Abstract: The present invention relates to NS5A inhibitors, to novel pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, in particular caused by hepatitis C (HCV) virus and hepatitis GBV-C virus. Alkyl [(S)-1-((S)-2-{5-[4-(4-{2-[(S)-1-((S)-2-methoxycarbonylamino-3-methyl-butyryl)-pyrrolidin-2-yl]-3 H-imidazol-4-yl}-buta-1,3-diynyl)-phenyl]-1H-imidazol-2-yl}-pyrrolidine-1-carbonyl)-2-methyl-propyl]-carbamate naphthaline-1,5-disulfonate of the general formula 1, possibly in crystalline or polycrystalline form, have been proposed, wherein: R is C1-C3 alkyl.

Abstract: The present invention relates to novel chemical compounds of the general formula 1—intermediate products in synthesis of androgen receptor inhibitors which are of interest as anticancer medicaments. The subject of the invention is also a method for preparation of novel compounds of the general formula 1.1—androgen receptor inhibitors. Substituted 3-(4-methylcarbamoyl-3-fluorophenylamino)tetrahydrofuran-3-encarboxylic acids, or their esters of the general formula 1, 1.1 and stereoisomers thereof, wherein: R1=C1-C4alkyl; R2=H, CH2OCH2CH2Si(CH3)3; wherein: R1=H, C1-C4alkyl; R2=H, CH2OCH2CH2Si(CH3)3.

Abstract: The invention relates to the field of pharmaceutics, in particular, to solid pharmaceutical composition comprising 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or pharmaceutically acceptable salt thereof, stabilizer, lubricant and filler; to method for preparation of pharmaceutical composition, to medicaments for immune suppression and treating multiple sclerosis. 2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol represents an immune modulator, which causes redistribution of lymphocytes from blood flow into secondary lymphoid tissue that leads to immune suppression. The invention provides uniform distribution of the active ingredient in the solid composition, high stability and improved flowability of the solid pharmaceutical composition. Due to the improved flowability the compositions suggested in the invention can be used on automated equipment.

Abstract: The present invention relates to novel cyclic N,N?-diarylurea—androgen receptor antagonist, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of breast cancer disease. Cyclic N,N?-diarylthioureas or N,N?-diarylureas of the general formula 1, their optical (R)- and (S)-isomers and pharmaceutically acceptable salts thereof exhibiting properties of androgen receptor antagonists have been proposed, wherein: R1 represents C1-C3 alkyl; R4 and R5 represent hydrogen; or R4 represents hydrogen, R5 represents methyl; or R4 represents methyl, R5 represents CH2R6 group in which R6 is C1-C3 alkoxycarbonyl, carboxyl, hydroxyl group optionally substituted with methyl or benzyl; or R4 and R5 together with the carbon atom they are attached to form 5- or 6-membered saturated heterocycle including at least one oxygen atom or nitrogen atom optionally substituted with methyl.

Abstract: The invention relates to novel N,N?-disubstituted 2-thioxo-7-oxa-1,3-diaza-spiro[4.4]nonan-4-one-androgen receptor (AR) antagonists, an anticancer agent, a pharmaceutical composition, a medicament, and a method for treating prostate cancer. 4-[3-(4-Cyano-3-trifluoromethyl-phenyl)-4-oxo-2-thioxo-7-oxa-1,3-diaza-spiro[4.4]non-1-yl]-2-fluoro-benzamide of general formula 1 and enantiomer thereof wherein: R represents C1-C3alkyl.

Abstract: The present invention relates to novel neuraminidase activity inhibitors and use thereof for prophylaxis and treatment of influenza infection, that is to fluorosubstituted4-acetamido-5-guanidino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylic acids and their esters of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, wherein R is hydrogen, an optionally substituted C1-C5alkyl, C2-C5alkenyl or C2-C5alkynyl; Rf is CH2F or CHF2. A pharmaceutical composition is provided, a method for its preparation, as well as a method for prophylaxis and treatment of viral diseases.

Abstract: The instant invention relates to a novel compound representing a substituted phosphoramidic acid—a (2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-yl)methyl aryl phosphoramidate of formula 1 or a (S)-(2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-yl)methyl aryl phosphoramidate of formula 2, or a pharmaceutically acceptable salt, a hydrate, a crystalline form or a stereoisomer thereof, as defined in the specification. The novel compound is used for a pharmaceutical composition with at least one pharmaceutically acceptable excipient as well as with an inosine 5 monophosphate dehydrogenase inhibitor, HCV protease NS3 inhibitor, HCV protease NS3/4A inhibitor, and RNA polymerase NS5A inhibitor. The novel compound is useful as a viral polymerase HCV NS5B inhibitor and can be used for treating a disease caused by hepatitis C virus (HCV).

Abstract: The invention relates to pharmacology and medicine, more particularly to novel pharmaceutical compositions and pharmaceutical kits for treating bacterial infections, and to novel method for treating diseases caused by bacterial infections including tuberculosis. The pharmaceutical composition is disclosed comprising Rifamycin and interferon inducer in pharmacologically effective doses, and also pharmaceutical kit for treating diseases caused by bacterial and healthcare acquired infections, comprising pharmacologically effective doses of Rifamycin in the form of a tablet, a capsule or an injection, interferon inducer in the form of a tablet, a capsule or an injection, and instruction for administration of the components of this pharmaceutical kit.

Abstract: The present invention relates to novel substituted methyl-amines, serotonin 5-HT6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and “molecular tools”, in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.

Abstract: The present invention relates to novel neuraminidase activity inhibitors and use thereof for prophylaxis and treatment of influenza infection, that is to fluorosubstituted4-acetamido-5-guanidino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylic acids and their esters of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, wherein R is hydrogen, an optionally substituted C1-C5alkyl, C2-C5alkenyl or C2-C5alkynyl; Rf is CH2F or CHF2. A pharmaceutical composition is provided, a method for its preparation, as well as a method for prophylaxis and treatment of viral diseases.

