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US 2003/0149019 A1Published application
New compounds
AssigneeBiovitrum AB
InventorsUlf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Lori Sutin, Andrew Mott, Jan Tejbrant
Life of this patent
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Abstract
The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system. 1
Claims19
A compound of the formula (I)
- 272
- or a pharmaceutically acceptable salt thereof, wherein
- X is
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- R1 and R3 are independently
- (a) H
- (b) C1-6 alkyl,
- (c) C1-6 alkoxy,
- (d) straight or branched C1-6 hydroxyalkyl,
- (e) straight or branched C1-6 alkylhalides;
- or
- (f) a group Ar;
- Ar is
- (a) phenyl,
- (b) 1-naphthyl,
- (c) 2-naphthyl,
- (d) benzyl,
- (e) cinnamoyl,
- (f) a 5 to 7-membered, partially or completely saturated, heterocyclic ring containing 1 to 4 heteroatoms, selected from oxygen, nitrogen and sulfur, or
- (g) a bicyclic ring system consisting of two heterocyclic rings as defined under (f), or a bicyclic ring system consisting of one benzene ring and one heterocyclic ring as defined under (f);
- alternatively, R1 and R3 are linked to form a group (CH2)2O, (CH2)4O, or (CH2)3-5 in formula (Ib);
- optionally, the group Ar is substituted with
- (a) Y, or
- (b) a 5 to 7-membered, partially or completely saturated, heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur;
- Y is
- (a) H,
- (b) halogen,
- (c) C1-6 alkyl,
- (d) CF3,
- (e) hydroxy,
- (f) C1-6 alkoxy,
- (g) C1-4 alkenyl;
- (h) phenyl;
- (i) phenoxy,
- (j) benzyloxy,
- (k) benzoyl,
- (l) OCF3,
- (m) CN,
- (n) straight or branched C1-6 hydroxyalkyl,
- (o) straight or branched C1-6 alkylhalides,
- (p) NH2,
- (q) NHR6,
- (r) NR6R7,
- (s) NO2,
- (t) —CONR6R7,
- (u) NHSO2R6,
- (v) NR6COR7,
- (x) SO2NR6R7,
- (z) —C(═O)R6,
- (aa) —CO2R6, or
- (ab) S(O)nR6;
- wherein n is 0, 1, 2 or 3;
- R2 and R4 are independently:
- (a) —SO2R1,
- (b) H,
- (c) C1-6 alkyl,
- (d) C1-C3 alkenyl,
- (e) C1-C3 alkylaryl,
- (f) Ar as defined above for R1,
- (g) —C(═O)R6,
- (h) —C(O)NR6R7,
- (i) —C(S)NR6R7,
- (j) —CO2R6;
- (k) —C(S)R6;
- (l) straight or branched C1-6 hydroxyalkyl, or
- (m) straight or branched C1-6 alkylhalides;
- alternatively, R2 and R4 are linked to form a group (CH2)2O, (CH2)4O, or (CH2)3-5 in formula (Ia);
- R5 is selected from the group consisting of the following chemical groups:
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- R6 and R7 are independently
- (a) H,
- (b) C1-6 alkyl,
- (c) C3-7 cycloalkyl, or
- (d) Ar, as defined above for R1;
- alternatively, R6 and R7 are linked to form a group (CH2)2O, (CH2)4O or (CH2)3-5;
- R8 is
- (a) H, or
- (b) C1-6 alkyl.
75 more elements
Dependencies are inferred from the claim text.