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IN THE CANADIAN PATENT OFFICE
DECISION OF THE COMMISSIONER OF PATENTS
Patent application 564,700 having been rejected under Rule 47(2)
of the Patent Regulations, the Applicant asked that the Final
Action of the Examiner be reviewed. The rejection has
consequently been considered by the Patent Appeal Board and by
the Commissioner of Patents. The findings of the Board and the
ruling of the Commissioner are as follows:
Agent for Applicant
Gowling, Strathy & Henderson
P.O. Box 466, Terminal A
Ottawa, Ontario
K1N 8S3
COMMISSIONER'S DECISION SUMMARY
C.D. 1165...App'n 564700 (COO)
Deficiency of Description:
The application contains claims directed to a class of
compounds referred to as N6-substituted adenines and their use,
but not to a process for making them. The application satisfies
the Section 34 (1) (b) provision of the Patent Act in that it
refers to published articles which set out the various steps of
making some of the compounds of the class of compounds claimed.
Since the specification is directed to persons skilled in the art
and the articles are not obscure, a skilled artisan could prepare
the compounds without excessive experimentation. Furthermore, it
is unnecessary to provide information on every specific compound
since it is merely necessary to make a sound prediction.
Rejection withdrawn.
This decision deals with the applicant's request for review by
the Commissioner of Patents of the Final Action on application
564,700 (class 260-242.3) filed April 21, 1988. It is assigned
to Whitby Research, Inc. and is entitled N6-Substituted 9-
Methyladenines: a new class of Adenosine Receptor Antagonists.
The inventor is Ray A. Olsson. The Examiner in charge issued a
Final Action on January 18, 1990 refusing to allow the
application. A Hearing was held on January 7, 1992 at which
applicant was represented by Ms. Judy Errat and Mr. David Watson
of the firm Cowling, Strathy & Henderson.
The application relates to a class of compounds referred to as
N6-substituted adenines and defined by claim 1 of the application
as follows:
1. Novel compounds represented by the general formula:
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wherein R1 is selected from the group consisting of
cycloalkyl radicals having from 3 to 7 ring carbon atoms,
alkyl radicals having from 2 to 10 carbon atoms, aryl
radicals having from 6 to 10 carbon atoms, aralkyl radicals
having from 7 to 10 carbon atoms and heteroatom substituted
derivatives, wherein said heteroatom may be selected
from the group consisting of halogen, nitrogen, phosphorous,
sulfur and oxygen; R2 may be hydrogen or R1, and R3 is an
alkyl group comprising from 1 to 4 carbon atoms.
Claims 2 to 14 are dependent on claim 1 and define more specific
embodiments of the class of compounds. Claims 15 to 20 define
the use of one or more of the compounds for antagonizing the
adenosine receptor in a subject. There are no claims directed to
a process for making the alleged novel compounds.
On May 25, 1989 the Examiner issued a report containing the
following paragraph:
This application is refused under Section 34(1) (formerly
Section 36(1)) of the Patent Act, because the disclosure
does not correctly and fully describe the invention and its
operation or use as contemplated by the inventor, in full,
clear, concise, and exact terms. The disclosure must be
complete without reference to any other document [Minerals
Separation North American Corporation vs. Noranda Mines
Limited (1947) Ex. C.R. 306 at 316]. Therefore this
application is refused for insufficiency in view of Section
34(1) of the Patent Act.
In an effort to overcome the foregoing refusal applicant
requested, by amendment letter dated November 23, 1989 that the
following passage be entered at page 2 of the application:
It is well known in the art that the preparation of N6-
Substituted-9-Methyladenines may be accomplished by reaction
of the 6-chloro-9-methyladenine with an appropriate amine
(Robins, R.K., and Lin, H.H., J. Amer. Chem. Soc., 79, 490,
1957). Continuing, the synthesis and characterization of
various 9-alkyl-6-chloropurines is well known as disclosed
in Montgomery, J.A. and Temple, C., Amer. Chem. Soc. 79,
5238 (1957) and Montgomery, J.A. and Temple C.J., J. Amer.
