1
wherein
when Y is
2
or heteroaryl;
A is —O(CH
2
)
m
, S, —NH(CH
2
)
m
, or (CH
2
)
n
where n is 0-3 and m is 0-2;
and R
1
to R
6
are as defined herein.
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 one, two or more other antidiabetic agents, and/or one, two or more hypolipidemic agents.
The present invention provides a 1-thio-D-glucitol compound of the following formula, which shows the action of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt of the compound, or a hydrate of the compound or the salt; and a pharmaceutical comprising such a compound as an active ingredient, especially, a pharmaceutical for preventing or treating diabetes, diabetes-related disease, or diabetic complication. The invention also provides a method for producing the 1-thio-D-glucitol compound and its intermediate.
Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives
申请人:Fujikura Hideki
公开号:US20050080022A1
公开(公告)日:2005-04-14
The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula:
wherein R
1
represents a hydrogen atom or a hydroxy(lower alkyl) group; and R
2
represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a hydroxy(lower alkyl) group, a hydroxy(lower alkoxy) group, a hydroxy(lower alkylthio) group etc., and salts thereof, which have an excellent inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, obesity etc., and intermediates thereof.
Process for selective production of aryl 5-thio-beta-d- aldohexopyranosides
申请人:Sato Masakazu
公开号:US20050256317A1
公开(公告)日:2005-11-17
The present invention provides a method for preparing an aryl 5-thio-β-D-aldohexopyranoside derivative of Formula (III), which comprises reacting a 5-thio-D-aldohexopyranose derivative of Formula (I) with Ar—OH of Formula (II) in the presence of a phosphine represented by PR
11
R
12
R
13
and an azo reagent represented by R
21
—N═N—R
22
in accordance with the following scheme.
Aryl 5-thio-beta-d-glucopyranoside derivatives and remedies for diabetes containing the same
申请人:Sato Masakazu
公开号:US20050209309A1
公开(公告)日:2005-09-22
There is provided a 5-thio-β-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, particularly a prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which comprises such a compound as an active ingredient.