NICHOLS et al. V. TABAKOFF et al. - Page 20





               Interference No. 104,522 Paper1108                                                                                          
               Nichols v. Tabakoff Page 20                                                                                                 
               43. The handwritten entries on Ex 2036, including compound identification name,                                             
               structure, molecular weight and molecular formula, were made by Dr. Nichols. The NIH                                        
               did not analyze sample 94A-85-1 for chemical structure or any other physical property.                                      
               [NR, p. 100, 1. 10 - p. 102,1. 23; pp. 220-22 1, interrogatory nos. 10-13.]                                                 
                                                L analysis of evidence                                                                     
                       Notebook Ex 2032, taken alone, is insufficient to establish that the predicted                                      
               reactions and theoretically expected products did in fact occur. While the proton NMR                                       
               data is not inconsistent with the chemical structure drawn by Dr. Nichols thereon (Ex                                       
               2034), the proton NMR data alone is insufficient to independently corroborate that                                          
               sample 94A-85-1 is in fact (NN-diethyl)-4-ureido-5,7-dichloro-2-carboxy-quinoline                                           
               methyl ester. No additional analytical data, e.g., carbon NMR, mass spectral data, etc.                                     
               have been offered for sample 94A-85-1. Moreover, even without considerations of the                                         
               missing/exchangeable 17 th proton and inconclusive methoxy peak, Mr. Ezell testified                                        
               that proton NMR data alone does not provide enough data to assign a chemical                                                
               structure to a compound. Further, the NIH did not determine the chemical structure or                                       
               any other physical property of sample 94A-85-1. Thus, none of Exs 2034, 2035 or 2036                                        
               (Ex A), alone or in combination, independently corroborate Nichols' alleged synthesis of                                    
               (NN-diethyl)-4-ureido-5,7-dichloro-2-carboxy-quinoline methyl ester. Finally, according                                     
               to Dr. Nichols, sample 94A-85-1 did not show anticonvulsant activity in NIH testing.8                                       


                       8 In reply to Interrogatory No. 18, i.e., "According to your letter, Exhibit B, the substance tested [by            
               NIH], 94A-85-1 (ADD # 00234001). did not exhibit adequate anticonvulsant activity to warrant further                        
               testing, is that right?", Mr. Stables replied, "No - only we were not interested in pursuing if (NR, p. 222).               
               Assuming without determining that sample 94AO85-1 exhibited de minimus anticonvulsant activity in some                      
               unexplained test, Dr. Nichols did not appreciate that sample 94A-85-1 would work for its intended purpose                   
               as shown by his notation "8/2/92 No NIH activity" (Ex 2032, third page).                                                    







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