Quinazoline derivatives having tyrosine kinase inhibitory activity
    1.
    发明授权
    Quinazoline derivatives having tyrosine kinase inhibitory activity 有权
    具有酪氨酸激酶抑制活性的喹唑啉衍生物

    公开(公告)号:US08349857B2

    公开(公告)日:2013-01-08

    申请号:US13359326

    申请日:2012-01-26

    摘要: A compound which inhibits both of EGF receptor tyrosine kinase and HER2 tyrosine kinase is provided.A compound represented by the general formula (I): wherein RX is a group represented by the formula: wherein R1 is a hydrogen atom, optionally substituted alkyl, etc.; Z is —O—, —N(R10)—, etc.; R10 is a hydrogen atom, alkyl, etc.; R2 is a hydrogen atom, optionally substituted alkyl, etc.; R18 is a hydrogen atom, optionally substituted alkyl, etc.; R19 is optionally substituted alkyl, etc.; W1 is an optionally substituted non-aromatic nitrogen-containing group; R17 is a hydrogen atom, optionally substituted alkyl, etc.; R3 and R4 are independently a hydrogen atom, optionally substituted alkyl, etc.; X is —O—, —S—, or —N(R12)—, etc.; R12 is a hydrogen atom, alkyl, etc.; and A is phenyl optionally having a substituent, etc., its pharmaceutically acceptable salt, or a solvate thereof.

    摘要翻译: 提供抑制EGF受体酪氨酸激酶和HER2酪氨酸激酶两者的化合物。 由通式(I)表示的化合物:其中RX是由下式表示的基团:其中R1是氢原子,任选取代的烷基等; Z是-O - , - N(R 10) - 等; R10是氢原子,烷基等; R2是氢原子,任选取代的烷基等; R18是氢原子,任意取代的烷基等; R19是任选取代的烷基等; W1是任选取代的非芳族含氮基团; R 17是氢原子,任选取代的烷基等; R3和R4独立地是氢原子,任选取代的烷基等; X是-O-,-S-或-N(R 12) - 等; R12是氢原子,烷基等; 和A是任选具有取代基的苯基等,其药学上可接受的盐或其溶剂合物。

    Quinazoline derivatives having tyrosine kinase inhibitory activity
    2.
    发明授权
    Quinazoline derivatives having tyrosine kinase inhibitory activity 有权
    具有酪氨酸激酶抑制活性的喹唑啉衍生物

    公开(公告)号:US08202879B2

    公开(公告)日:2012-06-19

    申请号:US11884819

    申请日:2006-02-22

    摘要: A compound which inhibits both of EGF receptor tyrosine kinase and HER2 tyrosine kinase is provided.A compound represented by the general formula (I): wherein RX is a group represented by the formula: wherein R1 is a hydrogen atom, optionally substituted alkyl, etc.; Z is —O—, —N(R10)—, etc.; R10 is a hydrogen atom, alkyl, etc.; R2 is a hydrogen atom, optionally substituted alkyl, etc.; R18 is a hydrogen atom, optionally substituted alkyl, etc.; R19 is optionally substituted alkyl, etc.; W1 is an optionally substituted non-aromatic nitrogen-containing group; R17 is a hydrogen atom, optionally substituted alkyl, etc.; R3 and R4 are independently a hydrogen atom, optionally substituted alkyl, etc.; X is —O—, —S—, or —N(R12)—, etc.; R12 is a hydrogen atom, alkyl, etc.; and A is phenyl optionally having a substituent, etc., its pharmaceutically acceptable salt, or a solvate thereof.

    摘要翻译: 提供抑制EGF受体酪氨酸激酶和HER2酪氨酸激酶两者的化合物。 由通式(I)表示的化合物:其中RX是由下式表示的基团:其中R1是氢原子,任选取代的烷基等; Z是-O - , - N(R 10) - 等; R10是氢原子,烷基等; R2是氢原子,任选取代的烷基等; R18是氢原子,任意取代的烷基等; R19是任选取代的烷基等; W1是任选取代的非芳族含氮基团; R 17是氢原子,任选取代的烷基等; R3和R4独立地是氢原子,任选取代的烷基等; X是-O-,-S-或-N(R 12) - 等; R12是氢原子,烷基等; 和A是任选具有取代基的苯基等,其药学上可接受的盐或其溶剂合物。

    Preparation of .beta.-lactam compounds, and intermediates therefor
    4.
    发明授权
    Preparation of .beta.-lactam compounds, and intermediates therefor 失效
    β-内酰胺化合物及其中间体的制备

    公开(公告)号:US5580976A

    公开(公告)日:1996-12-03

    申请号:US425225

    申请日:1995-04-18

    摘要: A process for preparing a .beta.-lactam compound of the formula (I): ##STR1## which comprises cyclization of an azetidinone derivative of the formula: ##STR2## is provided in which R.sup.1 is hydrogen, alkyl which is optionally substituted, or amino which is optionally substituted; R.sup.2 is a carboxy-protecting group; and X is alkylene which is optionally intervened by --O-- or --S--, and/or which is optionally substituted; and R.sup.3 is aryl which is optionally substituted.

