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Combinations comprising 6-benzylphenyl-2-sulfurterahydropyran-3,4,5-triol derivatives as sodium-glucose 1 and 2 cotransporter inhibitors for use in diabetic patients
专利权人:
Lexicon Pharmaceuticals; Inc.
发明人:
BROWN, Philip Manton,FREIMAN, Joel Philip,POWELL, David Reed
申请号:
ES11707324
公开号:
ES2609104T3
申请日:
2011.03.01
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
Dose of 300 mg / day or less (eg, 250, 200, 150, 100 or 50 mg / day or less) of a dual SGLT1 / 2 inhibitor of the formula: ** Formula ** or a pharmaceutically acceptable salt of same, for use in improving the cardiovascular or metabolic health of a diabetic or prediabetic patient currently taking a DPP-4 inhibitor, wherein: each R1A is independently hydrogen, alkyl, aryl, or heterocycle; each R6 is independently hydrogen, hydroxyl, amino, alkyl, aryl, cyano, halogen, heteroalkyl, heterocycle, nitro, C≡CR6A, OR6A, SR6A, SOR6A, SO2R6A, C (O) R6A, CO2R6A, CO2H, CON (R6A) (R6A), CONH (R6A), CONH2, NHC (O) R6A or NHSO2R6A; each R6A is independently alkyl, aryl, or heterocycle; each R7 is independently hydrogen, hydroxyl, amino, alkyl, aryl, cyano, halogen, heteroalkyl, heterocycle, nitro, C≡CR7A, OR7A, SR7A, SOR7A, SO2R7A, C (O) R7A, CO2R7A, CO2H, CON (R7A) (R7A), CONH (R7A), CONH2, NHC (O) R7A, or NHSO2R7A; each R7A is independently alkyl, aryl, or heterocycle; m is 1-4; n is 1-3; p is 0-2; and wherein each alkyl, aryl, heteroalkyl, or heterocycle is optionally substituted by one or more of alkoxy, amino, cyano, halo, hydroxyl, or nitro, and wherein the DPP-4 inhibitor is sitagliptin.Dosis de 300 mg/día o menos (por ejemplo, 250, 200, 150, 100 o 50 mg/día o menos) de un inhibidor de SGLT1/2 dual de la fórmula:**Fórmula** o una sal farmacéuticamente aceptable del mismo, para su uso en la mejora de la salud cardiovascular o metabólica de un paciente diabético o prediabético que toma actualmente un inhibidor de DPP-4, en la que: cada R1A es independientemente hidrógeno, alquilo, arilo o heterociclo; cada R6 es independientemente hidrógeno, hidroxilo, amino, alquilo, arilo, ciano, halógeno, heteroalquilo, heterociclo, nitro, C≡CR6A, OR6A, SR6A, SOR6A, SO2R6A, C(O)R6A, CO2R6A, CO2H, CON(R6A)(R6A), CONH(R6A), CONH2, NHC(O)R6A o NHSO2R6A; cada R6A es independientemente alquilo, arilo o heterociclo; cada R7 es independientemente hidrógeno, hidroxilo, amino, alquilo, arilo, cian
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