摘要:
The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity. (I)
摘要:
The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity. (I)
摘要:
This invention relates to compounds that are of formula (I) wherein A is heteroaryl and R1 and R2 are both cyclic residues, that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial .
摘要:
The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins which are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity, as well as methods for treating diseases that are associated with proteins which are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity.
摘要:
The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins which are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity, as well as methods for treating diseases that are associated with proteins which are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity.
摘要:
The present invention relates to new therapeutically active and selective inhibitors of the enzyme DPP-IV. Novel 2-substituted unsaturated heterocyclic compounds are provided, wherein a nitrogen atom in the heterocyclic ring is attached via an amide bond or a peptide bond to an amino acid or an amino acid derivative. These compounds are potent and selective inhibitors of DPP-IV, and are effective in treating conditions that may be regulated or normalised via inhibition of DPP-IV.
摘要:
4,5,6,7-tetrahydro-thieno[3,2-c]pyridine derivative modulate the activity of molecules with glucose-6-phosphate recognition units, including glucose-6-phosphatases (G-6-Pases) in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings, and are useful in the treatment of diseases related to glucose metabolic pathways.
摘要:
Nouveaux composés de pipéridine correspondant à la formule (I) dans laquelle R3 représente 3,4-méthylènedioxyphényle, phényle, naphtyle, ou un groupe hétérocyclique à 5 ou 6 éléments contenant un ou deux atomes N, O ou S en cours de saturation partiellement saturés ou aromatiques qui sont facultativement remplacés par un ou plusieurs halogènes, amino, amino C1-6-alkyle monosubstitué ou bisubstitué, C1-6-alkoxy, cyano, C1-6-alkyle monohalogéné ou polyhalogéné, C2-6-alcényle, C1-6-alkyle, C3-5-alkylène, trifluorométhoxy, hydroxy, hydroxy C1-4-alkyle, ou trifluorométhyle; n est compris entre 0 et 4; R1 représente hydrogène, C1-8-alkyle linéaire ou ramifié, C1-8-alkoxy-C1-8-alkyle, C3-8-cycloalkyle, C2-6-alcényle, C4-8-cycloalkylalkyle, acétyle ou C2-6-alcényle; X représente un ou plusieurs amino, NO2, amino C1-6-alkyle monosubstitué ou disubstitué, C1-8-alcanoylamino, carboxy, ureido C1-6-alkyle monosubstitué ou disubstitué, C1-6-alkyle substitué par des amino qui sont facultativement monosubstitués ou disubstitués par C1-6-alkyle, carbamoyle non substitué ou C1-6-alkyle facultativement remplacé par phényle et/ou hydroxy carbamoyle, N-monosubstitué ou disubstitué, sulfamoyle non substitué, C1-6-alkyle sulfamoyle N-substitué, C1-6-alkyle sulfamoyle S-substitué, C1-6-alkyle sulfamoyle N- et S-substitué, ou un groupe hétérocyclique à 5 ou 6 éléments contenant un ou deux atomes N, O ou S en cours de saturation, partiellement substitués ou aromatiques, le groupe hétérocyclique pouvant être intégré dans l'anneau et, lorsque Y représente NR et/ou lorsque n est compris entre 1 et 4 X représente halogène, C1-6-alkyle, C2-6-alcényle, C3-8-cycloalkyle, C4-8-cycloalkylalkyle, C1-6-alcoxy, cyano, monohalogéné ou polyhalogéné C1-6-alkyle, hydroxy ou hydrogène; Y représente O, S ou NR dans lequel R représente hydrogène ou C1-15-alkyle, ou un sel de ce dernier avec un acide pharmaceutiquement acceptable. Ces nouveaux composés sont utiles dans le traitement de l'anoxie, des blessures traumatiques, de l'ischémie, de la migraine, de
摘要:
The present invention relates to therapeutically active and selective inhibitors (Formula II)of the enzyme DPP-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity. The present inhibitors are novel purine derivatives, attached at position 8 of the purine skeleton to a diamine.