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    • 5. 发明授权
      US07166695B2 Affinity markers for human serum albumin 失效
    • Affinity markers for human serum albumin
    • 人血清白蛋白的亲和标记
    • US07166695B2
    • 2007-01-23
    • US10934841
    • 2004-09-02
    • Alexander Krantz , Wolin Huang , Arthur M. Hanel , Darren L. Holmes , Dominique P. Bridon
    • Alexander Krantz , Wolin Huang , Arthur M. Hanel , Darren L. Holmes , Dominique P. Bridon
    • C07K7/06
    • A61K49/0021 , A61K38/00 , A61K47/62 , A61K47/6901 , A61K49/0043 , A61K49/0056 , C07K14/665
    • Methods and compositions are provided for identifying compounds having affinity or complementarity to a target molecule. Compounds according to the invention may be described by the formula E-Ca—R—Cb-A, wherein E is a therapeutic or diagnostic agent, R is a reactive group, Ca and Cb are connector groups between E and R and between R and A, respectively, and A is an affinity group comprising the sequence F-1-Y-E-E. Compounds according to the invention may be used for labeling the target molecule, particularly where the target molecule is naturally found in a complex mixture, such as a physiological fluid, like blood. By affinity labeling in vivo, the lifetime of physiologically active entities can be greatly enhanced by becoming bound to long-lived blood components. The covalently bound entity may also serve as an antagonist or agonist of a particular binding protein or as an enzyme inhibitor.
    • 提供了用于鉴定与靶分子具有亲和力或互补性的化合物的方法和组合物。 根据本发明的化合物可以用下式描述：其中E是治疗剂或诊断剂，R是反应性基团，C < 分别是E和R之间以及R和A之间的连接器组，A是包含序列F-1 -YEE的亲和基团。 根据本发明的化合物可以用于标记靶分子，特别是当目标分子天然存在于复杂混合物如生理液体如血液中时。 通过体内亲和标记，生理活性实体的寿命可以通过与长寿命的血液成分结合而大大增强。 共价结合的实体也可以用作特异性结合蛋白的拮抗剂或激动剂或作为酶抑制剂。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 9. 发明授权
      US4745116A 2-oxy-4H-3,1-benzoxazin-4-ones and related compounds and pharmaceutical use 失效
    • 2-oxy-4H-3,1-benzoxazin-4-ones and related compounds and pharmaceutical use
    • 2-氧-4H-3,1-苯并恶嗪-4-酮及相关化合物及药物用途
    • US4745116A
    • 1988-05-17
    • US945751
    • 1986-12-23
    • Alexander Krantz , Robin Spencer , Tim Tam , Teng J. Liak
    • Alexander Krantz , Robin Spencer , Tim Tam , Teng J. Liak
    • C07D265/26 , C07F9/6533 , A61K31/535 , C07D265/36
    • C07D265/26 , C07F9/65335
    • 2-Oxy-4H-3,1-benzoxazin-4-ones, useful as serine protease inhibitors, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein:a is an integer of 1 to 4;A is a bond, or alkylene having one to eight carbon atoms;R is hydrogen, phenyl, imidazolyl or cycloalkyl having three to six carbon atoms, wherein the phenyl, imidazolyl or cycloalkyl ring is optionally substituted with 1 to 3 substituents independently selected from the group consisting of lower alkyl having one to four carbon atoms, lower alkoxy having one to four carbon atoms, --N(R.sup.1).sub.2, --NO.sub.2, halo or lower alkylthio having one to four carbon atoms, and,each R' is independently selected from the group consisting of hydroxy, benzyloxy, lower alkyl having one to six atoms, lower alkenyl having two to six carbon atoms, lower alkoxy having one to six carbon atoms, lower alkylthio or halo-lower alkyl having one to six carbon atoms, halo, --NO.sub.2, --N(R.sup.1).sub.2, --NR.sup.1 CO.sub.2 R.sup.2, --NR.sup.1 COR.sup.2, and --NR.sup.1 C(O)N(R.sup.1).sub.2,in whicheach R.sup.1 is independently hydrogen or lower alkyl having one to four carbon atoms, or together form a piperidine or a piperazine ring optionally substituted at the ring nitrogen by lower alkyl having one to four carbon atoms or --CH.sub.2 CH.sub.2 OH;each R.sup.2 is independently lower alkyl having one to four carbon atoms,A is an alkylene group if R is hydrogen,or a pharmaceutically acceptable acid addition salt thereof.
