  • Vitamin D3 derivatives
  • Retinoids
  • Multiple monoclonal antibodies and receptor biologics targeting TNF-alpha, IL-6R, IL-12/23, IL-17R, IL-5/IL-5R, IL-13/IL-4R/IL-13R, IL-1R, IgE, BAFF, CD19
  • Kappa opioid agonists
  • Neurokinin receptor 1 antagonists
  • Dihydropteroate synthase inhibitors
  • Histamine H1 antagonists
  • CysLT receptor antagonists
  • CRTH2 inhibitors
  • Topical anti-septics

This combination claim is not limited to a particular indication in the claim text. It is defined by a very broad set of partner actives. That breadth can be a strength in enforcement against multi-drug regimens, but it also raises the bar for novelty/non-obviousness as a combination category if prior art broadly teaches combination use.

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Where does the patent likely sit in the competitive landscape (claim-structure-based assessment)?

Without prosecution history and without the patent’s full specification context, the most reliable landscape read comes from claim architecture:

1. Genus claim 1 with extensive substituent freedom
   • Typical of patents seeking to cover an entire class of close analogs rather than a single molecule.
2. Sub-genus claims 6 and 7 with constrained sets
   • Typical of medicinal-chemistry series follow-ups where core potency and selectivity motifs are known.
3. Enumerated compounds in claim 8 plus single-compound claims 9–12
   • Typical of anchor candidates that the applicant expects to commercialize or to pursue as immediate follow-on assets.
4. Combination claim 13
   • Typical of strategy to block combination regimens and to capture claims tied to fixed partner lists.

Business implication: competitors are exposed if they stay within the formula (I) variable framework, or if they adopt any listed anchor compounds, and are additionally exposed if they seek combination formulations with the listed classes.

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Hard practical claim coverage map (what to test in freedom-to-operate)

A. Structural inclusion tests for formula (I)

In a risk screening exercise, the first pass is whether a candidate compound can be expressed with the claim’s variable assignments:

• Does it fit “2-(pyrazolopyridin-3-yl)pyrimidine” with:
  • X = --NR³--,
  • G¹ = --O--R⁶,
  • Q ∈ {Qa, Qb, Qc} with corresponding Q-substituent definitions,
  • R¹/R² in the permitted sets,
  • and R⁴/R⁵/G² in the permitted sets?

B. Anchor-compound match

If a candidate matches any named compound in claim 8 (or the tighter molecules in claims 9–12), that is a direct claim-reading trigger because those claims are explicit.

C. Stereochemical sensitivity

Claims 8-12 include (2S)/(2R)/(3R)/(1S)/(1R) patterns in at least several enumerations. If a competitor distributes a single stereoisomer, the claim’s “stereoisomer” language can still maintain infringement exposure for other isomeric forms of the same underlying structure depending on claim construction.

D. Combination pairing triggers

If a marketed product pairs one of the claim 1 compounds with any partner active from the claim 13 list, the combination product claim is implicated.

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Key Takeaways

• Claim 1 is a broad genus built from a multi-variable formula (I) framework covering salts/solvates/N-oxides/stereoisomers/deuterated forms, with wide latitude in R¹/R², R³, R⁴/R⁵, Q variants, G², and R⁶.
• Claims 2–7 are narrowing scaffolds that keep enforceable fallback positions by restricting substitution patterns and selecting Q = Qa (claim 5) and key functional group patterns (notably R⁴/R⁵ and R⁶).
• Claims 8–12 create litigation anchors: a large enumerated set (claim 8) and multiple single-compound claims (claims 9–12), each with the same variant-form catch-all language.
• Claim 13 is a very broad combination-product claim that pairs the claimed compounds with a long list of immunology and inflammation-related agents, including multiple biologics and pathway-specific inhibitors.

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FAQs

1) Is claim 1 limited to specific Q variants?

Claim 1 defines Q as Qa, Qb, or Qc. Dependent claim 5 selects Q = Qa, narrowing within the genus.

2) Do the claims cover stereochemistry and deuterated analogs?

Yes. Claim 1 and the narrower dependent claims include stereoisomers and deuterated derivatives alongside salts/solvates/N-oxides.

3) What is the fastest way to assess infringement risk for a candidate molecule?

First, test whether it fits the formula (I) variable constraints in claim 1. Second, test whether it matches any explicitly listed compound in claim 8 or the single-compound definitions in claims 9–12.

4) How does claim 7 differ from claim 6 in practical scope?

Claim 7 constrains multiple fields simultaneously, including R⁵ = --CH2CN, narrows G² to pyrimidine or pyridine with only fluorine substitutions, and restricts R⁶ to a defined list of ether/alkyl/hydroxyalkyl motifs.

5) Does claim 13 require both drugs to be in one dosage form?

Claim 13 is a combination product comprising (i) at least one claim 1 derivative and (ii) at least one additional active ingredient chosen from the listed classes, which in practice targets combination co-formulations or packaged combination regimens.

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References

[1] United States Patent US 10,759,793. Claimed subject matter and claim text as provided in the prompt.

Details for Patent 10,759,793

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Jubilant Hollisterstier Llc	N/A	positive skin test control-histamine	Injection	103891	March 13, 1924		2036-06-10