Novel renin inhibitory amino acid derivatives
    6.
    发明授权
    Novel renin inhibitory amino acid derivatives 失效
    新型肾素抑制性氨基酸衍生物

    公开(公告)号:US4857650A

    公开(公告)日:1989-08-15

    申请号:US879741

    申请日:1986-06-27

    摘要: New renin inhibitory amino acid derivatives represented by formula (I): ##STR1## wherein A represents an alkoxycarbonyl group having 2 to 7 carbon atoms, ##STR2## wherein R.sup.1 and R.sup.2 are defined as in the specification below or ##STR3## wherein X and Y are defined as in the specification herein below, n represents zero or one, Z represents --O-- or --NH--, and R represents a straight- or branched chain alkyl group having 1 to 7 carbon atoms, and pharmaceutically acceptable salts thereof, useful as a therapeutic agent are disclosed. The amino acid derivatives have a renin inhibitory effect when administered orally and are useful for treatment of hypertension, especially renin-associated hypertension.

    摘要翻译: 由式(I)表示的新的肾素抑制性氨基酸衍生物:其中A表示碳原子数2〜7的烷氧基羰基,其中R1和R2如下面的说明书所定义, 其中X和Y如下面的说明书中所定义,n表示0或1,Z表示-O-或-NH-,R表示具有1至7个碳原子的直链或支链烷基, 公开了可用作治疗剂的盐。 当口服给药时,氨基酸衍生物具有肾素抑制作用,可用于治疗高血压,特别是肾素相关性高血压。

    Oxime ether compound, processes for preparing the same and fungicide
containing the same
    8.
    发明授权
    Oxime ether compound, processes for preparing the same and fungicide containing the same 失效
    肟醚化合物,其制备方法和含有它们的杀真菌剂

    公开(公告)号:US5449803A

    公开(公告)日:1995-09-12

    申请号:US214188

    申请日:1994-03-17

    摘要: Disclosed are an oxime ether compound represented by the formula (I): ##STR1## wherein R.sup.1 represents an alkyl group having 1 to 6 carbon atoms; R.sup.2 represents OR.sup.5 or NHR.sup.6 where R.sup.5 and R.sup.6 each represent an alkyl group having 1 to 6 carbon atoms; R.sup.3 represents a cycloalkyl group having 3 to 8 carbon atoms; R.sup.4 represents an alkenyloxy group having 3 to 6 carbon atoms, an alkynyloxy group having 3 to 6 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, a benzyloxy group, an alkoxycarbonyl group having 2 to 7 carbon atoms, a halogen atom, a cyano group, an alkylthio group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms, a haloalkyl group having 1 to 6 carbon atoms or an acyl group having 2 to 7 carbon atoms; and n represents an integer of 0 to 5.processes for preparing the same and a fungicide containing the same as an effective ingredient.

    摘要翻译: 公开了由式(I)表示的肟醚化合物:其中R 1表示具有1至6个碳原子的烷基; R 2表示OR 5或NHR 6,其中R 5和R 6各自表示具有1至6个碳原子的烷基; R3代表具有3-8个碳原子的环烷基; R4表示碳原子数3〜6的烯氧基,碳原子数3〜6的炔氧基,碳原子数1〜10的烷氧基,苄氧基,碳原子数2〜7的烷氧基羰基,卤素原子, 氰基,碳原子数1〜6的烷硫基,碳原子数1〜6的烷基,碳原子数1〜6的卤代烷基或碳原子数2〜7的酰基。 n表示0〜5的整数。其制备方法和含有该有效成分的杀真菌剂。

    Method of constructing teritiary structure of protein composed of plural chains
    9.
    发明申请
    Method of constructing teritiary structure of protein composed of plural chains 审中-公开
    构建由多条链构成的蛋白质三元结构的方法

    公开(公告)号:US20050192757A1

    公开(公告)日:2005-09-01

    申请号:US10887104

    申请日:2004-07-09

    CPC分类号: C07K1/00

    摘要: A method is provided of constructing a tertiary structure of a protein composed of plural chains having given arbitrary amino acid sequences by extending an comparative modeling method of constructing a tertiary structure of a protein composed of a single chain having a given arbitrary amino acid sequence (extended modeling method). In this method, an input file format of the plural chains in a computer software program is each corrected so as to present a form of a temporary single chain (correction of sequence alignment) and the tertiary structure is constructed based on the modeling method while assuming that the structure has plural chains in calculation of a potential formula by the computer software program, thereby constructing the tertiary structure of the target protein. Namely, a method is provided of constructing the tertiary structure of an arbitrary protein having plural chains, which serves as a particularly important key factor in developing drugs or the like, highly accurately and much more efficiently than by a conventional method.

    摘要翻译: 提供了构建由具有任意氨基酸序列的多个链构成的蛋白质的三级结构的方法,通过扩展构建由具有给定的任意氨基酸序列的单链构成的蛋白质的三级结构的比较建模方法(延伸 建模方法)。 在该方法中,对计算机软件程序中的多个链的输入文件格式进行校正,以呈现临时单链的形式(校正序列比对),并且基于建模方法构建三级结构,同时假设 通过计算机软件程序计算潜在公式,结构具有多个链,从而构建靶蛋白的三级结构。 即,提供了构建具有多个链的任意蛋白质的三级结构的方法,其作为开发药物等中特别重要的关键因素,比通过常规方法高度精确和高效率地构成。

    Protein structure analysis method, protein structure analyzing instrument, program and recording medium
    10.
    发明申请
    Protein structure analysis method, protein structure analyzing instrument, program and recording medium 审中-公开
    蛋白质结构分析方法,蛋白质结构分析仪器,程序和记录介质

    公开(公告)号:US20090319234A1

    公开(公告)日:2009-12-24

    申请号:US10973096

    申请日:2004-10-26

    IPC分类号: G06F17/50

    摘要: This invention fragments ions ionized by an electro-spray ionization method or the like for a target protein whose three-dimensional structure is to be predicted, to fragment ions by a hexapole CID method or the like, and measures a fragmentation spectrum. The present invention determines fragment ion assignment information on an amino acid sequence of the target protein based on the measured fragmentation spectrum. The present invention specifies a region of the amino acid sequence of the target protein in which region the ions are dissociated to the fragment ions according to the determined fragment ion assignment information, and determines easily cleavable domain information on the amino acid sequence of the target protein according to the specified region. The present invention predicts the three-dimensional structure of the target protein. The present invention outputs predicted three-dimensional structure prediction data and the determined easily cleavable domain information while making them correspond to each other.

    摘要翻译: 本发明通过电喷雾离子化法等离子化对于要预测其三维结构的靶蛋白进行离子化离子化,通过六极CID法等分离离子,测定碎裂光谱。 本发明基于测定的断裂谱,确定靶蛋白的氨基酸序列的片段离子分配信息。 本发明根据确定的片段离子分配信息指定靶蛋白的氨基酸序列的区域,其中离子被离解为片段离子,并且确定易于切割的关于靶蛋白的氨基酸序列的结构域信息 根据指定区域。 本发明预测了靶蛋白的三维结构。 本发明输出预测的三维结构预测数据和确定的容易切割的域信息,同时使它们彼此对应。