摘要:
Provided are a process for producing an acid addition salt of a 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic acid alkyl ester by reacting a 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic acid alkyl ester with an acid, and a process for producing 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic acid using the acid addition salt as an intermediate. By using as an intermediate an acid addition salt of a 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic acid alkyl ester to produce 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)piperidino]propionic acid, the metals used in the synthetic reaction steps and the organic compounds mainly by-produced during production are readily separated from a reaction liquid by a simple procedure, and the by-products are sufficiently removed without using a purification step by chromatography, thereby enabling mass production and enhancing production efficiency.
摘要:
Provided is a process for producing 1,2,4-triazole compound (5), or a salt or hydrate thereof which comprises reacting compound (1) with Rc-X (2) to give compound (3), reacting compound (3) with a nitrilization agent to give compound (4), and then removing the group Rc, as shown by the reaction scheme: (Wherein Ra, Rb and Rd represent a group, Rc represents a group which can be removed by an acid) A 1,2,4-triazole compound (5) having an optionally substituted 2-cyanopyridin-4-yl group at 3-position and an optionally substituted aromatic group at 5-position which inhibits a xanthine oxidase and is useful for treatment of gout and hyperuricemia can be obtained from compound (1) in a high yield without requiring isolation of reaction products in the course of reactions.
摘要:
A compound represented by the formula (1) or a salt thereof ( represents a single bond, or a double bond; R1 represents hydrogen atom, or an alkyl group; R2 and R3 represent hydrogen atom, or an alkyl group; R4 and R5 represent hydrogen atom, hydroxy group, an alkoxyl group, a halogen atom, or a mono- or di-alkyl-substituted amino group; R6 represents hydrogen atom, cyano group, an alkoxycarbonyl group, or carboxy group; R7 represents one or two of substituents on the benzene ring (the substituents are selected from hydrogen atom, a halogen atom, nitro group, cyano group, hydroxy group, amino group, an alkyl group, and an alkoxyl group); A represents a 5-membered or 6-membered non-aromatic heterocyclic ring containing one or two contiguous sulfur atoms (the sulfur atoms may independently form oxide); W represents oxo group, hydrogen atom, an alkyl group, hydroxy group, an alkoxyl group, or a halogen atom; and X represents oxygen atom, or sulfur atom), or a salt thereof, which has a superior suppressing action against prostaglandin E2 production and is useful as an active ingredient of medicaments with reduced adverse reactions such as gastrointestinal disorders.
摘要翻译:由式(1)表示的化合物或其盐(表示单键或双键; R1表示氢原子或烷基; R2和R3表示氢原子或烷基; R4和R5表示 氢原子,羟基,烷氧基,卤素原子或一或二烷基取代的氨基; R 6表示氢原子,氰基,烷氧基羰基或羧基; R 7表示一个或两个取代基 在苯环上(取代基选自氢原子,卤素原子,硝基,氰基,羟基,氨基,烷基和烷氧基); A表示5元或6元非 含有一个或两个相邻硫原子的杂环(硫原子可以独立地形成氧化物); W表示氧代基,氢原子,烷基,羟基,烷氧基或卤素原子; X表示氧原子 ,或硫原子)或其盐 对前列腺素E2产生的抑制作用较差,并且可用作具有减少的不良反应如胃肠道疾病的药物的活性成分。
摘要:
A compound represented by the formula (1) or a salt thereof ( represents a single bond, or a double bond; R1 represents hydrogen atom, or an alkyl group; R2 and R3 represent hydrogen atom, or an alkyl group; R4 and R5 represent hydrogen atom, hydroxy group, an alkoxyl group, a halogen atom, or a mono- or di-alkyl-substituted amino group; R6 represents hydrogen atom, cyano group, an alkoxycarbonyl group, or carboxy group; R7 represents one or two of substituents on the benzene ring (the substituents are selected from hydrogen atom, a halogen atom, nitro group, cyano group, hydroxy group, amino group, an alkyl group, and an alkoxyl group); A represents a 5-membered or 6-membered non-aromatic heterocyclic ring containing one or two contiguous sulfur atoms (the sulfur atoms may independently form oxide); W represents oxo group, hydrogen atom, an alkyl group, hydroxy group, an alkoxyl group, or a halogen atom; and X represents oxygen atom, or sulfur atom), or a salt thereof, which has a superior suppressing action against prostaglandin E2 production and is useful as an active ingredient of medicaments with reduced adverse reactions such as gastrointestinal disorders.
