Title:
The Tranylcypromine derivative as inhibitor of hysterics Tonde methylase LSD1 and/or LSD2
Document Type and Number:
Japanese Patent JP5934184
Kind Code:
B2
Abstract:
Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R3 are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.
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Inventors:
Saverio Minucci
Antonello Mai
Andrea Matevi
Antonello Mai
Andrea Matevi
Application Number:
JP2013505423A
Publication Date:
June 15, 2016
Filing Date:
April 15, 2011
Export Citation:
Assignee:
Universita Degli Studio Di Roma La Sapienza
Fondazione Jeo
Universita Degli Studio Di Pavia
Universita Degli Studio Di Milan
Fondazione Jeo
Universita Degli Studio Di Pavia
Universita Degli Studio Di Milan
International Classes:
A61K31/167; C07C233/44; A61K31/27; A61K31/381; A61P31/12; A61P35/00; A61P35/02; C07C231/12; C07C233/80; C07C259/06; C07C269/06; C07C271/22; C07C271/28; C07C273/18; C07C275/16; C07D333/60
Domestic Patent References:
| JP2004502670A |
Foreign References:
| WO2010043721A1 | ||||
| WO2010084160A1 | ||||
| WO2010143582A1 | ||||
| WO2011035941A1 | ||||
| WO2005007614A1 | ||||
| WO1994027947A1 | ||||
| US5773644 | ||||
| WO2008117175A1 |
Other References:
GOODEN,DAVID M.,ET AL.,"Facile synthesis of substituted trans-2-arylcyclopropylamineinhibitors of the human histone demethylase LSD1 and monoamine oxidases A and B",BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2008年,VOL.18,NO.10,PP.3047-3051
BINDA,CLAUDIA,ET AL.,"Biochemical, Structural, and Biological Evaluation of Tranylcypromine Derivatives as Inhibitors of Histone Demethylases LSD1 and LSD2",JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,2010年,VOL.132,NO.19,PP.6827-6833
SCHMIDT,DAWN M. Z.,ET AL.,"trans-2-Phenylcyclopropylamine Is a Mechanism-Based Inactivator of the Histone Demethylase LSD1",BIOCHEMISTRY,2007年,VOL.46,NO.14,PP.4408-4416
CULHANE, JEFFREY C., ET AL.,"Comparative Analysis of Small Molecules and Histone Substrate Analogues as LSD1 Lysine Ddemethylase Inhibitors",JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,2010年,VOL.132,NO.9,PP.3164-3176
UEDA, RIE,ET AL.,"Identification of Cell-Active Lysine Specific Demethylase 1-Selective Inhibitors",JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,2009年,VOL.131,NO.48,PP.17536-17537
BINDA,CLAUDIA,ET AL.,"Biochemical, Structural, and Biological Evaluation of Tranylcypromine Derivatives as Inhibitors of Histone Demethylases LSD1 and LSD2",JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,2010年,VOL.132,NO.19,PP.6827-6833
SCHMIDT,DAWN M. Z.,ET AL.,"trans-2-Phenylcyclopropylamine Is a Mechanism-Based Inactivator of the Histone Demethylase LSD1",BIOCHEMISTRY,2007年,VOL.46,NO.14,PP.4408-4416
CULHANE, JEFFREY C., ET AL.,"Comparative Analysis of Small Molecules and Histone Substrate Analogues as LSD1 Lysine Ddemethylase Inhibitors",JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,2010年,VOL.132,NO.9,PP.3164-3176
UEDA, RIE,ET AL.,"Identification of Cell-Active Lysine Specific Demethylase 1-Selective Inhibitors",JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,2009年,VOL.131,NO.48,PP.17536-17537
Attorney, Agent or Firm:
Yasuhiko Murayama
Masatake Shiga
Takashi Watanabe
Shinya Mitsuhiro
Masatake Shiga
Takashi Watanabe
Shinya Mitsuhiro
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