1005142-15-3

Upstream product

• 1004779-87-6 1-bromo-4-fluoro-2,5-bis(((2-methoxypropan-2-yl)oxy)methyl)benzene 
• 1004779-86-5 (5-bromo-2-fluoro-4-hydroxymethylphenyl)methanol 
• 1004779-85-4 5-bromo-2-fluoro-4-(hydroxymethyl)benzaldehyde 
• 202865-66-5 2-bromo-5-fluorobenzyl alcohol 
• 1005142-81-3 (1S,3'R,4'S,5'R,6'R)-3',4',5'-tris(benzyloxy)-6'-(benzyloxymethyl)-6-[(4-ethylphenyl)methyl]-5-fluoro-3',4',5',6'-tetrahydro-spiro[isobenzofuran-1(3H),2'-[2H]pyran] 

Relevant academic research and scientific papers

SUBSTITUTED SPIROKETAL DERIVATIVES AND USE THEREOF AS THERAPEUTIC DRUG FOR DIABETES

The present invention provides a compound represented by Formula (II): wherein R1 is a chlorine atom, a fluorine atom, a methyl group or an ethynyl group; Ar is a group represented by the following Formula (a), Formula (b), Formula (c) or Formula (d): wherein R2 is a C1-6 alkyl group which may be substituted with one or more halogen atoms, a C1-6 alkoxy group which may be substituted with one or more halogen atoms, a C1-3 alkylthio group, a halogen atom, a C1-3 alkylcarbonyl group or a C2-5 alkynyl group which may be substituted with —OR4; R3 is a hydrogen atom or a C1-3 alkyl group; R4 is a hydrogen atom or a C1-3 alkyl group; provided that Ar is a group represented by Formula (a) when R1 is a fluorine atom, methyl group or an ethynyl group, and that R2 is methoxy group, an ethoxy group, an isopropyl group, a propyl group, a trifluoromethyl group, a trifluoromethoxy group, 2-fluoroethyl group or 1-propynyl group when R1 is a methyl group or a pharmaceutically acceptable salt or a solvate thereof and a pharmaceutical agent, a pharmaceutical composition and so on comprising the compound.

Exploration of O-spiroketal C-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors

A series of novel O-spiroketal C-arylglucosides have been prepared and evaluated in cell-based functional assays for activity against human sodium-dependent glucose co-transporters 1 and 2 (SGLT1 and 2). The core spiro[isobenzofuran-1,2′-pyran] structure proved to be an effective scaffold for diversification and a number of compounds with single digit nanomolar potency and high selectivity have been synthesized. Compound 5a promoted glucosuria when administered in vivo in rats and produced a significant blood glucose reduction effect.

SUBSTITUTED SPIROKETAL DERIVATIVE AND USE THEREOF AS DRUG FOR TREATING DIABETES

The present invention provides a compound represented by Formula (II): wherein R1 is a chlorine atom, a fluorine atom, a methyl group or an ethynyl group; Ar is a group represented by the following Formula (a), Formula (b), Formula (c) or Formula (d): wherein R2 is a C1-6 alkyl group which may be substituted with one or more halogen atoms, a C1-6 alkoxy group which may be substituted with one or more halogen atoms, a C1-3 alkylthio group, a halogen atom, a C1-3 alkylcarbonyl group or a C2-5 alkynyl group which may be substituted with -OR4; R3 is a hydrogen atom or a C1-3 alkyl group; R4 is a hydrogen atom or a C1-3 alkyl group; provided that Ar is a group represented by Formula (a) when R1 is a fluorine atom, methyl group or an ethynyl group, and that R2 is methoxy group, an ethoxy group, an isopropyl group, a propyl group, a trifluoromethyl group, a trifluoromethoxy group, 2-fluoroethyl group or 1-propynyl group when R1 is a methyl group or a pharmaceutically acceptable salt or a solvate thereof and a pharmaceutical agent, a pharmaceutical composition and so on comprising the compound.