Ex parte OPITZ

Board of Patent Appeals and Interferences

Mar 24, 1998

07953439 (B.P.A.I. Mar. 24, 1998)

Application for patent filed September 29, 1992. 1
According
to applicant, this application is a continuation of
Application 07/675,835, filed March 27, 1991, now abandoned.
Applicant also claims the benefit under 35 U.S.C. § 119 of the
March 29, 1990, filing date of Federal Republic of Germany
Application P 4010079.0.
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THIS OPINION WAS NOT WRITTEN FOR PUBLICATION
The opinion in support of the decision being entered today
(1) was not written for publication in a law journal and
(2) is not binding precedent of the Board.
Paper No. 34
UNITED STATES PATENT AND TRADEMARK OFFICE
____________
BEFORE THE BOARD OF PATENT APPEALS
AND INTERFERENCES
____________
Ex parte K. OPITZ
____________
Appeal No. 94-4129
Application 07/953,4391
____________
ON BRIEF
____________
Before WINTERS, SCHAFER, and GRON, Administrative Patent
Judges.
GRON, Administrative Patent Judge.
Appeal No. 94-4129
Application 07/953,439
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DECISION ON APPEAL UNDER 35 U.S.C. § 134
1. Introduction
This is an appeal from an examiner’s rejection of
Claims 16-19. Nonelected Claims 11-15 and 20 have been
withdrawn from further consideration by the examiner in
accordance with
37 CFR § 1.142(b). Claims 16-19 stand finally rejected under
35 U.S.C. § 103 as being unpatentable in view of the combined
teachings of Davis, U.S. 4,663,318 (patented May 5, 1987), and
Bundesrepublik Deutschland Patentschrift DE 3,843,239
(published February 22, 1990). Though the examiner named the
German patent publication as the basis for the rejection, both
the examiner and appellant have throughout the prosecution of
this application liberally referred to its U.S. counterpart,
Hille et al.
(Hille I), U.S. 5,089,267 (patented February 18, 1991; prior
art under 35 U.S.C. § 102(e) based on its U.S. filing date of
December 18, 1989), as the English translation. So shall we.
Appellant cites Wislicki, “Nivalin (Galanthamine
Hydrobromide), An Additional Decurarizing Agent, Some
Introductory Observations,” British Journal of Anaesthesia,
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Application 07/953,439
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Volume 39, pages 963-968 (1967), for the proposition that
“galanthamine has only one tenth of the activity of
neostigmine which has the same activity as physostigmine”
(Brief on Appeal, page 7, second full paragraph). While we
find in Wislicki a statement that “the potency of neostigmine
[as an anesthetic] is considered to be ten times as great [as]
. . . galanthamine” (Wislicki, page 965, column 2, last
paragraph), we cannot find a statement that “neostigmine . .
. has the same activity as physostigmine” anywhere in Wislicki
or in the specification. To the contrary, appellant’s
specification teaches at pages 4-5, bridging paragraph):
Due to its pharmacological properties galanthamine
belongs
to the group of the reveribly [sic, reversibly] acting
cholinesterase inhibitors. The effects of galanthamine
are similar to those of physostigmine and neostigmine,
however, it has additional special effects. The
therapeutic range
of galanthamine is 3 to 6 times larger than that of
physostigmine or neostigmine, because of its lower
toxicity (Paskov, D.S., ed. Springer-Verlag, Berlin -
Heidelberg - New York - Tokyo, 653-672 (1986).
Moreover, the specification also teaches at page 5:
In contrast to neostigmine, galanthamine overcomes the
blood-brain barrier and opposes the cerebral effect of
cholinergic poisons. Galanthamine has the effect of
awakening the patient from the twilight sleep caused by
scopolamine (Baraka, . . . J. Amer. Med. Assoc. 238,
2293-2294 (1977).
Appeal No. 94-4129
Application 07/953,439
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Due to the long duration of action, galanthamine,
which incorporates the properties of physostigmine
and neostigmine, is a valuable agent in anesthesiology,
since many patients suffer from a central anticholinergic
syndrome after a general anaesthesia (Cozanitis, . . .
Anaesthesist 26, 649-650 (1977).
The claims on appeal are directed to a transdermal
applicator comprising (a) an impermeable backing layer, (b) a
polymer matrix which contains galanthamine and is connected to
the backing layer, and (c) a pressure-sensitive adhesive
element for affixation to the skin. Claim 16, which is
representative of the claimed subject matter, is reproduced in
the attached Appendix.
We hereby cite for the first time Hille et al. (Hille
II),
U.S. 5,700,480, patented December 23, 1997 (copy attached),
