4-AZETIDINYL-1-HETEROATOM LINKED-CYCLOHEXANE ANTAGONISTS OF CCR2
申请人:Zhang Xuqing
公开号:US20100267668A1
公开(公告)日:2010-10-21
The present invention comprises compounds of Formula (I).
wherein: X, R
1
, R
2
, R
3
, and R
4
are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
[EN] CEPHALOSPORIN DERIVATIVES USEFUL AS ß-LACTAMASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF<br/>[FR] DÉRIVÉS DE LA CÉPHALOSPORINE UTILES COMME INHIBITEURS DE LA ?-LACTAMASE ET LEURS COMPOSITIONS ET PROCÉDÉS D'UTILISATION
申请人:DMITRIENKO GARY IGOR
公开号:WO2011103686A1
公开(公告)日:2011-09-01
The present invention relates to cephalosporin derivatives having β- lactamase inhibitory activity. The compounds are useful in preventing or treating bacterial resistance to an antibiotic, e.g. a β-lactam antibiotic. Disclosed herein are compounds that are inhibitors of class B metallo-β-lactamases, as well as class A, C, and D serine β-lactamases. In some preferred embodiments, the compounds are 3'- thiobenzoate derivatives of a cephalosporin. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the compounds are also disclosed.
HETERO BIARYL DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS
申请人:Bunker Amy Mae
公开号:US20090029995A1
公开(公告)日:2009-01-29
This invention provides compounds defined by Formula I
or a pharmaceutically acceptable salt thereof,
wherein R
1
, Q, S, T, U, V, and R
2
are as defined in the specification. The invention also provides pharmaceutical compositions and methods of treating diseases.
[Object]: To provide a compound having a novel structure effective against
Hemophilus influenzae
and erythromycin resistant bacteria (for example, resistant pneumococci and streptococci) as well as against conventional erythromycin sensitive bacteria.
[Solution]: A novel 10a-azalide compound represented by the formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof, or an intermediate for the preparation of the same. The compound of the present invention has superior antibacterial activity against
Hemophilus influenzae
, erythromycin resistant pneumococci and the like, and therefore, the compound can be used as a therapeutic agent of infectious diseases.
A cephalosporin derivative of the formula I:
in which X is S, 0, CH2 or SO. R1 is (optionally- substituted)imidazol-2-yl or one of the C-7 acyl groups known in the cephalosporin art, R2 is hydrogen or methoxy, R3 is carboxy or a biodegradiable ester thereof and -R4 is of the formula XII, XIII or XIV: R35
in which R32-R40 inclusive are as defined in the specification; and the salts thereof. Pharmaceutical compositions methods of manufacture and intermediates are also described.