Details for Patent: 8,101,629

Summary for Patent: 8,101,629

Title:	Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
Abstract:	The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation.
Inventor(s):	Jérôme Emile Georges Guillemont, Paul Theodoor Agnes Stevens, Alex Herman Copmans, Jozef Peeters, Alfred Elisabeth Stappers, Roger Petrus Gerebern Vandecruys, Paul Stoffels
Assignee:	Janssen Pharmaceutica NV
Application Number:	US12/845,463
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,101,629
Patent Claim Types: see list of patent claims	Composition; Compound; Dosage form;

United States Patent 8,101,629: What Its Claims Cover, How It Reads in Practice, and Where It Sits in the US Landscape

Patent US 8,101,629 claims a specific solid oral dosage construct for a compound defined as “a compound of formula (I-a)” using carrier + wetting agent, with additional, layered limitation around polymorphic Form A plus particle size and tablet core formulations.

This is a formulation and solid-state identity patent, not a composition-of-chemical-entity patent. The claim language makes infringement depend on (1) using formula (I-a), (2) delivering it in the claimed tablet/wetting-agent carrier system, and (3) matching the claimed Form A solid-state profile when those dependent claims are asserted.

---

What is the independent claim scope for US 8,101,629?

Claim 1 scope (base structure)

Claim 1 is the primary claim spine. It requires all of the following:

• A tablet
• Containing 25 mg base equivalent of the compound of formula (I-a)
• In a pharmaceutically acceptable carrier
• The carrier comprises a wetting agent

This yields a broad “tablets with wetting agent carrier” framework, but only at the 25 mg base-equivalent strength level for the independent claim.

Claim 10, 12, 14, 16 (strength-anchored independents)

The patent also has multiple independent claim blocks at higher strengths:

• Claim 10: 50 mg base equivalent tablet with wetting agent carrier
• Claim 12: 75 mg base equivalent tablet with wetting agent carrier
• Claim 14: 100 mg base equivalent tablet with wetting agent carrier
• Claim 16: 150 mg base equivalent tablet with wetting agent carrier

So the patent’s core market coverage is strength-by-strength. If a competitor launches at different dose strengths and avoids the exact mg base-equivalent recitations, it can change the claim map even if formulation concepts overlap.

---

How do the dependent claims narrow the scope (polymorph, FTIR/XRD, particle size, formulation recipes)?

Polymorphic Form A identity is claim-limiting

The patent’s tightest narrowing lever is Form A defined by X-ray powder diffraction (XRPD) peaks and FTIR absorption bands.

Claim 2: XRPD peak triad

If asserted, the tablet must use polymorphic Form A characterized by XRPD peaks at:

• 9.7° ± 0.2°
• 13.5° ± 0.2°
• 15.0° ± 0.2°

This is already specific enough to drive lab-method disputes (instrument, baseline, sample prep), but on the claim face it sets a fingerprint.

Claim 3: XRPD expanded set

Further narrows Form A to also include additional XRPD peaks at:

• 9.1° ± 0.2°
• 11.0° ± 0.2°
• 14.6° ± 0.2°
• 22.0° ± 0.2°
• 25.0° ± 0.2°
• 25.3° ± 0.2°
• 26.7° ± 0.2°

So Form A is not a single “one peak” polymorph; it is a multi-peak pattern. A competitor that uses a different polymorph, even with partial overlap, can attempt to avoid matching all recited peak positions.

Claim 4: FTIR bands first set

Requires FTIR absorption bands at about:

• 2217, 1652, 1497, 1435, 1338, 1199 and 550 cm−1

Claim 5: FTIR bands expanded

Further requires additional FTIR absorption bands at about:

• 1631, 1596, 1537, 1504, 1249, 1214, 1179, 1152 and 1070 cm−1

Net effect: dependent coverage is built to bind Form A by two orthogonal analytical modalities (XRPD + FTIR). This increases the odds that an accused formulation is either inside the fingerprint or clearly outside it.

