Merck accidentally published a series of editors' notes in a patent filing for a new antibiotic, and inadvertently described a previously unknown Merck compound.
Amongst pages of tightly written formulae, several paragraphs suddenly speak with the voice of a patent lawyer instructing the author with the words,
You don't want to include synergy data for these eompouds? [sic] It would be helpful to include it, ...
The instructions name a chemical, "MK-8712," using Merck's code for drugs in development. As Derek Lowe of In the Pipeline points out:
That MK designation is Merck's usual method of showing a compound that's been recommended for the clinic, but this is the first that anyone seems to have heard about this one.
The patent application begins straighforwardly enough:
This invention relates to novel beta-lactamase inhibitors and their use against bacterial antibiotic resistance.
It then quickly dissolves into impenetrable chemistry-speak:
HetA is a 4- to 9-niembered saturated or mono-unsaturated heterocyclic ring containing from 1 to 3 heteroatoms independently selected from N, O and S, wherein any ring S is optionally oxidized to S(O) or S(O)2 and either 1 or 2 ring carbons are optionally oxidized to C(O); ...
This goes on for about 120 pages until you encounter this, the unmistakeable scribbling of a boss who's happy to tell you what to write as long as he or she ain't writing it:
I plan to DELETE the entries in Table 3 for Ess. 2, 6, 7 and 8 because this data duplicates the data in Table 2. HOWEVER, the entry In Table 2 for Ex. 7 is "1.1" NOT "11" as shown in Table 3. Also, the entries in Table 2 for Ex. 8 are both "1.6", not "16" as shown in Table 3. Please clarify these differences.
Is the data shown for Ex. IA data generated in a separate run, or is it supposed to be the same as for Ex. 1? Note "208" in Table 2 vs. "210" in Table 3 - why different? I propose to delete the entry for Example IA from Table 3 as it's essentially the same as the entry in Table 2 for Example 1.
You don't want to include synergy data for these eompouds? It would be helpful to include it, at least for some of the examples (could put in a separate table). Recommend we include it for Ex. 14, since this is a likely backup candidate.
We have a comparison to sulbactam in Table 2. How does MK-8712 compare to this? Is it worth including 8712 comparative data? Any other structurally similar known compounds that you may have run a comparison?
Yeah, dude, what about those other structurally similar known compounds that you may have run for comparison? Hmmm? Must I do everything myself around here?