    摘要翻译: 提供了式(I)的β-内酰胺化合物的制备方法:其中包括下式所示的氮杂环丁酮衍生物(II)的环化:其中R 1是氢,烷基是 任选取代的,或任选取代的氨基; R2是羧基保护基; 并且X是任选被-O-或-S-所介导的亚烷基,和/或任选被取代的; 并且R 3是任选被取代的芳基。

    Indolomorphinan Derivative Having Carboxy in 6'-Position
    5.
    发明申请
    Indolomorphinan Derivative Having Carboxy in 6'-Position 审中-公开
    吲哚并吗啡衍生物具有6'位的羧基

    公开(公告)号:US20080227803A1

    公开(公告)日:2008-09-18

    申请号:US11792876

    申请日:2005-12-13

    CPC分类号: C07D491/20

    摘要: A compound represented by the formula (I): (wherein R1 denotes hydrogen or —CHRARB (wherein RA denotes a lower alkoxycarbonyloxy, cycloalkoxycarbonyloxy, acyloxy or a group represented by (where R2 denotes hydrogen or a lower alkyl with or without a substituent), and RB denotes hydrogen or methyl, or any of pharmaceutically acceptable salts thereof or any of solvates thereof.

    摘要翻译: 由式(I)表示的化合物:(其中R 1表示氢或-CHR B)其中R A 表示低级烷氧基羰基氧基,环烷氧基羰基氧基,酰氧基或由(其中R 2表示氢或具有或不具有取代基的低级烷基)表示的基团,和R B >表示氢或甲基,或其任何药学上可接受的盐或其任何溶剂合物。

    Thioalkylthio carbacephalosporin derivatives
    6.
    发明授权
    Thioalkylthio carbacephalosporin derivatives 失效
    硫代烷硫基碳孢霉素衍生物

    公开(公告)号:US5362724A

    公开(公告)日:1994-11-08

    申请号:US128770

    申请日:1993-09-17

    摘要: A compound of the formula I: ##STR1## wherein Acyl is C.sub.1 -C.sub.12 acyl; Het is an optionally substituted monocyclic heteroaromatic group containing one or more hetero atoms; R.sup.1 is a single bond or C.sub.1 -C.sub.4 alkylene; R.sup.2 is a straight or branched C.sub.1 -C.sub.4 alkylene; and Y is a hydrogen atom or methoxy group, or a pharmaceutically acceptable salt or an amino-, carboxy- and/or hydroxy-protected derivative thereof, which have a potent antibiotic activity.

    摘要翻译: 式I的化合物:其中酰基是C 1 -C 12酰基; Het是含有一个或多个杂原子的任选取代的单环杂芳基; R1是单键或C1-C4亚烷基; R2是直链或支链C1-C4亚烷基; 并且Y是具有有效抗生素活性的氢原子或甲氧基,或其药学上可接受的盐或氨基,羧基和/或羟基保护的衍生物。

    Glass antenna system for an automobile
    7.
    发明授权
    Glass antenna system for an automobile 失效
    汽车玻璃天线系统

    公开(公告)号:US4439771A

    公开(公告)日:1984-03-27

    申请号:US378329

    申请日:1982-05-14

    CPC分类号: H01Q1/1278

    摘要: A glass antenna system for an automobile comprises a main antenna disposed at an upper part of a glass plate for a rear window of the automobile and a defogging electric heating element disposed below and separate from the main antenna and comprising a plurality of heating strips and a pair of bus bars for supplying electricity to the heating strips. The glass antenna system is characterized in that a lead wire is connected to a predetermined portion of the lower most heating strip among said heating strips and a feeding point for connection to an antenna feeder line is provided on the lead wire, whereby the defogging electric heating element constitutes a subsidiary antenna having a directivity different from the directivity of the main antenna.