---

Wetting agent selection is narrowed in Claim 6

• Claim 6: wetting agent is polysorbate 20

This is important. Claim 1 only requires “a wetting agent.” Claim 6 narrows it to polysorbate 20. If a generic uses a different wetting agent (e.g., poloxamers, sodium lauryl sulfate, bile salts, or other excipients that function as wetting agents), the infringement posture depends on which dependent claims are asserted and whether “wetting agent” is interpreted broadly enough to still capture the alternative excipient.

---

Tablet coating is covered

• Claim 7: tablet is film-coated

So even if a design-around changes core excipients, the coating status can still be a dependent infringement hook.

---

Tablet core formulations: two alternative recipes at 25 mg (Claims 8 and 9)

The patent includes two distinct tablet core composition embodiments for the 25 mg strength.

Claim 8: 25 mg core with Hypromellose 2910 (HPMC 15 mPa·s)

Tablet core lists (amounts as given):

• Compound of formula (I-a): 27.5 mg
• Lactose monohydrate: 242.0 mg
• Hypromellose 2910 15 mPa·s: 2910? (as written: 2910)
• Polysorbate 20: 5.6 mg
• Microcrystalline cellulose: 52.5 mg
• Croscarmellose sodium: 17.5 mg
• Colloidal silicon dioxide: 1.05 mg
• Magnesium stearate: 2.45 mg

Claim 9: 25 mg core with PVP (polyvinylpyrrolidone)

Tablet core lists:

• Compound of formula (I-a): 27.5 mg
• Lactose monohydrate: 55.145 mg
• Polyvinylpyrrolidone: 3.25 mg
• Polysorbate 20: 0.35 mg
• Silicified microcrystalline cellulose: 16.605 mg
• Croscarmellose sodium: 6.05 mg
• Magnesium stearate: 1.10 mg

The existence of two different excipient packages signals the patent drafter wanted to capture two manufacturing formulation routes (e.g., binder system difference, different swelling/disintegrant balance, different silica and microcrystalline carrier styling), while keeping the core requirements (wetting agent, Form A when dependent claims apply, particle size when dependent claims apply).

---

Tablet core formulations at 50 mg (Claim 11)

• Compound of formula (I-a): 55 mg
• Lactose monohydrate: 214.5 mg
• Hypromellose 2910 15 mPa·s: (written as 2910?)
• Polysorbate 20: 5.6 mg
• Microcrystalline cellulose: 52.5 mg
• Croscarmellose sodium: 17.5 mg
• Colloidal silicon dioxide: 1.05 mg
• Magnesium stearate: 2.45 mg

This is structurally similar to Claim 8’s recipe pattern, scaled to 50 mg base-equivalent coverage.

---

Tablet core formulations at 75 mg (Claim 13)

• Compound of formula (I-a): 82.5 mg
• Lactose monohydrate: 165.435 mg
• Polyvinylpyrrolidone: 9.75 mg
• Polysorbate 20: 1.05 mg
• Silicified microcrystalline cellulose: 49.815 mg
• Croscarmellose sodium: 18.15 mg
• Magnesium stearate: 3.30 mg

Again, PVP-based recipe structure.

---

Tablet core formulations at 100 mg (Claim 15)

• Compound of formula (I-a): 110 mg
• Lactose monohydrate: 159.5 mg
• Hypromellose 2910 15 mPa·s: (written as 2910)
• Polysorbate 20: 5.6 mg
• Microcrystalline cellulose: 52.5 mg
• Croscarmellose sodium: 17.5 mg
• Colloidal silicon dioxide: 1.05 mg
• Magnesium stearate: 2.45 mg

This resembles the HPMC-based embodiment.

---

Tablet core formulations at 150 mg (Claim 17)

• Compound of formula (I-a): 165 mg
• Lactose monohydrate: 330.87 mg
• Polyvinylpyrrolidone: 19.5 mg
• Polysorbate 20: 2.1 mg
• Silicified microcrystalline cellulose: 99.63 mg
• Croscarmellose sodium: 36.30 mg
• Magnesium stearate: 6.6 mg

PVP-based embodiment, higher scale.

