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Patent: 6,037,361
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Summary for Patent: 6,037,361
| Title: | Fluorinated butyric acids and their derivatives as inhibitors of matrix metalloproteinases |
| Abstract: | Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1, and also collagenase, matrilysin, and MMP-13, and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer\'s disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson\'s disease, Huntington\'s disease, prion diseases, myasthenia gravis, and Duchenne\'s muscular dystrophy. |
| Inventor(s): | Roth; Bruce David (Plymouth, MI), O\'Brien; Patrick Michael (Stockbridge, MI), Sliskovic; Drago Robert (Saline, MI) |
| Assignee: | Warner-Lambert Company (Ann Arbor, MI) |
| Application Number: | 09/036,751 |
| Patent Claims: | see list of patent claims |
| Patent landscape, scope, and claims summary: | Critical Analysis of US Patent 6,037,361 Claim Scope and the U.S. Patent Landscape US Patent 6,037,361 is a U.S. small-molecule composition-of-matter and broad method-of-use patent built around Formula I compounds with dibenzofuran or dibenzothiophene-type aryl scaffolds bearing difluoro substitution patterns and α-oxo/α-hydroxyimino and acid/amidic functional groups (plus prodrugs and salts). The claims are dense but commercially oriented: they cover a wide genus of fluorinated metalloproteinase (MMP) inhibitors and then expand into many disease areas where MMP activity is implicated, using functional language at the disease level. This estate can create substantial entry friction for generic or follow-on developers because (1) claim 1 is a genus with multiple substituent positions and multiple allowed heteroaryl/aryl and linker options, (2) dependent claims narrow to particular Y linkers and specific fluorinated acid sub-genuses, and (3) the methods claims are framed as inhibition of specific MMPs (gelatinase A, stromelysin-1, collagenase, matrilysin, MMP-13) and as treatment/prevention of plaque rupture, restenosis, and a broad set of inflammatory, wound-healing, ocular, autoimmune, neurodegenerative and cancer indications. What patents protect US 6,037,361 Formula I metalloproteinase inhibitors?Answer: US 6,037,361 protects (i) Formula I compounds and their isomers, prodrugs, and salts, (ii) pharmaceutical compositions, and (iii) methods of inhibiting MMPs and treating/preventing a wide set of diseases tied to tissue invasion and matrix remodeling. What is the core claim technology in claim 1?Claim 1 recites:
How broad is the genus in practical freedom-to-operate terms?Claim 1 is broad in three ways that matter for generics and licensing:
This structure makes it easier for an inventor in the same chemical family to land “inside” the same claim 1 genus, even if they avoid specific embodiments named later. What do the dependent claims add?
From an enforcement perspective, claim 7’s enumerated examples create a clean set of “anchor” molecules for claim construction and validity arguments, because you can map real structures into the claim language without relying solely on interpretive flexibility. Which exact compounds are named in claim 7, and why does that matter?Answer: Claim 7 lists a set of specific fluorinated dibenzofuran/dibenzothiophene acids, hydroxyimino variants, thioxo variants, enone (“but-2-enoic”) variants, and specific aryl-substituted analogs, each with difluoro patterns and acid or amide functional groups, plus “corresponding isomers,” prodrugs and salts. Named embodiments (examples in claim 7)The claim includes compounds such as:
Why listing matters for enforcement and validity
What methods claims does US 6,037,361 include, and how might they expand infringement?Answer: The patent includes methods of inhibiting specific MMPs (matrix metalloproteinase, gelatinase A, stromelysin-1, collagenase, matrilysin, MMP-13) and then expands to prevention/treatment of indications including atherosclerotic plaque rupture, aortic aneurysm, heart failure, restenosis, periodontal disease, corneal ulceration, burns, decubital ulcers, wound healing, and cancer, plus arthritis, autoimmune/inflammatory disorders, multiple sclerosis, inflammation and pain, and a list of neurodegenerative disorders (stroke, head trauma, spinal cord injury, Alzheimer’s, ALS, cerebral amyloid angiopathy, AIDS, Parkinson’s, Huntington’s, prion diseases, myasthenia gravis, Duchenne muscular dystrophy). How the methods are drafted
Litigation risk pattern if a competitor sells an MMP inhibitor in this classIf a marketed product uses a compound that falls under claim 1’s genus, then:
What is the composition-of-matter and formulation coverage in US 6,037,361?Answer: The patent includes pharmaceutical compositions as claim 31–32: a compound according to claim 1 in admixture with pharmaceutically acceptable excipient/diluent/carrier, with and without specifying “therapeutically effective amount.” Why this matters for generics and follow-on formulations
How strong is the patent estate for this chemical series in the U.S.?Answer: Based on the claims alone, US 6,037,361 has high structural coverage (broad genus plus fluorine/linkage constraints) and broad use coverage (multiple MMPs and many indications). The estate’s strength relative to competitors will depend on whether later continuations, divisionals, or related patents exist in the same filing family that capture:
This analysis cannot map the full family without the application/patent history, publication numbers, and other U.S. patents in the same priority chain. What generic entry risks exist for products that target MMPs using similar fluorinated dibenzofuran motifs?Answer: If a generic or follow-on applicant’s active ingredient is within claim 1, then generic launch is blocked at least by the composition and genus coverage, and may also be blocked by method-of-use risk depending on FDA labeling and actual use. Where design-arounds typically fail against this claim set
Practical consequence for a challengerA developer would need to ensure the active ingredient structure falls outside:
What are the likely infringement “claim mapping” hotspots?Answer: The easiest-to-prove claim elements against accused products are the structural provisos and the functional group class. Hotspots within claim 1
Key Takeaways
FAQs1) Does US 6,037,361 cover prodrugs and salts? 2) Which MMP targets are explicitly named in the methods claims? 3) Are both compound and method of treatment claims present? 4) Do the dependent claims narrow “Y” to specific linkages? 5) What is the practical workaround most likely to fail against this patent? References
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Details for Patent 6,037,361
| Applicant | Tradename | Biologic Ingredient | Dosage Form | BLA | Approval Date | Patent No. | Expiredate |
|---|---|---|---|---|---|---|---|
| Smith & Nephew, Inc. | SANTYL | collagenase | Ointment | 101995 | June 04, 1965 | 6,037,361 | 2018-03-09 |
| >Applicant | >Tradename | >Biologic Ingredient | >Dosage Form | >BLA | >Approval Date | >Patent No. | >Expiredate |
