Peptides, peptidomimetics and small molecules, collectively referred to as “decoy peptides”, are provided, which interfere with binding to a TIR domain of a toll-like receptor 4 (TLR4), and inhibit a TLR4-induced signaling pathway. These decoy peptides may be useful for treating diseases associated with induction of TLR4 signaling pathway such as a disease or disorder secondary to a cardiovascular disease, sepsis or an inflammatory disease.

The present application relates to compounds of Formula (I) and salts thereof. The compounds of Formula (I) have antibacterial and anti-biofilm activities. The present application also relates to compositions comprising the compounds of Formula (I) or salts thereof, methods of treating or preventing bacterial infections using the compounds of Formula (I) or salts thereof, and methods of inhibiting biofilm formation using the compounds of Formula (I) or salts thereof. ##STR00001##

The present invention discloses a polypeptide compound, a pharmaceutical composition, and a preparation method and use thereof. The structural formula of the polypeptide compound is shown in general formula (I):

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Such polypeptide compounds as κ-opioid receptor agonists have the advantages of better activity and the potential to become clinical candidate compounds.

The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

An object to be achieved by the present invention is to provide a technique for enhancing the anticancer effect of ubenimex; in particular, enhancing its anticancer effect on solid cancer. This object can be achieved by a compound containing a chain structure in which a plurality of ubenimex molecules is linked to a chain polymer.

Compounds useful for the treatment of malaria, cancer, Parkinson's disease, diabetes, and bacterial infection.

The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VI). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

Disclosed herein, inter alia, are methods of use and composition of novel inhibitors that target the Smac binding site of a variety of inhibitor of apoptosis proteins that contain a Bir domain, including XIAP, cIAP1, cIAP2, or other IAP proteins.

The present invention relates to a compound of formula (I), wherein X is CO, CS or BOH; Y is an electrophile and Z is a leaving group, or YZ is an electrophile; R.sup.1 comprises or consists of (a) (i) a first group binding to a proteolytic site of a proteasome, said first group being bound to X; and (ii) optionally a second group enhancing delivery; or (b) a group binding between subunits 1 and 2 of a proteasome; R.sup.2 and R.sup.3 are independently selected from H, methyl, methoxy, ethyl, ethenyl, ethinyl and cyano, wherein methyl and ethyl maybe substituted with OH or halogen.

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Compositions comprising an antioxidant directed or indirectly conjugated to an aromatic-cationic peptide are provide. Said antioxidants are selected from TEMPO, Tro, PBN, AHDP, DBHP, Caf and Hem and may be conjugated to the aromatic-cationic peptide directly or indirectly via a linker to the N-terminus, C-terminus or a side chain of an amino acid residue of the aromatic-cationic peptide. In some embodiments, the aromatic-cationic peptide is 2,6-Dmt-D-Arg-Phe-Lys-NH.sub.2, Phe-D-Arg-Phe-Lys-NH.sub.2 or D-Arg-2,6-Dmt-Lys-Phe-NH.sub.2. These conjugates have increased antioxidant activity as compared to the unconjugated aromatic-cationic peptide and have utility in treating complex regional pain syndrome.