    • 2-氧代-4H-3,1-苯并恶嗪-4-酮，其可用作丝氨酸蛋白酶抑制剂，由下式表示：其中：a为1的整数 到4; A是键或具有1-8个碳原子的亚烷基; R是氢，苯基，咪唑基或具有3至6个碳原子的环烷基，其中苯基，咪唑基或环烷基环任选地被1至3个独立地选自具有1至4个碳原子的低级烷基，低级烷氧基 具有1-4个碳原子的-N（R 1）2，-NO 2，卤素或具有1至4个碳原子的低级烷硫基，并且每个R'独立地选自羟基，苄氧基，具有一个至 六个原子，具有2-6个碳原子的低级烯基，具有1-6个碳原子的低级烷氧基，具有1-6个碳原子的低级烷硫基或卤代低级烷基，卤素，-NO 2，-N（R 1）2，-NR 1 CO 2 R 2， -NR1COR2和-NR1C（O）N（R1）2，其中每个R1独立地是氢或具有1-4个碳原子的低级烷基，或者一起形成在环氮上被低级烷基任意取代的哌啶或哌嗪环 具有1-4个碳原子或-CH 2 CH 2 OH; 每个R 2独立地是具有1-4个碳原子的低级烷基，如果R是氢，则A是亚烷基，或其药学上可接受的酸加成盐。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 10. 发明授权
      US4665070A 2-oxy-4H-3,1-benzoxazin-4-ones and pharmaceutical use 失效
    • 2-oxy-4H-3,1-benzoxazin-4-ones and pharmaceutical use
    • 2-氧基-4H-3,1-苯并恶嗪-4-酮和药物用途
    • US4665070A
    • 1987-05-12
    • US748631
    • 1985-06-25
    • Alexander Krantz , Robin Spencer , Tim Tam , Teng J. Liak
    • Alexander Krantz , Robin Spencer , Tim Tam , Teng J. Liak
    • C07D265/24 , A61K31/535 , A61K31/536 , A61P43/00 , C07D265/18 , C07D265/26 , C07F9/6533 , C07D265/36
    • C07D265/26 , C07F9/65335
    • 2-Oxy-4H-3,1-benzoxazin-4-ones represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-4;A is a bond, or alkylene having one to eight carbon atoms;R is hydrogen, phenyl, imidazolyl or cycloalkyl having three to six carbon atoms, wherein the phenyl, imidazolyl or cycloalkyl ring is optionally substituted with 1-3 substituents independently selected from the group consisting of lower alkyl having one to four carbon atoms, lower alkoxy having one to four carbon atoms, --N(R.sup.1).sub.2, --NO.sub.2, halo or lower alkylthio having one to four carbon atoms, and,each R' is independently selected from the group consisting of lower alkyl having one to six atoms, lower alkenyl having two to six carbon atoms, lower alkoxy having one to six carbon atoms,lower alkylthio or halo-lower alkyl having one to four carbon atoms, halo, --NO.sub.2, --N(R.sup.1).sub.2, ##STR2## --NR.sup.1 COR.sup.2, and ##STR3## in which each R.sup.1 is independently hydrogen or lower alkyl having one to four carbon atoms, or together form a piperidine or a piperazine ring optionally substituted at the ring nitrogen by lower alkyl having one to four carbon atoms or --CH.sub.2 CH.sub.2 OH,each R.sup.2 is independently lower alkyl having one to four carbon atoms,A is an alkylene group if R is hydrogen,and the pharmaceutically acceptable acid addition salts thereof are useful as serine protease inhibitors in humans and animals.
    • 由式（I）表示的2-氧代-4H-3,1-苯并恶嗪-4-酮及其药学上可接受的酸加成盐，其中：a为0-4的整数; A是键或具有1-8个碳原子的亚烷基; R是氢，苯基，咪唑基或具有3至6个碳原子的环烷基，其中苯基，咪唑基或环烷基环任选地被1-3个独立地选自具有1-4个碳原子的低级烷基，低级烷氧基 具有1-4个碳原子的-N（R 1）2，-NO 2，卤代或低级烷硫基，每个R'独立地选自具有1-6个原子的低级烷基，低级烷基 具有2-6个碳原子的烯基，具有1-6个碳原子的低级烷氧基，具有1-4个碳原子的低级烷硫基或卤代低级烷基，卤素，-NO 2，-N（R 1）2，-NR 1 COR 2和 其中每个R 1独立地为氢或具有1-4个碳原子的低级烷基，或者一起形成哌啶或哌嗪环，其任选在环氮上被具有1-4个碳原子的低级烷基或-CH 2 CH 2 OH取代，每个R 2 独立地是低级烷基 g为1-4个碳原子，如果R为氢，则A为亚烷基，其药学上可接受的酸加成盐可用作人和动物中的丝氨酸蛋白酶抑制剂。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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