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。
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:
The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.
摘要:
The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.
摘要:
The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.
摘要翻译:本发明涉及由以下通式表示的5-脒基-2-羟基苯磺酰胺衍生物:其中R 1是氢原子或任选取代的低级烷基; R 2是二(低级烷基)氨基,低级烷基,环烷基,任选取代的芳基,任选取代的杂环烷基或任选取代的芳族杂环基; T是氧原子,硫原子,磺酰基等; Q是氢原子或任意取代的低级烷基; Z是氢原子,羟基等,或其药学上可接受的盐,其具有有效和选择性的活化凝血因子X抑制活性,并且可用作预防或治疗疾病的药剂, 活化凝血因子X,包含其的药物组合物,其药物用途及其中间体。
摘要:
The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.
摘要翻译:本发明涉及由以下通式表示的5-脒基-2-羟基苯磺酰胺衍生物:其中R 1是氢原子或任选取代的低级烷基; R 2是二(低级烷基)氨基,低级烷基,环烷基,任选取代的芳基,任选取代的杂环烷基或任选取代的芳族杂环基; T是氧原子,硫原子,磺酰基等; Q是氢原子或任意取代的低级烷基; Z是氢原子,羟基等,或其药学上可接受的盐,其具有有效和选择性的活化凝血因子X抑制活性,并且可用作预防或治疗疾病, 活化凝血因子X,包含其的药物组合物,其药物用途及其中间体。
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:
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。
摘要:
The present invention provides a compound represented by general formula (I): or pharmaceutically acceptable salts thereof, wherein W is O, S(O)m, CH2 and the like; R1 is halogen, lower alkyl, halo-lower alkyl, CN and the like; R3 is hydrogen and the like; R4 is hydrogen, halogen, alkyl, halo-lower alkyl, substituted alkyl, aryl, aralkyl, alkoxy, substituted alkoxy, alkanoyl, aroyl, —CONR7(R8), —S(O)mR9, —SO2NR7(R8) and the like; R5 is hydrogen, halogen, alkyl, substituted alkyl and the like; A is —N(R6)CO-A1-COR10 and the like; pharmaceutical compositions containing them and their uses, which have a high affinity to human thyroid hormone receptors, in particular human thyroid hormone receptor β.
摘要翻译:本发明提供由通式(I)表示的化合物或其药学上可接受的盐,其中W为O,S(O)m,CH 2等 ; R 1是卤素,低级烷基,卤代低级烷基,CN等; R 3是氢等; R 4是氢,卤素,烷基,卤代低级烷基,取代的烷基,芳基,芳烷基,烷氧基,取代的烷氧基,烷酰基,芳酰基,-CONR 7 S(O)m R 9,-SO 2 NR 7,S(O) (R 8 S 8)等; R 5是氢,卤素,烷基,取代的烷基等; A是-N(R 6)CO-A 1 -COR 10等; 含有它们的药物组合物及其用途,其对人甲状腺激素受体,特别是甲状腺激素受体β具有高亲和力。
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。