Chem. Soc. 80, 409 (1958). Therefore one skilled in the art
would be aware that the reaction of the known 9-alkyl-6-
chloropurine with an appropriate amine would result in the
claimed N6-Substituted-9-Methyladenines. That is, the
reaction of 9-methyl-6-chloropurine with endo-2-
aminonorborane provides N6-(endo-2-norbornyl)-9-
methyladenine.
The Examiner, however, was not satisfied that the foregoing
amendment overcame the rejection and on January 18, 1990 issued a
Final Action in which the refusal of the application under
Section 34(1) of the Patent Act as being insufficient in
description was maintained. The Final Action contains the
following statement:
Examination of the disclosure yields no indication on how
one could successfully perform the invention (i.e. make the
alleged new compounds) having only the specification as
filed. In particular, the disclosure leaves it to those
skilled in the art to conduct a series of experiments in
order to ascertain the best method of performance and
conditions of experimentation.
Further in reference to the amendment to the disclosure and the
supporting comments by the applicant the Examiner made the
following statement:
The applicant has attempted to overcome the objection to
insufficiency by indicating that the methods and means of
experimentation are well known in the art and that anyone
skilled in the art would be able to carry out the invention
accordingly (pages 2 and 3 of the amendment dated November
23, 1989). This argument fails for the following reason.
It is true that the methods and procedures per se are well
known in the art however the applicant has failed to
sufficiently teach in the disclosure whether these methods
or procedures will work in this particular instance. In
particular, there is no evidence of experimentation in the
disclosure that will allow one to carry out the alleged
invention (ie making the alleged new compounds) having only
the specification as filed. Hence, the disclosure fails due
to insufficiency and is therefore rejected under Section
34 (1) of the Patent Act.
In summary, then, the issue before the Board is whether the
disclosure is sufficient to meet the requirements of Section
34(1) of the Patent Act in respect to making the alleged new
compounds of the invention.
The disclosure contains, at page 12, a list of 21 compounds
indicated as Example Nos. 1 to 21 as follows:
Example No. Compound
1 Adenine
2 9-Methyladenine-(9-MA)
3 N6-Cyclobutyl-9-MA
4 N6-Cyclopentyl-9-MA
5 N6-Methylcyclopentyl-9-MA
6 N6-Cyclohexyl-9-MA
7 N6-Methyl-9-MA
8 N6-3-Pentyl-9-MA
9 N6-Pheny 1-9 -MA
10 N6-2-Fluorophenyl-9-MA
11 N6-Benzyl-9-MA
12 N6-2-Phenethyl-9-MA
13 N6-2-(3,4,5-Trimethoxy-
phenylethyl-9-MA
14 N6-2-(3-Pyridylethyl)-9-MA
15 N6-2-(3-Thienylethyl)-9-MA
16 N6-R-1-Phenyl-2-propyl-9-MA
17 N6-S-1-Phenyl-2-propyl-9-MA
18 O6-Phenyl-9-Methyhypoxanthine
(9MH)
19 O6-(2-Fluorophenyl)-9-MH
20 O6-(3-Fluorophenyl)-9-MH
21 O6-(4-Fluorophenyl)-9-MH
Examples 3, 4, 6 and 8 through 17 are compounds within the ambit
of the alleged invention. Examples 1, 2, 5, 7 and 18 to 21 are
included for comparative purposes. Another compound, N6-(endo-
2-norbornyl-9-methyladenine, is mentioned on page 2a. However
this compound is not considered to be part of applicant's alleged
disclosed invention as it did not appear in the specification
when the application was filed, but was inserted into the
application by subsequent amendment (see above).