摘要翻译:由式(1)表示的化合物或其盐(表示单键或双键; R1表示氢原子或烷基; R2和R3表示氢原子或烷基; R4和R5表示 氢原子,羟基,烷氧基,卤素原子或一或二烷基取代的氨基; R 6表示氢原子,氰基,烷氧基羰基或羧基; R 7表示一个或两个取代基 在苯环上(取代基选自氢原子,卤素原子,硝基,氰基,羟基,氨基,烷基和烷氧基); A表示5元或6元非 含有一个或两个相邻硫原子的杂环(硫原子可以独立地形成氧化物); W表示氧代基,氢原子,烷基,羟基,烷氧基或卤素原子; X表示氧原子 ,或硫原子)或其盐 对前列腺素E2产生的抑制作用较差,并且可用作具有减少的不良反应如胃肠道疾病的药物的活性成分。
摘要:
A novel 1,2,4-triazole compound which is useful as a therapeutic agent for hyperuricemia and gout due to hyperuricemia is provided. A compound is represented by the following general formula (1): wherein R2 represents an unsubstituted or substituted pyridyl group, R1 represents a similar pyridyl group, a pyridine-N-oxide group corresponding to these pyridyl groups, or a phenyl group, and R3 represents hydrogen or a lower alkyl group substituted with pivaloyloxy group and R3 bonds to a nitrogen atom in the ring. A process for production of a compound by reacting a nitrile and a hydrazide, and a therapeutic agent, particularly a xanthine oxidase inhibitor are also provided.
摘要:
A novel 1,2,4-triazole compound which is useful as a therapeutic agent for hyperuricemia and gout due to hyperuricemia is provided. A compound is represented by the following general formula (1): wherein R2 represents an unsubstituted or substituted pyridyl group, R1 represents a similar pyridyl group, a pyridine-N-oxide group corresponding to these pyridyl groups, or a phenyl group, and R3 represents hydrogen or a lower alkyl group substituted with pivaloyloxy group and R3 bonds to a nitrogen atom in the ring. A process for production of a compound by reacting a nitrile and a hydrazide, and a therapeutic agent, particularly a xanthine oxidase inhibitor are also provided.
摘要:
A local air cleaning apparatus (1) is provided with a push hood (2) having an air flow opening face (23) for blowing out a cleaned uniform air flow and a guide (3) provided on a side of the push hood (2) having the air flow opening face (23), the guide (3) extending from the side thereof having the air flow opening face (23) toward a downstream side of the uniform air flow to form an opening face (31) at a downstream end portion thereof. The push hood (2) is arranged such that the uniform air flow blown out from the air flow opening face (23) passes through the inside of the guide (3) and then collides with an air collision face (W) on a downstream side of the opening face (31). The opening face (31) of the guide (3) is spaced apart from and opposed to the air collision face (W) to form an open region between the opening face (3) and the air collision face (W). The cleaned uniform air flow blown out from the air flow opening face (23) collides with the air collision face (W) and flows out of the opening region, thereby allowing the inside of the guide (3) and the inside of the open region to have higher cleanliness than other regions.
摘要:
Disclosed is an exhaust gas purification catalyst carrier which includes a phosphate salt represented by formula: MPO4 (wherein M represents Y, La, or Al) or a zirconium phosphate represented by formula ZrP2O7; an exhaust gas purification catalyst containing a noble metal at least containing Rh and supported on the carrier; and an exhaust gas purification catalyst product having a catalyst support made of a ceramic or metallic material, and a layer of the exhaust gas purification catalyst, the layer being supported on the catalyst support.
摘要:
According to one embodiment, the luminescent material shows a luminescence peak in a wavelength range of 570 to 670 nm when excited with light having an emission peak in a wavelength range of 250 to 520 nm. The luminescent material includes a host material having a crystal structure substantially same as the crystal structure of Sr2Si7Al3ON13. The host material is activated by Eu, and includes Sr and Ca to satisfy a relationship of 0.008≦MCa/(MSr+MCa)≦0.114, where MCa is a number of moles of Ca and MSr is a number of moles of Sr.
摘要翻译:根据一个实施方案,发光材料在具有在250至520nm的波长范围内的发光峰的光激发时,显示在570至670nm的波长范围内的发光峰。 发光材料包括具有与Sr 2 Si 7 Al 3 ON 13的晶体结构基本相同的晶体结构的主体材料。 主体材料由Eu活化,包括Sr和Ca,以满足0.008&nlE的关系; MCa /(MSr + MCa)≦̸ 0.114,其中MCa是Ca的摩尔数,MSr是Sr的摩尔数 。
摘要:
According to one embodiment, a light emitting device includes a base substrate, first and second substrates, first and second semiconductor light emitting elements. The first and second substrates are provided on a major surface of the base substrate and include first and second reflection regions, respectively. The first and second semiconductor light emitting elements include first and second structural bodies including first and second light emitting layers, respectively. Each of the first and second semiconductor light emitting elements is inputted with a power not less than 1 Watt. An area of a face of the first semiconductor light emitting element is S1, and a gap between the first light emitting layer and the first substrate is t1. An area R1 of the first reflection region satisfies a relationship (S1+100t12)≦R1≦(S1+10000t12). A gap L between the first and the second semiconductor light emitting elements satisfies the relationships 100t1≦L≦10000t1.