---

Particle size dependence can be a practical design-around

Claims 18, 19, 20, 21 add particle size limitations:

• Claim 18: Formulation tablet where compound particle size < 50 μm
• Claim 19: tablet where particle size < 25 μm
• Claim 20: particle of formula (I-a) where particle size < 50 μm
• Claim 21: particle of formula (I-a) where particle size < 25 μm

If the business strategy uses a different milling method or a different particle-size distribution target, these dependent claims provide a clear “exit ramp” if avoided.

---

How does US 8,101,629 function as a patent in the landscape? (Scope map for enforcement risk)

1) The “tablet with wetting agent” concept sets the perimeter

Across independent claims (25/50/75/100/150 mg), the required construct is:

• Tablet
• Formula (I-a)
• Wetting agent present in the pharmaceutically acceptable carrier

This creates broad potential infringement if:

• the product is within one of the exact base-equivalent strengths, and
• a wetting agent is present (not necessarily polysorbate unless Claim 6 is used).

2) Polymorphic Form A claims convert “same drug” into “same solid-state”

Dependent claims 2-5 force analytical identity:

• XRPD peak set matches Form A
• FTIR bands match Form A

This matters for generic entry scenarios where the applicant might use an alternative polymorph, amorphous form, solvate, or process-created solid form.

3) Polysorbate 20 and film-coating are additional mechanical hooks

Dependent claim 6 locks wetting agent to polysorbate 20 if asserted. Dependent claim 7 locks to film-coated tablets if asserted.

4) Exact tablet core recipes narrow to a likely manufacturing similarity

Claims 8, 9, 11, 13, 15, 17 list excipient recipes. These are narrower than the independent “wetting agent” concept and likely align with a known manufacturing process.

5) Particle size provides a process-parameter escape

Claims 18-21 tie to a particle size threshold. A challenger can attempt to shift particle size outside the claimed cutoffs while keeping other requirements.

---

Claim-by-claim coverage matrix (what you must do to be within scope)

Claim	Strength anchor	Core limitation(s) that must be met	Additional identity constraints
1	25 mg base eq	Tablet with compound (I-a) + pharmaceutically acceptable carrier comprising a wetting agent	None stated in claim 1
2	25 mg (via claim 1)	Form A	XRPD peaks: 9.7°, 13.5°, 15.0° (±0.2°)
3	25 mg (via claim 2)	Form A	XRPD expanded peaks: 9.1°, 11.0°, 14.6°, 22.0°, 25.0°, 25.3°, 26.7°
4	25 mg (via claim 2-3)	Form A	FTIR bands: 2217, 1652, 1497, 1435, 1338, 1199, 550 cm−1
5	25 mg (via claim 4)	Form A	Additional FTIR bands: 1631, 1596, 1537, 1504, 1249, 1214, 1179, 1152, 1070 cm−1
6	25 mg (via claim 1)	Wetting agent is polysorbate 20	None
7	25 mg (via claim 1)	Film-coated	None
8	25 mg (via claim 1)	Specific tablet core composition	None beyond composition
9	25 mg (via claim 1)	Alternative core composition	None beyond composition
10	50 mg base eq	Tablet with compound (I-a) + wetting agent carrier	None
11	50 mg (via claim 10)	Specific tablet core composition	None
12	75 mg base eq	Tablet with compound (I-a) + wetting agent carrier	None
13	75 mg (via claim 12)	Specific tablet core composition	None
14	100 mg base eq	Tablet with compound (I-a) + wetting agent carrier	None
15	100 mg (via claim 14)	Specific tablet core composition	None
16	150 mg base eq	Tablet with compound (I-a) + wetting agent carrier	None
17	150 mg (via claim 16)	Specific tablet core composition	None
18	Tablet (via claim 1)	Compound particle size < 50 μm	None
19	Tablet (via claim 1)	Compound particle size < 25 μm	None
20	Particle (separate claim)	Particle of formula (I-a) size < 50 μm	None
21	Particle (separate claim)	Particle of formula (I-a) size < 25 μm	None

---

Patent landscape implications in the US (practical competitive takeaways)

Strength targeting means design-around can be dose-centric

Because independents recite specific base-equivalent strengths (25, 50, 75, 100, 150 mg), competitive strategies that land on:

• other strengths, or
• formulations that require different base-equivalent mapping, can shift infringement risk away from these independents. Dependent claims are tied back to the independent claim they depend on, so the dose mapping impacts the entire dependent chain.

