Preferably, when X is -PO(OH)OR 22 or (CR 17R 18) nP(O)(OH)OR 22, then R 22 is not H or methyl. In one embodiment, Y 4 is -(CR 45R 46) P-W 2-(CR 47R 48) q-; W 2 is -CR 49R 50-, -NR 49-, -O-, -S- or -SO 2-; p and q are independently 0-4, provided that when q is O and W 2 is -NR 49-, -O-, -S- or -SO 2-, then Z 2 is -CR 41R 42-; R 45, R 46, R 47, R 48, R 49 and R 50 are independently hydrogen, C 1-C 9 alkyl, …
Well,…lets give it a rest. Let it suffice if I tell you that large portions of this pharmaceutical patent application are taken up by text that runs very much like this, although the index numbers and some atoms vary as it steamrolls through almost 200 pages. That’s stuff straight from hell for every research chemist, and it is precisely what might cause him or her to utter something like ” patents, ugh…“
Why am I telling you all this? Well, because you should really continue reading this disclosure if you are interested in inhibitors of N-acetylated-alpha-linked acidic dipeptidase (NAALADase), which happens to be the prostate specific membrane antigen (PSMA). Just skip all the convoluted gibberish I sampled above – its only for the lawyers -, and go on to those of the 200 pages that are crammed full with chemical information and hard medicinal chemistry data. This document allows you to extract so much biological information that you can build quantitative structure activity relationships (QSARs) for this entire chemical class of NAALADase inhibitors. And there are just no comparable public datasets on this subject in the peer review literature.
That’s what we at H.M. Pharma Consultancy like about medicinal chemistry patents. Patent attorneys are handed something to fret about: in their client’s critical new compound, could Y 4 be -(CR 45R 46) P-W 2-(CR 47R 48) q– if Z 2 does not meet the definition given for -CR 41R 42– ? But those knowledge seekers who are interested in the the biological data and how they are linked to the chemical structure just go to these pages. It is this aspect which our THIRDSPACE patent knowledge database project focuses on. Once again… stay tuned!