Abstract: Lipidated analogs of prolactin-releasing peptides (PrRP) and their use in controlling and lowering blood glucose in mammals is disclosed. Useful compounds included lipidated analogs of PrRP20 and PrRP31. Pharmacological effects are demonstrated both in vitro and in vivo. Peripheral administration of the lipidated peptides towers blood glucose levels. These treatments are applicable for treating impaired glucose tolerance (IGT), and glucose intolerance condition. The disclosed compounds have application in treating medical conditions including diabetes, pre-diabetes, eating disorders, and obesity.

Abstract: The disclosure provides compounds having formula (I): and the pharmaceutically acceptable salts thereof, wherein R1, R2, R2?, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

Abstract: Process for the preparation of azidoperfluoroalkanes and azidopolyfluoroalkanes of general formula RF—N3, where RF is chosen from a group containing CnF2n+1, CnFxH2n+1?x, CnFxX2n+1?x or R1CF2CF2, where n is an integer in the range of 1 to 10, x is an integer in the range of 2 to 20, X is Cl, Br, or I, R1 is C1-10 alkyl, ArO, ArS, imidazolyl, benzimidazolyl, or pyrazolyl and Ar is phenyl or substituted phenyl, by the reaction of electrophilic azidation reagent of general formula R2—N3, where R2 is n-C4F9SO2, ArSO2, Br, I, with synthetic equivalent of polyfluoroalkylated carbanion of general formula [RF]?.

Abstract: A macromolecular water-soluble conjugates based on synthetic copolymers to which at least one affinity tag, at least one imaging probe and at least one targeting ligand are bound via covalent bonds. The macromolecular conjugate may be used in identification, visualization, quantification or isolation of proteins and/or cells.

Abstract: A group of substituted thienopyrrolopyrimidine ribonucleosides of general formula I, in which R shows strong cytostatic and cytotoxic activities preferably against cancer cell lines of broad spectrum of diseases including tumors of various histogenetic origin.

Abstract: Substituted heteropentadieno-pyrrolopyrimidine ribonucleosides of general formula I, where R is selected from the group comprising furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl or chloro, and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers.

Abstract: A macromolecular water-soluble conjugates based on synthetic copolymers to which at least one affinity tag, at least one imaging probe and at least one targeting ligand are bound via covalent bonds. The macromolecular conjugate may be used in identification, visualization, quantification or isolation of proteins and/or cells.

Abstract: Synthetic analogs of general formula (I-A), (I-A) a-Ile-b-c-d-e-f-Lys-Lys-g-h-i-j-Ile-k-Lys-NH2 where a is Gly, Lys or ?-Ala; b is Met, Leu, Nle, Ile, Trp, Val or Phe; c is Ser, Lys, Arg or Orn; d is Ser, Lys, Arg or Orn; e is Leu, Nle, Ile, Trp, Val or Phe; f is Met, Leu, Nle, Ile, Trp, Val or Phe; g is Leu, Nle, Ile or Trp; h is Lys, Arg, Orn or Ala; i is Lys, Arg, Orn or Ala; j is Ile, Leu, Nle or His; k is Lys, Arg, Orn or Ala; where amino acids in all positions may be in D-configuration, and their use for the treatment of topical infections caused by pathogenic bacteria or yeasts.

Abstract: Synthetic macromolecular conjugate for selective interaction with proteins has a synthetic copolymer, and at least one binding group and at least one further group selected from an affinity tag and an imaging probe, and at least one binding group and at least one further group being bound via covalent bond to the synthetic copolymer. The macromolecular conjugate is suitable in particular for identification, visualization, quantification or isolation of proteins and/or cells.

Abstract: Amphiphilic compounds with tetradecahydrophenanthrene skeleton and their enantiomers, exhibiting neuroprotective effects, their use in methods of treatment of neuropsychiatric disorders associated with an imbalance in glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post-traumatic stress disorder and diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addiction, multiple sclerosis, epilepsy, glioma, and a pharmaceutical composition containing compound.

Abstract: Lipidated peptides, analogs of both forms of the prolactin-releasing peptide, PrRP31 and PrRP20, represent anorexigenic compounds that lower food intake and function in the brain after peripheral administration. The analogs PrRP31 and PrRP20 lipidated at the N-terminus by myristic or palmitic acids bind with high affinity to the endogenous receptor GPR10 in the rat pituitary cell line RC-4B/C and CHO cell line with transfected human receptor. These lipidated peptides also significantly decrease, in a dose-dependent manner, the food intake in fasted mice and have similar effects in comparable doses as centrally administered natural PrRP31, these effects are, however, stronger and longer lasting. Lipidation of an effective anorexigenic neuropeptide PrRP induces a central effect after peripheral administration and thus makes the lipidated analogs of PrRP a promising anti-obesity drug.

Abstract: Helquat derivatives of general formula I, in which substituents R1 and R2 are independently selected from a group comprising H and C1 to C4 alkyl, up to three of S1,2, S1?,2?, S3,4 and S3?,4? are present, each of S1,2, S1?,2?, S3,4 and S3?,4? independently represents a linker consisting of a bivalent hydrocarbon chain having 3-6 carbon atoms, preferably hydrocarbon chain having 4 carbon atoms, and one to four atoms selected from the carbon atoms with the descriptor 2, 4, 2?, and 4? are substituted with a substituent R3 of general formula II, wherein R4 is substituted or unsubstituted heteroaryl, T1 and T2 are independent linkers that bridge atoms N5 with C8 and N5? with C8?, wherein T1 and T2 independently represent a bivalent hydrocarbon chain having 2-5 carbon atoms, preferably 2 or 3 carbon atoms; and anions (X1)? and (X2)? independently represent anions of pharmaceutically acceptable salts.

