Background: A critical factor for maintenance of glucose balance is the renal recovery of glucose from the glomerular filtrate mediated primarily by sodium glucose co-transporter 2 (SGLT2). This capacity can be modulated by SGLT2 inhibitors thereby providing a unique insulin independent method of treatment of diabetes. Objective/method: A discussion of the evolution of SGLT inhibitors as inferred from patents published from 2005 to 2009 is prefaced by a brief review of the role of SGLT in glucose transport and the clinical findings illustrating the therapeutic potential of SGLT inhibitors as anti-diabetic agents. These compounds comprise O, C and N-glycosides generated by attachment of an appropriate lipophilic aglycone component to a suitable glucose analogue. Conclusion: The realization that the in vivo potency of O-glucosides was markedly less than that of C-glucosides necessitated a shift in medicinal chemistry focus of the pharmaceutical companies pursuing SGLT2 inhibitors. Particular emphasis is pla...

Evolution of sodium glucose co-transporter 2 inhibitors as anti-diabetic agents.

The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments.

Uses of DPP-IV inhibitors

Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).

Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives

The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.

Process for the preparation of compounds useful as inhibitors of sglt

The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof. The compound or a salt thereof or a prodrug thereof has a GPR40 receptor function modulating action and is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

Fused cyclic compounds

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.

1-thio-d-glucitol derivatives

Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action. A C-phenyl glycitol compound represented by Formula (I) below or a pharmaceutically acceptable salt thereof or a hydrate thereof wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, R3 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, Y is a C1-6 alkylene group, -O-(CH2)n- (n is an integer of 1 to 4) or a C2-6 alkenylene group, provided that when Z is NHC(= NH)NH2 or -NHCON(RB)RC, n is not 1, Z is -CONHRA, -NHC(=NH)NH2 or -NHCON(RB)RC, Formula (A) or Formula (B).

C-phenyl glycitol compound for the treatment of diabetes

A C-phenyl 1-thioglucitol compound represented by the formula (I), a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the pharmaceutically acceptable salt. (I) wherein X represents a hydrogen atom or a C1-6 alkyl group; Y represents a C1-6 alkylene group or ~O-(CH2)n- (n represents an integer ranging from 1 to 5); and Z represents ~CONHRA or ~NHCONHRB (provided that, when Z represents ~NHCONHRB, n is not 1), where RA represents a C1-6 alkyl group substituted by 1 to 3 groups independently selected from a hydroxyl group and ~CONH2; and RB represents a hydrogen atom or a C1-6 alkyl group substituted by 1 to 3 groups independently selected from a hydroxyl group and ~CONH2. The compound, the salt or the solvate can inhibit the SGLT1 activity to prevent the absorption of glucose or the like, or can inhibit both the SGLT1 activity and the SGLT2 activity to prevent the absorption of glucose or the like and excrete a urine sugar, and is therefore useful as a prophylactic or therapeutic agent for diabetes.

C-phenyl 1-thioglucitol compound

Disclosed is a 1-phenyl 1-thio-D-glucitol compound having the formula (I) or the like, a pharmaceutically acceptable salt thereof, a hydrate of the compound or the pharmaceutically acceptable salt, or a pharmaceutical agent comprising the compound, the pharmaceutically acceptable salt or the hydrate as an active ingredient, which can inhibit both the activities of SGLT1 and SGLT2 and has both of an effect of inhibiting the absorption of glucose through a digestive tract and an urinary glucose excretion effect, and therefore is useful as a new type of prophylactic or therapeutic agent for diabetes, a diabetes-related disease or a diabetic complication.

1-phenyl 1-thio-d-glucitol derivative

The object is to provide a novel phenyl 5-thioglucoside compound which can control IGT (impaired glucose tolerance) by inhibiting the SGLT1 activity and inhibiting the absorption of glucose through a digestive tract. Provided is a phenyl 5-thioglucoside compound represented by the formula (I), a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the salt. (I) wherein R1 and R2 independently represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom; Z represents –NHSO2-phenyl, -NHSO2NH2 or –Y-Q; Y represents a single bond, a C1-6 alkylene group or an alkenylene group; and Q represents –NHC(=NH)NH2, -NHCON(RA)RB, -CONH(RC) or a 4- to 6-membered heterocycloalkyl group substituted by at least one member selected from a C1-6 alkyl group and an oxo group (the heterocycloalkyl group may be fused with a phenyl group).

Phenyl 5-thio glycoside compound

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