Empirical studies on some drugs for patent lawsuits in the age of manufacturing patents

• Published in: Yakushigaku zasshi Vol. 44; no. 2; p. 71
• Main Authors: Yamakawa, Koji, Nishitani, Kiyoshi
• Format: Journal Article
• Language: Japanese
• Published: Japan 2009
• Subjects: History, 19th Century; History, 20th Century; Japan; Patents as Topic - history; Patents as Topic - legislation & jurisprudence; Pharmaceutical Preparations - history; Japan
• ISSN: 0285-2314

Empirical studies on patent lawsuits for some drugs by author (K.Y.) from 1953-1998, are described. Case 1: One of the authors (K.Y.) clarified that silylmethylation of a penicillin derivative gave either N, O-disilylmethylated product or O-monosilylmethylated product. However, only O-silylmethylated product was obtained after the usual work-up (Fig. 1). Case 2: A point under discussion of the trial is whether the reported manufacturing process of "metoclopramide" is possible or not. One of the authors (K. Y.) clarified the possibility by means of a careful synthetic experiment (Fig. 2). Case 3: The essential effective structure of herbicides, Roundup (Monsanto Co.) and Sulfosate (Stoph Co.), was the same in highly diluted solution (Fig. 3). Case 4: Cimetidine has been prepared by the Oxy procedure (SKB Co.), but another cimetidine (Fujimoto Co.) was prepared by the Lek procedure. Is it true? Experimental preparations of both cimetidines by the respective Oxy and Lek processes, were achieved by the authors. The cimetidine in the tablet named "Cylock" by Fujimoto Pharm. Co., Ltd. should be manufactured by the Oxy process on the basis of the by-products analysis (Fig. 4). Finally, a short history of patents in Japan from 1899-1975 is described.