73930-39-9Relevant academic research and scientific papers
Tranylcypromine-Based LSD1 Inhibitors: Structure-Activity Relationships, Antiproliferative Effects in Leukemia, and Gene Target Modulation
Fioravanti, Rossella,Romanelli, Annalisa,Mautone, Nicola,Di Bello, Elisabetta,Rovere, Annarita,Corinti, Davide,Zwergel, Clemens,Valente, Sergio,Rotili, Dante,Botrugno, Oronza A.,Dessanti, Paola,Vultaggio, Stefania,Vianello, Paola,Cappa, Anna,Binda, Claudia,Mattevi, Andrea,Minucci, Saverio,Mercurio, Ciro,Varasi, Mario,Mai, Antonello
, p. 643 - 658 (2020/02/18)
Abstract: LSD1 is a lysine demethylase highly involved in initiation and development of cancer. To design highly effective covalent inhibitors, a strategy is to fill its large catalytic cleft by designing tranylcypromine (TCP) analogs decorated with long,
Site-Selective and Stereoselective C-H Functionalization of N-Cyclopropylamides via a Directed Remote Metalation Strategy
Ermolovich, Yuri,Barysevich, Maryia V.,Adamson, Jasper,Rogova, Oksana,Kaabel, Sandra,J?rving, Ivar,Gathergood, Nicholas,Snieckus, Victor,Kananovich, Dzmitry G.
supporting information, p. 969 - 973 (2019/02/14)
A new methodology for site-selective and stereoselective C-H functionalization of aminocyclopropanes via directed remote lithiation has been developed. Treatment of N-directing group (DG = pivaloyl, tetramethylsuccinimidoyl) arylcyclopropanes with t-BuLi
HDAC INHIBITORS, ALONE OR IN COMBINATION WITH BTK INHIBITORS, FOR TREATING CHRONIC LYMPHOCYTIC LEUKEMIA
-
Page/Page column 48, (2017/11/15)
Disclosed are histone deacetylase (HDAC) inhibitors, or combinations comprising an HDAC inhibitor and a Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of chronic lymphocytic leukemia in a subject in need thereof. Also provided herein are methods for treating chronic lymphocytic leukemia in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor, or a combination comprising an HDAC inhibitor and a BTK inhibitor. Other related methods are disclosed.
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4
Cheung, Mui,Bao, Weike,Behm, David J.,Brooks, Carl A.,Bury, Michael J.,Dowdell, Sarah E.,Eidam, Hilary S.,Fox, Ryan M.,Goodman, Krista B.,Holt, Dennis A.,Lee, Dennis,Roethke, Theresa J.,Willette, Robert N.,Xu, Xiaoping,Ye, Guosen,Thorneloe, Kevin S.
supporting information, p. 549 - 554 (2017/05/19)
Transient Receptor Potential Vanilloid 4 (TRPV4) is a member of the Transient Receptor Potential (TRP) superfamily of cation channels. TRPV4 is expressed in the vascular endothelium in the lung and regulates the integrity of the alveolar septal barrier. Increased pulmonary vascular pressure evokes TRPV4-dependent pulmonary edema, and therefore, inhibition of TRPV4 represents a novel approach for the treatment of pulmonary edema associated with conditions such as congestive heart failure. Herein we report the discovery of an orally active, potent, and selective TRPV4 blocker, 3-(1,4′-bipiperidin-1′-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide (GSK2193874, 28) after addressing an unexpected off-target cardiovascular liability observed from in vivo studies. GSK2193874 is a selective tool for elucidating TRPV4 biology both in vitro and in vivo.
HDAC INHIBITORS FOR THE TREATMENT OF DIABETIC PERIPHERAL NEUROPATHY
-
Paragraph 0117; 0118, (2017/06/23)
The invention relates to HDAC inhibitors for use in the treatment of diabetic peripheral neuropathy in a subject in need thereof. Also provided herein are methods for treating diabetic peripheral neuropathy in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor.
INCREASING EXPRESSION OF INTERFERON REGULATED GENES WITH COMBINATONS OF HISTONE DEACETYLASE INHIBITORS AND IMMUNOMODULATORY DRUGS
-
Page/Page column 53; 54, (2017/09/08)
Provided herein is a combination comprising an HDAC inhibitor and an IMiD for increasing interferon regulated gene expression or decreasing c-MYC gene expression in a cancer cell or tumor in a subject in need thereof. Increasing interferon regulated gene expression may result in increased recognition of tumors by innate or adaptive immune system and an increase in programmed cell death (apoptosis) gene expression, increasing apoptosis in cancer cells and tumors. The cells can be multiple myeloma cells or diffuse large B-cell lymphoma cells. Also provided are methods for treating myelodysplastic syndromes/acute myeloid leukemia (MDS/AML) or pathogen infections in a subject in need thereof comprising administering to the subject an effective amount of HDAC inhibitor and an IMiD. The HDAC inhibitor can be an HDAC6-selective inhibitor.
METHODS OF USE AND PHARMACEUTICAL COMBINATIONS OF HDAC INHIBITORS WITH BET INHIBITORS
-
Page/Page column 38, (2018/01/17)
The disclosure relates to pharmaceutical combinations comprising an HDAC6 selective inhibitor and a BET inhibitor for the treatment of cancer in a subject in need thereof. Also provided herein are methods for treating cancer in a subject in need thereof, comprising administering to the subject an effective amount of an HDAC6 selective inhibitor and a BET inhibitor.
TREATMENT OF LEUKEMIA WITH HISTONE DEACETYLASE INHIBITORS
-
Page/Page column 41; 42, (2016/01/25)
Provided herein are combinations comprising an HDAC inhibitor and azacitidine for the treatment of leukemia in a subject in need thereof. Provided herein are combinations comprising an HDAC inhibitor and azacitidine for the treatment of acute myelogenous leukemia in a subject in need thereof. Also provided herein are methods for treating leukemia in a subject in need thereof, comprising administering to the subject an effective amount of the above combination or an HDAC inhibitor, as well as methods for treating acute myelogenous leukemia in a subject in need thereof, comprising administering to the subject an effective amount of the above combination or an HDAC inhibitor.
PYRIMIDINE HYDROXY AMIDE COMPOUNDS FOR TREATING PERIPHERAL NEUROPATHY
-
Page/Page column 19-20, (2016/06/28)
The invention relates to HDAC inhibitors for the treatment of peripheral neuropathy in a subject in need thereof. Also provided herein are methods for treating peripheral neuropathy in a subject in need thereof comprising administering to the subject a th
COMBINATIONS OF HISTONE DEACETYLASE INHIBITORS AND BENDAMUSTINE FOR USE IN THE TREATMENT OF LYMPHOMA
-
Page/Page column 30, (2016/06/28)
The invention relates to pharmaceutical combinations comprising an HDAC inhibitor and bendamustine; pharmaceutical compositions comprising the same; and methods of using such combinations and compositions for treating lymphoma in a subject in need thereof.
