Details for Patent: 7,067,522
Summary for Patent: 7,067,522
| Title: | 2,4,DI (hetero-) arylamino (-oxy)-5-substituted pyrimidines as antineoplastic agents |
| Abstract: | Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described. |
| Inventor(s): | Elizabeth Janet Pease, Emma Jane Williams, Robert Hugh Bradbury, Stuart Eric Pearson |
| Assignee: | AstraZeneca AB |
| Application Number: | US10/995,931 |
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Patent Claim Types: see list of patent claims | Use; Composition; Process; |
| Patent landscape, scope, and claims: | US Patent 7,067,522: Scope, Claims, and US Patent Landscape for Pyrimidine DerivativesUS Patent 7,067,522 claims a broad genus of pyrimidine derivatives defined by a tightly controlled core scaffold (Formula (I)) plus extensive enumerations of substituents on (i) the anilino/heteroaryl-linked pyrimidine rings (Q1 and Q2) and (ii) an anilino-like substituent set on the pyrimidine nitrogen- or carbon-linked position (R1, G, and substituent sets on the “anilines”/aryl rings). The claims also cover processes, pharmaceutical compositions, and method-of-use for cell-cycle inhibition, FAK inhibition, and selective CDK2/CDK4/CDK6 inhibition. What exactly is claimed? (Claim set overview)US 7,067,522 contains claims 1 to 15, with claims 1 to 9 covering compounds and the remainder covering downstream activities. Product (compound) claims
Method and enablement claims
How broad is Claim 1, structurally? (Formula (I) scope and degrees of freedom)Claim 1 is a genus built from four main “handles”: 1) Pyrimidine core substituted at an anilino position
2) G selects the linker type
3) R1 governs the pyrimidine’s other substituent
4) Q1 and Q2 carry extensive substituent setsFor each of Q1 and Q2, the claim allows up to:
Both Q1 and Q2 are permitted to contain:
Salt/ester coverage is explicit:
Business implication: Claim 1 is not limited to a single lead; it is a wide coverage net that captures many medicinal-chemistry permutations around a pyrimidine-anilino-like pharmacophore and preserves a wide substitution allowance on both aromatic appendages. What is the claim’s “chemical perimeter” (what is tightly constrained vs open)?Tight constraints
Open design space
Business implication: The patent is strongest where competitors stay within the formula architecture and substitute within these allowed aromatic and linker classes. How do the dependent claims narrow the genus (and where competitors might attack)?Claim 2: Q1 = phenyl
Claim 3: Q2 = phenyl or pyridyl
Claim 4: specific substituent set list
Claim 5: Q1 substitution position
Claim 6: G = —NH—
Claim 7: R1 limited
Claim 8: Q2 mono-substitution limited set
Claim 9: named examples
Business implication: Even if you design outside the exemplars, claim 1 still spans broad substitution space. Attacking the patent requires moving outside the claim’s formula boundaries (especially the scaffold identity, Q1/Q2 linking type, and the G class). What are the method-of-use hooks (and how they shape enforcement risk)?Claims 12-15 connect compounds of Formula (I) to target biology:
Business implication: This set is designed to support enforcement across: 1) broad anti-proliferation claims (lower threshold), 2) specific target engagement (FAK, CDKs), 3) and a functional readout (cell cycle inhibition). It also means the same chemical coverage can be argued across multiple therapeutic hypotheses if label statements or study reports align to those endpoints. What does Claim 10 cover on the chemistry side (process scope)?Claim 10 is a route claim that depends on whether G is —NR2—, with key elements:
Business implication: Process coverage can matter for contract manufacturing and for generic entry routes, even if competitor structures differ but still use the same core substitution strategy inside Formula (I). How would you map the patent landscape in the US (practical landscape logic for this specific patent)?This patent’s landscape impact typically falls into four buckets: 1) Freedom-to-operate risk anchored to Formula (I)
2) Target-label alignment risk
3) Synthesis-route overlap risk
4) Stepping-stone claim narrowing
Key takeaways
FAQs1) What is the central structure protected by US 7,067,522?A pyrimidine derivative of Formula (I) defined by Q1/Q2 aryl or heteroaryl linked via ring carbon, with linker G = —O— or —NR2— and a pyrimidine substituent R1 selected from enumerated classes, plus wide substitution options on Q1 and Q2 and on R2/Rc-related moieties. 2) Does the patent cover both ether and amine linker families?Yes. Claim 1 allows G = —O— (ether family) or G = —NR2— (amine family). Claim 6 narrows to G = —NH—. 3) Are salts and hydrolysable esters included?Yes. Claim 1 explicitly covers pharmaceutically acceptable salts and in vivo hydrolysable esters formed from available carboxy or hydroxy groups. 4) What biological targets and endpoints are claimed?
5) Are specific chemical examples explicitly listed?Yes. Claim 9 enumerates multiple named compounds, including 4-anilino-5-bromo-2-[substituted anilino]pyrimidines with specific substituent patterns on the anilino ring. References[1] US Patent 7,067,522, “Pyrimidine derivatives,” claims 1-15 (provided claim text). More… ↓ |
Drugs Protected by US Patent 7,067,522
| Applicant | Tradename | Generic Name | Dosage | NDA | Approval Date | TE | Type | RLD | RS | Patent No. | Patent Expiration | Product | Substance | Delist Req. | Patented / Exclusive Use | Submissiondate |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| >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: 7,067,522
| Foriegn Application Priority Data | ||
| Foreign Country | Foreign Patent Number | Foreign Patent Date |
| United Kingdom | 0004887 | Mar 01, 2000 |
International Family Members for US Patent 7,067,522
| Country | Patent Number | Estimated Expiration | Supplementary Protection Certificate | SPC Country | SPC Expiration |
|---|---|---|---|---|---|
| Austria | 472537 | ⤷ Start Trial | |||
| Australia | 2001233979 | ⤷ Start Trial | |||
| Australia | 3397901 | ⤷ Start Trial | |||
| >Country | >Patent Number | >Estimated Expiration | >Supplementary Protection Certificate | >SPC Country | >SPC Expiration |
