Details for Patent: 7,105,530

Summary for Patent: 7,105,530

Title:	Pyrimidineamines as angiogenesis modulators
Abstract:	Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also Includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
Inventor(s):	Amogh Boloor, Mui Cheung, Ronda Davis, Philip Anthony Harris, Kevin Hinkle, Robert Anthony Mook, Jr., Jeffery Alan Stafford, James Marvin Veal
Assignee:	Novartis AG
Application Number:	US10/451,305
Patent Claim Types: see list of patent claims	Use; Composition;

United States Patent 7,105,530 Scope, Claims Construction, and US Patent Landscape (Angiogenesis Inhibitors for Proliferative Retinopathy)

United States Patent US 7,105,530 is a small-molecule patent covering (i) compounds of a defined chemical formula (claim 1/6), (ii) pharmaceutical compositions using those compounds (claim 2/7 plus “additional agents” claims 3/4 and 8/9), and (iii) therapeutic methods for mammals with disorders characterized by inappropriate angiogenesis, specifically proliferative retinopathy (claim 5/10). The claim set is broad at the top level (formula compounds and generic “pharmaceutically acceptable” compositions) and then narrows only by functional context (angiogenesis; proliferative retinopathy) and compositional additions (anti-neoplastic and angiogenesis inhibitors).

Important limitation: the claim text you provided omits the actual chemical formula language (it appears as a placeholder). The “compound of the formula” scope therefore cannot be mapped to a specific active ingredient, Markush boundaries, or known competitor scaffolds without the full formula. Because the chemical identity is missing, a complete landscape tied to substituent space, named analogs, and citation-to-specific chemical structures cannot be produced from the provided record.

---

What does US 7,105,530 claim protect: compound formula, composition, and method-of-use?

Claim 1 and 6: “compound of the formula” (composition-agnostic core protection)

• Coverage type: product-by-structure.
• Independent claims: claim 1 and claim 6 are both directed to a compound of the claimed formula (and salts).
• Legal consequence: infringement can occur by manufacture, use, offer for sale, sale, or importation of the covered compound(s), regardless of whether a commercial product is marketed as treating retinopathy, assuming the compound itself is the accused product.

Claim 2 and 7: pharmaceutical composition (carrier and dose-form flexibility)

• Coverage type: product-by-combination with carriers.
• Core elements:
  • therapeutically effective amount of the formula compound (or salt),
  • one or more pharmaceutically acceptable carriers, diluents, and excipients.
• Practical scope: this is generally broad across oral/topical/ocular formulations unless the specification limits dosage forms or excipient classes. Your excerpt does not state dosage form restrictions.

Claim 3/4 and 8/9: combination therapy additions

• Claim 3 and 8 add at least one “additional agent” that is an anti-neoplastic agent.
• Claim 4 and 9 add an additional agent that inhibits angiogenesis.
• Key construction point: these are dependent claims. They require both:
  1. the formula compound (or salt), plus
  2. the specified additional agent class(es).
• Design-around implication: a competitor using the formula compound plus only an angiogenesis inhibitor that is argued not to meet the claim’s “additional agent” class criteria could avoid these dependent claims while still potentially implicating independent claims 1/2/5/6/7/10.

Claim 5 and 10: method-of-use for proliferative retinopathy

• Both independent method claims require:
  • administration of a therapeutically effective amount of the formula compound (or salt),
  • to a mammal,
  • treating a disorder characterized by inappropriate angiogenesis,
  • where the disorder is proliferative retinopathy.
• Scope consequence: a product containing the formula compound could infringe the method claims only when used in a way that meets the “proliferative retinopathy” and “inappropriate angiogenesis” treatment framing. In the US, method-of-use infringement often turns on labeling, advertising, physician instructions, and inducement theories.

---

How broad is the “formula compound” scope likely to be for US 7,105,530?

Markush coverage and salt inclusion

Your excerpt includes “or a salt thereof,” which typically expands literal scope to pharmaceutically acceptable salts that fall within the specification’s definition. Because the chemical formula is missing, the Markush variables cannot be quantified here. However, the claim drafting style (“compound of the formula”) suggests the claim is limited to a structured core with permitted substituent variations inside the Markush definition.

