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:
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 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 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 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:
A heat treatment operation can be executed, suppressing a wave-shaped deformation at a non heat-treatment region of an article to be heat treated. To an elongated-shaped article to be heat treated (10) to which a raised portion (11) extending in the longitudinal direction is formed, a hardening region as being a heat-treated region defined to be extended in a longitudinal direction at a part of the raised portion (11) and a non-hardening region as being non heat-treated region defined to be extended in the longitudinal direction at flange portion (13) and other parts of the raised portion (11) are arranged side by side in a width direction orthogonal to the longitudinal direction. The flange portion (13) is clamped by a first and a second clamping means (22), (23) arranged in the longitudinal direction, and one first clamping means (22) is a tight clamping means holding fixedly the flange portion (13) and a plurality of second clamping means (23) are loose clamping means clamping loosely the flange portion (13), allowing the article to be heat treated (10) to be convex on the side of the heated hardening region.