专利号:US-5521179-A 优先权日:1991-04-18 标题 :Heterocyclic amides 发明人:BERNSTEIN PETER R; SHAW ANDREW; THOMAS ROYSTON M; WARNER PETER; WOLANIN DONALD J 权利人:ZENECA LTD 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.
专利号:US-5728695-A 优先权日:1994-12-23 标题 :Spiroketal derivatives, compositions containing them and their use as therapeutic agents 发明人:HARRISON TIMOTHY; OWEN SIMON NEIL; SEWARD EILEEN MARY; SWAIN CHRISTOPHER JOHN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to spiroketal derivatives of formula (I) and pharmaceutically acceptable salts thereof wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 9a , R 9b , m and n are as defined in the specification, and to processes for their preparation, to intermediates used in their synthesis, to pharmaceutical compositions containing them, and to their use in therapy. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia. ##STR1##
专利号:EP-0693287-A1 优先权日:1994-07-18 标 题:RNA cleaving or binding oligonucleotides 发明人:PEYMAN ANUSCHIRWAN DR; UHLMANN EUGEN DR 权利人:HOECHST AG 摘要:There are therapeutic agents for inhibiting protein synthesis containing two antisense oligonucleotides AO-1 and AO-2 with about 6-100 nucleotides, which bind to the target RNA at an adjacent site and at the 5 'end or 3' -Ends are linked via suitable spacers to conjugate molecules A and B, the conjugate molecules A and B each not being reactive per se, but brought into spatial proximity, forming a unit, and thus able to cleave the RNA catalytically or activated by the spatial proximity leads to the covalent binding of RNA.
专利号:CN-106632268-A 优先权日:2016-11-18 标 题 :Synthesis method of calmodulin inhibitor for treating brain-derived diseases
[参考文献]: Junko Ohkanda, Et Al. Structure-Based Design Of Imidazole-Containing Peptidomimetic Inhibitors Of Protein Farnesyltransferase. Org Biomol Chem. 2006 Feb 7;4(3):482-92.
合成参考文献
参考文献:10.1016/j.bbrc.2023.08.050 摘要:Ikeda Y, Davis MI, Sumita K, Zheng Y, Kofuji S, Sasaki M, Hirota Y, Pragani R, Shen M, Boxer MB, Takeuchi K, Senda T, Simeonov A, Sasaki AT. Multimodal action of KRP203 on phosphoinositide kinases in vitro and in cells. Biochemical and Biophysical Research Communications. 2023 Oct;679():116–21. doi: 10.1016/j.bbrc.2023.08.050.