Optically active phenol derivatives and preparation thereof
    2.
    发明授权
    Optically active phenol derivatives and preparation thereof 失效
    光学活性酚衍生物及其制备方法

    公开(公告)号:US5354913A

    公开(公告)日:1994-10-11

    申请号:US85166

    申请日:1993-07-02

    摘要: An optically active tri-substituted methane compound having, as substituents, an aromatic ring group and a phenyl group having hydroxyl group at ortho or para position can be obtained by allowing a phenol compound unsubstituted at the ortho- or/and para-position to react with an optically active secondary carbinol compound having an aromatic ring group at the alpha-position in the presence of tri-substituted phosphine and diazodicarboxylate or diazodicarboxamide. These and other optically active tri-substituted methane compounds are useful as active ingredients for medicines or as intermediate compounds for preparing medicines.

    摘要翻译: 通过使在邻位或/或对位未取代的酚化合物反应,可以得到在邻位或对位具有芳环基和具有羟基的苯基作为取代基的光学活性三取代甲烷化合物 在三取代的膦和重氮二羧酸酯或重氮二甲酰胺的存在下,在α-位上具有芳环基的光学活性的仲甲醇化合物。 这些和其它光学活性三取代的甲烷化合物可用作药物的活性成分或用作制备药物的中间体化合物。

    Nitrosothiol derivatives and their use
    8.
    发明授权
    Nitrosothiol derivatives and their use 失效
    硝基苯酚衍生物及其用途

    公开(公告)号:US5116861A

    公开(公告)日:1992-05-26

    申请号:US562626

    申请日:1990-08-03

    摘要: Novel nitrosothiol derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.3 is a hydrogen atom, an acyl group or a hydrocarbon residue which may be substituted; X.sup.1 is a hydrogen atom, an acyl group, a lower alkoxy group or a hydrocarbon residue which may be substituted; X.sup.2 is an acyl group or a carboxyl group which may be esterified or which may form an amide; with proviso that when X.sup.2 is a carboxyl group X.sup.1 is not a hydrogen atom or acetyl group and that when both R.sup.1 and R.sup.2 are hydrogen atoms X.sup.1 is not acetyl group or .gamma.-glutamyl group, and salts thereof, show excellent hypotensive action, antiarrhythmic action, anti-anginal action, cardiotonic action or coronary vasodilation, thus being useful as therapeutic or prophylactic agents for the cardiovascular diseases such as hypertension and angina pectoris.

    Pyrazoloquinolone derivative and use thereof
    9.
    发明授权
    Pyrazoloquinolone derivative and use thereof 失效
    吡唑并喹啉衍生物及其用途

    公开(公告)号:US07842701B2

    公开(公告)日:2010-11-30

    申请号:US10589443

    申请日:2005-02-18

    IPC分类号: A61K31/437 C07D471/06

    CPC分类号: C07D471/04

    摘要: The present invention provides a pyarzoloquinolone derivative having kinase inhibitory activity. The derivative is represented by the formula: wherein R1 is an aryl group which may be substituted, or an aromatic heterocyclic group which may be substituted; R2 is a hydrogen atom, an amino group which may be substituted, a hydroxy group which may be substituted, or a thiol group which may be substituted; R3, R4, R5 and R6, which may be identical or different, are each (1) a hydrogen atom, (2) a nitro group, (3) a cyano group, (4) a halogen atom, (5) a hydrocarbon group which may be substituted, (6) an amino group which may be substituted, (7) a hydroxy group which may be substituted, or (8) a thiol group which may be substituted; and R3 and R4, R4 and R5, and R5 and R6 may respectively form a ring together with the adjacent carbon atom, or salt thereof.

    摘要翻译: 本发明提供具有激酶抑制活性的pyarzoloquinolone衍生物。 该衍生物由下式表示:其中R1是可被取代的芳基或可被取代的芳族杂环基; R2是氢原子,可被取代的氨基,可被取代的羟基,或可以被取代的硫醇基; R 3,R 4,R 5和R 6可以相同或不同,分别为(1)氢原子,(2)硝基,(3)氰基,(4)卤素原子,(5) 可以被取代的基团,(6)可以被取代的氨基,(7)可被取代的羟基,或(8)可以被取代的硫醇基; 并且R 3和R 4,R 4和R 5以及R 5和R 6可以与相邻的碳原子或其盐一起分别形成环。

    Nasal preparation of guanidinoimino quinoline derivatives
    10.
    发明授权
    Nasal preparation of guanidinoimino quinoline derivatives 失效
    胍基亚氨基喹啉衍生物的鼻制剂

    公开(公告)号:US06706732B1

    公开(公告)日:2004-03-16

    申请号:US09980391

    申请日:2001-11-28

    IPC分类号: A61K3147

    摘要: A nasal preparation comprising a compound represented by the formula: wherein Ring A is an optionally substituted 5- or 6-membered aromatic heterocyclic ring, Ring B is an optionally substituted 5- or 6-membered aromatic homocyclic or heterocyclic ring, R1 is a hydrogen atom, a hydroxyl group or a lower alkyl group, and n is 0 or 1, which has an Na—H exchange inhibiting activity, or a salt thereof exhibits excellent bioabsorbability and an Na—H exchange inhibiting activity superior to that of an oral preparation, thus being useful as a prophylactic and/or therapeutic agent for ischemic heart diseases such as myocardial infarct and arrhythmia.

    摘要翻译: 一种鼻制剂,其包含由下式表示的化合物:其中环A是任选取代的5元或6元芳族杂环,环B是任选取代的5或6元芳族碳环或杂环,R 1, 是氢原子,羟基或低级烷基,n为0或1,其具有Na-H交换抑制活性,或其盐表现出优于生物吸收性和Na-H交换抑制活性优于 口服制剂,因此可用作缺血性心脏病例如心肌梗塞和心律失常的预防和/或治疗剂。