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US 2002/0058655 A1Published application
New use
AssigneeBiovitrum AB
InventorsPatrizia Caldirola, Sukhwinder Jossan, Kjell S. Sakariassen, Jan Svartengren
Life of this patent
Estimating the term…
Abstract
The invention provides a method of treatment or prophylaxis of obesity, comprising administering to a patient in need of such treatment a therapeutically effective amount of an aryl sulfonamide compound of formula (I) or formula (II) 1 wherein the substituents are as described in the specification.
Claims20
Method of treatment or prophylaxis of obesity in mammals, including humans, comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of formula (I) or formula (II)
- 8
- wherein
- E is —SO2NH— or —NHSO2—;
- R2 is hydrogen, C1-6 alkyl or arylC1-6 alkyl;
- P is phenyl, naphthyl a bicyclic heterocyclic ring or is a 5- to 7-membered hererocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur;
- A is a single bond, a C1-6 alkylene or a C1-6 alkenylene group;
- R1 is halogen, C1-6 alkyl, optionally substituted by one or more halogen atoms, C3-6 cycloalkyl, COC1-6 alkyl, C1-6 alkoxy, OCF3, hydroxy, hydroxy C1-6 alkyl, hydroxy C1-6alkoxy, C1-6 alkoxy C1-6 alkoxy, C1-6 alkanoyl, acyl, nitro, amino, alkylamino or dialkylamino, cyano or SR11 where R11 is hydrogen or C1-6 alkyl or R1 is phenyl, benzyl, naphthyl, a bicyclic heterocyclic ring, or is a 5 to 7-membered heterocyclic ring, each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur;
- n is 0, 1, 2, 3, 4, 5 or 6;
- R3 is a group R5 or together with R5 forms a group (CH2)2O or (CH2)3O or R3 is linked to R2 to form a group (CH2)2 or (CH2)3;
- R4 is —X(CH2)p-R6 where X is a single bond, CH2, O, NH or N—C1-6-alkyl and p is 0 to 6 and R6 is an optionally substituted 5- to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from nitrogen, sulfur or oxygen, or R6 is NR7R8 where R7 and R8 are independently hydrogen, C1-6 alkyl or aryl C1-6 alkyl, or
- R4 is selected from a group of formula (i), (ii) or (iii)
- Formula (i)
- 9
- wherein
- R9 is C1-6 alkyl, or C1-6 alkyl substituted by one or more halogen atoms;
- m is 0, 1 or 2;
- q is 0, 1, 2, 3 or 4;
- or
- Formula (ii)
- 10
- wherein
- R9, m and q are as defined in formula (i);
- or
- Formula (iii)
- 11
- wherein R9, m and q are as defined in formula (i) and R7 is hydrogen or C1-6 alkyl;
- R5 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, optionally substituted with one or more fluorine atoms, C3-6 cycloalkyl, COC1-6 alkyl, C1-6 alkoxy, hydroxy, hydroxy C1-6 alkyl, hydroxy C1-6 alkoxy, C1-6 alkoxyC1-6 alkoxy, acyl, nitro, trifluoromethyl or together with R3 forms a group (CH2)2O or (CH2)3O, cyano or aryl;
- or pharmaceutically acceptable salts thereof.
25 more elements
Use of a compound of formula (I) or (II)
- 12
- wherein
- E is —SO2NH— or —NHSO2—;
- R2 is hydrogen, C1-6 alkyl or arylC1-6 alkyl;
- P is phenyl, naphthyl a bicyclic heterocyclic ring or is a 5- to 7-membered hererocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur;
- A is a single bond, a C1-6 alkylene or a C1-6 alkenylene group;
- R1 is halogen, C1-6 alkyl, optionally substituted by one or more halogen atoms, C3-6 cycloalkyl, COC1-6 alkyl, C1-6 alkoxy, OCF3, hydroxy, hydroxy C1-6 alkyl, hydroxy C1-6 alkoxy, C1-6 alkoxy C1-6 alkoxy, C1-6 alkanoyl, acyl, nitro, amino, alkylamino or dialkylamino, cyano or SR11 where R11 is hydrogen or C1-6 alkyl or R1 is phenyl, benzyl, naphthyl, a bicyclic heterocyclic ring, or is a 5 to 7-membered heterocyclic ring, each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur;
- n is 0, 1, 2, 3, 4, 5 or 6;
- R3 is a group R5 or together with R5 forms a group (CH2)2O or (CH2)3O or R3 is linked to R2 to form a group (CH2)2 or (CH2)3;
- R4 is —X(CH2)p-R6 where X is a single bond, CH2, O, NH or N—C1-6 -alkyl and p is 0 to 6 and R6 is an optionally substituted 5- to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from nitrogen, sulfur or oxygen, or R6 is NR7R8 where R7 and R8 are independently hydrogen, C1-6 alkyl or aryl C1-6 alkyl, or
- R4 is selected from a group of formula (i), (ii) or (iii)
- Formula (i)
- 13
- wherein
- R9 is C1-6 alkyl, or C1-6 alkyl substituted by one or more halogen atoms;
- m is 0, 1 or 2;
- q is 1, 2, 3 or 4;
- or
- Formula (ii)
- 14
- wherein
- R9, m and q are as defined in formula (i);
- or
- Formula (iii)
- 15
- wherein R9, m and q are as defined in formula (i) and R7 is hydrogen or C1-6 alkyl;
- R5 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, optionally substituted with one or more fluorine atoms, C3-6 cycloalkyl, COC1-6 alkyl, C1-6 alkoxy, hydroxy, hydroxy C1-6 alkyl, hydroxy C1-6 alkoxy, C1-6 alkoxy-C1-6 alkoxy, acyl, nitro, trifluoromethyl or together with R3 forms a group (CH2)2O or (CH2)3O, cyano or aryl;
- or pharmaceutically acceptable salts thereof, in the manufacture of a medicament for the treatment of obesity.
25 more elements
Dependencies are inferred from the claim text.