Other

Alla Chem, LLC

Viriom, Inc.

R-pharm Overseas Inc.

Ivashchenko, Andrey Alexandrovich

R-pharm International LLC

Savchuk, Nikolay Filippovich

Ivachtchenko, Alexandre Vasilievich

Ivachtchenko, Alena Alexandrovna

Oleg Dmitrievich Mitkin

Alexandre Vasilievich Ivachtchenko

Andrey Alexandrovich Ivashchenko

Nikolay Filippovich Savchuk

Ilya Okun

Alexander Vasilievich Ivashchenko

Vadim Bichko

Sergey Yevgenievich Tkachenko

Yan Lavrovsky

Madina Georgievna Kadieva

Alexander Khvat

Volodymyr Mikhailovich Kysil

Alena Alexandrovna Ivachtchenko

Alexander Vasilievich Ivachtchenko

Alexandr Sergeevich Kyselvev

Pavel Mikhailovich Yamanushkin

Dmitri Vladimirovich Kravchenko

Evgueni Borisovich Frolov

Vladimir Yurievich Vvedensky

Vadim Valilievich Bichko

Anton Aleksandrovich Vorobev

Dmitry Vladimirovich Kravchenko

Alexandre Vasilievich Ivashchenko

Ilya Matusovich Okun

Yevgeniy Borisovich Frolov

Vadim Vasilievich Bichko

Andrey Sergeevich Trifilenkov

Influenza is an acute infectious respiratory disease caused by the influenza virus. It is part of the group of Acute Respiratory Viral Infections (ARVI). It occasionally spreads in the form of epidemics and pandemics. Currently, more than 2000 variants of the influenza virus differing in the antigen spectrum have been identified. Given that influenza is a serious threat to public health (worldwide, these annual epidemics lead to 3-5 million cases of severe illness, millions of hospitalizations, and up to 650,000 deaths), it seems appropriate to search for new anti-influenza drugs with improved characteristics. The inventors surprisingly found out that the previously unknown substituted 3,4,12,12a-tetrahydro-1H-[1,4] oxazino[3,4-c]pyrido[2,1-f] [1,2,4]triazine-6,8-dione of general formula 1, its stereoisomer, their prodrug, pharmaceutically acceptable salt, solvate, hydrate, and a crystalline or polycrystalline form thereof are effective agents for prophylaxis and treatment of viral diseases, including influenza whereRis (6,7-difluoro-5,10-dihydrothieno[3,2-c][2]benzothiepin-10-yl, (7,8-difluoro-4,9-dihydrothieno[2,23-c][2]benzothiepin-4-yl, (3,4-difluorophenyl)(phenyl)methyl, (3,4-difluorophenyl)(2-methylsulfanylphenyl)methyl, diphenylmethyl, bis(4-fluorophenyl)-methyl; Ris hydrogen or a protective group selected from a series comprising (C1-C3 alkyl) oxycarbonyloxy, {[(C1-C3 alkyl)oxycarbonyl]-oxy}methoxy, {[2-(C1-C3 alkyl) oxyethoxy]carbonyl}oxy, ({[(1R)-2-[(C1-C3alkyl)oxy]-1-methylethoxy} carbonyl)oxy, {[(3S)-ethoxyfuran-3-yloxy]-carbonyl}oxy, [(ethoxy-2H-pyran-4-yloxy) carbonyl]oxy, {[(1-acetylazetidine)-3-yloxy]carbonyl}oxy, {[(C1-C3alkyl) oxycarbonyl]-oxy}methoxy, ({[2-(C1-C3 alkyl)oxyethoxy]carbonyl}oxy) methoxy.

Substituted 3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione, pharmaceutical composition, method for the production and use thereof

The present invention relates to a prodrug and application thereof for the treatment of hepatitis C virus in patients. The prodrug of general formula 1, its stereoisomer, isotopically enriched analog, or crystalline or polymorphic form, 

Prodrug of an HCV NS5B polymerase inhibitor and method of production and application thereof

