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    Novel use for carbamoyl benzoates
    4.
    发明授权
    Novel use for carbamoyl benzoates 失效
    氨基甲酰苯甲酸的新用途

    公开(公告)号：US4873232A

    公开(公告)日：1989-10-10

    申请号：US924246

    申请日：1986-10-29

    申请人： Alexander Krantz ,  John M. Young

    发明人： Alexander Krantz ,  John M. Young

    IPC分类号： A61K31/19

    CPC分类号： A61K31/19

    摘要： Novel alkoxycarbonylamino benzoates and related copounds (carbamoyl benzoates) are disclosed for treatment of auto-immune disease states, such as arthritis.

    摘要翻译： 公开了新型烷氧基羰基氨基苯甲酸酯和相关的助剂（氨基甲酰苯甲酸酯）用于治疗自身免疫疾病状态，例如关节炎。

    2-oxy-4H-3,1-benzoxazin-4-ones and related compounds and pharmaceutical use
    5.
    发明授权
    2-oxy-4H-3,1-benzoxazin-4-ones and related compounds and pharmaceutical use 失效
    2-氧-4H-3,1-苯并恶嗪-4-酮及相关化合物及药物用途

    公开(公告)号：US4745116A

    公开(公告)日：1988-05-17

    申请号：US945751

    申请日：1986-12-23

    申请人： Alexander Krantz ,  Robin Spencer ,  Tim Tam ,  Teng J. Liak

    发明人： Alexander Krantz ,  Robin Spencer ,  Tim Tam ,  Teng J. Liak

    IPC分类号： C07D265/26 ,  C07F9/6533 ,  A61K31/535 ,  C07D265/36

    CPC分类号： C07D265/26 ,  C07F9/65335

    摘要： 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.

    摘要翻译： 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。

    2-oxy-4H-3,1-benzoxazin-4-ones and pharmaceutical use
    6.
    发明授权
    2-oxy-4H-3,1-benzoxazin-4-ones and pharmaceutical use 失效
    2-氧基-4H-3,1-苯并恶嗪-4-酮和药物用途

    公开(公告)号：US4665070A

    公开(公告)日：1987-05-12

    申请号：US748631

    申请日：1985-06-25

    申请人： Alexander Krantz ,  Robin Spencer ,  Tim Tam ,  Teng J. Liak

    发明人： Alexander Krantz ,  Robin Spencer ,  Tim Tam ,  Teng J. Liak

    IPC分类号： C07D265/24 ,  A61K31/535 ,  A61K31/536 ,  A61P43/00 ,  C07D265/18 ,  C07D265/26 ,  C07F9/6533 ,  C07D265/36

    CPC分类号： C07D265/26 ,  C07F9/65335

    摘要： 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.

    摘要翻译： 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。

    Affinity markers for human serum albumin
    9.
    发明申请
    Affinity markers for human serum albumin 失效
    人血清白蛋白的亲和标记

    公开(公告)号：US20050037974A1

    公开(公告)日：2005-02-17

    申请号：US10934841

    申请日：2004-09-02

    申请人： Alexander Krantz ,  Wolin Huang ,  Arthur Hanel ,  Darren Holmes ,  Dominique Bridon

    发明人： Alexander Krantz ,  Wolin Huang ,  Arthur Hanel ,  Darren Holmes ,  Dominique Bridon

    IPC分类号： A61K38/00 ,  A61K47/48 ,  A61K49/00 ,  C07K14/665 ,  A61K38/08 ,  C07K7/06

    CPC分类号： A61K49/0021 ,  A61K38/00 ,  A61K47/62 ,  A61K47/6901 ,  A61K49/0043 ,  A61K49/0056 ,  C07K14/665

    摘要： 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 a group having an affinity for human serum albumin, wherein affinity group A comprises a sequence of amino acid residues —O1—O2—X1—X2—B in which the amino acid residues are independently selected from the group of all twenty naturally occurring amino acids. 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.

    摘要翻译： 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由式E-Ca-R-Cb-A描述，其中E是治疗或诊断剂，R是反应性基团，Ca和Cb是E和R之间的连接基团，R和 A，A是对人血清白蛋白具有亲和性的基团，其中亲和基团A包含氨基酸残基-O1-O2-X1-X2-B的序列，其中氨基酸残基独立地选自 的二十种天然存在的氨基酸。 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。

    Affinity labeling libraries with tagged leaving group
    10.
    发明授权
    Affinity labeling libraries with tagged leaving group 失效
    具有标记离去基团的亲和标记库

    公开(公告)号：US06403324B1

    公开(公告)日：2002-06-11

    申请号：US09042234

    申请日：1998-03-13

    申请人： Alexander Krantz ,  Arthur M. Hanel ,  Wolin Huang

    发明人： Alexander Krantz ,  Arthur M. Hanel ,  Wolin Huang

    IPC分类号： G01N3353

    CPC分类号： C40B30/04 ,  B01J2219/00592 ,  G01N33/6845

    摘要： Methods and compositions are provided for identifying compounds having affinity to a target site. The method provides for the affinity group to be a leaving group from a reactive functionality capable of forming a covalent bond to the target site. One can combine the compound comprising the target site with the library, and assay for the resulting composition of the leaving groups. The leaving groups having the highest concentration can be identified as the groups having the binding highest affinity for the target site. The selected compounds may then 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 proteins or as an enzyme inhibitor.

    摘要翻译： 提供方法和组合物用于鉴定对靶位点具有亲和性的化合物。 该方法提供了亲和基团为能够与靶位点形成共价键的反应性官能团的离去基团。 可以将包含靶位点的化合物与文库结合，并测定所得离去基团的组成。 具有最高浓度的离去基团可以被鉴定为对靶位点具有最高亲和力的结合基团。 然后可以将所选择的化合物用于标记靶分子，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。 通过体内的亲和标记，通过与长寿命血液成分结合，可以大大提高生理活性物质的寿命。 共价结合的实体还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。