which issued from Application 08/495,609, filed September 29,
1995. Hille II and this application appear to be commonly
assigned to LTS Lohman Therapie-Systeme GmbH & Co. KG. Hille
II claims a transdermal therapeutic system for therapeutic
administration of galanthamine comprising (a) an impermeable
backing layer, (b) a polyacrylate reservoir which contains
galanthamine and is connected to the backing layer, and (c) a
pressure-sensitive adhesive element for affixation to the
Appeal No. 94-4129
Application 07/953,439
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skin. As in this case, both Davis and Hille I are included in
the References Cited in Hille II. We find in Hille I an
express teaching that the reservoir layer of a transdermal
applicator for administering physostigmine may include a
polyacrylate matrix. Also, we take particular notice of two
statements in Hille II. First, at column 1, lines 26-27,
Hille II states, “Lately, galanthamine has been used in the
treatment of alcohol dependence (Opitz, K., DE 40 10 079).”
Second, at column 1, lines 40-55, Hille II states:
Accordingly, it is the object of the present
invention to provide galanthamine . . . in the form
of a transdermal therapeutic system which releases
galanthamine . . . over a period of at least 24 hours
in a controlled manner . . . .
With the present invention this object is achieved
in a surprising manner by a transdermal therapeutic
system.
This solution is remarkable all the more since the
structure of galanthamine is very similar to that of the
opiates. Opiates are considered to be a substance class
which only insufficiently penetrates human skin.
2. Findings
A. Galanthamine is useful in treating Alzheimer’s
Disease (Davis, column 1, lines 6-8).
B. Galanthamine may be administered to treat
Alzheimer’s Disease
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Application 07/953,439
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(a) orally in solution, tablet or capsule form,
(b) subcutaneously or intravenously by injection, or
(c) intracerebroventricularly by implanted reservoir
(Davis, column 1, line 60, to column 2, line 44).
C. Physostigmine is useful in treating Alzheimer’s
Disease (Hille, column 1, lines 10-13);
D. Physostigmine may be administered to treat
Alzheimer’s Disease transdermally via an applicator comprising
(a) an impermeable backing layer, (b) a polymer matrix which
contains physostigmine and is connected to the backing layer,
and (c) a pressure-sensitive adhesive element for affixation
to the skin (Hille I, column 1, line 58, to column 3, line
26).
E. Galanthamine and physostigmine have
significantly different molecular formula, structural formula,
melting points, and solubility characteristics (Brief on
Appeal, page 6, citing The Merck Index, Tenth Edition, Merck &
Co., Inc.,
pages 620 and 1061-1065 (1983); see also Davis, column 1,
line 67, to column 2, line 2).
F. Galanthamine, physostigmine, and neostigmine are
known reversibly acting cholinesterase inhibitors with similar
Appeal No. 94-4129
Application 07/953,439
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effects. However, galanthamine has additional special effects
due to its lower toxicity (Specification, pages 4-5, bridging
paragraph).
G. Galanthamine is ten times less potent as an
anesthetic than neostigmine (Wislicki, page 965, column 2,
last paragraph).
H. The evidence of record does not establish the
relative activities of galanthamine to physostigmine for any
purpose, of galanthamine to neostigmine for uses other than
anesthesia, and of physostigmine to neostigmine for any
utility.
I. In 1994, Hille II teaches that he considered the
discovery that galanthamine could be administered
transdermally remarkable “since the structure of galanthamine
is very similar to that of the opiates. Opiates are
considered to be a substance class which only insufficiently
penetrates human skin” (Hille II, column 1, lines 52-55).
J. The evidence of record does not establish whether or
not or the reasons why persons having ordinary skill in the
art might reasonably expect a known active agent to be
effectively administrable transdermally.
3. Discussion
Appeal No. 94-4129
Application 07/953,439
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“A patent may not be obtained . . . if the differences
between the subject matter sought to be patented and the prior
art are such that the subject matter as a whole would have
been obvious at the time the invention was made to a person
having ordinary skill in the art . . . .” 35 U.S.C. § 103.
In re Fine, 837 F.2d 1071, 5 USPQ2d 1596 (Fed. Cir. 1988),
teaches, 837 F.2d at 1074, 5 USPQ2d at 1598:
The PTO has the burden under section 103 to establish a
