Axiom Biotechnologies, Inc.

Other

Alla Chem, LLC

Albert Einstein College of Medicine

Ilya Okun

Alex Okun

Nikolay Filippovich Savchuk

Sergey Yevgenievich Tkachenko

Andrey Alexandrovich Ivashchenko

Alexander Khvat

Oleg Dmitrievich Mitkin

John Ransom

Yan Lavrovsky

Jean-Michel Andre Vernier

William Charles Ripka

David J Matthews

Alexandre Vasilievich Ivachtchenko

Alexander Vasilievich Ivashchenko

Ulrich G Steidl

Boris Rogovoy

Volodymyr Mikhailovich Kysil

Gregory Kaler

Patrick O'Connor

John May

Ashley M Eckel

Evgueni Borisovich Frolov

Dmitri Vladimirovich Kravchenko

Borys Rogovoy

Robert F Stanley

Sergey Malyarchuk

Alexandr Sergeevich Kyselvev

Alexander Vasilievich Ivachtchenko

Methods are disclosed for treating acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS) using compounds that inhibit p21 protein (Cdc42/Rac)-activated kinase (PAK1).

PAK1 inhibitors and uses 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

Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary diseases and disorders.

Antagonist of smoothened

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 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. 

Substituted indoles and a method for the production and use thereof

An apparatus and method for real-time measurement of a cellular response of a test compound or series of test compounds ( ) on a flowing suspension of cells ( ), in which a homogenous suspension of each member of a series of cell types ( ) is combined with a concentration of a test compound ( ), directed through a detection zone ( ), and a cellular response of the living cells is measured in real time as the cells in the test mixture are flowing through the detection zone ( ). The apparatus may be used in automated screening of libraries of compounds, and is capable of real-time variation of concentrations of test and standard compounds and generation of dose/response profiles within a short timespan.

Apparatus and method for real-time measurement of cellular response

Sensitive methods for identifying compounds having biological activity comprising combining living cells with two fluorescent membrane permeable ionic dyes having the same charge sign, the first of which has an emission spectrum which overlaps the excitation spectrum of the second fluorescent membrane penetrative dye. The fluorescence is then induced by illuminating the dyes at a wavelength corresponding to the excitation spectrum of the first fluorescent dye and emission is then registered at a wavelength corresponding to the emission spectrum of the second fluorescent dye (FRET). The change in the FRET is indicative of a modulation of cell membrane potential by the biologically active compounds.

Methods of registering trans-membrane electric potentials

An apparatus and method for real-time measurement of a cellular response of a test compound or series of test compounds (,) on a flowing suspension of cells (,), in which a homogeneous suspension of each member of a series of cell types (,) is combined with a concentration of a test compound (,), directed through a detection zone (,), and a cellular response of the living cells is measured in real time as the cells in the test mixture are flowing through the detection zone (,). The apparatus may be used in automated screening of libraries of compounds, and is capable of real-time variation of concentrations of test and standard compounds and generation of dose/response profiles within a short time span.

Cell flow apparatus and method for real-time of cellular responses

Cell flow apparatus and method for real-time measurements of cellular responses

An apparatus and method for real-time measurement of a cellular response of a test compound or series of test compounds (303) on a flowing suspension of cells (349), in which a homogeneous suspension of each member of a series of cell types (349) is combined with a concentration of a test compound (303), directed through a detection zone (355), and a cellular response of the living cells is measured in real time as the cells in the test mixture are flowing through the detection zone (355). The apparatus may be used in automated screening of libraries of compounds, and is capable of real-time variation of concentrations of test and standard compounds and generation of dose/response profiles within a short timespan.

Apparatus and method for compound profiling of living cells

An apparatus and method for real-time measurement of a cellular response of a test compound or series of test compounds on a flowing suspension of cells in which a homogeneous suspension of living cells is combined with a concentration of a test compound, directed through a detection zone, and a cellular response of the living cells is measured in real time as the cells in the test mixture are flowing through the detection zone. The apparatus may be used in automated screening of libraries of compounds, and is capable of real-time variation of concentrations of test and standard compounds and generation of dose/response profiles within a short timespan.

Growing community of inventors

San Diego, CA, United States of America

Ilya Okun