http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-076591-A1
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Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_1c89ce4d9ac03f9acd8ddede1162f94d |
filingDate | 2010-05-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2011-06-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | AR-076591-A1 |
titleOfInvention | MODULATORS OF ARIL METHYL BENZOQUINAZOLINE POSITIVE ALLOSTERICS OF THE RECEIVER M1 |
abstract | Positive allosteric modulators of the M1 receptor and which are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia and pain or sleep disorders. This also refers to pharmaceutical compositions comprising the compounds and the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. Claim 1: A compound of formula (1): and pharmaceutically acceptable salts thereof, wherein A is phenyl, naphthyl or pyridyl; R1 is selected from the group consisting of: hydrogen, -C6-10 aryl, -C5-10 heterocyclyl, halogen, -CN, -O-C1-6 alkyl, -C1-6 alkyl, -C2-6 alkenyl, - S (= O) n-R4, NR5AR5B, wherein said aryl, heterocyclyl, alkyl and alkenyl moiety is optionally substituted by one or more of Ra; R1 may be attached to the nitrogen atom in the pyridyl ring of formula (1) to form a naphthyl group; Ra is selected from the group consisting of: halogen, hydroxy, -O-C1-6 alkyl, -C1-6 alkyl, -S (= O) n-R8, -C2-6 alkenyl, -CN, -C ( = O) - (O) m-R6, -NR5AR5B, oxo, -C6-10 -aryl, -C5-10 heterocyclyl, -OC (= O) -R6, wherein the alkyl, alkenyl, aryl, heterocyclyl is optionally substituted by one or more halogen, -C 1-6 alkyl or -C 1-6 alkyl; R2 is selected from the group consisting of hydrogen, -C6-10 aryl, -C5-10 heterocyclyl, -O-C1-6 alkyl, -C1-6 alkyl, -C2-6 alkenyl, -S (= O) n -R4, -C3-8cycloalkyl, -C5-8cycloalkenyl, -NR5AR5B, wherein said aryl, heterocyclyl, alkyl, alkenyl, cycloalkyl and cycloalkenyl moiety is optionally substituted by one or more of Ra; R3 is selected from the group consisting of hydrogen, -C1-6 alkyl and -S (O) n-R4, wherein said alkyl radical R3 is optionally substituted by one or more halogen, cyano and -O-C1-alkyl 6, wherein said alkyl is optionally substituted by one or more halo; R4, R6 and R8 are independently selected from the group consisting of hydrogen, -C1-6 alkyl and - (CH2) n-aryl, wherein said alkyl or aryl moiety R4, R6 and R8 is optionally substituted by one or more halogen, cyano and -O-C1-6 alkyl, wherein said alkyl is optionally substituted by one or more halogen; R5A and R5B are selected from the group consisting of hydrogen, -C1-6alkyl, -C3-6cycloalkyl, -C (= O) -O- R6, -S (O) 2-R6, R5A and R5B are linked together with the nitrogen to which both are attached to form a 2-6 membered carbocyclic ring, in which one or two of the ring carbon atoms is optionally replaced by a nitrogen, oxygen or sulfur; m is 0 or 1; and n is 0, 1 or 2. |
priorityDate | 2010-05-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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