[EN] POLYOXAZOLINE ANTIBODY DRUG CONJUGATES<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT DE POLYOXAZOLINE
申请人:SERINA THERAPEUTICS INC
公开号:WO2016019340A1
公开(公告)日:2016-02-04
In the present disclosure, polymer conjugates, including polymer-antibody-drug conjugates (polymer ADCs) are described, as well as the use of such conjugates to treat human disease. The polymer conjugates can contain a large number of polymer-bound agents, thus effectively increasing the drug antibody ration (DAR) of the antibody significantly beyond the currently available technology. This may be of particular importance when antibodies to low density antigens are used as target antibodies. The described polymer-ADCs have improved pharmacokinetics and solubility relative to traditional ADCs. The linker between agent and the polymer can be tailored to provide release of toxin at the desired site and under the desired conditions within the tumor. An additional feature of the polymer-ADCs of the current disclosure is that a purification moiety can be attached to the polymer backbone to provide ease of purification of the polymer-ADCs.
The invention concerns quinoline derivatives of Formula I
or a pharmaceutically-acceptable salt thereof, wherein each of X
1
, p, R
1
, q, R
2
, R
3
, R
4
, R
5
Ring A, r and R
6
has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
[EN] QUINAZOLINE DERIVATIVES FOR USE IN THE TREATMENT OF CANCER<br/>[FR] DERIVES DE QUINAZOLINE UTILISES DANS LE TRAITEMENT DU CANCER
申请人:ASTRAZENECA AB
公开号:WO2004004732A1
公开(公告)日:2004-01-15
The invention concerns quinazoline derivatives of Formula (I) wherein each of Z, m, R1, n, R3,Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive or anti-proliferative agent in the containment and/or treatment of solid tumour disease.
[EN] RENIN INHIBITORS<br/>[FR] INHIBITEURS DE LA RÉNINE
申请人:MERCK FROSST CANADA LTD
公开号:WO2009070869A1
公开(公告)日:2009-06-11
The present invention relates to piperidinyl-based renin inhibitor compounds having the formula containing amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.
Method and compounds for cancer treatment utilizing NFkB as a direct or ultimate target for small molecule inhibitors
申请人:Vander Jagt L. David
公开号:US20060258752A1
公开(公告)日:2006-11-16
A method is described for cancer treatment through NFκB inhibition. NFκB is a direct or ultimate target for small molecule inhibitors. These small molecule inhibitors are aimed at suppression of NFκB directly or by indirect suppression of IKK, SFK kinases, or other upstream kinases. The present invention includes small molecule inhibitors comprising three, five, and seven carbon unsaturated spacers having one or two carbonyls, flanked by substituted aryl rings. The small molecule inhibitors can be symmetrical or unsymmetrical.