862728-59-4

Upstream product

• 20117-44-6 2-(cyclopropyloxy)ethan-1-ol 
• 98-59-9 p-toluenesulfonyl chloride 
• 18742-02-4 2-bromo-2-(2-ethyl)dioxolane 

Downstream Products

• 1118567-45-5 4-bromo-1-chloro-2-[[4-[2-(cyclopropyloxy)ethoxy]phenyl]methyl]benzene 
• 1118567-05-7 (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-(2-cyclopropoxyethoxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol 
• 1400980-44-0 1-chloro-2-(4-(2-cyclopropoxyethoxy)benzyl)-4-iodobenzene 
• 1358579-72-2 [(1S,2S,3S,4R,5S)-2,3,4-tri-benzyloxy-5-[4-chloro-3-[[4-[2-(cyclopropyloxy)ethoxy]phenyl]methyl]phenyl]-6,8-dioxabicyclo[3.2.1]octan-1-yl]methanol 
• 1358579-69-7 [(3S,4S,5R,6S)-3,4,5-tri-benzyloxy-6-[4-chloro-3-[[4-[2-(cyclopropyloxy)ethoxy]phenyl]methyl]phenyl]-2-(hydroxymethyl)-6-methoxytetrahydropyran-2-yl]methanol 
• 1358579-67-5 (2S,3S,4S,5R,6S)-3,4,5-tri-benzyloxy-6-[4-chloro-3-[[4-[2-(cyclopropyloxy)ethoxy]phenyl]methyl]phenyl]-6-methoxytetrahydropyran-2-formaldehyde 
• 1358579-65-3 [(2R,3R,4S,5R,6S)-3,4,5-tri-benzyloxy-6-[4-chloro-3-[[4-[2-(cyclopropyloxy)ethoxy]phenyl]methyl]phenyl]-6-methoxytetrahydropyran-2-yl]methanol 

Relevant academic research and scientific papers

Discovery of a Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor (HSK0935) for the Treatment of Type 2 Diabetes

A new class of potent and highly selective SGLT2 inhibitors is disclosed. Compound 31 (HSK0935) demonstrated excellent hSGLT2 inhibition of 1.3 nM and a high hSGLT1/hSGLT2 selectivity of 843-fold. It showed robust urinary glucose excretion in Sprague-Dawley (SD) rats and affected more urinary glucose excretion in Rhesus monkeys. Finally, an efficient synthetic route has been developed featuring a ring-closing cascade reaction to incorporate a double ketal 1-methoxy-6,8-dioxabicyclo[3.2.1]octane ring system.

Glucopyranosyl derivative and application thereof in medicines

The invention relates to a glucopyranosyl derivative used as a sodium-dependent glucose transporter (SGLT) inhibitor, a medicinal composition containing the derivative, and an application of the derivative and the medicinal composition in medicines, and especially relates to the glucopyranosyl derivative represented by formula (I) or a pharmaceutically acceptable salt or all stereoisomers thereof, or the medicinal composition containing the derivative, and a use of the derivative and the medicinal composition in the preparation of medicines for treating diabetes and diabetes related diseases.

PREPARATION OF HYDROXY-BENZYLBENZENE DERIVATIVES

Methods for preparing intermediates of SGLT2 inhibitors are provided, including crystalline forms and methods of crystallizing intermediates.

PREPARATION OF HYDROXY-BENZYLBENZENE DERIVATIVES

Methods for preparing intermediates of SGLT2 inhibitors are provided, including crystalline forms and methods of crystallizing intermediates.

PREPARATION OF HYDROXY-BENZYLBENZENE DERIVATIVES

Methods for preparing intermediates of SGLT2 inhibitors are provided, including crystalline forms and methods of crystallizing intermediates.

CRYSTALLINE FORM OF BENZYLBENZENE SGLT2 INHIBITOR

Crystalline forms of a compound having an inhibitory effect on sodium-dependent glucose cotransporter SGLT2 are disclosed. Pharmaceutical compositions, methods of preparing the crystalline compound, and methods of using the crystalline compound, independently or in combination with other therapeutic agents for treating diseases and conditions which are affected by SGLT or SGLT2 inhibition are also disclosed.

CRYSTALLINE FORM OF BENZYLBENZENE SGLT2 INHIBITOR

Crystalline forms of a compound having an inhibitory effect on sodium-dependent glucose cotransporter SGLT2 are disclosed. Pharmaceutical compositions, methods for preparing the crystalline compound, and methods of using the crystalline compound, independently or in combination with other therapeutic agents for treating diseases and conditions which are affected by SGLT or SGLT2 inhibition are also disclosed.

PROCESSES FOR THE PREPARATION OF SGLT2 INHIBITORS

Provided are processes for the preparation of complexes that are useful in purifying compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The processes can reduce the number of steps needed to obtain the target compounds and the complexes formed in the processes are typically provided in a crystalline form.

BENZYLBENZENE DERIVATIVES AND METHODS OF USE

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

Aminobenzoxazoles as therapeutic agents

A compound of Formula (I), wherein the substituents are as defined herein, which are useful as kinase inhibitors.