The only information provided in the application with regard to
the methods of preparation of the alleged new compounds is that
entered by the same amendment on November 23, 1989 and quoted in
full above. The Robins et al article referred to therein
discloses three methods for the preparation of N6-substituted-9-
methyladenines (formula XII, page 491) by reaction of 9-methyl-
6-chloro purine with substituted amines. The article discloses
the preparation of 9 specific N6-substituted-9-methyladenines, 4
of which fall within the ambit of applicant's claims (Table I,
page 492).
The specific compounds disclosed by the article include 4 having
the general formula of applicant's claim 1 wherein R1 is ethyl,
isopropyl or normal propyl (alkyl radicals having 2 or 3 carbon
atoms), R2 is hydrogen or ethyl and R3 is methyl (an alkyl
radical having 1 carbon atom). In each instance the article
provides clear information on starting materials, reaction
conditions, solvents, methods of isolation and purification of
the products and fields. Furthermore each compound is fully
characterized by melting point, elemental analysis and UV
absorption spectrum.
In addition the article discloses the preparation of the compound
listed on page 12 of the application as comparative Example 7 and
a closely related compound of applicant's formula wherein R1 is a
heterocyclic aralkyl radical, R2 is hydrogen and R3 is methyl.
Similarly the article by Montgomery and Temple (1957) discloses
the preparation of a specific compound, within the ambit of
applicant's claims, specifically 6-n-butylamino-9-ethylpurine
(formula XII, page 5239). This compound is a compound of
applicant's formula wherein R1 is normal butyl (an alkyl radical
having 4 carbon atoms), R2 is hydrogen and R3 is ethyl. Again
the method of preparation is fully described and the compound is
fully characterized.
Section 34(1) of the Patent Act reads as follows:
34. (1) An applicant shall in the specification of his
invention
(a) correctly and fully describe the invention and its
operation or use as contemplated by the inventor;
(b) set out clearly the various steps in a process, or the
method of constructing, making, compounding or using a
machine, manufacture or composition of matter, in such
full, clear, concise and exact terms as to enable any
person skilled in the art or science to which it
appertains, or with which it is most closely connected,
to make, construct, compound or use it;
(c) in the case of a machine, explain the principle thereof
and the best mode in which he has contemplated the
application of that principle;
(d) in the case of a process, explain the necessary
sequence, if any, of the various steps, so as to
distinguish the invention from other inventions; and
(e)particularly indicate and distinctly claim the part,
improvement or combination that he claims as his
invention.
The issue before the Board is whether or not applicant has
complied with subsection (b) of Section 34(1). Clearly the two
articles discussed above set out clearly the various steps in a
method of making 5 of the compounds of the class of compounds
applicant claims as new in such full, clear, concise and exact
terms as to enable a competent organic chemist to make the
compounds. The required information is not incorporated in the
text of the specification per se but the specification, as
amended, refers the worker to the two articles. The two articles
appear in the Journal of the American Chemical Society which is
widely available to organic chemists.
The jurisprudence, as exemplified by a number of court decisions
cited by the applicant, emphasizes that the specification is
directed to those skilled in the art. The present specification
directs the organic chemist to the two widely available journal
articles for information on the preparation of 5 compounds within
the ambit of applicant's claim. The information contained
therein would permit the competent organic chemist to prepare
these compounds with little or no experimentation. It is the
practice of the Patent Office to permit applicants for patents to
refer to the available literature in the specification for
information for the preparation of known compounds. The present
situation is unique in that the specification refers the worker
to the literature for information for the preparation of
compounds that are claimed as new. However the issue of novelty
is not before the Board and the disclosure is considered
sufficient insofar as it meets the requirements of Section
34(1)(b) in regard to making the 5 specific compounds discussed
above.
