SGLT-2 inhibitors, methods of making them, and uses thereof
AssigneeAlbany Molecular Research, Inc.
InventorsShuang Liu, Cheng Guo
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Abstract
The present invention relates to compounds which are inhibitors of sodium dependent glucose co-transporter-2 (SGLT-2). These compounds are used in the treatment of various disorders, including diabetes, impaired glucose tolerance, insulin resistance, retinopathy, nephropathy, neuropathy, cataracts, hyperglycemia, hyperinsulinemia, hyperchlolesterolemia, elevated blood level of free fatty acids or glycerol, hyperlipidemia, hypertriglyceridemia, obesity, wound healing, tissue ischemia, atherosclerosis, and hypertension. These compounds and compositions are also useful for treating and preventing kidney stones, hyperuricemia, gout, and hyponatremia. Methods of making these compounds are also described in the present invention.
Claims7
A compound of formula (III):
- wherein
- Y is
- R5 is Cl, F, or methyl;
- R6, R7, and R8 are H;
- R9 is CH2OH or SMe;
- R10 is H, lower alkyl, lower alkenyl, or lower alkynyl, wherein each lower alkyl, lower alkenyl, or lower alkynyl is optionally substituted 1-3 times by Re;
- R11 is H, methyl, ethyl, or gem-dimethyl;
- Re is halogen, CF3, CF2H, OCF3, OCF2H, CN, ORg, NRgRh, CORg, CONRgRh, NRgCORh, SO2Rg, 3 to 10-membered carbocycle, or 3 to 10-membered heterocycle, wherein the each of the 3 to 10-membered carbocycle or 3-10-membered heterocycle is optionally substituted 1-3 times with halogen, CF3, CF2H, OCF3, OCF2H, CN, ORg, NRgRh, CORg, CONRgRh, NRgCORh, or SO2Rg;
- and
- Rg and Rh are each, independently, H, lower alkyl, lower alkenyl, or lower alkynyl;
- or an oxide thereof, a pharmaceutically acceptable salt thereof, or a solvate thereof.
A compound of formula (III):
- wherein
- Y is
- R5 is Cl or methyl;
- R6, R7, and R8 are H;
- R9 is CH2OH;
- R10 is H, H lower alkyl, lower alkenyl, or lower alkynyl, wherein each lower alkyl, lower alkenyl, or lower alkynyl is optionally substituted 1-3 times by Re;
- R11 is H, methyl, ethyl or gem-dimethyl;
- Re is halogen, CF3, CF2H, OCF3, OCF2H, CN, ORg, NRgRh, CORg, CONRgRh, NRgCORh, SO2Rg, 3 to 10-membered carbocycle, or 3 to 10-membered heterocycle, wherein the each of the 3 to 10-membered carbocycle or 3-10-membered heterocycle is optionally substituted 1-3 times with halogen, CF3, CF2H, OCF3, OCF2H, CN, ORg, NRgRh, CORg, CONRgRh, NRgCORh, or SO2Rg;
- and
- Rg and Rh are each, independently, H, lower alkyl, lower alkenyl, or lower alkynyl;
- or an oxide thereof, a pharmaceutically acceptable salt thereof, or a solvate thereof.
Dependencies are inferred from the claim text.