http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-078733-A1

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filingDate 2010-10-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2011-11-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-078733-A1
titleOfInvention FUSIONED HETEROCICLICAL COMPOUNDS AS MODULATORS OF THE OREXINE RECEIVER
abstract Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseases, disorders and conditions mediated by orexin activity, such as insomnia. Claim 1: A chemical entity that is a compound of Formula (1): wherein: n is 0-1; R1 is a member selected from the group consisting of: A) phenyl substituted or unsubstituted with one or two Ra members, and substituted in the ortho position with Rb; Ra is independently selected from the group consisting of: halo, -C1-4 alkyl and -C1-4 alkoxy, wherein two adjacent Ra members can be joined to form a six-membered aromatic ring; Rb is a member selected from the group consisting of: a) halo, -C1-4 alkoxy, -CF3 or -CF2CHF2; b) a 5-membered heteroaryl ring containing an oxygen or sulfur member; c) a 5-6 membered heteroaryl ring containing one to three nitrogen members, optionally, containing an oxygen member, substituted or unsubstituted with halo, -C1-4 alkyl, tetrahydropyran-2-yl, or - N (CH3) 2; and d) phenyl substituted or unsubstituted with -F or -CH3; B) pyridine substituted or unsubstituted with one or two members Rc and substituted with Rd, where Rd is placed adjacent to the junction point by R1; Rc is a member independently selected from the group consisting of: -C1-4 alkyl, -CF3 and -C1-4 alkoxy; Rd is a member selected from the group consisting of: a) a 5-6 membered heteroaryl ring selected from the group consisting of: 1H-1,2,3-triazol-1-yl, 2H-1,2,3- triazol-2-yl, 1H-pyrazol-3-yl and 6-methyl-pyridin-2-yl; and b) -CF3, -Br or -C1-4 alkoxy; C) a 6-membered heteroaryl ring selected from the group consisting of: pyrimidin-yl or pyrazin-yl substituted or unsubstituted with a member independently selected from -CH3, -OCH3 or phenyl; D) a 5-membered heteroaryl ring selected from the group consisting of: 2-methyl-1,3-thiazol-yl, 5-methyl-isoxazol-4-yl, 2H-pyrazol-3-yl, 1H-pyrazole-4 -yl, isoxazolyl and 1,3-oxazol-4-yl, each substituted with phenyl substituted or unsubstituted with -F or -CI; and E) 3-methylfuran-2-yl, 9H-fluorene, 9H-fluoren-9-one, 3,5'-biisoxazole, [3-methyl-5- (4-methyl-1,2,3-thiadiazole- 5-iI) isoxazol-4-iI] or naphthyridine; R2 is a member selected from the group consisting of: A) a 6-membered heteroaryl ring containing two nitrogen members substituted or unsubstituted with one or more members independently selected from the group consisting of: halo, -C1-4 alkyl , -C1-4, -CF3, -NH2, -NHCH3 alkoxy, -N (C1-4) 1-2 alkyl, cyclopropyl-NH and phenyl; B) pyridine substituted or unsubstituted with one or two members independently selected from the group consisting of: -C1-4 alkyl, -N (C1-4 alkyl) 2 and -CF3; and C) quinoxalin-2-yl, benzooxazol-2-yl or 5-chloro-1,3-benzoxazole; and pharmaceutically acceptable salts of the compounds of Formula 1.
priorityDate 2009-10-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 65.