NOVEL PHENYLACETIC ACID DERIVATIVE
    1.
    发明申请
    NOVEL PHENYLACETIC ACID DERIVATIVE 有权
    新颖的苯甲酸衍生物

    公开(公告)号:US20100048666A1

    公开(公告)日:2010-02-25

    申请号:US12440540

    申请日:2007-09-10

    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。

    Phenylacetic acid derivative
    2.
    发明授权
    Phenylacetic acid derivative 有权
    苯乙酸衍生物

    公开(公告)号:US08148421B2

    公开(公告)日:2012-04-03

    申请号:US12440540

    申请日:2007-09-10

    IPC分类号: A61K31/382 C07D335/02

    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。

    Process for producing 1,2,4-triazole compound and intermediate therefor
    3.
    发明申请
    Process for producing 1,2,4-triazole compound and intermediate therefor 审中-公开
    生产1,2,4-三唑化合物及其中间体的方法

    公开(公告)号:US20060189811A1

    公开(公告)日:2006-08-24

    申请号:US10565678

    申请日:2004-07-23

    IPC分类号: C07D403/14

    CPC分类号: C07D403/14

    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.

    摘要翻译: 本发明提供了使化合物(1)与Rc-X(2)反应得到化合物(3),使化合物(3)与化合物(3)反应的1,2,4-三唑化合物(5)或其盐或水合物的方法, 与硝化剂反应得到化合物(4),然后除去Rc基团,如反应方案所示:(其中Ra,Rb和Rd表示基团,Rc表示可被酸除去的基团)A 1 ,3位具有任选取代的2-氰基吡啶-4-基的2,4-三唑化合物(5)和5位上任意取代的芳族基团,其抑制黄嘌呤氧化酶并且可用于治疗痛风和高尿酸血症 可以以高产率从化合物(1)获得,而不需要在反应过程中分离反应产物。

    Benzoxepino-11-piperidylidene compounds and process for production thereof
    4.
    发明申请
    Benzoxepino-11-piperidylidene compounds and process for production thereof 审中-公开
    苯并恶灵-11-哌啶基化合物及其制备方法

    公开(公告)号:US20060217556A1

    公开(公告)日:2006-09-28

    申请号:US10553034

    申请日:2004-04-14

    IPC分类号: A61K31/4741 C07D491/02

    CPC分类号: C07D491/04 A61K31/553

    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.

    摘要翻译: 提供了制备3- [4-(8-氟-5,11-二氢苯并[b]氧杂环庚烯并[4,3-b]吡啶-11-亚基)哌啶子基]丙酸烷基酯的酸加成盐的方法 通过使3- [4-(8-氟-5,11-二氢苯并[b]氧杂环庚烯并[4,3-b]吡啶-11-亚基)哌啶子基]丙酸烷基酯与酸反应, 使用酸加成盐作为中间体的3- [4-(8-氟-5,11-二氢苯并[b]氧杂环庚烯并[4,3-b]吡啶-11-亚基)哌啶子基]丙酸。 通过使用3- [4-(8-氟-5,11-二氢苯并[b]氧杂环庚烯并[4,3-b]吡啶-11-亚基)哌啶子基]丙酸烷基酯的酸加成盐 制备3- [4-(8-氟-5,11-二氢苯并[b]氧杂环庚烯并[4,3-b]吡啶]亚基)哌啶子基]丙酸,合成反应步骤中使用的金属和有机化合物 主要通过简单的方法容易地从生产中副产的副产物与反应液分离,并且副产物被充分除去,而不需要通过色谱法的纯化步骤,从而可以批量生产并提高生产效率。

    1 2 4-triazole compound
    5.
    发明授权
    1 2 4-triazole compound 有权
    1 2 4-三唑化合物

    公开(公告)号:US07074816B2

    公开(公告)日:2006-07-11

    申请号:US10495322

    申请日:2002-12-03

    IPC分类号: C07D249/08 A61K31/41

    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.

    摘要翻译: 提供了一种新颖的1,2,4-三唑化合物,其可用作高尿酸血症和由于高尿酸血症引起的痛风的治疗剂。 化合物由以下通式(1)表示:其中R 2代表未取代或取代的吡啶基,R 1代表类似的吡啶基,吡啶-N 对应于这些吡啶基的苯氧基或苯基,R 3表示氢或被三氟甲酰氧基取代的低级烷基和R 3键连接到氮原子上 在环中。 还提供了通过腈和酰肼反应生产化合物的方法,以及治疗剂,特别是黄嘌呤氧化酶抑制剂。

    Local air cleaning apparatus
    7.
    发明授权

    公开(公告)号:US10197302B2

    公开(公告)日:2019-02-05

    申请号:US14234737

    申请日:2012-06-22

    IPC分类号: F24F3/16 F24F13/068

    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.

    Light emitting device
    10.
    发明授权
    Light emitting device 有权
    发光装置

    公开(公告)号:US08921870B2

    公开(公告)日:2014-12-30

    申请号:US13037740

    申请日:2011-03-01

    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.

    摘要翻译: 根据一个实施例,发光器件包括基底衬底,第一和第二衬底,第一和第二半导体发光元件。 第一和第二基板设置在基底基板的主表面上,分别包括第一和第二反射区域。 第一和第二半导体发光元件分别包括包括第一和第二发光层的第一和第二结构体。 第一和第二半导体发光元件中的每一个都输入不小于1瓦特的功率。 第一半导体发光元件的面的面积为S1,第一发光层与第一基板的间隔为t1。 第一反射区域的区域R1满足关系(S1 + 100t12)≦̸ R1≦̸(S1 + 10000t12)。 第一和第二半导体发光元件之间的间隙L满足关系式100t1≦̸ L≦̸ 10000t1。