Salts: what this typically captures

• Pharmaceutically acceptable salts (e.g., acid addition salts, basic salts) are usually included unless explicitly excluded.
• Salt-only variants that keep the same free base structure generally do not escape a structure-based claim.

---

What patent estate questions matter: expiration, exclusivity, and continuation risk?

US 7,105,530 filing, grant, and term framework

US 7,105,530 is a US utility patent. The standard rule is a 20-year term from the earliest effective nonprovisional filing date, subject to adjustments and patent term extensions (PTE) if applicable. The user-supplied record does not include filing date, application number, priority date, or whether PTA/PTE was granted.

Continuation and claim scope evolution

Because claim 1/6 and claim 2/7 repeat parallel structure, the patent may include:

• early broad compound claims,
• later compositions and dependent combination therapy claims,
• method claims tied to angiogenesis/proliferative retinopathy. Without the application history (file wrapper) and the complete issued claim set, the continuation landscape cannot be reconstructed from the excerpt.

---

What formulations are protected by US 7,105,530?

Carrier-agnostic composition claims

Claims 2 and 7 require only:

• pharmaceutically acceptable carriers/diluents/excipients,
• therapeutically effective amount of the compound.

That language typically protects a wide formulation range:

• solutions, suspensions, emulsions,
• solid dosage forms,
• ocular formulations and topical formulations, depending on whether the specification supports them.

Combination therapy formulations

Claims 3/4 and 8/9 protect compositions that include:

• the formula compound plus an anti-neoplastic agent, and/or
• the formula compound plus an angiogenesis inhibitor, along with standard carriers.

---

What “additional agents” language could expand or narrow infringement risk?

Anti-neoplastic agent dependent claims (3 and 8)

• These are class-based (“anti-neoplastic agent”), so the key dispute is whether the additional agent qualifies as anti-neoplastic in the regulatory/pharmacology sense and whether the accused composition meets “further comprising.”
• If a competitor uses the formula compound without a second anti-neoplastic agent, it avoids these dependent claims.

Angiogenesis inhibitor dependent claims (4 and 9)

• This language is not limited to a specific mechanism beyond angiogenesis inhibition.
• Disputes can arise around:
  • whether the additional agent is truly an angiogenesis inhibitor (MOA),
  • whether a given drug is characterized as such for claim purposes,
  • whether the composition contains the additional agent “further comprising” in a therapeutically relevant amount.

---

Which disorders and therapeutic contexts are in-scope: inappropriate angiogenesis and proliferative retinopathy

Method claim disease specificity

Both method claims constrain the indication to:

• disorder characterized by inappropriate angiogenesis,
• specifically proliferative retinopathy.

This is not limited to a particular etiology (e.g., diabetic retinopathy, retinopathy of prematurity, ischemic retinopathy) unless the specification narrows the meaning of proliferative retinopathy.

Mammal scope

“mammal” is broad, typically including humans and animals. For infringement, commercial use in humans remains the primary commercial concern.

---

How does US 7,105,530 compare with typical angiogenesis inhibitor patent families (generics and biologics risk)?

Small-molecule angiogenesis inhibitor vs biologic VEGF-pathway agents

US 7,105,530 is claim-directed to a compound of a formula. That usually means:

• it is not a biologic claim family like antibodies/VEGF trap constructs,
• it competes more directly with other small-molecule angiogenesis inhibitors rather than intravitreal biologics.

Generic/biosimilar angle

• Generics risk: structure-based claims on a specific scaffold generally block generics that still fall within the formula Markush.
• Entry risk from non-identical scaffolds: competitors can avoid infringement by moving to distinct scaffolds outside the formula bounds.
• Biosimilars: not directly relevant unless the same disease mechanism is targeted with a biologic; this patent itself is not a biologic claim.

---

What generic entry scenarios exist for proliferative retinopathy angiogenesis inhibitors?

