Other

Avincuro Pharmaceuticals, Inc.

Alla Chem, LLC

Ivashchenko, Andrey Alexandrovich

Avineuro Pharmaceuticals, Inc.

Alexander Vasilievich Ivashchenko

Nikolay Filippovich Savchuk

Andrey Alexandrovich Ivashchenko

Oleg Dmitrievich Mitkin

Yan Lavrovsky

Volodymyr Mikhailovich Kysil

Ilya Okun

Vadim Bichko

Sergey Yevgenievich Tkachenko

Alexander Khvat

Madina Georgievna Kadieva

Sergey Malyarchuk

Pavel Mikhailovich Yamanushkin

Vladimir Yurievich Vvedensky

The invention relates to substituted 2-alkylsulfanyl-3-(arylsulfonyl)-cycloalkyl[e and d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, comprising the said conpounds as active ingredients, to novel medicaments and methods for treatment and prophylaxis of CNS diseases of humans and warm blooded animals pathogenesis of which is associated with 5-HT6 receptors. In general formulas 1 and 2 

Substituted cycloalcano[e and d] pyrazolo [1,5-a]pyrimidines/antagonists of serotonin 5-HT6 receptors and methods for production and the 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 present invention relates to serotonin 5-HTreceptor antagonists-novel substituted 3-sulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 3-sulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising drug substances as the mentioned above compounds and to the method of prophylaxis and treatment of various conditions and diseases of central nervous system in humans and warm-blooded animals pathogenesis of which is associated with serotonin 5-HTreceptors. In formulas 1 and 2 Ar is optionally substituted aryl or optionally substituted heterocyclyl; Ris hydrogen, optionally substituted lower C-Calkyl, substituted hydroxyl group, substituted sulfanyl group; Ris hydrogen or optionally substituted C-Calkyl; Ris hydrogen, optionally substituted C-Calkyl or tert.-butyloxycarbonyl.

Tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines as antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof

The invention relates to serotonin 5-HTreceptor antagonists&#x2014;novel 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines, drug substances and pharmaceutical compositions comprising the said drug substances as the said compounds, and also to method of prophylaxis and treatment of various diseases of central nervious system in humans and animals pathogenesis of which is associated with serotonin 5-HTreceptors including cognitive and neurodegenerative diseases. Substituted 2-amino-3-arylsulfonyl-6,7,8,9-tetrahydropyrazolo[1,5-a]pyrido[4,3-e]pyrimidines of the general formula 1 and substituted 2-amino-3-arylsulfonyl-5,6,7,8-tetrahydropyrazolo[1,5-a]pyrido[4,3-d]pyrimidines of the general formula 2 and pharmaceutically acceptable salts and/or hydrates thereof. wherein: Ar is optionally substituted aryl or optionally substituted heteroaryl; Ris hydrogen, optionally substituted C-Calkyl, C-Calkyloxycarbonyl; Ris hydrogen, halogen or optionally substituted C-Calkyl; Rand Rrepresent optionally alike: hydrogen, optionally substituted C-Calkyl or Rand Rtogether with the nitrogen atom to which they are attached form an optionally substituted azaheterocycle.

2-amino-3-sulphonyl-tetrahydro-pyrazolo[1,5-A]pyrido-pyrimidine antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof

The present invention relates to novel substituted 3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1 pharmaceutically acceptable salts and/or hydrates, to novel serotonin 5-HTreceptor antagonists, to novel drug substances, pharmaceutical compositions, medicaments and methods for their preparation and use for treatment and prophylaxis of pathological states and diseases of CNS, pathogenesis of which is associated with disturbance of serotonin 5-HTreceptor activation. In compounds of general formula 1 Ar represents optionally substituted aryl or heterocyclyl; R, Rand Rindependently of each other represent hydrogen, C-Calkyl or phenyl; Rrepresents hydrogen, optionally substituted C-Calkyl, substituted hydroxyl group or substituted sulfanyl group.

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The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of 'molecular pharmacological tools' for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins. The eight groups of the claimed compounds comprise the derivatives of 2,6-dihydro-7H-pyrazolo[3,4-d]pyridazine-7-one and 1,4-dihydropyrazolo[3,4-b][1,4]thiazine-5-one; N-acidylated 4-imidazo[1,2-a]pyrimidine-2-il-anilines; ([4H-thino[3,2-b]pyrrol-5-il) carbonyl]piperidine-4-carbonic acid amides; 2-(4carbomoilpyperidine-1-il)-isonicotinic acid amides; N-sylphonyl-1,2,3,4-tetrahydroquinoline-6-carbonic acid amides; and pyridine 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]N-acidylated 3-azole derivatives.

Heterocyclic inhibitors of an Hh-signal cascade, medicinal compositions based thereon and methods for treating diseases caused by the aberrant activity of an Hh-signal system

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 substituted 2-alkylamino-3-(arylsulfonyl)cycloalkyl[e or d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HTreceptor antagonists, to novel drug substances and pharmaceutical compositions comprising the said compounds as active ingredients, and to novel medicaments and method for treatment and prophylaxis of various CNS diseases. 2-Alkylamino-3-arylsulfonylcycloalkyl[e]pyrazolo[1,5-a]pyrimidines of general formula 1 and 2-alkylamino-3-arylsulfonylcycloalkyl[d]pyrazolo[1,5-a]pyrimidines of general formula 2, wherein: Ris hydrogen or C-Calkyl; Ris C-Calkyl; Ris hydrogen, one or more optionally identical halogen atoms, C-Calkyl or hydroxyl group optionally substituted with C-Calkyl; n is the whole numbers 1, 2 or 3.

(EN) 2-alkylamino-3-arylsulfonyl-cycloalcano [e OR d] pyrazolo [1,5-A]pyrimidines / antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof

The present invention relates to novel substituted 2-amino-3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1, to serotonin 5-HTreceptor antagonists, to novel drug substances and pharmaceutical compositions, to medicaments, methods for preparation thereof, and to methods for prophylaxis and treatment of various CNS diseases, pathogenesis of which is associated with disturbance of monoaminergic signaling pathways, more specifically over- or hypo-activation of serotonin 5-HTreceptors. Ar represents optionally substituted aryl or optionally substituted heterocyclyl; Rand Rindependently of each other represent C-Calkyl or aryl; Rrepresents hydrogen or C-Calkyl; R, and Rindependently of each other represent hydrogen, optionally substituted C-Calkyl or optionally substituted phenyl, or R, and Rtogether with nitrogen atom they are attached to form optionally substituted heterocyclyl.

(EN) substituted 2-amino-3-sulfonyl-pyrazolo[1,5-A] pyrimidines/antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof

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Encinitas, CA, United States of America

Alexander Vasilievich Ivashchenko