Kissei Pharmaceutical Co., Ltd.

Toshihiro Nishimura

Hideki Fujikura

Masayuki Isaji

Nobuhiko Fushimi

Kenji Katsuno

Kazuya Tatani

Takeshi Nakabayashi

Masahiro Hiratochi

Minoru Fujioka

Akira Iyobe

Norihiko Kikuchi

Yasunori Ueno

Kiyoshi Kasai

Masako Yoshida

Yoshimitsu Komatsu

Masahiro Kobayashi

Takashi Miyagi

Hirotaka Teranishi

Yoshiki Tokutake

A problem of the present invention is to provide a new compound which has NKreceptor antagonist activity, and thus is useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. A compound represented by the formula (I): wherein W represents a fluorine atom and the like, ring A represents a cycloalkyl and the like, Xrepresents CH or N, R represents methyl and the like, Y represents 0 to 2, U, Uand Ueach independently represents a single bond and the like, or a pharmaceutically acceptable salt thereof. The compounds of the present invention or pharmaceutically acceptable salts thereof have an excellent NKreceptor antagonist activity, and thus are also useful as an agent for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting.

NK1 receptor antagonist

[Problem] To provide a novel compound that exhibits an agonistic effect on dopamine Dreceptors. [Solution] The present invention provides a compound represented by the general formula (I): in which Ris Calkyl or the like; Ris hydrogen or the like; Rand Rare each hydrogen, Calkyl, RRN&#x2014;Calkyl, aralkyl, or the like; Rand Rare hydrogen or the like; and Ris hydrogen or the like, or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same and uses for said compound/salt and composition. The compounds of the present invention exhibit potent dopamine Dreceptor simulating activities and thus are useful as a treating or preventing agent for Parkinson's disease and the like.

[object Object]

The present invention provides compounds represented by the general formula (I): or pharmaceutical acceptable salts thereof, wherein Ris cyano or the like; Rand Rare hydrogen or the like; Ris Calkyl or the like; Ris Calkyl, halo-Calkyl, cycloalkyl, cycloalkyl-Calkyl, aralkyl or the like; Rand Rare each hydrogen, Calkyl, halo-Calkyl, cycloalkyl, Calkoxy-Calkyl, RRN&#x2014;Calkyl or the like, which exhibit potent dopamine Dreceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof. 

Octahydrothienoquinoline derivative, pharmaceutical composition comprising derivative, and use of these

The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; Rrepresents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

Glucopyranosyloxypyrazole derivatives and use thereof in medicines

The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein Xrepresents N or CR; Xrepresents N or CR; Xrepresents N or CR; Xrepresents N or CR; and with the proviso that one or two of Xto Xrepresent N; R represents optionally substituted Ccycloalkyl, optionally substituted Caryl, etc.; Rto Rrepresent H, a halogen atom, etc.) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an excellent 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 complications, obesity or the like, pharmaceutical compositions comprising the same, and medicinal uses thereof.

Nitrogen-containing heterocyclic derivatives, medicinal compositions containing the same and medicinal use 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 glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula:(wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; Rrepresents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLTand have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula:(wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; Rrepresents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R, Rand Rrepresent a hydrogen atom or a halogen atom; Rrepresents a lower alkyl group or a halo(lower alkyl) group; and Rrepresents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, etc., a pharmaceutically acceptable salt thereof or a prodrug thereof., which exert an excellent 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, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.

Glucopyranosyloxypyrazole derivatives and medicinal use thereof

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 provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein one of Q and T represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; Rrepresents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; Rrepresents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., which exert an excellent 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, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.

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 glucopyranosyloxypyrazole derivatives represented by the general formula: wherein Rrepresents a hydrogen atom or a lower alkyl group; one of Qand Trepresents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and Rrepresents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

Growing community of inventors

Nagano, Japan

Toshihiro Nishimura