Transcript New Molecule, Red, Lilly Brand PowerPointTemplate

Functional Claim Elements
in the Unpredictable Arts
2015 AIPLA Spring Meeting
Robert D. Titus – Sr. Director
Introduction
♦ The use of functional language in a peripheral claiming
paradigm is an efficient way to broaden claim scope.
♦ Unpredictability is a recognized property of the chemical arts
and there is a tension between claim scope and the written
description requirement of 35 U.S.C. § 112 as the University
of Rochester, Ariad, and AbbVie line of cases just discussed
aptly demonstrates.
♦ The AbbVie decision has important implications for the use of
functional elements in claims encompassing inventions in the
chemical arts.
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Context
♦ The pharmaceutical industry’s business model relies heavily
on robust patent exclusivity to sustain drug discovery and
development.
♦ Intellectual property rights to every product will be challenged
internationally.
♦ Experience with patent validity challenges and recent IPR
proceedings demonstrate that not all patent claims can
withstand post-grant review.
♦ It is through this lens that the following views of the
application of AbbVie are offered for your consideration.
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Problem Statement
♦ The question reduces to what level of written description is
required to support the desired claim scope breadth.
• “No bright-line rules govern the number of species that must
be disclosed to describe a genus claim, as this number
necessarily changes with each invention, and it changes with
progress in the field.”
• “The level of detail required to satisfy the written description
requirement varies depending on the nature and scope of the
claims and on the complexity and predictability in the
relevant technology.
♦ The impact of AbbVie in the chemical arts depends upon:
1) the field of technology of the claimed invention; and
2) the relationship of the functional claim element to the theory of
patentability of the claimed invention as a whole.
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Formulations
♦ Functional elements are commonly used in patent claims
encompassing this technology space: flavoring, colorant, coating,
lubricant, dispersant, diluent.
• Each represents a well-defined class of structures and a standard
understanding of function (USP; FDA; Remington, The Science and
Practice of Pharmacy)
♦ “A pharmaceutical formulation comprising Compound A, an antioxidant,
and optionally an enteric coating.”
• Compound A is novel;
• Functional elements are “antioxidant” and “enteric coating”
• Patentability of this formulation flows from the patentability of Compound A
♦ No specific formulation exemplification necessary to support claim
scope.
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Formulations
♦ A specific acid-labile coating is necessary to assure that Compound
B, a prior art molecule, is released at low pH to avoid base catalyzed
degradation.
• Patentability is no longer dependent upon the formulated molecule,
rather is now dependent upon the constituent elements of the
formulation itself.
♦ What claim scope could be pursued?
Compound
Coating
Functional Elements
Compound B
Specific coating
No
Compound B
Acid-labile coatings
Yes
Base-sensitive compounds
Specific coating
Yes
Base-sensitive compounds
Acid-labile coatings
Yes
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Formulations
♦ A claim limited to Compound B and the specific coating contains no
functional elements, so exemplification is limited to that which demonstrates
the claimed invention possesses the desired properties.
♦ A claim encompassing the functional element “acid-labile coatings” would
require sufficient exemplification to demonstrate that formulations with a
variety of coatings possess the desired properties.
• Suitable coatings would be part of a closed set of pharmaceutically
acceptable members, and so exemplification would not need to be
extensive.
♦ A claim encompassing the functional element “base-sensitive compound”
would require sufficient exemplification to demonstrate that the breadth of
coatings in the claim were generally applicable to compounds that have the
base-sensitivity property regardless of structure.
• This would require extensive exemplification to meet the AbbVie
standard.
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Process Claims
♦ Chemical process claims commonly employ functional elements:
reducing agent, buffer, acid, base, solvent.
• These functional elements have standard meanings in the art and
frequently the specification will include additional context to cabin the
intended scope of each term.
♦ Process claims directed to a method of preparing a novel molecule
can derive patentability from the molecule itself.
• A specific synthetic example would likely be sufficient.
♦ When the patentability of the process is no longer dependent upon
the molecule prepared and depends on aspects of the process per
se, however, the degree of specific exemplification must be
expanded to support the breadth of the functional elements if they
are central to the theory of patentability.
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Process Claims
“A method of oxidizing glucose comprising contacting an aqueous
solution of glucose with oxygen or an oxygen containing gas, and a
cupric catalyst.”
♦ Glucose and its oxidation product are well known in the art as are
oxygen (oxidizing agent) and water (solvent).
♦ Functional element is “cupric catalyst”
• In its broadest interpretation, “cupric catalyst” would be any copper (II)
complex that catalyzes the oxidation of glucose by elemental oxygen
• 6 cupric catalysts are specifically named in the specification and 4 of
these are demonstrated to be operative in the claimed process
• All named cupric catalysts are structurally similar chelates
♦ AbbVie holding increases risk in relying on claim with “cupric
catalyst” scope.