Abstract: Synthetic analogs of general formula (I-A), (I-A) a-Ile-b-c-d-e-f-Lys-Lys-g-h-i-j-Ile-k-Lys-NH2 where a is Gly, Lys or ?-Ala; b is Met, Leu, Nle, Ile, Trp, Val or Phe; c is Ser, Lys, Arg or Orn; d is Ser, Lys, Arg or Orn; e is Leu, Nle, Ile, Trp, Val or Phe; f is Met, Leu, Nle, Ile, Trp, Val or Phe; g is Leu, Nle, Ile or Trp; h is Lys, Arg, Orn or Ala; i is Lys, Arg, Orn or Ala; j is Ile, Leu, Nle or His; k is Lys, Arg, Orn or Ala; where amino acids in all positions may be in D-configuration, and their use for the treatment of topical infections caused by pathogenic bacteria or yeasts.

Abstract: Macromolecular water-soluble conjugates based on synthetic copolymers to which at least one affinity tag, at least one imaging probe, and at least one targeting ligand are bound via covalent bonds. The macromolecular conjugate may be used in identification, visualization, quantification or isolation of proteins and/or cells. The targeting ligand may be attached to the synthetic copolymer via a flexible linker.

Abstract: Synthetic macromolecular conjugate for selective interaction with proteins has a synthetic copolymer, and at least one binding group and at least one further group selected from an affinity tag and an imaging probe, and at least one binding group and at least one further group being bound via covalent bond to the synthetic copolymer. The macromolecular conjugate is suitable in particular for identification, visualization, quantification or isolation of proteins and/or cells.

Abstract: Amphiphilic compounds with tetradecahydrophenanthrene skeleton and their enantiomers, exhibiting neuroprotective effects, their use in methods of treatment of neuropsychiatric disorders associated with an imbalance in glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post-traumatic stress disorder and diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addiction, multiple sclerosis, epilepsy, glioma, and a pharmaceutical composition containing compound.

Abstract: A method for detection of active form of analytes in a sample and/or for determination of ability of tested substances to bind to the active site of these analytes has the following steps: a) analyte or group of analytes from the sample is immobilized on the surface of a solid carrier; b) analyte or group of analytes is incubated with a detection probe; c) then the solid carrier is washed to remove unbound detection probe; and subsequently, the amount of bound detection probe is determined.

Abstract: Helquat derivatives of general formula I, in which substituents R1 and R2 are independently selected from a group comprising H and C1 to C4 alkyl, up to three of S1,2, S1?,2?, S3,4 and S3?,4? are present, each of S1,2, S1?,2?, S3,4 and S3?,4? independently represents a linker consisting of a bivalent hydrocarbon chain having 3-6 carbon atoms, preferably hydrocarbon chain having 4 carbon atoms, and one to four atoms selected from the carbon atoms with the descriptor 2, 4, 2?, and 4? are substituted with a substituent R3 of general formula II, wherein R4 is substituted or unsubstituted heteroaryl, T1 and T2 are independent linkers that bridge atoms N5 with C8 and N5? with C8?, wherein T1 and T2 independently represent a bivalent hydrocarbon chain having 2-5 carbon atoms, preferably 2 or 3 carbon atoms; and anions (X1)? and (X2)? independently represent anions of pharmaceutically acceptable salts.

Abstract: Lipidated neuropeptides based on PrRP31, PrRP20, containing C14 and/or C16 fatty acid, in which sequence of IRPVGRF-NH2 at the C-terminus is variable in the site of isoleucine, valine and phenylalanine; the fatty acid is bound in position 1 or 11 for PrRP31 or its analog and in position 1 or 7 for PrRP20 or its analog; the fatty acid is bound directly or through a hydrophilic linker X2, for use in the treatment and prevention of neurodegenerative diseases such as Alzheimer's disease (AD), Parkinson's disease (PD), cognitive impairment no dementia (CIND), brain trauma, and neurodegenerative changes and disorders.

Abstract: The present invention provides long-acting stable peptide ghrelin analogs of general formulae (I) (Sar)S(Dpr-X1)mLSPEHQKAQQRKESKKPPA(K-Z)LQPR,? and/or (II) (Sar)S(Dpr-X2)FLSPEHQKAQQR(K-Z)ES, in which Dpr is diaminopropionic acid, Sar is sarcosin, X1 represents a fatty acid residue selected from the group comprising octanoyl, decanoyl, myristoyl, 9-decenoyl and N-10-undecynoyl bound to Dpr through an amide bond, X2 represents decanoyl or myristoyl, m represents a non-coded amino acid selected from the group comprising phenylalanine, naphtylalanine, cyclohexylalanine, t-butylalanine and dichlorophenylalanine, Z is palmitoyl which can be optionally bound to the secondary amino group of lysine through an amide bond or Z is not present. The compounds of the invention are suitable for use in a method of treatment of cachexia and/or anorexia.