prima facie case of obviousness. . . . It can satisfy
this burden only by showing some objective teaching in
the
prior art or that knowledge generally available to one of
ordinary skill in the art would lead that individual to
combine the relevant teachings of the references.
The consistent criterion for determining obviousness
under 35 U.S.C. § 103 is whether the prior art would have
reasonably suggested the claimed invention to one of ordinary
skill in the art with reasonable expectation of achieving
success. To resolve the issue, the full field of the
invention must be considered. The person having ordinary skill
is charged with knowledge of the entire body of technological
literature, including that which
leads to and that which leads away from the claimed invention.
In re Dow Chemical Co., 837 F.2d 469, 473, 5 USPQ2d 1529,
1531-32 (Fed. Cir. 1988).
Appeal No. 94-4129
Application 07/953,439
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Assuming that the evidence before us represents the full
field of the invention and the entire body of technological
literature to be considered by persons having ordinary skill
in the art in determining unpatentability under 35 U.S.C. §
103, we must reverse the examiner’s holding. We find no
evidence in the prior art which would have led persons having
ordinary skill in the art either to reasonably believe that
galanthamine should be administered transdermally for any
particular therapeutic benefit or to reasonably expect that
galanthamine could be administered transdermally with a
likelihood of therapeutic success.
The prior art reasonably would have taught persons having
ordinary skill in the art that galanthamine and physostigmine
are both reversibly acting cholinesterase inhibitors and that
both can be used to treat Alzheimer’s Disease when
administered in accordance with conventional wisdom in the
art. However, the prior art of record would not have led
persons having ordinary skill in the art to reasonably believe
that active agents possessing some particular property or
properties are more
or less likely to be administrable transdermally than active
agents not possessing those properties with therapeutic
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Application 07/953,439
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success. Persons having ordinary skill in the art with prior
knowledge that certain kinds of active agents may be
administered transdermally, might have been led to believe
that chemically, physically, and/or structurally similar
active agents could be administered in substantially the same
manner. However, here the prior art has established
therapeutic similarities only. We find no evidence of record
that the common therapeutic properties exhibited by
galanthamine and physostigmine would have reasonably suggested
to persons having ordinary skill in the art that galanthamine
could be administered transdermally with therapeutic success
similar to that achieved when transdermally administering
physostigmine, a compound which appears to be chemically,
physically and structurally dissimilar to galanthamine.
4. Conclusion
We reverse the examiner’s rejection of Claims 16-19 under
35 U.S.C. § 103.
5. Other Issues
The examiner should consider in the first instance the
patentability of Claims 16-19 of this application in light of
the subject matter claimed in Hille II, i.e., U.S. 5,700,480,
patented December 23, 1997 (copy attached). Note the
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Application 07/953,439
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following:
(1) the effective filing date of Hille II and this
application;
(2) the inventive entity of Hille II and this
application;
(3) the assignee of Hille II and this application;
(3) the reference to Opitz, K., DE 40 10 079 at column
1, lines 26-27, of Hille II; and
(4) the matrix polymers and matrix polymer additives
Hille I describes at column 2, lines 50-66, of Hille I,
U.S. 5,089,267, patented February 1991 (prior art to both
Hille II and this application), for use in transdermal
applicators.
REVERSED
Sherman D. Winters )
Administrative Patent Judge )
)
)
)
Richard E. Schafer ) BOARD OF PATENT
Administrative Patent Judge ) APPEALS AND
Appeal No. 94-4129
Application 07/953,439
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) INTERFERENCES
)
)
Teddy S. Gron )
Administrative Patent Judge )

Appeal No. 94-4129
Application 07/953,439
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Sprung Horn Kramer & Woods
660 White Plains Road, 4th Floor
Tarrytown, NY 10591-5144

Appeal No. 94-4129
Application 07/953,439
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APPENDIX