Patent claims chemical intermediates

The intermediate patents listed in the Orange Book present a category that may not literally claim the approved drug product. An intermediate patent claims a chemical compound that is used during the production of an active ingredient, but is not present in the final, marketed form of the drug product. The elaimed compound is an intermediate on the pathway to the approved drug. 

T]he conclusion is inescapable that, just as the practical utility of the compound produced by a chemical process is an essential element in establishing patentability of the process, (Brenner v. Manson) 383 U.S. 519 (86 S.Ct. 1033), so the practical utility of the compound, or compounds, produced from a chemical intermediate , the starting material in such a process, is an essential element in establishing patentability of that intermediate. It seems clear that, if a process for producing a product of only conjectural use is not itself useful within 101, it cannot be said that the starting materials for such a process—i.e., the presently claimed intermediates—are useful. ... 

Patentable subject matter is ... any new and useful process, machine, manufacture, or composition of matter, or any new and useful improvement thereof Patent laws provide that patents may be granted only for inventions that are deemed to be new and useful. These requirements exclude pharmaceutical inventions that have not been shown to be reasonably safe and effective and chemical compounds that have no use except as intermediates for additional research. However, some special considerations have traditionally been applied in the case of chemical compounds, particularly those possessing therapeutic or pharmacological activity. A compound that is useful as an intermediate for the manufacture of a pharmacologically active compound may be claimed and afforded patent protection because it satisfies the utility requirement and is considered to be useful. Further, a compound need not show therapeutic utility in humans to meet the utility requirement of patentability pharmacological activity in animals or in vitro activity is considered sufficient in some cases. If the patent application purports to claim the use of a compound for the treatment of humans, the inventor must show that the compoimd is both safe and effective in humans. 

The formation of halides by the nucleophilic substitution of leaving groups is commonly used in the synthesis of more elaborate structures. The synthesis of inexpensive bulk chemicals like solvents, however, is mostly done by oxidation or addition reactions. Halides are either used as intermediates or are valuable end products. Authors of publications, especially patent literature, often claim one reaction for three or even four halogens. In practice, this rarely holds true and each of the halogens quite often requires different conditions. The usual order of halide nucleophilicity is I" > Br > Cl > F". In dimethyl-formamide the reverse order Cl > Br > I is observed. This order goes along with the order of the basic... 

Excellent heat and mass transfer characteristics of the SDR have been confirmed by the study of a phase-transfer-catalyzed Darzens reaction for preparing a drug intermediate. The SDR allowed for a 99.9% reduction in reaction time, 99% reduction of inventory and 93% reduction in the level of impurities [106]. Other possible applications of the SDR include polymerizations and polycondensations (in both cases considerable time savings and more uniform product) as well as precipitation/crystallization (smaller crystals with much narrower size distribution). Two large chemical companies have patented processes based on spinning-disc technology. SmithKline Beecham has claimed a method to epoxidize substituted... 

---