Compounds of the invention

Several studies have been reported on the application of conformational restraint to the 1,5-diaryl-pyrazole series in an attempt to provide compounds with modified properties. In one approach, a Sanofi-Synthelabo patent application claimed a series of conformationally restrained compounds, exemplified by compound (391). Compounds of the invention were stated to be CBi receptor antagonists with K[ values below 5 x 10 M and selectivity over CB2 receptors of at least 10-fold [274]. 

The possibility of producing certain value-added compounds such as surfactants, which can be derived from intermediates produced in petroleum biodesulfurization processes, has been evaluated. HPBS is a molecule with amphiphilic characteristics desirable for surfactant applications [243], Several oxidation reactions, from the 4S pathway are considered before reaching the final product. The compounds of the invention include acyloxybiphenylsulfinates, acyloxybiphenylsulfonates, alkyl sulfinatobiphenyl ethers, and alkyl sulfonatobiphenyl ethers. The invention also provides methods of producing these compounds. 

As you scan through the remaining claims (3-9), take notice of the way the invention is sliced into different embodiments. Various compositions containing the compounds as well as methods of using the compounds of the invention are described. Although claim 1 may have been anticipated by reference A, the remaining claims... 

To see how the specific unpredictability of the art can argue in favor of nonobviousness, consider a case heard before the USPTO Board of Appeals that dealt with this issue. Ex parte Blattner concerns a set of claims that were rejected by an examiner at the USPTO.40 The rejected claims were subsequently appealed to the Board. The claimed subject matter in dispute concerned compound claims and methods directed to a set of azatetracyclic compounds for which the abbreviated claim 17, shown in Figure 8.10, was considered representative. Additional claims were directed to various structural subembodiments and pharmaceutical compositions containing the compounds of the invention as well as particular methods of use of the compounds including the treatment of agitation in a mammal. 

The claimed compound of the invention is produced by the reaction of epichloro-hydrin and bisphenol A and was well known in the art and was also known to be useful in the preparation of thermosetting epoxy resins. The claim preamble As a manufacture..., is equivalent to saying As a product of manufacture..., which in turn means that these two claims are compound claims. Although the compound was well known in the literature, it was reported in the context where it made up to 70% to 90% of a complex liquid mixture. According to the applicant s patent application specification, no method had been described that would allow the production of pure 2,2-bis-[(4)-2,3-epoxypropoxyphenyl]propane directly from a reaction mixture. Prior attempts to recover the product of the reaction resulted in, at best, a viscous liquid that adversely affected the usefulness of the product. In contrast to the prior art, applicant s methods resulted in material of sufficient purity that the compound was isolated as a free-flowing, crystalline powder. This material could be easily handled and allegedly could be used to prepare epoxy resins equal or superior to the liquid material prepared previously. 

The amount of experimentation required to make or use the invention in view of the direction provided in the disclosure. The direction provided in the disclosure is sufficient for the production of the compounds of the invention. 

The compounds of the invention were evaluated as antipruritic agents by measuring their ability to inhibit hind leg scratching induced in rats using a known pruritogenic agent according to the method of Berendsen (1). 

If compounds of the invention can form salts or exist as isomers, any ordinary inventor contemplates protecting them. His obvious thought is worthy, and patent practice respects it. He need not claim these derivatives specifically or genericaUy. To cover them, it suffices if he discloses them broadly in the patent specification, not individually in the special section devoted to claims. A competitor, consequently, cannot secure his own protection of the same compound merely by claiming a different salt or isomer of it. 

For example, the evidence of medical utility that a patent offers may be slight. It suffices if some compounds of the invention prove weakly active merely in a particular in vitro biochemical assay using isolated animal cells. 

When its term expires, a patent confers on the public the benefits of a chemical invention. It must therefore enable an interested party successfully to repeat the experiments it describes. To ascertain whether these efforts succeed, a helpful patent provides means to recognize compounds of the invention by their chjiracteristic physical properties like melting points and mass-to-charge ratios of molecular ions. Other physical data may replace or supplement the foregoing ones, so many strongly supported patents include details of infrEired, ultraviolet, proton, and carbon nuclear magnetic resonance spectra. 

A valid patent presents an invention capable of use. The inventor s instructions for implementing his idea must therefore be operable. Not surprisingly, the procedures furnished for making compounds of the invention must provide those substances. But patent law does not require the reactions employed to be efficient it suffices if they are merely effective. Indeed, the reactions employed may not even form part of the patent claims. Patent practice tolerates minute chemical yields if they faU within certain limits. Acceptable yields may be low enough to inspire disdain yet high enough to attract notice. Such scant yields do not invalidate claims. 

The patent specifications define the terms aryl, substituted, and lower alkyl. Aryl, for example, might be restricted to benzenoid aromatic rings. Typically, the specifications but not the general structure would cover any geometrical isomers or enantiomers formed by the compounds of the invention. 

Working examples take the familiar form of standard operating procedures that a chemist records in a scientific notebook as he carries out chemical reactions. They state concisely which compounds of the invention arise from these reactions. The accompmying list of compounds gives their complete chemical names or sometimes structural drawings. It identifies the compounds, which in either case can be recognized by the physical property or properties that the example furnishes. 

This ultimate claim to individual compounds can be important, even though it is the narrowest. It contains the name or structure of the best compound of the invention. If the research culminated in a clinical candidate or a drug in clinical development, then that valuable compound appears in this list. The list, however, does not identify the substance chosen as the drug for marketing or the compound for development, nor does it indicate that any compoimd was selected. Nevertheless, the list includes the substance and thereby satisfies the best mode requirement. 

Invention is a mental act in which the originator conceives the patentable idea and provides a workable means to realize it. His status as an inventor does not require or forbid him to actualize the idea himself, which coworkers may do instead. Although they elevate the idea to practice, their efforts— prolonged, extensive, or successful as they may be—do not entitle them to share inventorship. Merely making the compounds of the invention does not suffice to earn this status, even if one of these substances becomes a bestselling medicine. Joint inventorship of patents is commonplace, however, but because each of the inventors substantively contributes to at least one claim. 

The summary of the invention section, which is next, should set out the exact nature, operation, and purpose of the invention by describing it in one or more clear, concise sentences or paragraphs. " A detailed description of the invention will likely follow. There s some variation in which of these two will show the Markush describing compounds of the invention and the laundry list defining substituents thereof, but one or the other will always have this important information. In composition of matter patents, the summary may also describe the use of such compounds in pharmaceutical compositions and the use of such compositions to treat one or more diseases. 

Scheme 5.53 The illustration the methods by which compounds of the invention may be prepared...

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