公开(公告)号：US5441960A

公开(公告)日：1995-08-15

申请号：US44866

申请日：1993-04-08

申请人： Peter R. Bernstein ,  Philip D. Edwards ,  Andrew Shaw ,  Royston M. Thomas ,  Chris A. Veale ,  Peter Warner ,  Donald J. Wolanin

发明人： Peter R. Bernstein ,  Philip D. Edwards ,  Andrew Shaw ,  Royston M. Thomas ,  Chris A. Veale ,  Peter Warner ,  Donald J. Wolanin

IPC分类号： A61K38/55 ,  A61K38/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P29/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/08 ,  A61K31/505 ,  C07D239/22

CPC分类号： C07K5/0205 ,  C07K5/06191 ,  A61K38/00

摘要： The present invention relates to certain novel substituted ketones which are 1-pyrimidinylacetamide derivatives of formula I, ##STR1## set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates ##STR2## useful in the synthesis of these substituted ketones processes for preparing the substituted ketones pharmaceutical compositions containing such substituted ketones and methods for their use.

摘要翻译： 本发明涉及作为人白细胞弹性蛋白酶（HLE）抑制剂（也称为人嗜中性粒细胞弹性蛋白酶（HNE））的式I所示的1-嘧啶基乙酰胺衍生物的某些新的取代酮，其为 如果需要这种抑制作用，例如在药理学，诊断和相关研究中的研究工具以及涉及HLE的哺乳动物的疾病的治疗中是有用的。 本发明还包括可用于合成这些取代酮的中间体制备含取代酮的取代酮的药物组合物的方法及其使用方法。

公开(公告)号：US5254558A

公开(公告)日：1993-10-19

申请号：US930568

申请日：1992-08-14

申请人： Peter R. Bernstein ,  Philip D. Edwards ,  Royston M. Thomas ,  Chris A. Veale ,  Peter Warner ,  Donald J. Wolanin

发明人： Peter R. Bernstein ,  Philip D. Edwards ,  Royston M. Thomas ,  Chris A. Veale ,  Peter Warner ,  Donald J. Wolanin

IPC分类号： A61K31/505 ,  A61K38/00 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P29/00 ,  C07D239/46 ,  C07D239/47 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D409/04 ,  C07D409/14 ,  C07K5/06 ,  C07K5/08 ,  C07D239/22

CPC分类号： C07D239/47 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D409/04 ,  C07D409/14 ,  C07K5/06191 ,  A61K38/00

摘要： The present invention relates to certain novel substituted heterocycles which are 1-pyrimidinylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted heterocycles, processes for preparing the substituted heterocycles, pharmaceutical compositions containing such substituted heterocycles and methods for their use.

公开(公告)号：US5486529A

公开(公告)日：1996-01-23

申请号：US45496

申请日：1993-04-08

申请人： Peter R. Bernstein ,  Andrew Shaw ,  Royston M. Thomas ,  Chris A. Veale ,  Peter Warner ,  Donald J. Wolanin

发明人： Peter R. Bernstein ,  Andrew Shaw ,  Royston M. Thomas ,  Chris A. Veale ,  Peter Warner ,  Donald J. Wolanin

IPC分类号： A61K38/55 ,  A61K38/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P29/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K5/08 ,  A61K31/44 ,  C07D211/84 ,  C07D213/81 ,  C07D401/12

CPC分类号： C07K5/06191 ,  C07K5/0205 ,  C07K5/06139 ,  A61K38/00

摘要： The present invention relates to certain novel heterocyclic ketones which are 1-pyridylacetamide ketones of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic ketones, processes for preparing the heterocyclic ketones, pharmaceutical compositions containing such heterocyclic ketones and methods for their use.

摘要翻译： 本发明涉及作为人类白细胞弹性蛋白酶（HLE）抑制剂（也称为人嗜中性粒细胞弹性蛋白酶（HNE））的本文列出的作为式I的1-吡啶基乙酰胺酮的某些新型杂环酮，只要这种抑制 是期望的，例如在药理学，诊断和相关研究中的研究工具以及涉及HLE的哺乳动物的疾病的治疗。 本发明还包括可用于合成这些杂环酮的中间体，制备杂环酮的方法，含有该杂环酮的药物组合物及其使用方法。

公开(公告)号：US5521179A

公开(公告)日：1996-05-28

申请号：US045009

申请日：1993-04-08

申请人： Peter R. Bernstein ,  Andrew Shaw ,  Royston M. Thomas ,  Peter Warner ,  Donald J. Wolanin

发明人： Peter R. Bernstein ,  Andrew Shaw ,  Royston M. Thomas ,  Peter Warner ,  Donald J. Wolanin

IPC分类号： A61K38/00 ,  C07K5/06 ,  C07D237/00 ,  C07D211/72 ,  C07D215/14 ,  C07D401/00

CPC分类号： C07K5/06191 ,  A61K38/00

摘要： The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.

摘要翻译： 本发明涉及某些新颖的杂环酰胺，它们是本文列出的式I的1-吡啶基乙酰胺化合物，其是人类白细胞弹性蛋白酶（HLE）的抑制剂，也被称为人嗜中性粒细胞弹性蛋白酶（HNE）），使得它们在这种抑制 是期望的，例如在药理学，诊断和相关研究中的研究工具以及涉及HLE的哺乳动物的疾病的治疗。 本发明还包括可用于合成这些杂环酰胺的中间体，制备杂环酰胺的方法，含有这种杂环酰胺的药物组合物及其使用方法。