Interference No. 104,522 Paper108
Nichols v. Tabakoff Page 37
Method step as described in the following prior art
(1) react aniline with a dialkyl Harrison et al. ("Harrison"), J. Med. Chem.,
acetylenedicarboxylate, 33:3130-3132 (1990) (Ex 1003), p. 3132, Scheme
1, step (a).
(2) cyclize the product of (1 ) to form an alkyl ester Harrison, Ex 1003, p. 3132, Scheme 1, step (b).
of kynurenic acid
(3) aminate the alkyl ester of (2) with an Wright, Synthesis, 1984 (12):1058-1061 (Ex
isocyanate to form a 4-aminated derivative, and 1004), pp. 1058-1059.
(4) acylate the 4-aminated derivative of (3) with Leeson et al. ("Leeson"), J. Med. Chem.,
triphosgene and a secondary amine to produce a 34(11):1954-1968 (1992) (Ex 2016) at p. 1956
4-urea-2-quinoline alkyl carboxylate. where reaction with phosgene is shown in step (c)
of Scheme V.
also
Degering, Organic Chemist , 6th ed., Barnes &
Noble, Inc., New York (1957) (Ex 1008), p. 139
or
March, Advanced Orq2nic Chemistry, 4th ed.,
John Wiley & Sons, Inc., New York (1992) (Ex
1009), pp. 417-418
!EX 1007, %17-14.1
76. Not surprisingly, Dr. Nichols disagrees with Dr. Ruth's opinion and interpretation
of the prior art (NR, pp. 18-21, T% 4-19). (Dr. Ruth was not cross-examined.)
77. We find that Dr. Ruth's testimony is entitled to more weight than Dr. Nichols'
testimony. To the extent there is a conflict, we accept the testimony of Dr. Ruth and
reject that of Dr. Nichols. Dr. Ruth is an organic chemist; Dr. Nichols is not. Moreover,
Dr. Ruth's testimony is consistent with the fact that Nichols' synthesis method included
organic synthesis steps described in the prior art, e.g., Harrison, Wright, Leeson and
March, and with well-known principles of-organic chemistry, e.g., aromatic and aliphatic
compounds may have different chemical reactivities,
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