摘要:
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; R2 represents 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.
摘要翻译:本发明提供由以下通式表示的吡喃葡萄糖氧吡唑衍生物:其中R表示氢原子,低级烷基或形成前药的基团; Q和T表示由以下通式表示的基团:(其中P表示 氢原子或形成前药的基团),而另一个表示低级烷基或卤代(低级烷基)基团; R 2表示氢原子,低级烷基,低级烷氧基,低级烷硫基,卤代(低级烷基)或卤素原子; 并且条件是当R表示氢原子或低级烷基时,P不表示氢原子,或其药学上可接受的盐,其在人SGLT2中具有抑制活性并具有改善的口服吸收,因此可用作 用于预防或治疗与高血糖相关的疾病如糖尿病,糖尿病并发症或肥胖症的药剂及其药学上可接受的盐及其药学用途。
摘要:
The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a hydroxy(lower alkyl) group; and R2 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.
摘要翻译:本发明涉及由以下通式表示的吡喃葡萄糖氧基苄基苯衍生物:其中R 1表示氢原子或羟基(低级烷基); R 2表示低级烷基,低级烷氧基,低级烷硫基,羟基(低级烷基),羟基(低级烷氧基),羟基(低级烷硫基)等,及其盐 ,其在人SGLT2中具有优异的抑制活性,并且可用作预防或治疗糖尿病,肥胖症等及其中间体的药剂。
摘要:
The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a hydroxy(lower alkyl) group; and R2 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.
摘要:
The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 and X3 independently represent N or CH; X2 represents N or CR2; X4 represents N or CR3; and with the proviso that one or two of X1, X2, X3 and X4 represent N; R1 represents 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; R2 represents 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 R3 represents 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.
摘要翻译:本发明提供由以下通式表示的含氮杂环衍生物:其中X 1和X 3独立地表示N或CH; X 2表示N或CR 2; X 4表示N或CR 3; 并且条件是X 1,X 2,X 3和X 4中的一个或两个表示N; R 1表示氢原子,卤素原子,低级烷基,低级烷氧基,低级烷硫基,低级烷氧基取代的(低级烷基),低级烷氧基取代的(低级烷氧基) 低级烷氧基(低级烷氧基) - 取代(低级烷基)基团,环状低级烷基,卤代(低级烷基)基团或由通式HO-A表示的基团:其中A表示低级亚烷基, 低级亚烷基氧基或低级亚烷基硫基; R 2表示氢原子,卤素原子,低级烷基,环状低级烷基,低级烷氧基,氨基,(低级酰基)氨基,单(低级烷基)氨基或 二(低级烷基)氨基; R 3表示可用作预防或治疗与糖尿病,糖尿病并发症或肥胖症等高血糖症相关疾病的药剂的氢原子或低级烷基或其药学上可接受的盐或其前体药物,药物 含有它们的组合物,及其制药用途和生产中间体。
摘要:
A first pictorial communication apparatus for transmitting and receiving a pictorial signal and a sound signal through a first channel and a control message through a second channel, having a line interface for communicating with ISDN, a video codec portion for coding and decoding of the pictorial signal, a key input portion and a camera, further comprises a character storing portion for storing character codes in corporation with the key input portion, a data conversion portion for converting character data train read from the character storing portion into a character video signal. On arrival of a call in an automatic answering mode, the character data train is read and transmitted through the first channel in place of a video signal from the camera after the conversion. The second apparatus has similar structure. A called second apparatus transmits the character code data train included in the control message through the second channel in the automatic answering mode on the arrival of call without the conversion. The called apparatus detects the character code data train from the control message and indicates the character code data train as an answering message after conversion by the data conversion portion.
摘要:
An evaluation method of respiration and heart beat and its apparatus which permits one to forecast sudden infant death syndrome by investigating correlation between respiration and heart beat in the normal state and sleep-apnea of a newborn.
摘要:
An improved silica-based film-forming composition for diffusion of antimony in the doping works of semiconductors is proposed which comprises an organic solvent, a partial hydrolysis product of an alkoxy silane compound and an antimony compound dissolved in the organic solvent. The antimony compound in the inventive composition is an alkoxy antimony or aryloxy antimony compound so that the problem of corrosion of the coating apparatus can be entirely avoided without decreasing the dopant concentration in the semiconductor substrate, as well as to provide a film-forming composition which is advantageously stable in storage.
摘要:
Liquid compositions suitable for providing silica-based coating films on to various substrate surfaces are prepared by the reaction of an alkoxy-containing silane, a lower carboxylic acid and an alcohol in the presence of a reaction accelerator which is an organic acid different from the above mentioned lower carboxylic acid. The reaction proceeds very smoothly even in the absence of any halogen-containing compounds, and the resultant liquid coating compositions are free from the problem of corrosion due to the presence of a halogen-containing ingredient.
摘要:
A liquid coating composition for formation of a transparent conductive film, which comprises a solution of indium nitrate in a .beta.-diketone or a mixture of a .beta.-diketone and another organic solvent or a reaction product of indium nitrate with a .beta.-diketone, an activator and an organic solvent other than a .beta.-diketone, is disclosed.When this coating composition is coated on a substrate and the coated substrate is heat-treated at a temperature higher than about 350.degree. C., there can be obtained a transparent conductive film having excellent transparency, electrical conductivity and mechanical strength.
摘要:
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; R2 represents 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.