C-aryl glucoside SGLT2 inhibitors and method

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United States of America Patent

PATENT NO 6414126
SERIAL NO

09679027

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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SGLT2 inhibiting compounds are provided having the formula ##STR1## where R.sup.1, R.sup.2, and R.sup.2a are independently hydrogen, OH, OR.sup.5, lower alkyl, CF.sub.3, OCHF.sub.2, OCF.sub.3, SR.sup.5i or halogen, or two of R.sup.1, R.sup.2 and R.sup.2a together with the carbons to which they are attached can form an annelated five, six or seven membered carbocycle or heterocycle; R.sup.3 and R.sup.4 are independently hydrogen, OH, OR.sup.5a, OAryl, OCH.sub.2 Aryl, lower alkyl, cycloalkyl, CF.sub.3, --OCHF.sub.2, --OCF.sub.3, halogen, --CN, --CO.sub.2 R.sup.5b, --CO.sub.2 H, --COR.sup.6b, --CH(OH)R.sup.6c, --CH(OR.sup.5h)R.sup.6d, --CONR.sup.6 R.sup.6a, --NHCOR.sup.5c, --NHSO.sub.2 R.sup.5d, --NHSO.sub.2 Aryl, Aryl, --SR.sup.5e, --SOR.sup.5f, --SO.sub.2 R.sup.5g, --SO.sub.2 Aryl, or a five, six or seven membered heterocycle, or R.sup.3 and R.sup.4 together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle; R.sup.5, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.5d, R.sup.5e, R.sup.5f, R.sup.5g, R.sup.5h and R.sup.5i are independently lower alkyl; R.sup.6, R.sup.6a, R.sup.6b, R.sup.6c and R.sup.6d are independently hydrogen, alkyl,aryl, alkylaryl or cycloalkyl, or R.sup.6 and R.sup.6a together with the nitrogen to which they are attached form an annelated five, six or seven membered heterocycle; A is O, S, NH, or (CH.sub.2).sub.n where n is 0-3. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.

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Patent Owner(s)

  • ASTRAZENECA AB

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Ellsworth, Bruce Princeton, NJ 5 570
Meng, Wei Pennington, NJ 80 1072
Sher, Philip M Plainsboro, NJ 37 1765
Washburn, William N Titusville, NJ 48 1537
Wu, Gang Princeton, NJ 243 2891

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