ARYL-SULPHONAMIDIC DIMERS AS METALLOPROTEASES INHIBITORS
申请人:Bracco Imaging S.p.A
公开号:EP2149568A1
公开(公告)日:2010-02-03
The invention relates to dimeric aryl-sulphonamido compounds endowed with inhibitory activity against metalloproteases MMP, having formula (I) below
(M)-L-(M') (I)
wherein M and M', the same or different from each other, represent the residues of the mctalloprotcascs inhibitors of formula (II)
wherein R, R1, R2, R3, G and n have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.
ANTIMICROBIAL HYDROGELS, METHODS OF PREPARATION THEREOF, AND ARTICLES THEREFROM
申请人:Coady Daniel Joseph
公开号:US20120231060A1
公开(公告)日:2012-09-13
A covalently crosslinked hydrogel comprises a) three or more divalent poly(alkylene oxide) chains P′ covalently linked at respective first end units to a branched first core group C′, b) three or more divalent poly(alkylene oxide) chains P″ covalently linked at respective first end units to a branched second core group C″, the chains P″ comprising respective second end units which are covalently linked to between 0% and 100% of respective second end units of chains P′ by divalent linking groups L″, and c) at least one pendant cationic block copolymer chain A′-B′. A′-B′ comprises i) a divalent block A′ comprising a poly(alkylene oxide) backbone chain having an end unit covalently linked to a second end unit of one of the chains P′ by a divalent linking group L′, and ii) a monovalent block B′ comprising a first repeat unit, the first repeat unit comprising a backbone carbonate group and a cationic side chain group.
Diagnostic Agents Selective Against Metalloproteases
申请人:Bracco Imaging S.p.A
公开号:EP2147684A1
公开(公告)日:2010-01-27
The invention relates to aryl-sulphonamido compounds endowed with affinity against metallo proteases MMP, having formula (I) below
wherein R, R1, R2, R3, G and n have the meanings reported in the specification, properly labelled with diagnostic imaging moieties or even radiotherapeutic moieties. The invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as diagnostic imaging agents or radiotherapeutic agents.
The present invention relates to compounds conformationally constrained mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
The invention provides certain nucleic acids (e.g., double stranded siRNA molecules), as well as conjugates that comprise a targeting moiety, a double stranded siRNA, and optional linking groups. Certain embodiments also provide synthetic methods useful for preparing the conjugates. The conjugates are useful to target therapeutic double stranded siRNA to the liver and to treat liver diseases including hepatitis (e.g. hepatitis B and hepatitis D).