Solid-state fingerprinting is a defensive moat against “form switch” arguments

XRPD + FTIR constraints (claims 2-5) reduce the feasibility of a simple “we used a different polymorph” answer unless the alternative form is demonstrably outside the recited peaks and bands.

Recipe claims likely reflect a known manufacturing template

The presence of detailed excipient recipes across multiple strengths signals:

• the applicant’s own formulation work is part of the public claim set, and
• the patent can be leveraged where an accused product uses similar excipient categories and amounts.

Particle size caps create a process-parameter line

If a competitor’s particle-size control yields a distribution that does not meet <50 μm or <25 μm thresholds, the dependent particle-size claims can fall away even where wetting agent and polymorph requirements are met.

---

What are the actionable “claim traps” for competitors?

1. Presence of a wetting agent in the carrier: if a product uses a wetting agent in a manner that falls within “pharmaceutically acceptable carrier comprising a wetting agent,” the independent claim risk is immediate at matched strengths.
2. Polysorbate 20: if the product uses polysorbate 20, dependent claim 6 is a direct hook.
3. Form A analytical matching: if the formulation uses Form A and satisfies XRPD and FTIR peak sets, dependent claims 2-5 can attach.
4. Particle size: milling targets below 50 μm or 25 μm can pull a product into claims 18-21.
5. Film coating: if the tablet is film-coated, dependent claim 7 is triggered.

---

Key Takeaways

• US 8,101,629 is a tablet formulation + solid-state identity patent. Its independent claims cover tablets at specific mg base-equivalent strengths with wetting-agent-containing carriers.
• The tightest enforceable layer is Form A fingerprinting via multi-peak XRPD (claims 2-3) and FTIR band sets (claims 4-5).
• Polysorbate 20 and film coating provide additional dependent claim hooks (claims 6-7).
• Tablet core recipe embodiments (claims 8-9, 11, 13, 15, 17) narrow scope toward specific manufacturing-excipient mixes.
• Particle-size thresholds (<50 μm and <25 μm) add a process-parameter design-around axis (claims 18-21).

---

FAQs

1) What does the patent protect most strongly: the compound itself or the product form?

The claim set protects specific tablet constructions and Form A solid-state identity. Chemical-entity protection is not what the provided claims show; the claims tie coverage to tablet, carrier, wetting agent, and solid-state fingerprints.

2) If a competitor uses a different wetting agent, does it avoid infringement?

It can avoid dependent claim 6 if the wetting agent is not polysorbate 20. But independent claims 1/10/12/14/16 still require “a wetting agent,” so avoiding polysorbate does not necessarily avoid all claims if any wetting agent is present.

3) How do XRPD and FTIR terms affect enforceability?

They make infringement turn on whether the accused material matches the recited peak positions and band locations for Form A. The patent drafts enforceability around lab-measured identity.

4) Does claim coverage change by dose strength?

Yes. The independent claims are written at 25, 50, 75, 100, and 150 mg base equivalent. That structure makes dose selection a direct leverage point.

5) Can particle size help design around even if excipients and Form A match?

Yes. The dependent claims impose particle-size caps (<50 μm and <25 μm). A formulation that stays outside those thresholds can avoid those dependent claims while still meeting other conditions.

---

References

[1] US Patent 8,101,629, “Tablet comprising 25 mg base equivalent of a compound of formula (I-a) in a pharmaceutically acceptable carrier comprising a wetting agent,” claims 1-21 (provided claim text).

Drugs Protected by US Patent 8,101,629

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

Foreign Priority and PCT Information for Patent: 8,101,629

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	EP01203090	Aug 13, 2001
	EP02077748	Jun 10, 2002
Malaysia	PI20043578	Sep 02, 2004

International Family Members for US Patent 8,101,629

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1419152		C300529	Netherlands
European Patent Office	1419152		C300532	Netherlands
European Patent Office	1419152		PA2012008	Lithuania