Interference No. 104,522 Paper108
Nichols v. Tabakoff Page 47
5,7-dichloro-2-carboxy-quinoline, (NN-dipheny)-4-ureido-5,7-dichloro-2-carboxy
quinoline methyl ester or N-[2-methoxy]phenyl)-4-ureido-5,7-dichloro-2-carboxy
quinoline.
97. Tabakoff claims 18 and 19 are prod uct-by-process claims wherein the products
are (NN-diphenyl)-4-ureido-5,7-dichloro-2-carboxy-quinoline methyl ester or (NN
diphenyl)-4-ureido-5,7-dichloro-2-carboxy-quinoline, respectively.
98. Tabakofrs compounds are expressly "for treating withdrawal symptoms
manifested in a patient suffering withdrawal symptoms and/or withdrawal induced brain
damage" (Tabakoff claim 12),
99. Nichols relies on Exs 2012-2027 to support its motion.
100. As discussed above, Dr. Nichols testified that he conceived of a generic two-step
process for making 4-urea kynurenates involving (1) attaching a carbonyl group to the
4-amino group of a 4-amino kynurenate and (2) attaching a secondary amine to the
carbonyl group (Ex 2012, 138). Dr. Nichols further testified that used triphosgene
(source of the carbonyl group) and various nitrogen-containing compounds to form 4
urea derivatives (id., T 40). Among those various secondary amines were diethylamine
and diphenylamine (see Exs 2021 and 2024).
101. In a letter from Dr. Nichols to Dr. Tabakoff, Dr. Nichols states, in part, that
Dr. Yielding and I are please to have the opportunity to collaborate with
you and Lohocla Research [Tabakoffs assignee] in the design and
synthesis of compounds for the treatment of alcohol withdrawal. The
series of compounds in which you have expressed an interest are 5.7
dichloro-4-ureido-2-carboxyguinolines. [Ex 2027, emphasis added.] I"]
18 Tabakoffs interest in this series of compounds is shown in several other letters of record.
For example,
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