Back to results
US 7,094,777 B2Granted
5-HT2A receptor ligands
AssigneeMerk Sharp & Dohme Corp.
InventorsMark Stuart Chambers, Neil Roy Curtis, Angus Murray MacLeod, Robert James Maxey, Helen Jane Szekeres
Life of this patent
Estimating the term…
Abstract
Compounds of formula I: are antagonists of the human 5-HT2A receptor, and hence useful in treatment or prevention of a variety of neurological conditions.
Claims24
A compound of the formula I:
- wherein n is 0, 1, 2 or 3;
- W is CH2, CO, CHF or CH(OH);
- X is SO2, SO, CO or CH(OH);
- Y is CH2, CHF or CF2;
- Z is H, F or OH;
- Ar1 is phenyl or heteroaryl, wherein heteroaryl is selected from thiazole, imidazole and triazole, and wherein said phenyl or heteroaryl is unsubstituted or substituted with up to 3 substituents selected from halogen, CN, NO2, R1, OR2, COR2, CO2R2, OCOR1, SR2, S(O)tR1 where t is 1 or 2, N(R2)2, CON(R2)2, NR2COR1 and SO2N(R2)2;
- Ar2 is a mono- or bicyclic ring system selected from phenyl, naphthyl, pyrrole, oxazole, isoxazole, thiazole, isothiazole, and imidazole, and their benzo-fused and tetrahydrobenzo-fused derivatives, wherein said ring system is unsubstituted or substituted with up to 3 substituents selected from halogen, CN, NO2, R1 and OR2;
- R1 is C1-6alkyl or phenyl, which is unsubstituted or substituted with up to 5 fluorine substituents;
- and
- R2 is R1 or H;
- or two R2 groups attached to the same nitrogen atom may form a pyrrolidine, imidazole or triazole ring,
- or a pharmaceutically acceptable salt or hydrate thereof.
9 more elements
A compound which is:
- 1-(4-fluorophenyl)-4-(3-{[(4-fluorophenyl)sulfonyl]methyl}azetidin-1-yl)butan-1-one;
- or a pharmaceutically acceptable salt or hydrate thereof.
A compound which is:
- 1-(4-fluorophenyl)-2-(3-{[(4-fluorophenyl)sulfonyl]methyl}azetidin-1-yl)ethanone;
- or a pharmaceutically acceptable salt or hydrate thereof.
A compound which is:
- 6-fluoro-3-[(3-{[(4-fluorophenyl)sulfonyl]methyl}azetidin-1-yl)methyl]-1,2-benzisothiazole;
- or a pharmaceutically acceptable salt or hydrate thereof.
Dependencies are inferred from the claim text.