Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
    1.
    发明授权
    Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity 有权
    含有β分泌酶抑制活性的含硫杂环衍生物

    公开(公告)号:US08637504B2

    公开(公告)日:2014-01-28

    申请号:US12997802

    申请日:2009-06-11

    摘要: The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid β protein, for example, a compound represented by the formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R1 is optionally substituted lower alkyl or the like, R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or the like, R3a and R3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof.

    摘要翻译: 提供以下化合物作为治疗由淀粉样蛋白β蛋白质的生产,分泌和/或沉积引起的疾病的药剂,例如由式(I)表示的化合物:其中环A是任选取代的碳环基团或 任选取代的杂环基,R 1为任选取代的低级烷基等,R 2a和R 2b各自独立地为氢,任选取代的低级烷基等,R 3a和R 3c各自独立地为氢,卤素,羟基,任选取代的低级烷基等 ,或其药学上可接受的盐或其溶剂合物。

    Crystalline, enantiomerically pure salt form of a beta-agonist, and the use thereof as a drug
    2.
    发明授权
    Crystalline, enantiomerically pure salt form of a beta-agonist, and the use thereof as a drug 失效
    β激动剂的结晶,对映体纯盐形式及其作为药物的用途

    公开(公告)号:US08394791B2

    公开(公告)日:2013-03-12

    申请号:US12918374

    申请日:2009-02-17

    IPC分类号: C07D265/00

    CPC分类号: C07D265/18

    摘要: This invention concerns a crystalline, enantiopure hydrochloride salt of N-(5-{2-[3-(4,4-diethyl-2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-1,1-dimethyl-propylamino-1-hydroxy-ethyl}-2-hydroxy-phenyl)-methanesulfonamide, preferably of N-(5-{(R)-2-[3-(4,4-diethyl-2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-1,1-dimethyl-propylamino-1-hydroxy-ethyl}-2-hydroxy-phenyl)-methanesulfonamide and its action as a long acting beta-agonist, alone or in combination with one or multiple other active ingredients for the treatment of respiratory diseases.

    摘要翻译: 本发明涉及N-(5- {2- [3-(4,4-二乙基-2-氧代-4H-苯并[d] [1,3]恶嗪-1-基) - 1,1-二甲基 - 丙基氨基-1-羟基 - 乙基} -2-羟基 - 苯基) - 甲磺酰胺,优选N-(5 - {(R)-2- [3-(4,4-二乙基-2- 氧代-4H-苯并[d] [1,3]恶嗪-1-基)-1,1-二甲基 - 丙基氨基-1-羟基 - 乙基} -2-羟基 - 苯基) - 甲磺酰胺及其作为长效 β-激动剂,单独或与一种或多种其它活性成分组合用于治疗呼吸系统疾病。

    Hair dyeing composition
    3.
    发明授权
    Hair dyeing composition 有权
    染发组合物

    公开(公告)号:US08257448B2

    公开(公告)日:2012-09-04

    申请号:US13148690

    申请日:2010-02-19

    申请人: Beate Fröhling

    发明人: Beate Fröhling

    IPC分类号: A61Q5/10 C07D265/00

    摘要: The invention relates to hair dyeing composition comprising (a) a dye of formula (1); (b) a least one dye selected from the compounds of formulae (2) and (3), wherein D is the radical of a diazo component of the formula (2a) and (c) a quaternary ammonium salt selected from (c1) quaternary ammonium salts of the formula (4); (c2) imidazolium salts of the formula (5) and (c3) quaternary diammonium salts of the formula (6). The invention also relates to the dyeing methods for dyeing keratinous fibers comprising such dyeing composition.

    摘要翻译: 本发明涉及染发组合物,其包含(a)式(1)的染料; (b)选自式(2)和(3)的化合物中的至少一种染料,其中D是式(2a)和(c)的重氮组分的基团,选自(c1)四 式(4)的铵盐; (c2)式(5)和(c3)式(6)的季二铵盐的咪唑鎓盐。 本发明还涉及染色包含这种染色组合物的角质纤维的染色方法。

    Material for forming resist protective film and method for forming resist pattern using same
    4.
    发明授权
    Material for forming resist protective film and method for forming resist pattern using same 有权
    用于形成抗蚀剂保护膜的材料和使用其形成抗蚀剂图案的方法

    公开(公告)号:US07951523B2

    公开(公告)日:2011-05-31

    申请号:US11659006

    申请日:2005-07-29

    摘要: In the liquid immersion lithography process, by simultaneously preventing deterioration of a resist film and deterioration of an immersion liquid employed during liquid immersion lithography which uses various immersion liquids, including water, resistance to post exposure delay of the resist film can be improved without increasing the number of processes, thereby making it possible to form a high resolution resist pattern using liquid immersion lithography. Using an alkaline soluble polymer, a crosslinking agent, and a solvent capable of dissolving them as at least constituent component, a composition is prepared and a protective film is formed on the surface of the resist film to be used, using the composition.

    摘要翻译: 在液浸光刻工艺中,通过同时防止抗蚀剂膜的劣化以及使用包括水在内的各种浸渍液体的液浸光刻中所使用的浸渍液的劣化,可以提高抗蚀剂膜的后曝光延迟性,而不会增加 处理次数,从而可以使用液浸光刻法形成高分辨率抗蚀剂图案。 使用碱溶性聚合物,交联剂和能够溶解至少构成成分的溶剂,制备组合物,并使用该组合物在所使用的抗蚀剂膜的表面上形成保护膜。

    Renal-selective prodrugs for control of renal sympathetic nerve activity in the treatment of hypertension
    10.
    发明申请
    Renal-selective prodrugs for control of renal sympathetic nerve activity in the treatment of hypertension 审中-公开
    肾选择性前药用于控制治疗高血压的肾交感神经活动

    公开(公告)号:US20030220521A1

    公开(公告)日:2003-11-27

    申请号:US10151211

    申请日:2002-05-20

    申请人: G.D. Searle & Co.

    IPC分类号: C07D265/00 C07K005/04

    摘要: Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-null-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-null-hydroxylase inhibitors, of which N-acetyl-null-glutamyl fusaric acid hydrazide (shown below) is preferred. 1

    摘要翻译: 描述了肾选择性前药,其优先在肾中转化成能够抑制参与肾交感神经活性的儿茶酚胺型神经递质合成的化合物。 本文所述的前药衍生自能够抑制一种或多种参与儿茶酚胺合成的酶的抑制剂化合物,这些化合物可分类为酪氨酸羟化酶抑制剂,或作为多巴 - 脱羧酶抑制剂,或作为多巴胺-β-羟化酶抑制剂。 这些抑制剂化合物通过由主要位于肾中的酶选择性识别的可切割键与化学部分如谷氨酸衍生物连接。 释放的抑制剂化合物然后可用于肾脏中以抑制参与儿茶酚胺合成的一种或多种酶。 抑制肾脏儿茶酚胺合成可以抑制与钠滞留相关的疾病如高血压相关的增强的肾神经活动。 特别感兴趣的缀合物是多巴胺-β-羟化酶抑制剂的谷氨酰衍生物,其中N-乙酰基-γ-谷氨酰镰孢酸酰肼(如下所示)是优选的。