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Anti-cancer agents based on N-acyl-2, 3-dihydro-1H-pyrrolo[2,3-b] quinoline derivatives and a method of making

United States Patent

April 16, 2013
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The present disclosure relates to novel compounds that can be used as anti-cancer agents in the prostate cancer therapy. In particular, the invention relates to N-acyl derivatives of 2,3-dihydro-1H-pyrrolo[2,3-b]quinolines having the structural Formula (I), ##STR00001## stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or pharmaceutically acceptable salt and/or solvate thereof. The meaning of R1 is independently selected from H; C1-C6 Alkyl, cyclo-Alkyl or iso-Alkyl substituents; R2 is selected from C1-C6 Alkyl, cyclo-Alkyl or iso-Alkyl; substituted or non-substituted, fused or non-fused to substituted or non-substituted aromatic ring, aryl or heteroaryl groups. The invention also relates to methods for preparing said compounds, and to pharmaceutical compositions comprising said compounds.
Gakh; Andrei A. (Bethesda, MD), Krasavin; Mikhail (Moscow, RU), Karapetian; Ruben (Moscow, RU), Rufanov; Konstantin A. (Moscow, RU), Konstantinov; Igor (Moscow, RU), Godovykh; Elena (Rostov-Na-Donu, RU), Soldatkina; Olga (Moscow, RU), Sosnov; Andrey V. (Moscow, RU)
U.S. Department of Energy (Washington, DC)
12/ 822,237
June 24, 2010
CONTRACTUAL ORIGIN OF THE INVENTION The U.S. Government has certain rights in the present invention pursuant to Contract No. #3548 between the Department of Energy (DOE) (International Science and Technology Center) and the Chemical Diversity Research Institute, dated Jul. 1, 2007.