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filingDate 1998-01-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2000-08-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-011092-A1
titleOfInvention A COMPOUND DERIVED FROM TIAZOL BENZENSULFONAMIDES AS BETA3 AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY, A PHARMACEUTICAL COMPOSITION THAT IT UNDERSTANDS AND THE USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT.
abstract The thiazole-substituted benzenesulfonamides comprising formula I where: X is (1) a bond, (2) C1-C3 alkylene, optionally substituted with 1 or 2 groups selected from methyl and halogen, (3) C1-C3 alkylene, where said alkylene contains an oxygen, optionally with 1 or 2 selected groups of methyl and halogen; m is 0 to 5; A is (1) phenyl, (2) a 5- to 6-membered heterocyclic ring with from 1 to 4 heteroatoms selected from oxygen, sulfur and nitrogen, (3) a benzene ring fused to a C5-C10 carboxylic ring, (4) a 5- to 6-membered heterocyclic ring with from 1 to 4 heteroatoms selected from oxygen, sulfur, and nitrogen, or (5) a 5- or 6-membered heterocyclic ring with from 1 to 4 heteroatoms selected from deoxygen, sulfur, and nitrogen fused to a C5 carboxylic ring -C10; R1 is (1) C1-C10 alkyl optionally substituted with up to 5 groups as defined in the specification, they are beta3 adrenergic receptor agonists with little beta1 and beta2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in the cells. The compounds therefore have potent activity for the treatment of obesity and type II diabetes. The compounds can also be used to lower triglyceride levels and cholesterol levels or to raise high-density lipoprotein levels or to decrease intestinal motility. In addition, the compounds can be used to reduce neurogenic inflammation or as antidepressant agents. The compounds are prepared by substituted coupling. The pharmaceutical compositions and uses of said compounds for the manufacture of a medicament for use in treatment for use in the treatment of diabetes and obesity are described.
priorityDate 1997-01-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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