Appeal No. 2001-1947
Application 08/333,202
teaching in Friedmann that less than 20 ppm aloe-emodin content of diacetylrhein is
desirable or attainable. Brief, page 5.
With respect to the Merck reference cited by the examiner, appellants argue that
“Friedmann begins preparation of his product using Sennosides A and B as set forth in
the Merck Index. Friedmann then goes on to state that the “crude” rhein is collected.
Thus, Friedmann himself certainly leads the skilled artisan to the conclusion that one
would have to purify the product prepared according to the Merck Index.” Brief,
page 7.
In the Declaration under 37 CFR § 1.132 , Dr. Grimminger states:
To appreciate the significance of the now claimed invention, one must
be familiar with the state-of-the-art preparations commercially available
and the techniques used for industrial preparations. At present, there are
two principal methods of preparing diacerein on an industrial scale. . . .
These two methods are 1) oxidation of acetyl aloin and 2) acetylation of
rhein. Declaration, page 3. Dr. Grimminger states that, “[t]ests have
shown that diacerein, which according to reference 4 in the literature, is
prepared from acetylated aloin, still has a total aloe emodin content of
approximately 3500 ppm at a concentration of 95%. Following the
increase in concentration to >98% by means of recrystallization which is
required for medicinal products, the residue of total aloe emodin still
exceeds 1000 ppm.” Declaration, pages 3-4.
As to differing properties associated with the claimed diacetylrhein, Dr.
Grimminger indicates that “[g]enotoxicity tests performed parallel to the clinical
development provide positive findings in the mouse lymphoma test and in the CHO test
with a substance containing in excess of 1000 ppm triacetyl aloe emodin. Repeated
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