摘要:
An object of the invention is to find out intermediates usful for the synthesis of pyrazol-fused ring derivatives (such as 7-phenylpyrazolo[1,5-a]pyridine derivatives) and a method for producing the same. A method for producing compound represented by the general formula (II), wherein Z1 and Z2 each independently represents a methine group or a nitrogen atom; R1 represents an ethyl group or the like; R5 represents a hydrogen atom or the like; R2 and R3 each independently represents a C1-6 alkyl group or the like, salts thereof, or solvates of both, comprising the step of: reacting a compound represented by the general formula (I), wherein Z1, Z2, R5, R1, R2 and R3 each has the same definition as described above, with an organometallic reagent; and then reacting the resulting product with pentafluoroiodobenzene.
摘要翻译:本发明的目的是找出有用于合成吡唑稠合环衍生物(如7-苯基吡唑并[1,5-a]吡啶衍生物)的中间体及其制备方法。 由通式(II)表示的化合物,其中Z 1和Z 2各自独立地表示次甲基或氮原子的方法; R 1表示乙基等; R 5表示氢原子等; R 2和R 3各自独立地表示C 1-6烷基等,其盐或两者的溶剂合物,包括 步骤:使通式(I)表示的化合物,其中Z 1,Z 2,R 5,R 5, 1,R 2和R 3各自具有与上述相同的定义与有机金属试剂; 然后使所得产物与五氟碘苯反应。
摘要:
Intermediates useful for the synthesis of pyrazole-fused ring derivatives, such as 7-phenylpyrazolo [1,5-a]pyridine derivatives, and method for producing the same. Method for producing compound represented by the general formula (II), wherein Z1 and Z2 each independently represents a methine group or a nitrogen atom; Rl represents an ethyl group or the like; R5 represents a hydrogen atom or the like; R2 and R3 each independently represents a C1-6 alkyl group or the like, salts thereof, or solvates of both, comprising the step of: reacting a compound represented by the general formula (I), wherein Z1, Z2, R5, R1, R2 and R3 each has the same definition as described above, with an organometallic reagent; and then reacting the resulting product with pentafluoroiodobenzene.
摘要翻译:用于合成吡唑稠合环衍生物如7-苯基吡唑并[1,5-a]吡啶衍生物的中间体及其制备方法。 制备由通式(II)表示的化合物的方法,其中Z1和Z2各自独立地表示次甲基或氮原子; R1表示乙基等; R5表示氢原子等; R 2和R 3各自独立地表示C 1-6烷基等,其盐或两者的溶剂合物,包括以下步骤:使通式(I)表示的化合物与其反应,其中Z1,Z2,R5,R1, R2和R3各自具有与上述相同的定义,与有机金属试剂; 然后使所得产物与五氟碘苯反应。
摘要:
The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action.That is, it provides a novel condensed imidazole compound which has an adenosine A2 receptor antagonist action, is effective for preventing or treating diabetes mellitus and diabetic complications, and is represented by the formula (I); (wherein R1 represents e.g. an amino group which may be substituted with an alkyl group; R2 represents e.g. hydrogen atom, an alkyl group, a cycloalkyl group or an alkyl group, alkenyl group or alkynyl group which may be substituted with hydrox etc.; R3 represents e.g. an optionally substituted alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, pyridinone group, pyrimidinone group or piperadinone group; Ar represents e.g. an optionally substituted aryl or heteroaryl group; and Q and W are the same as or different from each other and each represents N or CH), a pharmacologically acceptable salt or hydrates thereof.
摘要翻译:本发明提供了一种基于腺苷A2受体拮抗剂作用的新型糖尿病和糖尿病并发症的预防或治疗剂。即提供了具有腺苷A2受体拮抗剂作用的新颖的缩合咪唑化合物,是 有效预防或治疗糖尿病和糖尿病并发症,并由式(I)表示;(其中R 1表示例如可被烷基取代的氨基; R 2表示例如氢原子, 可以被羟基取代的烷基,环烷基或烷基,烯基或炔基; R 3表示例如任选取代的烷基,烯基,炔基,芳基,杂芳基, 吡啶酮基,嘧啶酮基或哌嗪酮基; Ar表示例如任选取代的芳基或杂芳基; Q和W彼此相同或不同,每个代表 N或CH),其药理学上可接受的盐或其水合物。
摘要:
A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.
摘要:
A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R1, R2, R3, R4, and R5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.
摘要:
A crystal of 1-[1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)-ethyl]piperidin-4-yl]-N-methyl-1H-indole-6-carboxamide fumarate which has peaks at chemical shifts of about 124.0 ppm and about 26.8 ppm in a 13C solid NMR spectrum.
摘要:
In an active matrix liquid crystal display unit for displaying data on a liquid crystal panel in response to a control signal, a drain driver is supplied with the control signal to supply a first alternating voltage signal of a predetermined phase to odd-numbered drain buses for drain electrodes of thin-film transistors arranged in a matrix of the panel and to supply even-numbered drain buses with a second alternating voltage signal having a reversed phase which is reversed relative to the predetermined phase. A gate driver supplies the gate buses with electric power cyclically in cycles. Preferably, the first and the second alternating voltage signals have a common period which is equal to a time interval during which the electric power is supplied successively to two adjacent ones of the gate buses. This avoids flicker and cross talk in a display of the data. More preferably, the first and the second alternating voltage signals are given either in each cycle or in a preselected plurality of cycles one of a predetermined number of voltages to cope with a greater number of steps of a tone of the display.
摘要:
In producing a spark plug including a central electrode having a first chip including noble metal and an earth electrode having a second chip including the noble metal, a spark gap being disposed between the first and second chips, a chip including the noble metal. The chip is welded to an end of the central electrode and to an end of the earth electrode. The welded chip is cut to form the first and second chips and the spark gap.
摘要:
An active-matrix LCD device drives the LCD panel by using a dot reversible driving technique. The switching between two sets of input signals or two resolution modes is conducted by applying a DC voltage between the pixel electrode and the common electrode in each pixel before restart of the image display of a switched signal. The DC voltage has the same polarity among the pixels in the pixel array to thereby reduce the flicker after the restart of the image display.
摘要:
The present invention provides an industrially advantageous process for preparing a 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo[4,5-b]pyridine derivative represented by the following formula (II) which is a precursor of an antagonist against an angiotensin II receptor useful as an antihypertensive drug, a biphenyl derivative which is a precursor of the substituent of the pyridine derivative, a process for the preparation thereof, and an intermediate useful for the preparation of the biphenyl derivative: ##STR1##