On the other hand the specification does not offer any specific
information with respect to the making of any of the specific
compounds of applicant's alleged invention listed on page 12 of
the application (other than the one listed as comparative Example
7). The Robins et al article however discloses a general
reaction scheme for the preparation of N6-substituted-9-
methyladenines (compounds of applicant's alleged invention where
R3 is methyl) by reacting 9-methyl-6-chloropurine with a
substituted amine (page 491). Selection of the amine
substituents will dictate the substituents at the N6 position on
the final product (indicated as R1 and R2 on applicant's general
formula). The article also discloses three general methods of
carrying out the reaction (page 494). With the information
provided by the article it should be possible for a skilled
organic chemist to prepare a whole range of N6-substituted-9-
methyladenines including the specific compounds disclosed by
applicant with a minimum of experimentation. Similarly the
Montgomery and Temple (1957) article discloses methods of
preparing N6-substituted-9-ethyl adenines (R3=ethyl) by reacting
6-chloro-9-ethylpurine with substituted amines. Again a skilled
organic chemist could prepare a whole series of N6-substituted-
9-ethyl adenines by using appropriate substituted amines by
following the teachings of the 2 articles and with a minimum of
experimentation. The Montgomery and Temple (1958) article
discloses 9-n-butyl-6-chloropurine (formula IIIa, page 410) which
a skilled chemist could use as a starting material together with
the substituted amines to prepare a series of N6-substituted-9-
butyladenines of applicant's alleged invention (where R3=butyl,
an alkyl radical of 4 carbon atoms).
It is clear then that a skilled chemist using the information
provided in the three articles referred to in the disclosure
could prepare the compounds of applicant's alleged invention
without an excessive amount of experimentation. This conclusion
is supported by the affidavit of James V. Peck submitted by the
applicant by letter on July 16, 1990.
The application does not contain any claims to a process for
making the alleged novel compounds but is restricted to claims to
the compounds and their use. Applicant emphasized that the
alleged inventive feature lies in the compounds, their activity
and use, not the process of manufacture.
Applicant argues that it has done all that is required under
Section 34(1)(b) with respect to the making of the compounds.
Specific information for the making of 5 compounds within the
ambit of the claims is provided. General information for making
all compounds within the ambit of the claims is also provided.
Further a list of 13 specific alleged novel compounds are
provided which are characterized by their relative potency with
each other and with other related compounds. Applicant has
referred to a number of court decisions in support of the
argument. Of particular interest is Monsanto Co. v. Commissioner
of Patents (1979) 42 C.P.R. (2d) 161 at pages 161-180. Monsanto
along with a number of other decisions emphasizes at page 173
that:
"a patent specification is addressed to a person skilled in
the art."
As such it is unnecessary to provide information on every
specific compound. It is merely necessary to make a "sound
prediction" (See page 176). The Monsanto decision shows that
there should be no rejection unless there is evidence that the
prediction is wrong. (See page 179). The Examiner has provided
no evidence that any of the compounds falling within the ambit of
the claims could not be prepared by the methods disclosed in the
articles referred in the amended disclosure. The question of
sound prediction does not apply to the specific compounds listed
on page 12 of the disclosure as applicant has successfully
prepared them as evidenced by their characterization of their
relative activities as adenosine acceptor antagonists. The Board
therefore considers the rejection of the application on the
specific issue of sufficiency of disclosure with regard to the
making of the compounds of the alleged invention to be unfounded.
The Board recommends that the rejection of the application under
Section 34(1) of the Act for insufficiency of disclosure be
withdrawn. The Board also recommends that the application be
returned to the Examiner for prosecution dealing fully with all
outstanding issues.
F.H. Adams E.A. Maner J.W. Hilchie
Chairman Member Member
Patent Appeal Board Patent Appeal Board Patent Appeal Board
I concur with the findings and the recommendations of the Patent
Appeal Board. Accordingly, I withdraw the rejection of the
application and I remand it for prosecution consistent with the
recommendations.
J.H.A. Gari‚py
Commissioner of Patents
Dated at Hull, Quebec
this 31st day of January 1992
Gowling, Strathy & Henderson
P.O. Box 466, Terminal A
Ottawa, Ontario
K1N 8S3