    摘要翻译: 一种用于汽车的玻璃天线系统包括设置在汽车后窗玻璃板的上部的主天线和设置在主天线下方并与主天线分离的除雾电加热元件,并且包括多个加热带和 一对用于向加热带供电的母线。 玻璃天线系统的特征在于,引线与所述加热带中的最下部加热条的预定部分连接,并且在引线上设置用于连接到天线馈线的馈电点,由此除雾电加热 元件构成具有与主天线的方向性不同的方向性的辅助天线。

    Preparation of .beta.lactam compounds
    8.
    发明授权
    Preparation of .beta.lactam compounds 失效
    制备β-内酰胺化合物

    公开(公告)号:US5563264A

    公开(公告)日:1996-10-08

    申请号:US423725

    申请日:1995-04-18

    摘要: A process for preparing a .beta.-lactam compound of the formula (I): ##STR1## which comprises cyclization, in the presence of a catalyst, of an azetidinone derivative of the formula: ##STR2## is provided in which R.sup.1 is hydrogen, alkyl which is optionally substituted, or amino which is optionally substituted; R.sup.2 is a carboxy-protecting group; and X is alkylene which is optionally intervened by --O-- or --S--, and/or which is optionally substituted; and R.sup.3 is aryl which is optionally substituted. The catalyst is preferably a transition metal salt (especially rhodium) or is an acid.

    摘要翻译: 制备式(I)的β-内酰胺化合物的方法:其中包括在催化剂存在下环化下式的氮杂环丁酮衍生物:(II) 其中R1是氢,任选被取代的烷基,或被任意取代的氨基; R2是羧基保护基; 并且X是任选被-O-或-S-所介导的亚烷基,和/或任选被取代的; 并且R 3是任选被取代的芳基。 催化剂优选为过渡金属盐(特别是铑)或者是酸。

    Thioalkylthio cephalosporin derivatives
    9.
    发明授权
    Thioalkylthio cephalosporin derivatives 失效
    硫代烷硫基头孢菌素衍生物

    公开(公告)号:US5352792A

    公开(公告)日:1994-10-04

    申请号:US25628

    申请日:1993-03-02

    摘要: A novel thioalkylthio cephalosporin antibiotic compound of formula I: ##STR1## wherein Acyl is C.sub.1 -C.sub.12 acyl; Het is optionally substituted monocyclic heteroaromatic group containing one or more hetero atoms; R.sup.1 is a single bond or C.sub.1 -C.sub.4 alkylene; R.sub.2 is a straight or branched C.sub.1 -C.sub.4 alkylene; X is a sulfur atom or sulfoxide group; and Y is a hydrogen atom or methoxy group, or a pharmaceutically acceptable salt or an amino-, carboxy- and/or hydroxy-protected derivative thereof, a formulation containing the same and a method for treating bacterial infections.

    摘要翻译: 式I的新型硫代烷硫基头孢菌素抗生素化合物:其中酰基是C 1 -C 12酰基; Het是含有一个或多个杂原子的任选取代的单环杂芳基; R1是单键或C1-C4亚烷基; R2是直链或支链C1-C4亚烷基; X为硫原子或亚砜基; 并且Y是氢原子或甲氧基,或其药学上可接受的盐或氨基,羧基和/或羟基保护的衍生物,含有该衍生物的制剂和治疗细菌感染的方法。

    Structure for installing mirror base on glass plate and method for
installing mirror base on glass plate
    10.
    发明授权
    Structure for installing mirror base on glass plate and method for installing mirror base on glass plate 失效
    用于安装玻璃板上的镜面的结构和用于安装玻璃板上的镜面基板的方法

    公开(公告)号:US5160780A

    公开(公告)日:1992-11-03

    申请号:US434673

    申请日:1989-09-19

    摘要: This invention relates to a mirror base-installing structure for installing a mirror base on the surface of a glass plate, characterized in that said mirror base is bonded to the surface of said glass plate with a film-like or sheet-like heat-curable adhesive interposed between the mirror base and the glass plate, said adhesive having elasticity or plasticity after heat-cured, and a method for installing the same. The mirror base can be bonded simultaneously with the preparation of a bilayer glass, thereby simplifying the working process.

    摘要翻译: PCT No.PCT / JP88 / 01320 Sec。 371日期:1989年9月19日 102(e)日期1989年9月19日PCT提交1988年12月23日PCT公布。 公开号WO89 / 05782 日期:1989年6月29日。本发明涉及一种用于在玻璃板的表面上安装镜座的反射镜基座安装结构,其特征在于,所述反射镜底座以薄膜状结合到所述玻璃板的表面 或夹在玻璃基板和玻璃板之间的片状热固性粘合剂,所述粘合剂在热固化后具有弹性或可塑性,以及其安装方法。 镜底可以同时制备双层玻璃,从而简化了工作过程。