Drug preparation methods patentability

Cheng, J. Davis, M.E. Khin, K.T. Cyclodextrin-Based Polymers for Therapeutics Delivery. US Patent 20040077595 Al, Apr 22, 2004 Insert Therapeutics, Inc. Pasadena, CA. Allemann, E. Gurny, R. Doelker, E. Drug-loaded nanoparticles—preparation methods and drug targeting issues. Eur. J. Pharm. Biopharm. 1993, 39, 173-191. 

Muller BW, Brauns U, inventors. Pharmaceutical compositions containing drugs which are instable or sparingly soluble in water and methods for their preparation. Janssen Phar-maceutica N.V. assignee US Patent 6,407,079, June 18, 2002. 

Only a small number of examples of chiral compounds that are produced at high volume have been given in this chapter. The comparison to the first edition s top ten pharmaceutical list shows that asymmetric synthesis is now beginning to play an important role in the synthesis of drugs. Although fermentation and resolution approaches are still in abundance, the drugs that are prepared by these methods are mature and nearing the end of their patent lives. There is no reason to doubt that... 

Other types of drug-related patents include process, use, and formulation patents. Chemists are responsible for process patents, which describe an improved method of preparation of some drug substance but are minimally involved with the others. Use patents are based on the discovery of some unobvious utility of a compound that is either part of the public domain or covered by an existing patent such discoveries are most likely to be made by biologists. Formulation patents disclose a preferred means of drug delivery of a known drug substance. 

Platz, R.M. Ip, A. Whitham, C.L. Process for Preparing Micronized Polypeptide Drugs. US patent 5,354,562, 1994. Platz, R.M. Utsumi, J Satoh, Y Naruse, N Pharmaceutical Aerosol Formulation of Solid Formulation of Solid Polypeptide Microparticles and Method for the Preparation Thereof. World IPO 9,116,038, 1991. 

Multiple patents may be issued that provide protection for the same new drug product because a single invention may be claimed in a number of different ways. For example, a patent may claim the compound itself, a novel use for the compound in treating disease, and a method for preparing and administering the compound. 

Preparations of liposomes via SCF processing are designated as critical fluid liposomes (CFLs). CFLs have successfully encapsulated hydrophobic drugs such as taxoids, camptothecins, doxorubicin, vincristine, and cisplatin. In addition, stable paclitaxel liposomes with a size of 150-250 nm were obtained. Aphios Co. s patent (US Patent 5,776,486) on Super-Fluids CFL describes a method that is useful for the nanoencapsulation of paclitaxel and campothecin in aqueous liposomal formulations called Taxosomes and Camposomes , respectively. 

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... 

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