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US 6,890,956 B2Granted
Cyclohexyl sulphones as gamma-secretase inhibitors
AssigneeMerck Sharp & Dohme Corp.
InventorsIan Churcher, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Andrew Pate Owens, Duncan Edward Shaw, Joanne Thomson, Susannah Williams
Life of this patent
Estimating the term…
Abstract
Compounds of formula I: inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease.
Claims9
A compound of formula I:
- wherein n is 1 or 2;
- R1 represents CF3 or C1-6alkyl, C2-6alkenyl, C3-9cycloalkyl or C3-6cycloalkylC1-6alkyl, any of which may bear up to 2 substituents selected from halogen, CN, CF3, OR3, COR3, CO2R3, OCOR4, SO2R4, N(R5)2, and CON(R5)2,
- or R1 represents aryl, arylC1-6alkyl, C-heterocyclyl or C-heterocyclylC1-6alkyl;
- R2 represents H or C1-4alkyl;
- R3 represents H, C1-4alkyl, phenyl or heteroaryl;
- R4 represents C1-4alkyl, phenyl or heteroaryl;
- R5 represents H or C1-4alkyl, or two R5 groups together with a nitrogen atom to which they are mutually attached complete an azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine or thiomorpholine-1,1-dioxide ring;
- Ar1 and Ar2 independently represent phenyl or heteroaryl, either of which bears 0-3 substituents independently selected from halogen, CN, NO2, CF3, CHF2, OH, OCF3, CHO, CH═NOH, C1-4alkoxy, C1-4alkoxycarbonyl, C2-6acyl, C2-6alkenyl and C1-4alkyl which optionally bears a substituent selected from halogen, CN, NO2, CF3, OH and C1-4alkoxy;
- aryl at every occurrence thereof refers to phenyl or heteroaryl which optionally bear up to 3 substituents selected from halogen, CN, NO2, CF3, OCF3, OR3, COR3, CO2R3, OCOR4, N(R5)2, CON(R5)2 and optionally-substituted C1-6alkyl, C1-6alkoxy, C2-6alkenyl or C2-6alkenyloxy wherein the substituent is selected from halogen, CN, CF3, phenyl, OR3, CO2R3, OCOR4, N(R5)2 and CON(R5)2;
- and
- C-heterocyclyl and N-heterocyclyl at every occurrence thereof refer respectively to a heterocyclic ring system bonded through carbon or nitrogen, said ring system being non-aromatic and comprising up to 10 atoms, at least one of which is O, N or S, and optionally bearing up to 3 substituents selected from oxo, halogen, CN, NO2, CF3, OCF3, OR3, COR3, CO2R3, OCOR4, OSO2R4, N(R5)2, CON(R5)2 and optionally-substituted phenyl, C1-6alkyl, C1-6alkoxy, C2-6alkenyl or C2-6alkenyloxy wherein the substituent is selected from halogen, CN, CF3, OR3, CO2R3, OCOR4, N(R5)2 and CON(R5)2;
- or a pharmaceutically acceptable salt thereof.
9 more elements
Dependencies are inferred from the claim text.