摘要:
The present invention is 3,4-disubstituted-benzo[b]thiophene derivatives represented by general formula (I) and processes for preparing compounds represented by general formula (V) from compounds represented by general formula (IV), preparing a mixture of compounds represented by the following formula (II) and the following formula (III) and preparing the benzo[b]thiophene derivatives represented by the above formula (I): wherein, R1 and R2 represent each a halogen atom, a trihalomethyl group, a C1-4 alkyl group or a C1-4 alkoxy group; X represents a hydroxy group or a halogen atom; R3 and R4 represent each a hydrogen or a halogen atom, a trihalomethyl group, a C1-4 alkyl group or a C1-4 alkoxy group; and R5 represents a C1-3 alkyl group or a trifluoromethyl group.
摘要翻译:本发明是由通式(I)表示的3,4-二取代 - 苯并[b]噻吩衍生物和由通式(Ⅳ)表示的化合物制备由通式(Ⅴ)表示的化合物的方法,制备化合物 由下式(II)和下式(III)表示并制备由上式(I)表示的苯并[b]噻吩衍生物:其中R 1和R 2 代表卤素原子,三卤代甲基,C 1-4烷基或C 1-4烷氧基; X表示羟基或卤素原子; R 3和R 4各自表示氢或卤素原子,三卤代甲基,C 1-4烷基或C 1-4烷基, C 1-4烷氧基; R 5表示C 1-3烷基或三氟甲基。
摘要:
The present invention is a method of producing a 3-hydroxymethyl-benzo[b]thiophene derivative without the possible concomitant formation of isomers, which comprises selectively cyclizing a sulfoxide having X shown in the reaction scheme below: wherein R1 to R3 are, same or independently, a hydrogen atom, an alkyl group having 1 to 4 carbons, a trihalomethyl group, an alkoxy group having 1 to 4 carbons, an alkylthio group having 1 to 4 carbons, or a trihalomethoxy group; R4 is an acyl group; X is a halogen atom, a hydroxy group, an amino group, a mercapto group, an alkylthio group having 1 to 9 carbons, an acyloxy group having 1 to 9 carbons, an acylamino group having 1 to 9 carbons, or a trihalomethoxy group.
摘要:
A benzimidazole derivative or its medically acceptable salt, represented by the following formula (1), that is a human chymase activity inhibitor capable of being applied clinically: wherein, R1 and R2 represent a hydrogen atom, an alkyl group or an alkoxy group, etc., A represents an alkylene group or an alkenylene group, E represents —COOR3, —SO3R3, —CONHR3 or —SO2NHR3, etc., G represents an alkylene group, M represents a single bond or —S(O)m—, J represents a heterocyclic group, and X represents —CH═ or a nitrogen atom.
摘要:
The present invention is a thiobenzimidazole derivative represented by the following formula (1) or a medically acceptable salt thereof wherein said thiobenzimidazole derivative and a medically acceptable salt thereof have a potent activity of inhibiting human chymase. Thus, they are potential preventive and/or therapeutic agents clinically applicable to various diseases in which human chymase is involved.
摘要:
The present invention provides acid salts, such as sulfate, hydrochloride, and methanesulfonate, of 4-(1-((4-methylbenzothiophen-3-yl)methyl)benzimidazol-2-ylthio)butanoic acid and the crystals thereof. These benzimidazole derivatives and the crystals thereof have an in vivo chymase inhibitory activity and can be used as a preventive or therapeutic agent for inflammatory diseases, allergic diseases, respiratory diseases, circulatory diseases, or bone/cartilage metabolic diseases.
摘要:
Various crystal forms of 4-(1-((4-methylbenzothiophen-3-yl)methyl)benzimidazol-2-ylthio)butanoic acid from a solvent, and a process for production thereof are provided.
摘要:
Various crystal forms of 4-(1-((4-methylbenzothiophen-3-yl)methyl)benzimidazol-2-ylthio)butanoic acid from a solvent, and a process for production thereof are provided.
摘要:
It is an object of the present invention to provide drugs which are effective for treatment of hypertension, cardiac disease (cardiac hypertrophy, cardiac failure, myocardial infarction, etc.), cerebral apoplexy, nephritis and the like. The invention also provides circulatory disease treatment agents in forms that allow combined use of chymase inhibitors and ACE inhibitors, and circulatory disease treatment methods which produce simultaneous chymase inhibition and ACE inhibition.
摘要:
Systems, methods, and programs for updating map data create differential data in a server by comparing an old version of map data stored in the server with a new version of map data and transmit the differential data from the server to a relay device. The systems, methods and programs create updated map data by combining the differential data received from the server with map data previously stored in the relay device. The relay device may then be connected to an updated data storing device that disconnectably connects to both the relay device and the navigation system. The systems, methods, and programs, may then transfer the updated map data from the relay device to the updated data storing device and from the updated data storing device to the navigation system.
摘要:
The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.