Kissei Pharmaceutical Co., Ltd.

Kyorin Pharmaceutical Co., Ltd.

Kazuya Tatani

Masayuki Isaji

Hideki Fujikura

Nobuhiko Fushimi

Toshihiro Nishimura

Norihiko Kikuchi

Kenji Katsuno

Tatsuhiro Kondo

Atsushi Kondo

Naohiro Kawamura

Yasushi Kohno

Masahiro Hiratochi

Shigeki Seto

Yoshinori Nonaka

Takashi Miyagi

Kazuo Shimizu

Shigeru Yonekubo

Hirotaka Teranishi

Takeshi Nakabayashi

Akira Iyobe

Minoru Fujioka

Yu Kuramochi

Yoshiki Tokutake

The present invention provides a compound represented by the general formula (I) of the present invention, which has EPreceptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Yrepresents a Calkylene group or the like; Yrepresents a single bond or the like; Z represents &#x2014;C(&#x2550;O)&#x2014;NHSOR, an acidic 5-membered hetero ring group, or the like; Rrepresents a hydrogen atom or the like; Rrepresents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; Rrepresents a halogen atom, a Calkoxy group, or the like; Rrepresents a hydrogen atom, a halogen atom, or the like; Rrepresents a hydrogen atom or the like; and Rrepresents a Calkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

Indole derivative and pharmacologically acceptable salt thereof

The present invention provides a compound represented by the general formula (I) of the present invention, which has EPreceptor antagonism: wherein A represents a pyridine ring, a furan ring, or the like; Yrepresents a Calkylene group; Yrepresents a single bond or the like; Rrepresents &#x2014;C(&#x2550;O)&#x2014;NH&#x2014;SOR, an acidic 5-membered hetero ring group, or the like; Rrepresents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; Rrepresents a halogen atom, a Calkoxy group, or the like; Rrepresents a hydrogen atom, a halogen atom, or the like; Rrepresents a hydrogen atom or the like; and Rrepresents a Calkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

Indole derivative, and pharmacologically acceptable salt thereof

A compound (I) of the present invention, which has an EPreceptor antagonism: 

Indole derivative or pharmaceutically acceptable salt thereof

The present invention provides an 8-modified purinenucleoside derivative which is useful for diseases associated with an abnormality of plasma uric acid level. An 8-modified purinenucleoside derivative represented by the following formula (I), a prodrug thereof or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, is useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; Ris a hydrogen atom or a hydroxyl group; Ris a hydrogen atom, a hydroxyl group, a thiol group, an amino group or a chlorine atom; ring J represents an optionally substituted 2-naphthyl group, or a group represented by the following general formula (II) wherein Y represents a single bond or a connecting group; ring Z represents an optionally substituted aryl group or heteroaryl group or the like; and Rto R, Pand Q represents a halogen atom, a cyano group or the like. 

Purine nucleoside derivative modified in 8-position and medical use thereof

The present invention provides benzimidazole derivatives represented by the following formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an inhibitory activity on sodium-dependent nucleoside transporter 2 and are useful for a disease associated with an abnormality of plasma uric acid level. The compounds of the present invention are useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; Rand Rare H, a halogen atom, cyano group, optionally substituted alkyl group, optionally substituted aryl group or the like; Ris H, a halogen atom, optionally substituted alkyl group or the like; Rand Rare H, a halogen atom, OH or the like; and Rand Rare H or OH: Ris F or OH. 

Benzimidazole derivatives and medical uses thereof

The present invention provides glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein P represents a hydrogen atom or a group forming a prodrug; Rrepresents a hydrogen atom, an optionally substituted amino group, a carbamoyl group, an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, etc.; Rrepresents a hydrogen atom or a lower alkyl group; and Rrepresents an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkylthio group, etc., which have an improved oral absorption, and exert an inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, or pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

Glucopyranosyloxybenzylbenzene derivatives and medicinal use thereof

The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein Rrepresents a hydrogen atom or a hydroxy(lower alkyl) group; and Rrepresents 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.

Glucopyranosyloxy benzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives

The present invention provides crystals of 2-(4-methoxybenzyl)phenyl 6-O-ethoxycarbonyl-&#x3b2;-D-glucopyranoside, pharmaceutical compositions containing the same and their uses, which exhibit excellent SGLT2 inhibitory activities, and are useful for treating or preventing diseases associated with hyperglycemia.

Crystals of glucopyranosyloxybenzyl benzene derivative

The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein Xand Xindependently represent N or CH; Xrepresents N or CR; Xrepresents N or CR; and with the proviso that one or two of X, X, Xand Xrepresent N; Rrepresents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted (lower alkoxy) group, a lower alkoxy(lower alkoxy)-substituted (lower alkyl) group, a cyclic lower alkyl group, a halo(lower alkyl) group or a group represented by the general formula: HO-A- wherein A represents a lower alkylene group, a lower alkyleneoxy group or a lower alkylenethio group; Rrepresents a hydrogen atom, a halogen atom, a lower alkyl group, a cyclic lower alkyl group, a lower alkoxy group, an amino group, a (lower acyl)amino group, a mono(lower alkyl)amino group or a di(lower alkyl)amino group; and Rrepresents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, or prodrugs thereof which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses and production intermediates thereof.

Nitrogenous heterocyclic derivatives, medicinal compositions containing the same, medicinal uses thereof, and intermediates therefor

The present invention relates to glucopyranosyl-oxybenzylbenzene derivatives represented by the general formula: wherein Rrepresents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group etc.; Rrepresents a hydrogen atom or a lower alkyl group; and Rrepresents a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group, a substituted or unsubstituted(lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.

Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof

The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein Rrepresents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted (lower alkyl) group, a substituted or unsubstituted (lower alkoxy) group etc.; Rrepresents a hydrogen atom or a lower alkyl group; and Rrepresents a substituted or unsubstituted (lower alkyl) group, a substituted or unsubstituted (lower alkoxy) group, a substituted or unsubstituted (lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.

The present invention relates to benzylphenol derivatives represented by the general formula: 

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Nagano, Japan

Kazuya Tatani