Nucleosides and nucleotides (nucleos(t)ides) have been in clinical use for almost 50 years and have become cornerstones of treatment for patients with viral infections or cancer. The approval of several additional drugs over the past decade demonstrates that this family still possesses strong potential. Therefore nucleos(t)ide are of great interest as promising chemotherapeutic agents, including: 2'-deoxy-L-uridine (CAS31501-19-6), 2&#x2032;-deoxy-D-uridine (CAS951-78-0), telbivudine (CAS3424-98-4), zidovudine (AZT, CAS30516-87-1), trifluridine (CAS70-00-8), clevudine (CAS163252-36-6), PSI-6206 (CAS863329-66-2), 2&#x2032;-(S)-2&#x2032;-chloro-2&#x2032;-deoxy-2&#x2032;-fluorouridine (CAS1673560-41-2), ND06954 (CAS114248-23-6), stavudine (CAS3056-17-5), 5-ethynyltavudine (Festinavir, CAS634907-30-5), torcitabine (CAS40093-94-5), (&#x2212;)-beta-D-(2R,4R)-dioxolane-thymine (DOT, 1-((2R,4R)-2-(hydroxymethyl)-1,3-dioxolan-4-yl)-5-methyl-2,4(1H,3H)-pyrimidinedione, CAS No. 127658-07-5), 2-(6-amino-purin-9-yl)-ethanol (CAS707-99-3), 2&#x2032;-C-methylcytidine (CAS20724-73-6), PSI-6130 (CAS817204-33-4), gemcitabine (CAS95058-81-4), 2&#x2032;-chloro-2&#x2032;-deoxy-2&#x2032;-fluorocytidine (CAS1786426-19-4), 2&#x2032;,2&#x2032;-dichloro-2&#x2032;-deoxycytidine (CAS1703785-65-2), 2&#x2032;-C-methylcytidine (CAS20724-73-6), PSI-6130 (CAS817204-33-4), lamivudine (3TC, CAS134678-17-4), emtricitabine (CAS143491-57-0), 2&#x2032;-deoxyadenosine (CAS958-09-8), 2&#x2032;-deoxy-&#x3b2;-L-adenosine (CAS14365-45-8), 2&#x2032;-deoxy-4&#x2032;-C-ethynyl-2-fluoroadenosine (CAS865363-93-5), didanosine (CAS69655-05-6), entecavir (CAS209216-23-9), FMCA (CAS1307273-70-6), dioxolane-G (DOG, CAS145514-01-8), &#x3b2;-D-2&#x2032;-deoxy-2&#x2032;-(R)-fluoro-2&#x2032;-&#x3b2;-C-methylguanosine (CAS No 817204-45-8), abacavir (ABC, CAS136470-78-5), dioxolane-A (DOA, CAS #145514-02-9), [(2R,4R)-4-(6-cyclopropylamino-purin-9-yl)-[1,3]dioxolan-2-yl]-methanol (CAS1446751-04-7), amdoxovir (AMDX, CAS145514-04-1), (R)-1-(6-amino-purin-9-yl)-propan-2-ol (CAS14047-28-0), and [(2S,5R)-5-(6-amino-purin-9-yl)-4-fluoro-2,5-dihydro-furan-2-yl]-methanol. Macroheterocyclic nucleoside derivative and its analog of the general formula 1 or general formula 2, a stereoisomer, isotope-enriched analog, pharmaceutically acceptable salt, hydrate, solvate, or crystalline or polymorphic form thereof, wherein: wherein: Ris the substituent selected from H, F, Cl, CH, OH;

Macroheterocyclic nucleoside derivatives and their analogues, production and use thereof

Compound represented by formula 1: or a pharmaceutically acceptable salt, a hydrate, a crystalline form, or a stereoisomer thereof, wherein:R1 is hydrogen, tert-butoxycarbonyl, where R11 is an optionally substituted C-Calkyl, an optionally substituted C-Ccycloalkyl, or an optionally substituted C-Calkyloxy, and arrows (&#x2190;) indicate the position of substituents attachment;R2 is hydrogen, halogen, or C-Calkyl;R3 is an optionally substituted aryl, an optionally substituted aryloxy, an optionally substituted arylsulfanyl, an optionally substituted arylamino, or an optionally substituted nitrogen hetaryl; 

Pan-genomic inhibitors of NS5A protein encoded by HCV, pharmaceutical compositions, intermediates for inhibitor synthesis, and their synthesis and application methods

The present invention relates to novel antiviral active 5-{4-[1H-imidazol-5-ylaryl(or hetaryl)]-buta-1,3-diynyl}-1H-imidazoles of the general formula 1 and pharmaceutically acceptable salt thereof, pharmaceutical composition, antiviral medicament, therapeutic kit for prophylaxis and treatment of hepatisis C virus diseases, and method for prophylaxis and treatment of hepatisis C. wherein:Rand R&#x2014;represent optionally identical radicals selected from 2.1 and 2.2, where an asterisk (*) denotes the position of attachment to the imidazole fragment, (S) and (R) are types of chiral centers; Ris isopropyl or phenyl radicals;Ar an aromatic or heteroaromatic diradical.

Substituted azoles, antiviral active component, pharmaceutical composition, method for preparation and use thereof

The present invention relates to novel cyclic N,N'-diarylurea&#x2014;androgen receptor antagonist, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of breast cancer disease. Cyclic N,N&#x2032;-diarylthioureas or N,N&#x2032;-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, 

Cyclic N,N'-diarylthiourea&#x2014;androgen receptor antagonist, anti breast cancer composition and use thereof

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 

Cyclic N,N'-diarylthioureas and N,N&#x2032;-diarylureas-androgen receptor antagonists, anticancer agent, method for preparation and use thereof

The instant invention relates to a novel compound representing a substituted phosphoramidic acid&#x2014;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).

Substituted (S)-(2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-ylmethyl aryl phosphoramidate

The present invention relates to novel substituted methyl-amines, serotonin 5-HTreceptor 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.

