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US 2006/0142269 A1Published application
New compounds
OwnerGraeme Dykesinventor
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds of the general Formula (I), wherein R1, R2 and R3 are as defined in the description; to pharmaceutical compositions comprising these compounds; and to the use of the compounds for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes, and/or CNS disorders.
Claims20
A compound of Formula (I)
- wherein
- one of R1 and R2 is selected from Formula (II) or (III)
- while the other one of R1 and R2 is selected from group of Formula (IV)-(XV)
- wherein
- t is 0, 1, or 2;
- R8 is each independently
- (a) hydrogen,
- (b) methyl, or
- (c) ethyl, and
- when t=2, the R8 groups can be attached to the same or different carbon atom(s);
- R9 is
- (a) H,
- (b) C1-6 alkyl, or
- (c) benzyl;
- R3 is selected from
- (a) hydrogen,
- (b) C1-4-alkyl,
- (c) halogen, and
- (d) C1-4-alkoxy,
- wherein the said R3 group is attached to a carbon atom in the 5-membered or the 6-membered ring;
- R4 is selected from
- (a) aryl,
- (b) heteroaryl,
- (c) heterocyclyl, provided that R1 or R2 is selected from a group of Formula (II),
- (d) aryl-C1-2-alkyl, provided that R1 or R2 is selected from a group of Formula (II), and
- (e) cinnamyl, provided that R1 or R2 is selected from the group of Formula (II),
- wherein any aryl and heteroaryl is optionally substituted in one or more positions with a substituent selected from:
- (a) halogen,
- (b) C1-6-alkyl,
- (c) CF3,
- (d) C1-6-alkoxy,
- (e) C2-6-alkenyl,
- (f) phenyl,
- (g) phenoxy,
- (h) benzyloxy,
- (i) benzoyl,
- (j) —OCF3,
- (k —CN,
- (l) hydroxy-C1-4-alkyl,
- (m) —CH2—(CH2)pF, wherein p is 0, 1, 2, or 3,
- (n) —CHF2,
- (o) —NR5R5,
- (p) —NO2,
- (q) —CONR5R5,
- (r) —NHSO2R7,
- (s) —NR6COR7,
- (t) —SO2NR6R7,
- (u) —C(═O)R7,
- (v) —CO2R6,
- (z) —S(O)nR7, wherein n is 1 or 2,
- (aa) C1-6-alkylthio,
- (ab) —SCF3,
- (ac) C2-4-alkynyl, and
- (ad) hydroxyl;
- R5 is each independently selected from
- (a) H,
- (b) C1-6-alkyl, and
- (c) C3-7-cycloalkyl,
- wherein the two R5 groups together with the nitrogen to which they are attached form a heterocyclic ring;
- and when the two R5 groups form a piperazine ring, the hydrogen bearing nitrogen of the piperazine ring may be optionally substituted with a group selected from
- (a) C1-4-alkyl,
- (b) 2-cyanoethyl,
- (c) hydroxy-C2-4-alkyl,
- (d) C3-4-alkenyl,
- (e) C3-7-cycloalkyl,
- (f) C3-7-cycloalkyl-C1-4-alkyl, and
- (g) C1-4-alkoxy-C2-4-alkyl;
- R6 is each independently selected from
- (a) hydrogen, and
- (b) C1-4-alkyl;
- and
- R7 is independently selected from
- (a) C1-6-alkyl
- (b) aryl, and
- (c) heteroaryl,
- wherein any heteroaryl or aryl residue is optionally substituted with a substituent selected from
- (a) halogen,
- (b) C1-4-alkyl,
- (c) C1-4-alkylthio,
- (d) C1-4-alkoxy,
- (e) —CF3, and
- (f) —CN;
- and a pharmaceutical acceptable salt thereof.
80 more elements
A pharmaceutical formulation containing a compound according claim as an active ingredient, in combination with a pharmaceutically acceptable diluent or carrier.
Dependencies are inferred from the claim text.