RE: Preparing for bids10 Apr 2026 14:07
Opti_mystic is correct that Avacta will have (tried to) cover all the bases in the patent application in order to protect their IP and deny Me-Too type variations. They will be working on a schematic model of how their model drug fits the FAP enzyme — lipohilic vs hydrophilic regions, electophilicity, hydrogen bonding, etc. — and will design their patent claims accordingly. We don't know what those 500+ compounds are that they've made but they will have been used to first define and then confirm their model of structure vs activity and those 500+ will be fewer than all the possibilities covered in the patent, as illustrated below.
This is the patent: https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2026002995
And this is the beginning of the definitions part (the whole lot is too long for this post) of the first claim of 11 general structural claims:
CAM is a camptothecin;
R′ is -LA-RA, hydrogen, halogen, -ORO, -CO2RO, -N(RN)2, -C(=O)N(RN)2, C1-30 alkyl, C1-30 haloalkyl, C1-30 heteroalkyl, C2-30 alkenyl, C2-30 heteroalkenyl, C2-30 alkynyl, C2-30 heteroalkynyl, C3-10 carbocyclyl, 3- to 10-membered heterocyclyl, C6-10 aryl, 5- to 10-membered heteroaryl, polyethylene glycol (PEG), polysarcosine (PSar), or any combination thereof, wherein each alkyl, haloalkyl, heteroalkyl, alkenyl, heteroalkenyl, alkynyl, heteroalkynyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, PEG, or PSar is independently optionally substituted;
RA is a reactive handle;
LA is a bond, C1-30 alkylene, C1-30 haloalkylene, C2-30 alkenylene, C2-30 alkynylene, C1-30 heteroalkylene, C2-30 heteroalkenylene, C2-30 heteroalkynylene, C3-10 carbocyclylene, 3- to 10-membered heterocyclylene, C6-10 arylene, 5- to 10-membered heteroarylene, polyethylene glycol (PEG), polysarcosine (PSar), or any combination thereof, wherein each alkylene, haloalkylene alkenylene, alkynylene, heteroalkylene, heteroalkenylene, heteroalkynylene, carbocyclylene, heterocyclylene, arylene, heteroarylene, PEG, or PSar is independently optionally substituted;
L1 is a bond, C3-10 carbocyclylene, C6-10 arylene, 3- to 10-membered heterocyclylene, or 5- to 10-membered heteroarylene, wherein the carbocyclylene, arylene, heterocyclylene, or heteroarylene is optionally substituted;
R2 and each instance of R2A are independently hydrogen or optionally substituted C1-C6 alkyl; or optionally wherein LA and R2 are joined together, or LA and R2A are joined together, with the intervening atoms to form a 5- to 10-membered heterocyclic ring, wherein the heterocyclic ring is optionally substituted;
...
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THE REALLY GOOD NEWS is that all the claims are based around and include the core D-Ala-L-Pro pre|CISION dipeptide that is protected until 2035 so no competitors can infringe on the basic structure. The claims in the above patent are thus spreading the net very wide so that Avacta can claim specific structures within the coverage if THEY find better Me-Toos.
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