Scenario 1: accused generic contains the claimed scaffold

• High infringement risk on product claims (1/6) and composition claims (2/7).
• Method claims (5/10) also create labeling/inducement exposure if the generic is marketed for proliferative retinopathy using the claimed compound.

Scenario 2: generic uses the same scaffold but excludes “composition with carriers” requirements

This scenario is unlikely because carriers are inherent to any formulation. Composition claims are typically easy to satisfy if the generic includes the compound in a pharmaceutically acceptable formulation.

Scenario 3: generic uses different scaffold but matches indication

• Likely avoids literal infringement on the compound formula claims.
• Could still face doctrine of equivalents exposure depending on claim construction and prosecution history estoppel, but those inputs are not present here.

---

What is the Orange Book status of US 7,105,530?

No Orange Book listing mapping can be provided from the excerpt. Orange Book status is tied to specific FDA-approved drug products and active ingredients plus listed patents for specific NDA/ANDA products. The missing chemical identity prevents a reliable match.

---

What patent litigation affects US 7,105,530 (Paragraph IV, settlements, injunctions)?

No litigation docket, settlement agreement, or Paragraph IV activity is provided in the user record. Without an accused product identity or the patent’s application/active ingredient mapping, litigation outcomes cannot be tied to this patent number in a way that is decision-grade.

---

How many patents cover this therapeutic approach around US 7,105,530?

Because the active chemical formula is missing from the provided claim excerpt, the patent landscape cannot be quantified (count of related continuations, related continuations-in-part, continuation families, and overlapping method/composition patents). Any numeric “how many patents” statement would be speculative.

---

Key takeaways

• US 7,105,530 protects a specific compound formula scaffold (claims 1/6), broad pharmaceutical compositions using that scaffold with pharmaceutically acceptable carriers (claims 2/7), and methods for treating proliferative retinopathy via inappropriate angiogenesis in mammals (claims 5/10).
• The patent has dependent combination-therapy hooks for adding an anti-neoplastic agent (claims 3/8) and/or an angiogenesis inhibitor (claims 4/9) to formulations containing the scaffold.
• The commercial risk profile depends on whether an accused product contains the same scaffold (structure infringement) and whether clinical/marketing use targets proliferative retinopathy (method exposure).
• A complete landscape (Orange Book mapping, expiration calendar, Paragraph IV and settlement history, and chemical competitor coverage) cannot be determined from the excerpt because the defining chemical formula text is not included.

---

FAQs

1. Can a product infringe US 7,105,530 without being marketed for proliferative retinopathy?
   Yes, depending on whether product and composition claims are met by containing the claimed compound and formulation. Method claims require treatment of proliferative retinopathy.

2. Do the dependent combination claims require both an anti-neoplastic agent and an angiogenesis inhibitor?
   No. They are separate dependent claims: claim 3/8 require an anti-neoplastic agent; claim 4/9 require an angiogenesis inhibitor.

3. Would using a different salt form avoid infringement?
   Not if the salt is a pharmaceutically acceptable salt that falls within the patent’s “salt thereof” scope and is covered by the specification definitions.

4. What are the main design-around paths for competitors?
   Moving outside the claimed chemical formula boundaries for the compound claims, and/or avoiding formulations that meet the dependent combination-agent definitions, and/or avoiding labeled/induced use for proliferative retinopathy for method claims.

5. Does US 7,105,530 likely cover ocular formulations specifically?
   The method claim targets proliferative retinopathy, but composition claims are carrier-based and not limited in your excerpt. Ocular support depends on the specification and claim interpretation.

---

References (APA)

1. United States Patent 7,105,530. (n.d.). Claims and specification (as provided in user excerpt).

Drugs Protected by US Patent 7,105,530

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: 7,105,530

PCT Information
PCT Filed	December 19, 2001	PCT Application Number:	PCT/US01/49367
PCT Publication Date:	August 01, 2002	PCT Publication Number:	WO02/059110

International Family Members for US Patent 7,105,530

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1343782		C300456	Netherlands
European Patent Office	1343782		CA 2010 00024	Denmark
European Patent Office	1343782		91710	Luxembourg