The present invention relates to a compound of formula (I), wherein X is C═O, C═S or B—OH; Y is an electrophile and Z is a leaving group, or Y═Z is an electrophile; R.sup.1 comprises or consists of (a) (i) a first group binding to a proteolytic site of a proteasome, the first group being bound to X; and (ii) optionally a second group enhancing delivery; or (b) a group binding between subunits β1 and β2 of a proteasome; R.sup.2 and R.sup.3 are independently selected from H, methyl, methoxy, ethyl, ethenyl, ethynyl and cyano, wherein methyl and ethyl may be substituted with OH or halogen. ##STR00001##

The present invention relates to a compound of formula (I), wherein X is C═O, C═S or B—OH; Y is an electrophile and Z is a leaving group, or Y═Z is an electrophile; R.sup.1 comprises or consists of (a) (i) a first group binding to a proteolytic site of a proteasome, the first group being bound to X; and (ii) optionally a second group enhancing delivery; or (b) a group binding between subunits β1 and β2 of a proteasome; R.sup.2 and R.sup.3 are independently selected from H, methyl, methoxy, ethyl, ethenyl, ethynyl and cyano, wherein methyl and ethyl may be substituted with OH or halogen. ##STR00001##

The invention relates to a pharmaceutically active substance comprising at least one peptide portion having the amino acid sequences m-v-v-y-f-r (first peptide portion), characterised in that the pharmaceutically active substance comprises at least additional one amino acid and/or peptide portion at the N-terminal end and/or at the C-terminal end of the first peptide portion (second peptide portion and/or third peptide portion) being directly bound to the peptide portion having the amino acid sequences m-v-v-y-f-r (first peptide portion). The invention further relates to a pharmaceutical composition and a drug for the treatment of cancer.

The invention relates to a pharmaceutically active substance comprising at least one peptide portion having the amino acid sequences m-v-v-y-f-r (first peptide portion), characterised in that the pharmaceutically active substance comprises at least additional one amino acid and/or peptide portion at the N-terminal end and/or at the C-terminal end of the first peptide portion (second peptide portion and/or third peptide portion) being directly bound to the peptide portion having the amino acid sequences m-v-v-y-f-r (first peptide portion). The invention further relates to a pharmaceutical composition and a drug for the treatment of cancer.

Field of application: The invention relates to organic and bioorganic combinatorial chemistry, namely, to new combinatorial libraries of derivatives oligopeptides and supramolecular structures based on them, which when used without separation into individual components possess powerful antiviral properties. The essence of the invention: The invention is based on the task of synthesizing combinatorial derivatives of oligopeptides with antiviral properties and with a new mechanism of action, the use of which will significantly increase the effectiveness of treatment and reduce the treatment time for viral diseases such as influenza, herpes virus infections.

The present disclosure is directed to a pharmaceutical formulation intended for oral delivery of synthetic or natural poorly permeable molecules or salts/solvates thereof having a therapeutic activity. The pharmaceutical formulation can include a synthetic or natural poorly permeable molecule or salt or solvate thereof in an amount 0.01-10 wt. % of the total weight of the formulation; a lipophilic phase comprising triglycerides of fatty acids in an amount of 50-80 wt. % of the total weight of the formulation; and at least one lipophilic surfactant comprising partial esters of polyol and fatty acids in an amount of about 10-50 wt. % of the total weight of the formulation.

The present disclosure is directed to a pharmaceutical formulation intended for oral delivery of synthetic or natural poorly permeable molecules or salts/solvates thereof having a therapeutic activity. The pharmaceutical formulation can include a synthetic or natural poorly permeable molecule or salt or solvate thereof in an amount 0.01-10 wt. % of the total weight of the formulation; a lipophilic phase comprising triglycerides of fatty acids in an amount of 50-80 wt. % of the total weight of the formulation; and at least one lipophilic surfactant comprising partial esters of polyol and fatty acids in an amount of about 10-50 wt. % of the total weight of the formulation.

The invention relates to methods for treating traumatic brain injury by targeting specific innate and adaptive immune responses generated after the injury. The specific innate and adaptive immune responses may be targeted, for instance, using CLIP inhibitors, MIF antagonists and CD74 cleavage inhibitors and combinations thereof.

The invention relates to methods for treating traumatic brain injury by targeting specific innate and adaptive immune responses generated after the injury. The specific innate and adaptive immune responses may be targeted, for instance, using CLIP inhibitors, MIF antagonists and CD74 cleavage inhibitors and combinations thereof.

The invention relates to methods for treating traumatic brain injury by targeting specific innate and adaptive immune responses generated after the injury. The specific innate and adaptive immune responses may be targeted, for instance, using CLIP inhibitors, MIF antagonists and CD74 cleavage inhibitors and combinations thereof.