Combination therapy with SGLT-2 inhibitors and their pharmaceutical compositions

Combination therapy with SGLT-2 inhibitors and their pharmaceutical compositions

  • CN 101,534,815 A
  • Filed: 11/08/2007
  • Published: 09/16/2009
  • Est. Priority Date: 11/09/2006
  • Status: Active Application
First Claim
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1. pharmaceutical composition, it comprises one or more SGLT-2 inhibitor compounds and one or more are suitable for treating second therapeutic agent of one or more metabolic diseases, wherein:

  • I) described one or more SGLT-2 inhibitor compounds comprise the benzene derivative that glycopyranosyl replaces, and it is selected from chemical compound 1-17;

    (1) 1-chloro-2-(4-cyclopentyloxy benzyl)-4-(β

    -D-glucopyranose-1-yl)-benzene(2) 1-chloro-4-(β

    -D-glucopyranose-1-yl)-2-[4-((R)-oxolane-3-base oxygen base)-benzyl]-benzene;

    (3) 1-chloro-4-(β

    -D-glucopyranose-1-yl)-2-[4-((S)-oxolane-3-base oxygen base)-benzyl]-benzene;

    (4) 1-chloro-4-(β

    -D-glucopyranose-1-yl)-2-[4-(oxolane-2-ketone-3-base oxygen base)-benzyl]-benzene;

    (5) 1-chloro-4-(β

    -D-glucopyranose-1-yl)-2-(4-cyclobutyl oxygen base-benzyl)-benzene;

    (6) 1-chloro-4-(β

    -D-glucopyranose-1-yl)-2-(4-cyclohexyl oxygen base-benzyl)-benzene;

    (7) 1-chloro-4-(β

    -D-glucopyranose-1-yl)-2-[4-(tetrahydropyran-4-base oxygen base)-benzyl]-benzene;

    (8) 1-chloro-4-(β

    -D-glucopyranose-1-yl)-2-[4-(1-acetyl group-piperidin-4-yl oxygen base)-benzyl]-benzene;

    (10) 1-(β

    -D-glucopyranose-1-yl)-4-methyl-3-[4-(oxolane-3-base oxygen base)-benzyl]-benzene;

    (11) 1-(β

    -D-glucopyranose-1-yl)-4-methyl-3-[4-(2-trimethyl silyl-ethyl)-benzyl]-benzene;

    (12) 1-chloro-4-(β

    -D-glucopyranose-1-yl)-2-(4-acetenyl-benzyl)-benzene;

    (13) 1-chloro-4-(β

    -D-glucopyranose-1-yl)-2-[4-(piperidin-4-yl oxygen base)-benzyl]-benzene;

    (14) 1-fluoro-4-(β

    -D-glucopyranose-1-yl)-2-(4-acetenyl-benzyl)-benzene;

    (15) 1-(β

    -D-glucopyranose-1-yl)-3-(4-acetenyl-benzyl)-benzene;

    (16) 1-acetenyl-4-(β

    -D-glucopyranose-1-yl)-2-(4-ethyoxyl-benzyl)-benzene;

    With(17) 1-methoxyl group-4-(β

    -D-glucopyranose-1-yl)-2-(4-acetenyl-benzyl)-benzene,Or its tautomer, stereoisomer, its mixture or its salt;

    Or wherein one or more hydroxyls of this β

    -D-glycopyranosyl are selected from (C 1-3-alkyl) carbonyl, (C 1-6-alkyl) oxygen base carbonyl, phenylcarbonyl group, phenyl-(C 1-3-alkyl)-carbonyl, phenyl oxygen base carbonyl and phenyl-(C 1-3-alkyl)-prodrug of the group acidylate of oxygen base carbonyl, or its officinal salt;

    AndIi) described second therapeutic agent that one or more are suitable for treating one or more metabolic diseases comprises;

    A) biguanide,B) sulfonylureas (SU),C) thiazolidinedione (PPAR gamma agonist),D) alpha-Glucosidase blocker,E) insulin and insulin analog,F) GLP1 and GLP1 analog,G) PPAR gamma modulators,H) PPAR γ

    /alpha modulators,I) glucose-dependent-insulinotropic polypeptide agonist,J) beta-3 agonist, orK) activators of glucokinase.

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