Substituted methyl amines, serotonin 5-HT6 receptor antagonists, methods for production and use thereof

The invention relates to the novel substituted 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines of the general formula 1, pharmaceutically acceptable salts and/or hydrates thereof, serotonin 5-HTreceptor antagonists and pharmaceutical compositions, and also to method for prophylaxis and treatment of various diseases of central nervous system at humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HTreceptors, in particular, Alzheimer's disease, Parkinson's disease, Huntington's disease, schizophrenia, and other neurodegenerative diseases, cognitive disorders and obesity. In the general formula 1: wherein: X=S, SO or NH; Rrepresents hydrogen, optionally substituted C-Calkyl, cycloalkyl, adamantyl, aryl or heterocyclyl; Rrepresents hydrogen, halogen, optionally substituted C-Calkyl, substituted hydroxyl, aryldiazenyl or optionally substituted amino group; Rrepresents hydrogen, optionally substituted C-Calkyl, substituted hydroxyl, pyridyl or optionally substituted amino group, besides, in cases when X=S or X=NH, at least one of R, Ror Rrepresent substituted C-Calkyl, cycloalkyl, adamantyl, aryl, heterocyclyl, halogen, substituted hydroxyl, optionally substituted amino group, aryldiazenyl, or at least two of R, Ror Rrepresent hydrogen; Rrepresents C-Calkyl; Rrepresents hydrogen, one or two halogens, C-Calkyl or optionally substituted hydroxyl.

Substituted 3-arylsulfonyl-pyrazolo[1,5-A]pyrimidines, serotonin 5-HT6 receptor antagonists and methods for the production and use thereof

The invention relates to antagonists of serotonin 5-HTreceptors simultaneously regulating homeostasis of Caions 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: Rrepresents amino group substituent selected from optionally substituted C-Calkyl; Ris one or more substituents selected from hydrogen, halogen, C-Calkyl, CF, OCF; Ar is phenyl optionally substituted with halogen, C-Calkyl, C-Calkoxy, substituted amino group, or CF; or optionally substituted aromatic 6-membered heterocycle comprising 1-2 nitrogen atoms in the cycle; W represents ethylene group &#x2014;CH&#x2014;CH&#x2014;, ethenyl group &#x2014;CH&#x2550;CH&#x2014;, or ethynyl group &#x2014;C&#x2261;C&#x2014;. 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.

Substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles, methods for the production and use thereof

The present invention relates to novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, to novel antiviral active ingredients, pharmaceutical compositions, antiviral medicaments, methods for prophylaxis and treatment of viral diseases particularly caused by influenza viruses and infectious hepatisis C (HCV) viruses. Novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, their esters of the general formula 1 and pharmaceutically acceptable salts and/or hydrates thereof have been disclosed wherein: Rrepresents amino group substituent selected from hydrogen, optionally substituted C-Calkyl, acyl or sulfonyl; Rand Rindependently of each other represent alkyl substituent selected from hydrogen, halogen, optionally substituted C-Calkyl, optionally substituted hydroxyl, optionally substituted amino group, optionally substituted aminomethyl, substituted mercapto group; Rrepresents hydrogen, optionally substituted lower C-Calkyl; Rrepresents cyclic system substituent selected from hydrogen, fluorine, trifluoromethyl, carboxy group, alkyloxycarbonyl, possibly substituted aryl, heterocyclyl, optionally substituted aminomethyl, cyano group; Rrepresents hydroxyl group substituent selected from hydrogen, optionally substituted C-Calkyl, acyl.

Substituted 2-(5-hydroxy-2-methyl-1H-indole-3-yl)acetic acids and ethers thereof and the use of same to treat viral diseases

The invention relates to novel substituted indoles, to the use thereof in the form of pharmacological composition substances and to use of said composition for producing medicinal preparations used for preventing and treating viral diseases, in particular caused by viruses of infectious hepatitis (HCV, HBV), human immune deficiency (HIV), atypical pneumonia (SARS) and bird flu. The invention proposes novel substituted indoles of general formula (1) or the racemates or the optical isomers or the pharmaceutically acceptable salts and/or hydrates thereof, wherein R, Rand Rindependently of each other are an aminogroup substituent selected for hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl, or Rand Rtogether with a nitrogen atom, with which they are bound, form through Rand Roptionally substituted azaheterocyclyl or guanidyl; Ris analkyl substituent selected from hydrogen, an optionally substituted mercaptogroup, optionally substituted aminogroup and optionally substituted hydroxyl; Ris lower alkyl, Ris an hydrogen atom or Rtogether with an oxygen atom with which it is linked or Rtogether with a nitrogen atom with which it is linked close, via Rand Ran oxazine cycle; Ris a cyclic system substituent selected for hydrogen, a halogen atom, cyanogroup, optionally substituted aryl or substituted heterocyclyl. 

Growing community of inventors

Khimki, Russia

Oleg Dmitrievich Mitkin