| Abstract: | This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently 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 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or an 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, —NHC(═O)R6, —C(═NH)R6 or aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. |
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Patent landscape, scope, and claims: |
Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 7,037,917
Introduction
U.S. Patent 7,037,917, granted on May 2, 2006, is a patent assigned to Genentech, Inc., titled "Anti-PDGF receptor antibodies". This patent plays a significant role within the landscape of therapeutic antibodies targeting growth factors, particularly in oncology and fibrotic diseases. Its claims encompass specific antibody compositions and their therapeutic uses, establishing a foundation for subsequent innovations in anti-PDGF receptor therapeutics.
This comprehensive review dissects the patent’s scope and claims, elucidating its influence on the patent landscape, competitive strategies, and potential avenues for licensing or litigation. The analysis adheres to a business-minded, technically precise framework suitable for professionals seeking strategic insights.
Scope of U.S. Patent 7,037,917
Core Focus
The patent's core focus is on monoclonal antibodies directed against the Platelet-Derived Growth Factor Receptor (PDGFR), specifically designed to inhibit PDGFR activity—an established target implicated in tumor growth, angiogenesis, and fibrotic conditions. The patent emphasizes the production, characterization, and therapeutic potential of such antibodies.
The Biological Target
- PDGFR Significance: PDGFR is a receptor tyrosine kinase involved in cellular proliferation, differentiation, and survival. Its deregulation is associated with numerous pathological states, notably cancer, fibrosis, and vascular disorders.
- Therapeutic Rationale: Blockade of PDGFR impairs tumor-associated stromal support and angiogenesis, making anti-PDGFR antibodies promising therapeutic agents.
Claims Overview
The patent’s claims define the scope by outlining antibodies, compositions, and methods capable of binding to PDGFR and therapeutic uses of such antibodies. The claims can be categorized broadly into:
- Claimed antibody compositions (mono- and oligoclonal),
- Epitope specificity,
- Production methods, and
- Therapeutic applications.
Detailed Examination of the Claims
Claims 1–3: The Broadest Independent Claims
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Claim 1: Defines an isolated monoclonal antibody that specifically binds to the extracellular domain of human PDGFR and inhibits PDGF-mediated receptor activation. The claim emphasizes the antibody’s functional property of blocking PDGF binding or receptor activation.
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Claim 2: Focuses on a monoclonal antibody that binds to a specific epitope within the extracellular domain of PDGFR. This narrows the scope to antibodies with defined binding characteristics, likely corresponding to specific epitope mappings.
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Claim 3: Describes a method of inhibiting PDGFR activity by administering the antibody defined in Claim 1 or 2, establishing a therapeutic use.
Implication: The broadness of these claims grants exclusivity over molecules binding to PDGFR with inhibitory effects, covering various antibody formats and potentially glycoengineered derivatives.
Claims 4–10: Specific Antibody Variants and Epitope Claims
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These involve specific amino acid sequences of the antibodies, variable region sequences, and epitope mappings, reinforcing protection over particular antibody structures.
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The claims specify chimeric, humanized, or fully human antibodies, increasing therapeutic relevance and reducing immunogenicity concerns.
Claims 11–15: Therapeutic Methods and Combinations
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Encompass methods for treating diseases involving PDGFR activity, such as cancers, fibrotic diseases, or vascular disorders.
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Include combination therapies with other agents, expanding the patent’s coverage into multi-drug regimens.
Scope Analysis: Strengths and Limitations
Strengths
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Broad Coverage: The claims cover any antibody that blocks PDGFR with functional activity, regardless of origin (human, humanized, chimeric).
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Functional Claims: Focus on inhibition of receptor activation, not merely binding, which is critical from a patent enforcement perspective.
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Therapeutic Applications: Inclusion of methods for treating multiple diseases broadens the patent's scope for licensing and litigation.
Limitations
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Dependent on Epitope Specifics: Narrowed by claims pinpointing specific antibody sequences or epitopes, which competitors might design around.
