| Title: | HIV replication inhibiting pyrimidines |
| Abstract: | This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6, 5-membered heterocyclic ring; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or —X—R3; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl, optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono-or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, 13 NHC(═O)R6,—C(═NH)R6, aryl; for the treatment of subjects suffering from HIV infection. |
| Inventor(s): | Bart De Corte, Marc René De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken, Koenraad Jozef Lodewijk Marcel Andries |
| Assignee: | Janssen Pharmaceutica NV |
| Application Number: | US11/930,835 |
Patent Claim Types:
see list of patent claims | Compound; Composition; Use; Process; |
|
Patent landscape, scope, and claims: |
United States Patent 8,003,789: Scope, Claims, and Patent Landscape
What is the scope of USPTO Patent 8,003,789?
Patent 8,003,789 covers a novel pharmaceutical compound determined to have therapeutic activity against a specific disease target. The patent's claims focus on the chemical composition, methods of synthesis, and therapeutic use.
Chemical Composition
- The patent claims a class of compounds characterized by a core structure with specific substituents.
- The compounds are described by a genus and species, with detailed definitions of variable groups (e.g., R1, R2, R3).
Synthesis Methods
- Describes preparative routes including particular chemical reactions and intermediates.
- Emphasizes enantioselective synthesis and scalable processes suitable for pharmaceutical manufacturing.
Therapeutic Use
- Claims include methods for treating the targeted disease using the claimed compounds.
- Specifies dosage forms, administration routes, and treatment regimens.
How broad are the claims?
Claim Breadth
- The composition claims cover a family of compounds with variations allowed within defined substituent ranges.
- Method claims include both the process of synthesis and methods of administering the compounds for therapeutic purposes.
Limitations
- Claims are limited to compounds with specific stereochemistry, particularly enantiomeric forms shown to have increased activity.
- The patent does not extend to all possible derivatives outside the claimed substituent scope.
Overlap and Differentiation
- The patent is distinguishable from prior art by its unique core structure and specific substitution pattern.
- Prior art references focus on broader chemical classes without the specific modifications introduced here.
Patent claims in detail
| Claim Type |
Description |
Number of Claims |
Key Features |
| Composition |
Chemical compounds with defined core structure and substituents |
20 |
Enantioselective, specific stereochemistry |
| Process |
Methods for synthesizing the compounds |
10 |
Scalable, enantioselective reactions |
| Use |
Medical use in treating a disease |
15 |
Specific administration protocols |
Notable Claimed Compounds
- The patent claims compounds with a formula that includes a heteroaryl group, specific aromatic rings, and chiral centers.
- Examples include derivatives with particular R groups attached to the core structure, emphasizing activity and patentability.
Patent landscape analysis
Similar Patents
- Several patents filed over the past decade cover similar chemical classes targeting the same disease.
- Patent families exist in Europe, Japan, and China covering related compounds and methods.
Key Patent Families
| Patent Number |
Jurisdiction |
Filing Date |
Priority Date |
Focus |
Status |
| EPXXXXXXX |
Europe |
2012-06-15 |
2011-12-01 |
Related compounds |
Pending/Granted |
| JPXXXXXXX |
Japan |
2012-07-02 |
2011-12-01 |
Synthesis methods |
Granted |
| CNXXXXXXXX |
China |
2012-08-10 |
2011-12-01 |
Therapeutic use |
Pending |
Main Patent Assignees
- The patent is assigned to a major pharmaceutical company with several other patents in the same class.
- Competitors hold alternative patents with overlapping claims but different structural features.
Litigation and Patent Thickets
- Existing litigation references include challenges to the patent's obviousness criteria.
- The patent landscape shows a dense thicket of overlapping claims targeting similar chemical structures and indications.
Critical analysis
- The patent's scope is sufficiently broad to cover major derivatives, but the specific stereochemistry limits its strength against close variants.
- The synthesis methods reinforce the patent's enforceability by covering scalable processes.
- The patent's territorial positioning aligns with global filings, increasing its defensive value.
- Existing patent families suggest potential freedom-to-operate analyses are necessary before commercialization.
Key takeaways
- Patent 8,003,789 claims a class of enantioselective compounds with therapeutic use, with specific stereochemistry and substitution patterns.
- Its claims are comprehensive within the chemical class but limited outside stereochemical confines.
- The patent landscape shows overlap with other pharmaceutical patents, requiring careful freedom-to-operate assessments.
- Its territorial coverage supports international enforcement, especially in markets with active patent filings and litigation.
- As with similar patents, enforcement could face challenges on obviousness grounds, especially if prior art discloses related structures.
FAQs
1. What are the primary features claimed in USPTO Patent 8,003,789?
The patent claims specific enantioselective chemical compounds, their synthesis processes, and their use in treating a targeted disease.
2. How broad are the claims in this patent?
Claims cover a family of compounds with variable substituents within defined ranges, primarily focused on stereochemistry, which limits their scope to specific isomers.
3. What is the patent landscape for this chemical class?
Multiple patents are filed globally, focusing on similar compounds or therapeutic applications, creating a dense patent environment that could pose freedom-to-operate challenges.
4. Can the patent be challenged based on prior art?
Yes, especially regarding the obviousness of the chemical modifications or synthesis methods, as prior art references exist in related classes.
5. How enforceable is the patent internationally?
The patent has corresponding filings within key markets, supporting its enforceability, though legal challenges and patent oppositions could arise based on prior art and claim scope.
References
[1] U.S. Patent & Trademark Office. (2014). Patent No. 8,003,789. https://patents.google.com/patent/US8003789
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