Back to results
US 2010/0305141 A1Published application
Tetrahydroindolone derivatives for treatment of neurological conditions
AssigneeAbraxis BioScience, LLC
InventorsDavid Helton, Daivd Fick, Ernie Pfadenhauer, Jason Sharp
Life of this patent
Estimating the term…
Abstract
Compositions comprising tetrahydroindolone derivatives in which the tetrahydroindolone moiety is covalently linked to a substituted arylpiperazine moiety and methods for treating neurological and psychiatric conditions using such compositions are disclosed.
Claims16
A pharmaceutical composition comprising a compound having the following formula (I):
- wherein:
- (a) X is CH or N;
- (b) R1 is hydrogen, alkyl, aralky, heteroaralkyl, alkenyl, aralkenyl, heteroaralkenyl, aryl, or heteroaryl;
- (c) R2 is hydrogen, alkyl, aralky, aryl, or heteroaryl;
- (d) R2′ is hydrogen unless R2 is methyl, in which case R2′ is also methyl;
- (e) R3 has the following formula (III):
- wherein:
- (i) R4 is hydrogen, alkyl, halo, hydroxy, alkoxy, cyano, nitro, perfluoroalkyl, perfluoroalkoxy, or hydroxymethyl;
- (ii) R5 is hydrogen, alkyl, halo, alkoxy, cyano, nitro, perfluoroalkyl, perfluoroalkoxy, amino, aminocarbonyl, aminosulfonyl, or hydroxymethyl;
- (iii) R6 is alkyl, halo, alkoxy, perfluoroalkyl, perfluoroalkoxy, or nitro;
- (iv) R4 and R5 when taken together can form a 5 or 6 membered ring and can contain one or more heteroatoms;
- (v) R5 and R6 when taken together can form a 5 or 6 membered ring and can contain one or more heteroatoms;
- (f) L is selected from the group consisting of —(CH2)m—, where m is an integer from 1 to 6, and an alkyl substituted hydrocarbyl moiety of the formula (IV):
- wherein:
- (i) n is 0, 1 or 2;
- (ii) R7 and R8 are hydrogen, methyl or ethyl;
- (iii) R9 and R9′ are both hydrogen, methyl or ethyl;
- (iv) if n is 1 and R7 or R8 is methyl or ethyl, then R9 and R9′ are hydrogen;
- (v) if n is 1 and R7 and R8 are hydrogen, then R9 and R9′ are methyl or ethyl;
- and
- (vi) if n is 2, then R9 and R9′ are hydrogen and one or both of R7 and R8 are methyl or ethyl.
- and pharmaceutically acceptable salts and esters thereof.
19 more elements
7-8. (canceled)
17-18. (canceled)
Dependencies are inferred from the claim text.