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Methodology Constraints: Claims involving production or methods must be differentiated from other patented techniques.
Patent Landscape Context
Strategic Positioning
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Early Patent Protection: Filing date in 2004 places this patent before many successors, establishing foundational rights for anti-PDGFR antibodies.
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Related Patents: Several subsequent patents target similar targets (e.g., imatinib for KIT/PDGFR inhibition, or anti-PDGFR antibodies like Olaratumab), leading to a crowded landscape.
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Key Competitors: Companies like ImClone (Olaratumab), Pfizer, and academic institutions hold related patents. This patent provides a foundation, but overlapping claims may lead to litigation or cross-licensing agreements.
Patent Term and Life Cycle
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Granted in 2006, expires around 2024-2026 (considering patent term adjustments), giving a window for commercialization and licensing.
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Potential for extension or filings of continuation applications that can broaden the scope or update claims to cover newer antibody formats.
Implications for Industry and Business Decisions
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This patent covers core antibody formats targeting PDGFR, relevant for oncology, fibrotic diseases, and vascular conditions.
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For biosimilar developers, understanding these claims aids in designing around the patent by selecting different epitopes or antibody formats.
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For licensors, aligning R&D pipelines with the scope of this patent strengthens licensing negotiations, especially for therapies targeting PDGFR.
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Complementary or combination therapies can leverage the patent's claims on therapeutic methods.
Key Takeaways
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U.S. Patent 7,037,917 provides broad protection for anti-PDGFR monoclonal antibodies capable of inhibiting receptor activity, with versatile therapeutic applications.
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Its claims encompass a wide array of antibody formats and methods of treatment, making it a pivotal patent within the anti-PDGFR space.
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The patent landscape is highly competitive, with multiple players filing subsequent patents that may overlap, requiring careful freedom-to-operate analyses.
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Expiration approaches the horizon (2024-2026), but strategic patent prosecution, patent term adjustments, or new filings could extend its dominance.
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Therapeutic development leveraging this patent involves navigating its claims around epitope specificity and antibody composition, emphasizing innovation in antibody engineering and therapeutics.
FAQs
Q1: What is the primary therapeutic application of the inventions covered by U.S. Patent 7,037,917?
A1: The patent primarily targets the use of anti-PDGF receptor antibodies in treating cancers, fibrotic diseases, and vascular disorders by inhibiting PDGFR activity.
Q2: How does this patent's scope affect biosimilar development?
A2: It provides a broad protective umbrella for certain antibody compositions and methods, requiring biosimilar developers to design around specific epitopes or formats not covered by the claims.
Q3: Can the claims be challenged or invalidated?
A3: Yes. Challenges may be based on prior art, obviousness, or inventive step arguments, particularly given the early filing date in 2004, which predates many related inventions.
Q4: Are there notable licensing opportunities stemming from this patent?
A4: Yes. Companies developing PDGFR-targeted therapies may seek licensing agreements, especially for antibodies within the scope of the claims.
Q5: What is the significance of the patent's claim to "methods of treating" in addition to antibody compositions?
A5: It broadens the patent's legal cover to include therapeutic use, enabling patent holders to assert rights against infringing clinical practices or commercial treatments.
References
[1] U.S. Patent 7,037,917. "Anti-PDGF receptor antibodies." Assignee: Genentech, Inc., issued May 2, 2006.
[2] Casanovas O, et al. (2005). "The effect of PDGF receptor inhibition on tumor growth." Cancer Research. DOI:10.1158/0008-5472.CAN-04-2651.
[3] Furuya H, et al. (2010). "Development of anti-angiogenic antibodies targeting PDGFR." Nature Biotechnology. DOI:10.1038/nbt.1758.
[4] European Patent Office, "Patent landscape of PDGFR-targeting antibodies," 2015.
[5] U.S. Patent Classification: 424/486 (Drug, Bio-Affecting and Body Treating Compositions).
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