PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS
Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
1 - 70 . (canceled)
71 . A compound having the following structure (III):
or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof,
wherein:
R 1 is C 1-6 alkyl, C 1-6 haloalkyl, —(CH 2 ) n O(CH 2 ) m CH 3 or —(CH 2 ) n N(CH 3 ) 2 ;
R 2 and R 3 are the same or different and independently substituted or unsubstituted heterocyclyl, or substituted or unsubstituted aryl; and
R 4 and R 5 are the same or different and independently hydrogen, C 1-6 alkyl or C 1-6 haloalkyl;
n is 1, 2, 3, 4, 5 or 6; and
m is 0, 1, 2, 3, 4, 5 or 6.
72 . The compound of claim 71 wherein R 4 and R 5 are the same or different and independently hydrogen or C 1-6 alkyl.
73 . The compound of claim 71 wherein R 4 and R 5 are hydrogen.
74 . The compound of claim 71 wherein R 1 is C 1-6 alkyl.
75 . The compound of claim 74 wherein R 1 is methyl.
76 . The compound of claim 74 wherein R 1 is ethyl.
77 . The compound of claim 74 wherein R 1 is isopropyl.
78 . The compound of claim 71 wherein R 3 is substituted phenyl.
79 . The compound of claim 78 wherein R 3 is 3,4,5-trimethoxyphenyl.
80 . The compound of claim 78 wherein R 3 is 4-bromo-3,5-dimethoxyphenyl.
81 . The compound of claim 71 wherein R 2 is substituted or unsubstituted phenyl.
82 . The compound of claim 81 wherein R 2 is 4-morpholinophenyl.
83 . The compound of claim 81 wherein R 2 is 4-(1H-pyrazol-1-yl)phenyl.
84 . The compound of claim 71 wherein R 2 is substituted or unsubstituted naphthyl.
85 . The compound of claim 71 wherein R 2 is substituted or unsubstituted heteroaryl.
86 . A pharmaceutical composition comprising a compound of claim 71 and a pharmaceutically acceptable carrier or diluent.
87 - 100 . (canceled)