Other

Alla Chem, LLC

Ivashchenko, Andrey Alexandrovich

R-pharm International LLC

Yan Lavrovsky

Andrey Alexandrovich Ivashchenko

Nikolay Filippovich Savchuk

Oleg Dmitrievich Mitkin

Ilya Okun

Alexander Vasilievich Ivashchenko

Sergey Yevgenievich Tkachenko

Ting Xu

Alexandre Vasilievich Ivachtchenko

Alexander Khvat

Kangping Guo

Vasily Ignatiev

Mikhail Samsonov

Alexey Repik

Madina Georgievna Kadieva

Dmitri Vladimirovich Kravchenko

Anna Krotkova

Sergey Malyarchuk

Evgueni Borisovich Frolov

Elena Batienko

Ilya Matusovich Okun

Yevgeniy Borisovich Frolov

Alexandre Vasilievich Ivashchenko

Tao Xu

A therapeutic composition is described that can be used for treating or prevention of diseases association with modulation of activity of human IL-1&#x3b2;. In certain aspects, the disclosed invention is based, on engineering of a heterodimeric protein assembly that is capable of binding to human IL-1&#x3b2; and attenuating its function. The heterodimeric protein assembly comprises extracellular portions of human IL1-R1 and of human IL-1RAcP, or their functional fragments. Each, the IL1-R1 portion and the IL-1RAcP portion, is fused to a distinct mutant of Fc portion of the human Ig Gamma-1. The two distinct Fc mutants in the heterodimeric protein assembly are engineered as to favor the heteromeric dimer formation between the two Fc mutants over any homomeric assembly. The therapeutic composition has been formulated for administration into humans and animals.

Human IL1-R1 derived inhibitor of IL-1&#x3b2;

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 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

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San Diego, CA, United States of America

Yan Lavrovsky