Other

Dogwood Pharmaceuticals, Inc.

Selvita S.a.

National Institutes of Health, a Component of the US Dept. of Health & Human Services

The United States of America As Represented by the Department of Health

Avalon Pharmaceuticals, Inc.

Wieslaw Marek Cholody

Janak Khimchand Padia

Yi Zang

Jeffrey William Strovel

Karina Zuck

Jeffrey W H Watthey

Zoe Ohler

Sheela Chellappan

Christopher J Michejda

Michal Galezowski

Wojciech Czardybon

Krzysztof Brzózka

Mariusz Milik

Tomasz Rzymski

Katarzyna Wiklik

Aleksandra Sabiniarz

Renata Windak

Raymond Horvath

Magdalena Zawadzka

Pawel Guzik

Gene Ohler

Ewelina Wincza

Stanislaw Wieslaw Pikul

Marta Prokop

Stanislaw Pikul

Norman Eugene Ohler

Norman E Ohler

Valentina Petukhova

Sean O'Brien

Teresa Kosakowska-Cholody

Lidia Hernandez

Jeffrey Strovel

Krzysztof BRZÓZKA

Jeffrey WH Watthey

Janak Padia

Krzysztof Brzozka

The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3- and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.

Benzimidazole derivatives as kinase inhibitors

Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/&#x3b2;-catenin signaling pathway, and serve to reduce &#x3b2;-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.

Derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine and uses thereof

Benzimidazole derivatives as Kinase Inhibitors

The invention provides novel, water-soluble 2-aminoimidazoline derivatives having general Formula (I) as well as some precursors of Formula (I), which are very potent inducers of G2/M cell cycle arrest. In treated tumor cells, compounds of Formula (I) give gene expression profile distinct from known antimitotic agents. The invention also provides methods for preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools. 

Derivatives of 1-(substituted sulfonyl)-2-aminoimidazoline as antitumor and antiproliferative agents

Chemical agents of the general formula (I) and (II), such as derivatives of 3-hydroxy-pyrrole containing hydroxamic acid, and including salts thereof, that modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.

Derivatives of 3-hydroxy-pyrrole-2,4-dicarboxylic acid and uses thereof

The invention provides imidazoacridone compounds of general formula (1) which have cytotoxic and anti-tumor activity. The invention also provides methods of preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools.

1,8-naphthalimide imidazo&lcub;4,5,1-de&rcub;acridones with anti-tumor activity

The present invention provides an anticancer compound having the structure: ##STR1## wherein R is --H, --CH.sub.3, or --C.sub.2 H.sub.5 ; R1 and R2 are independently --H, --OH, --NH.sub.2, --OCH.sub.3, --C(CH.sub.3).sub.3, or a halogen atom; n is 2 to 6; X and X' are independently --N or --NO.sub.2 ; Y and Y' are independently --N, --CH, or --H; and the double-slash represents a double bond or no bond; such that when X or X' is --N, Y or Y' is --CH or --N, and the double-slash is a double bond, and when X or X' is --NO.sub.2, Y or Y' is --H, and the double-slash is no bond. The present invention also provides a pharmaceutical composition comprising the compound above and a pharmaceutically acceptable carrier.

Bis-acridone chemotherapeutic derivatives

Growing community of inventors

Frederick, MD, United States of America

Wieslaw Marek Cholody