Abstract: The present invention relates to novel substituted methyl-amines, serotonin 5-HT6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and “molecular tools”, in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.

Abstract: The present invention relates to novel substituted tetrahydro-4H-thieno-pyrrolo[3,2-c]pyridines of the general formula 1, geometrical isomers, mixtures of geometrical isomers, and pharmaceutically acceptable salts thereof, wherein Th represents annelated thienic cycle; W represents ordinary bond (in this case R3 is bound directly to N-atom of pyrrole cycle), methylene, 1,2-ethylene, 1,2-vinyl, 1,2-ethynylene, 1,3-propanediyl or 1,3-propenylene, optionally substituted with hydroxy group; R1 and R2 represent hydrogen, C1-C4alkyl, halogen or —CH2OH; R3 represents hydrogen, optionally substituted phenyl, optionally substituted azaheteroaryl; R4 represents C1-C4alkyl, CO2C2H5 or CO2C(CH3)3; R5, R6, R7 independently of each other represent hydrogen or C1-C4alkyl, or R5 and R6 form together ethylene bridge, and R7 represents hydrogen, or R5 and R7 form together ethylene bridge, and R6 represents hydrogen.

Abstract: The present invention relates to novel azoles, novel antiviral active components of the general formulas 1A and 1B, pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, particularly caused by hepatitis C viruses (HCV). In general formulas 1A and 1B wherein: solid lines with accompanying dotted lines () represent ordinary bond or double bond, provided that one of them is an ordinary bond, the other one is double bond; X and Y accept various meanings, one of them is—nitrogen, the other—oxygen, sulfur or NH group; R1 and R2—optionally the same radicals selected from 2-(R)- and (S)-substituted N-acyl pyrrolidine derivatives; N-methyl-N-[2-(R) and (S)-substituted 2,2-disubstituted acetamides; methyl[2-(R) and (S)-substituted ((methyl)amino)-(1-oxobutan-2-yl)-2-(R)-] and (S)-iso-propyl)-carbamates.

Abstract: The present invention relates to novel cyclic N,N?-diarylurea-androgen receptor antagonist, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of breast cancer disease. Cyclic N,N?-diarylthioureas or N,N?-diarylureas of the general formula 1, their optical (R)- and (S)-isomers and pharmaceutically acceptable salts thereof exhibiting properties of androgen receptor antagonists have been proposed, wherein: R1 represents C1-C3 alkyl; R4 and R5 represent hydrogen; or R4 represents hydrogen, R5 represents methyl; or R4 represents methyl, R5 represents CH2R6 group in which R6 is C1-C3 alkoxycarbonyl, carboxyl, hydroxyl group optionally substituted with methyl or benzyl; or R4 and R5 together with the carbon atom they are attached to form 5- or 6-membered saturated heterocycle including at least one oxygen atom or nitrogen atom optionally substituted with methyl.

Abstract: The invention relates to antagonists of serotonin 5-HT6 receptors simultaneously regulating homeostasis of Ca+2 ions in cells, representing substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles of the general formula 1, pharmaceutically acceptable salts and/or hydrate thereof. In the general formula 1: R1 represents amino group substituent selected from optionally substituted C1-C5 alkyl; R2i is one or more substituents selected from hydrogen, halogen, C1-C3 alkyl, CF3, OCF3; Ar is phenyl optionally substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group, or CF3; or optionally substituted aromatic 6-membered heterocycle comprising 1-2 nitrogen atoms in the cycle; W represents ethylene group —CH2—CH2—, ethenyl group —CH?CH—, or ethynyl group —C?C—. The invention also relates to the novel compounds selected from the compounds of the general formula 1, methods for their preparation, pharmaceutical compositions and methods of their use.

Abstract: The invention relates to novel antiviral active components of the general formula 1, pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, particularly caused by hepatisis C viruses (HCV). In the general formula 1 R1 represents hydrogen, optionally substituted C1-C4 alkyl, C6 cycloalkyl, aryl, ethoxycarbonyl, nitro group; R2 represents hydrogen; R3 represents N-mono- or N,N-disubstituted 1-methylene-piperidine-3-carboxamide of the general formula 1a or N-mono- or N,N-disubstituted 1-methylene-piperidine-4-carboxamide of the general formula 1b; R4 represents hydrogen, optionally substituted C1-C3 alkyl; or R2 and R3 together with the C-atoms they are attached to form substituted 2,3,4,9-tetrahydro-1H-carbazole of the general formula 1.1, or R2, R3, and R4 together with the atoms they are attached to form substituted azaheterocycles of the general formula 1.

Abstract: The present invention relates to novel cyclic N,N?-diarylureas and N,N?-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer.

Abstract: The invention relates to antagonists of serotonin 5-HT6 receptors simultaneously regulating homeostasis of Ca+2 ions in cells, representing substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles of the general formula 1, pharmaceutically acceptable salts and/or hydrate thereof. In the general formula 1: R1 represents amino group substituent selected from optionally substituted C1-C5 alkyl; R2, is one or more substituents selected from hydrogen, halogen, C1-C3 alkyl, CF3, OCF3; Ar is phenyl optionally substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group, or CF3; or optionally substituted aromatic 6-membered heterocycle comprising 1-2 nitrogen atoms in the cycle; W represents ethylene group —CH2—CH2—, ethenyl group —CH?CH—, or ethynyl group —C?C—. The invention also relates to the novel compounds selected from the compounds of the general formula 1, methods for their preparation, pharmaceutical compositions and methods of their use.