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    Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses
    5.
    发明授权
    Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses 失效
    金属蛋白酶抑制剂，含有它们的药物组合物及其药物用途

    公开(公告)号：US5985900A

    公开(公告)日：1999-11-16

    申请号：US49949

    申请日：1998-03-30

    申请人： Steven L. Bender ,  Melwyn A. Abreo

    发明人： Steven L. Bender ,  Melwyn A. Abreo

    IPC分类号： C07C311/29 ,  C07C323/58 ,  C07C323/60 ,  C07D213/32 ,  C07D213/64 ,  C07D213/68 ,  C07D233/54 ,  C07D261/08 ,  C07D405/12 ,  C07D413/12 ,  A01N43/40 ,  A01N37/28 ,  A01N43/50 ,  A01N43/80

    CPC分类号： C07D213/64 ,  C07C311/29 ,  C07C323/58 ,  C07C323/60 ,  C07D213/32 ,  C07D213/68 ,  C07D233/64 ,  C07D261/08 ,  C07D405/12 ,  C07D413/12

    摘要： Compounds of the formula I: ##STR1## wherein Y is O or S, Ar is an aryl group or a heteroaryl group, R is H, an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, or --C(O)R.sub.1, wherein R.sub.1 is hydrogen, an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, or NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3 independently are hydrogen, an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, or a heteroaryl group, and X is --NH--OH or --OH. Pharmaceutically acceptable prodrugs, salts and solvates of these compounds. Methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt of solvate thereof. Pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates.

    摘要翻译： 式I化合物：其中Y是O或S，Ar是芳基或杂芳基，R是H，烷基，环烷基，杂环烷基，芳基，杂芳基或-C （O）R 1，其中R 1是氢，烷基，环烷基，杂环烷基，芳基，杂芳基或NR 2 R 3，其中R 2和R 3独立地是氢，烷基，环烷基， 杂环烷基，芳基或杂芳基，X是-NH-OH或-OH。 这些化合物的药学上可接受的前药，盐和溶剂合物。 通过施用式I化合物或其前药，其溶剂合物的盐来抑制金属蛋白酶的活性的方法。 包含有效量的这些化合物，前药，盐和溶剂合物的药物组合物。

    Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their pharmaceutical uses
    6.
    依法登记的发明
    Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their pharmaceutical uses 有权

    公开(公告)号：USH1992H1

    公开(公告)日：2001-09-04

    申请号：US09372064

    申请日：1999-08-11

    申请人： Steven L. Bender ,  Arlindo L. Castelhano

    发明人： Steven L. Bender ,  Arlindo L. Castelhano

    IPC分类号： C07D21132

    摘要： The present invention relates to compounds of formula I: wherein Ar is an aryl group or a heteroaryl group; X is —NH—OH or —OH; R1 is H, —CH(R3)(R4), —C(O)R3, a cycloalkyl group, a heterocycloalkyl group, an aryl group, or a heteroaryl group, wherein R3 is H or any suitable substituent and R4 is H, an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, or a heteroaryl group; R2 is CH2-R5, wherein R5 is H or any suitable substituent, or wherein R5 and R4 are optionally substituted carbon atoms singly- or double-bonded to one another; and pharmaceutically acceptable prodrugs, salts, and solvates thereof. The invention further relates to methods of using these compounds, particularly as metalloproteinase inhibitors.

    Photographic materials and processes comprising oxoindolizine and oxoindolizinium compounds
    7.
    发明授权
    Photographic materials and processes comprising oxoindolizine and oxoindolizinium compounds 失效
    摄影材料和方法，包括氧代二氢化茚和氧代吲哚啉鎓化合物

    公开(公告)号：US4368247A

    公开(公告)日：1983-01-11

    申请号：US278013

    申请日：1981-06-29

    申请人： George L. Fletcher, Jr. ,  Steven L. Bender ,  Donald H. Wadsworth

    发明人： George L. Fletcher, Jr. ,  Steven L. Bender ,  Donald H. Wadsworth

    IPC分类号： C09B57/00 ,  C07D471/04 ,  G03C1/73 ,  G03C1/52

    CPC分类号： C07D471/04 ,  G03C1/73

    摘要： Oxoindolizine and oxoindolizinium dyes are useful in photographic materials and processes as image dyes. These dyes are formed in unexposed areas of photographic materials, especially photothermographic materials, by the reaction of a photosensitive cyclopropenone with a pyridine compound. Oxoindolizine and oxoindolizinium dyes are alternatively formed by (1) reaction of a photosensitive cyclopropenone with a pyridine compound and (2) reaction of the resulting product with a color forming coupler. The photographic material is imagewise exposed and then heated to a processing temperature to form a dye image. Alternatively, the oxoindolizine and oxoindolizinium dyes are produced by imbibing at least one of the reactants into the photographic material comprising a photosensitive cyclopropenone.

    摘要翻译： 氧代吲哚啉和氧代吲哚ium嗪染料可用作照相材料和作为图像染料的方法。 这些染料通过感光环丙烯酮与吡啶化合物的反应在照相材料的未曝光区域，特别是光热照相材料中形成。 氧化吲哚啉和氧代吲哚ium嗪染料可以通过（1）光敏环丙烯酮与吡啶化合物的反应和（2）所得产物与形成成色剂的反应形成。 将照相材料成像曝光，然后加热至加工温度以形成染料图像。 或者，通过将至少一种反应物吸收到包含光敏环丙烯酮的照相材料中来制备氧代取代二氮杂和氧代吲哚ium嗪染料。

    Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses, and methods and intermediates useful for their preparation
    9.
    发明授权
    Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses, and methods and intermediates useful for their preparation 失效
    金属蛋白酶抑制剂，含有它们的药物组合物及其药物用途，以及可用于其制备的方法和中间体

    公开(公告)号：US06849732B2

    公开(公告)日：2005-02-01

    申请号：US10298842

    申请日：2002-11-18

    申请人： Scott E. Zook ,  Raymond Dagnino, Jr. ,  Michael E. Deason ,  Steven L. Bender ,  Michael J. Melnick

    发明人： Scott E. Zook ,  Raymond Dagnino, Jr. ,  Michael E. Deason ,  Steven L. Bender ,  Michael J. Melnick

    IPC分类号： C07D239/04 ,  C07D241/04 ,  C07D279/12 ,  C07D401/12 ,  C07D417/12

    CPC分类号： C07D401/12 ,  C07D239/04 ,  C07D241/04 ,  C07D279/12 ,  C07D417/12

    摘要： The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder are carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates. The invention still further relates to methods and intermediates useful for preparing these compounds, prodrugs, salts, and solvates.

    摘要翻译： 本发明涉及式1化合物：其中：Z为O或S; V是与C *和N一起形成具有六个环原子的环的二价基团，其中除C *和N之外的所述环原子各自独立地是未取代的或被合适的取代基取代，并且所述另一个环中的至少一个 原子是选自O，N和S的杂原子，其余为碳原子; Ar为芳基或杂芳基; 及其药学上可接受的前药，其盐和溶剂化物。 本发明还涉及这些化合物的药学上可接受的前药，盐和溶剂化物。 本发明还涉及通过给予式I化合物或其前药，盐或溶剂化物来抑制金属蛋白酶活性的方法。 本发明还涉及包含有效量的这些化合物，前药，盐和溶剂合物的药物组合物。 本发明还涉及可用于制备这些化合物，前药，盐和溶剂合物的方法和中间体。