[EN] TERMINALLY MODIFIED POLYMERS AND CONJUGATES THEREOF<br/>[FR] POLYMÈRES MODIFIÉS EN EXTRÉMITÉ ET LEURS CONJUGUÉS
申请人:MERSANA THERAPEUTICS INC
公开号:WO2014008375A1
公开(公告)日:2014-01-09
A terminally modified polymer is provided herein. At least one terminus of the polymer is -O-(CH2)2-LM or -O-CH2-CH(OH)-CH2-CR1=CR2R3. LM, R1, R2, and R3 are defined herein Also disclosed are terminal conjugates comprising the polymer and a pharmaceutically useful modifier, as well as compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
[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.
SYNTHESIS OF CAROTENOID ANALOGS OR DERIVATIVES WITH IMPROVED ANTIOXIDANT CHARACTERISTICS
申请人:Foss Bente J.
公开号:US20090099061A1
公开(公告)日:2009-04-16
A method is described for synthesizing and administering carotenoid compounds with improved antioxidant characteristics. In some embodiments, extension or improvement of conjugation may be employed in structural modification of carotenoids. In other embodiments, reduction of ring/chain steric hindrance may improve the lambda max, and hence, the overall antioxidant capability, of particular compounds. In other embodiments, introduction and/or increase in synthetic handles for conjugation may improve the stoichiometric ratios of conjugating moieties to the polyene backbone. The methods may be used to improve natural and/or synthetic compounds for medicinal application in the treatment of disease.
A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L
D
-D, the protein based recognition-molecule being connected to the polymeric carrier by L
P
. Each occurrence of D is independently a therapeutic agent having a molecular weight ≦5 kDa. L
D
and L
P
are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L
D
-D, the protein based recognition-molecule being connected to the polymeric carrier by L
P
. Each occurrence of D is independently a therapeutic agent having a molecular weight ≦5 kDa. L
D
and L
P
are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.