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US 8,557,992 B2Granted
Heterocyclic fused phenanthrolinone M1 receptor positive allosteric modulators
AssigneeMerck Sharp & Dohme Corp.
InventorsScott D. Kuduk, Jason W. Skudlarek
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Abstract
The present invention is directed to heterocyclic fused phenanthrolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
Claims13
A compound of formula (I):
- or a pharmaceutically acceptable salt thereof, wherein
- X represents —CH, or —O;
- R represents C6-10 aryl or C5-10 heterocyclyl;
- wherein said aryl and heterocyclyl is optionally substituted with one or more of RX
- RX represents:
- (a) halogen,
- (b) hydroxy,
- (c) —O—C1-6 alkyl, said alkyl optionally substituted with 1 to 3 groups of halo;
- (d) —C1-6 alkyl, said alkyl optionally substituted with 1 to 3 groups of halo;
- (e) cyano,
- (f) NRARB
- (g) —C(═O)—RC,
- (h) —S(O)n—RC;
- or
- (i) C5-10 heterocyclyl, said heterocyclyl optionally substituted with 1 to 3 groups of RC;
- RA and RB are independently selected from the group consisting of
- (i) hydrogen,
- (ii) —C1-6 alkyl,
- or RA and RB are linked together with the nitrogen to which they are both attached to form a 2-6 membered carbocyclic ring, wherein one or two of the ring carbon atoms is optionally replaced by a nitrogen, oxygen or sulfur, and the carbocyclic is optionally substituted with one or more C1-6 alkyl,
- RC is selected from the group consisting of
- (i) hydrogen, or
- (ii) —C1-6 alkyl, and
- n is 0, 1 or 2.
20 more elements
Dependencies are inferred from the claim text.