[EN] 2,5-DIOXOIMIDAZOLIDIN-4-YL ACETAMIDES AND ANALOGUES AS INHIBITORS OF METALLOPROTEINASE MMP12. [FR] 2,5-DIOXOIMIDAZOLIDINE-4-YL ACETAMIDES ET ANALOGUES SERVANT D'INHIBITEURS DE LA METALLOPROTEINASE MMP12.
[EN] 2,5-DIOXOIMIDAZOLIDIN-4-YL ACETAMIDES AND ANALOGUES AS INHIBITORS OF METALLOPROTEINASE MMP12. [FR] 2,5-DIOXOIMIDAZOLIDINE-4-YL ACETAMIDES ET ANALOGUES SERVANT D'INHIBITEURS DE LA METALLOPROTEINASE MMP12.
The present invention relates to metalloprotein inhibitors comprising: a. an organic substituent and at least one zinc binding group (ZBG) covalently attached thereto; or
b. a ZBG substituted by a side chain wherein the ZBG is of formula (I):
wherein X is O or S and each R
1
, R
2
, R
3
, and R
4
is individually hydrogen or an organic radical. The metalloprotein inhibitors are useful for preventing or treating a pathological disease, condition, or symptom that is associated with pathological metalloprotein activity and/or that is alleviated by inhibition of said activity.
DIPROVOCIMS: A NEW AND POTENT CLASS OF TLR AGONISTS
申请人:The Scripps Research Institute
公开号:EP3445758B1
公开(公告)日:2020-11-04
[EN] EPOXIDE INHIBITORS OF CYSTEINE PROTEASES<br/>[FR] INHIBITEURS ÉPOXYDE DE CYSTÉINE PROTÉASES
申请人:UNIV LELAND STANFORD JUNIOR
公开号:WO2008042480A2
公开(公告)日:2008-04-10
[EN] Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent. [FR] La présente invention concerne de nouveaux inhibiteurs époxyde de cystéine protéases, des compositions contenant ces inhibiteurs époxyde, et des produits pharmaceutiques conditionnés. L'invention concerne également des procédés d'inhibition d'une cystéine protéase appartenant à la famille de la papaïne et des procédés de traitement ou de prévention d'une maladie grâce à l'administration d'une composition contenant un inhibiteur époxyde selon l'invention. Les compositions peuvent être administrées sous forme combinée à un autre agent thérapeutique.
[EN] 2,5-DIOXOIMIDAZOLIDIN-4-YL ACETAMIDES AND ANALOGUES AS INHIBITORS OF METALLOPROTEINASE MMP12.<br/>[FR] 2,5-DIOXOIMIDAZOLIDINE-4-YL ACETAMIDES ET ANALOGUES SERVANT D'INHIBITEURS DE LA METALLOPROTEINASE MMP12.
申请人:ASTRAZENECA AB
公开号:WO2004020415A1
公开(公告)日:2004-03-11
The invention provides compounds of formula (I) in which L, X, Y, Z1, Z2, R1, R2, R3 and G2 have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds of the invention are inhibitors of metalloproteinase MMP12 and are among other things useful for the treatment of obstructive airways diseases, such as asthma and chronic obstructive pulmonary disease (COPD).