404385-38-2Relevant academic research and scientific papers
DIFLUOROHALOALLYLAMINE SULFONE DERIVATIVE INHIBITORS OF LYSYL OXIDASES, METHODS OF PREPARATION, AND USES THEREOF
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, (2021/01/29)
The present invention relates to methods for preparing a variety of difluorohaloallylamine derivatives. The present invention also relates to novel difluorohaloallylamine derivatives that are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for the treatment of a variety of indications, e.g., fibrosis, cancer and/or scarring in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as uses thereof.
HALOALLYLAMINE SULFONE DERIVATIVE INHIBITORS OF LYSYL OXIDASES AND USES THEREOF
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Paragraph 0252, (2020/02/23)
The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as i
INHIBITORS OF VAP-1
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Paragraph 0475-0476, (2020/05/12)
Provided herein are compounds and methods of use thereof for the modulation of VAP-1 activity.
Identification and Optimization of Mechanism-Based Fluoroallylamine Inhibitors of Lysyl Oxidase-like 2/3
Findlay, Alison D.,Foot, Jonathan S.,Buson, Alberto,Deodhar, Mandar,Jarnicki, Andrew G.,Hansbro, Philip M.,Liu, Gang,Schilter, Heidi,Turner, Craig I.,Zhou, Wenbin,Jarolimek, Wolfgang
, p. 9874 - 9889 (2019/11/03)
Lysyl oxidase-like 2 (LOXL2) is a secreted enzyme that catalyzes the formation of cross-links in extracellular matrix proteins, namely, collagen and elastin, and is indicated in fibrotic diseases. Herein, we report the identification and subsequent optimi
HALOALLYLAMINE PYRAZOLE DERIVATIVE INHIBITORS OF LYSYL OXIDASES AND USES THEREOF
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Paragraph 0180-0181, (2018/09/20)
The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as i
INDOLE AND AZAINDOLE HALOALLYLAMINE DERIVATIVE INHIBITORS OF LYSYL OXIDASES AND USES THEREOF
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Paragraph 0188, (2017/09/05)
The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as i
The discovery and development of selective 3-fluoro-4-aryloxyallylamine inhibitors of the amine oxidase activity of semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 (SSAO/VAP-1)
Foot, Jonathan S.,Deodhar, Mandar,Turner, Craig I.,Yin, Ping,Van Dam, Ellen M.,Silva, Diego G.,Olivieri, Aldo,Holt, Andrew,McDonald, Ian A.
scheme or table, p. 3935 - 3940 (2012/07/03)
A new class of 3-fluoroallyl amine-based SSAO/VAP-1 inhibitors is reported. These compounds have excellent selectivity over diamine oxidase, MAO-A and MAO-B. Synthesis and SAR studies leading to compound 28 (PXS-4159A) are reported. The pharmacokinetic profile of 28 in the rat, together with activity in a murine model of lung inflammation are also disclosed.