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Composition of matter
♦ Purely functional elements are commonly employed in claims
directed to a composition of matter, expanding the structural space
encompassed by the claims without structural limitation.
•
•
•
•
leaving group
protecting group
electron withdrawing group
prodrug
♦ The function these terms describes is typically well-accepted, but
the structural space encompassing moieties that possess these
functions is vast.
• The skilled person would appreciate that not every member performing
the desired function generally works in all instances.
♦ How could the AbbVie decision impact claims incorporating these
functional elements?
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Functional Elements
“A compound of Formula I or a prodrug thereof.”
♦ A prodrug is a derivative or analog of a molecule that must undergo
transformation to the active moiety prior to exhibiting the desired
pharmacological activity.
• The complexity of in vivo conversion coupled with distribution and
metabolism of the resulting compound renders the prodrug arts highly
unpredictable.
♦ The prodrug functional element applies to two sites:
R1 is H or Prodrug
R2 is H or Prodrug wherein only 1 of R1 and R2 is H.
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Functional elements
♦ The functional element “prodrug” encompasses a breathtaking
scope.
• Approximately 40 potential prodrug moieties were listed in the
specification
• 20 different prodrug moieties were specifically exemplified
• The specification reports data for only 1 prodrug derivative of the parent
molecule that demonstrates the requisite properties.
♦ What claim scope would meet written description after AbbVie?
• Claim with functional element “prodrug” would not.
– Vast structural space
– Highly unpredictable art
– Exemplification sparse relative to scope of functional element
• Claim encompassing exemplified and/or listed species likely would.
– Beware enablement challenge!
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“Quasi-functional” elements
♦ “Quasi-functional” elements are used in composition of matter
claims.
• derivative thereof
• analog thereof
♦ These terms expand claim scope into structural space constrained
only by a relationship to exemplified compounds and their utility.
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“Quasi-functional” elements
“A conjugate of peptide A or analog thereof.”
• “Analog” defined to be “a derived protein with substitution, deletion or
addition of one or several amino acids in the amino acid sequence
defined by SEQ ID NO: 1, while maintaining activities of peptide A.”
• Only 1 specific example of an analog is provided in the specification and
it is shown to possess the requisite activity.
♦ What claim scope would meet written description after AbbVie?
• Claim containing functional element “analog thereof” would not.
• Claim encompassing peptide A and the exemplified analog would.
• No written description to anything of intermediate scope.
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“Quasi-functional” elements
“A compound of formula (I):
wherein A represents a heteroaryl group which is unsubstituted or
mono-, di-, or tri-substituted, wherein the substituents are
independently selected from the group consisting of halogen, C1-C4
alkyl, C3-C6 cycloalkyl, and phenyl.”
♦ Is it possible for a generic structural term (heteroaryl) to be
construed as a quasi-functional element to which AbbVie would
apply?
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“Quasi-functional” elements
♦ Taken alone, the term “heteroaryl” is expansive, particularly when
multiple substitutions are contemplated.
♦ The following definition is commonly used: “The term heteroaryl
means a 5- to 10-membered monocyclic or bicyclic aromatic ring
containing 1, 2, or 3 heteroatoms independently selected from
oxygen, nitrogen, and sulfur.”
♦ Used as a claim element, it is effectively expanding claim scope to
include a molecule within formula 1 that bears a heteroaryl moiety
within the definition that possesses the utility asserted for the genus
as a whole.
• If AbbVie applies to this situation, the level of exemplification and
definitions in the specification will need to be significantly expanded to
for the written description to support the quasi-functional element
“heteroaryl”.
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Recommendations
♦ AbbVie increases the risk of relying on claims where functional
elements are central to the theory of patentability for the invention as
a whole. The increased risk will impact:
• Due diligence assessments
• FTO assessments
• Risk-sharing expectations in licensing arrangements
♦ A mitigation strategy would be to:
• Avoid or minimize the use of functional elements altogether;
• Increase the degree of disclosure in the specification related to the
functional element:
– Add prophetic examples/substituent charts (prior art impact; effect OUS);
– Add actual examples (increased costs; additional research required);
– Add data demonstrating efficacy across greater structural space;
• Increase specific basis for variable claim scope for structural element.
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Thank You!
An excellent review on PTAB treatment of functional claiming is:
Tom Brody, Functional Elements in Patent Claims as Construed by the
Patent Trial and Appeal Board (PTAB), 13 J. MARSHALL REV.
INTELL. PROP. L. 251(2014).
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