Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
    11.
    发明授权
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 失效
    吡喃葡萄糖氧基苄基苯衍生物,含有它们的药物组合物及其制备中间体

    公开(公告)号:US07129381B2

    公开(公告)日:2006-10-31

    申请号:US10978413

    申请日:2004-11-02

    CPC分类号: C07H15/203

    摘要: The present invention relates to glucopyranosyl-oxybenzylbenzene derivatives represented by the general formula: wherein R1 represents 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.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents 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.

    摘要翻译: 本发明涉及由以下通式表示的吡喃葡萄糖基 - 氧苄基苯衍生物:其中R 1表示氢原子,羟基,取代或未取代的氨基,氨基甲酰基,取代或未取代的( 低级烷基)基团,取代或未取代的(低级烷氧基)基团等; R 2表示氢原子或低级烷基; 和R 3表示取代或未取代的(低级烷基)基团,取代或未取代的(低级烷氧基)基团,取代或未取代的(低级烷硫基)等,或其药学上可接受的盐,其中 在人SGLT2中具有抑制活性,并且可用作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,包含其的药物组合物及其中间体。

    PURINE NUCLEOSIDE DERIVATIVE MODIFIED IN 8-POSITION AND MEDICAL USE THEREOF
    12.
    发明申请
    PURINE NUCLEOSIDE DERIVATIVE MODIFIED IN 8-POSITION AND MEDICAL USE THEREOF 失效
    嘌呤核苷衍生物8位置修饰及其医疗用途

    公开(公告)号:US20100249054A9

    公开(公告)日:2010-09-30

    申请号:US11717741

    申请日:2007-03-13

    IPC分类号: A61K31/7076 C07H19/16

    摘要: 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; RA is a hydrogen atom or a hydroxyl group; R1 is 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 R2 to R4, P1 and Q represents a halogen atom, a cyano group or the like.

    摘要翻译: 本发明提供了可用于与血浆尿酸水平异常相关的疾病的8-修饰的嘌呤核苷衍生物。 由下式(I)表示的8-修饰的嘌呤核苷衍生物,其前体药物或其药学上可接受的盐或其水合物或溶剂合物可用于预防或治疗痛风,高尿酸血症,尿结石病,高尿酸性肾病或 类似。 在该式中,n为1或2; RA是氢原子或羟基; R1是氢原子,羟基,硫醇基,氨基或氯原子; 环J表示任选取代的2-萘基,或由以下通式(II)表示的基团,其中Y表示单键或连接基团; 环Z表示任选取代的芳基或杂芳基等; R2和R4,P1和Q表示卤原子,氰基等。

    Pyrazole derivative, medicinal composition containing the same, medicinal use thereof and intermediate in producing the same
    17.
    发明申请
    Pyrazole derivative, medicinal composition containing the same, medicinal use thereof and intermediate in producing the same 失效
    吡唑衍生物,含有该吡唑衍生物的药物组合物,其药学用途及其制造中间体

    公开(公告)号:US20060128635A1

    公开(公告)日:2006-06-15

    申请号:US10529895

    申请日:2003-09-30

    IPC分类号: A61K31/7052 C07H17/02

    摘要: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group selected from the following groups: and the other represents —(CH2)n—Ar wherein Ar represents an optionally substituted C6-10 aryl group or an optionally substituted C1-9 heteroaryl group; and n represents an integral number from 0 to 2, an optionally substituted C1-6 alkoxyl group, an optionally substituted amino group, an optionally substituted C2-9 heterocycloalkyl group or an optionally substituted heterocycle-fused phenyl group; R represents an optionally substituted C3-8 cycloalkyl group, an optionally substituted C6-10 aryl group etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human 1,5-anhydroglucitol/fructose/mannose transporter and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose or a disease associated with hyperglycemia (e.g., diabetic complications, diabetes, etc.), and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.

    摘要翻译: 本发明提供由以下通式表示的吡唑衍生物:其中R 1表示H,任选取代的C 1-6烷基等; Q和T之一表示选自以下基团的基团:另一个表示 - (CH 2)n Ar -Ar其中Ar表示任选取代的C 1 -C 6烷基, 6-10芳基或任选取代的C 1-19杂芳基; 并且n表示0至2的整数,任选取代的C 1-6烷氧基,任选取代的氨基,任选取代的C 2-9杂环烷基 或任选取代的杂环稠合的苯基; R表示任选取代的C 3-8环烷基,任选取代的C 6-10芳基等,其药学上可接受的盐或其前药,其表现出优异的 在人1,5-脱水葡萄糖醇/果糖/甘露糖转运蛋白中的抑制活性,并且可用作预防,抑制与至少一种选自葡萄糖,果糖和甘露糖的碳水化合物过量摄取相关的疾病进展或治疗的药剂 或与高血糖相关的疾病(例如,糖尿病并发症,糖尿病等),以及包含该疾病的药物组合物,其药学用途和用于生产的中间体。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
    18.
    发明授权
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 失效
    吡喃葡萄糖氧基苄基苯衍生物,含有它们的药物组合物及其制备中间体

    公开(公告)号:US07053060B2

    公开(公告)日:2006-05-30

    申请号:US10432905

    申请日:2001-11-20

    CPC分类号: C07H15/203

    摘要: The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein R1 represents 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.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents 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.

    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,羟基,取代或未取代的氨基,氨基甲酰基,取代或未取代的(低级烷基 )基团,取代或未取代的(低级烷氧基)基团等; R 2表示氢原子或低级烷基; 和R 3表示取代或未取代的(低级烷基)基团,取代或未取代的(低级烷氧基)基团,取代或未取代的(低级烷硫基)等,或其药学上可接受的盐,其中 在人SGLT2中具有抑制活性,并且可用作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,包含其的药物组合物及其中间体。

    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
    20.
    发明申请
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof 失效
    吡喃葡萄糖氧基苄基苯衍生物,含有它们的药物组合物及其制备中间体

    公开(公告)号:US20050059614A1

    公开(公告)日:2005-03-17

    申请号:US10978413

    申请日:2004-11-02

    CPC分类号: C07H15/203

    摘要: The present invention relates to glucopyranosyl-oxybenzylbenzene derivatives represented by the general formula: wherein R1 represents 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.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents 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.

    摘要翻译: 本发明涉及由以下通式表示的吡喃葡萄糖基 - 氧苄基苯衍生物:其中R 1表示氢原子,羟基,取代或未取代的氨基,氨基甲酰基,取代或未取代的(低级烷基) 取代或未取代的(低级烷氧基)等。 R 2表示氢原子或低级烷基; 和R 3表示具有抑制活性的取代或未取代的(低级烷基)基团,取代或未取代的(低级烷氧基)基团,取代或未取代的(低级烷硫基)等,或其药学上可接受的盐 人SGLT2,并且可用作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,包含其的药物组合物及其中间体。