4DQSAR
Bluelighter
- Joined
- Feb 3, 2025
- Messages
- 5,443
I'm still waiting to read a proper 'trip report on an OX1`/OX2 modulator.
Belsomra (suvorexant)
Quviviq (daridorexant)
Dayvigo (lemborexant)
What immediately strikes me about all three is that they are all are chiral and in each case just one stereoisomer is used. This goes against the practice of 'evergreening' and suggests that the TI if the raecamates might not be favourable.
Several more are in stage 3 trails but many more have been abandoned - which may suggest that the TI IS the issue. One contains deutirium (heavy hydrogen). Now, for a while a lot of pharmacutical companies believed that swapping H for D was another way of evergreening. Then a court made it clear that ONLY IF swapping a H for a D demonstrably improved the medication in question could a patent be obtained.
I know this all sounds very boring, but this is the 99% of drug design that isn't simply drawing a structure.
Belsomra (suvorexant)
Quviviq (daridorexant)
Dayvigo (lemborexant)
What immediately strikes me about all three is that they are all are chiral and in each case just one stereoisomer is used. This goes against the practice of 'evergreening' and suggests that the TI if the raecamates might not be favourable.
Several more are in stage 3 trails but many more have been abandoned - which may suggest that the TI IS the issue. One contains deutirium (heavy hydrogen). Now, for a while a lot of pharmacutical companies believed that swapping H for D was another way of evergreening. Then a court made it clear that ONLY IF swapping a H for a D demonstrably improved the medication in question could a patent be obtained.
I know this all sounds very boring, but this is the 99% of drug design that isn't simply drawing a structure.
