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Heterocyclic modulators of lipid synthesis for use against cancer and viral infections

A technology of heterocycles, compounds, in the field of lipid synthesis heterocycle regulators for use against cancer and viral infections

Active Publication Date: 2016-09-28
GANNEX PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The present disclosure addresses deficiencies in antiviral and anticancer therapy by providing novel heterocyclic modulators of lipid synthesis with improved antiviral and anticancer activities

Method used

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  • Heterocyclic modulators of lipid synthesis for use against cancer and viral infections
  • Heterocyclic modulators of lipid synthesis for use against cancer and viral infections
  • Heterocyclic modulators of lipid synthesis for use against cancer and viral infections

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0164] Synthesis of Compounds of the Disclosure

[0165] General: All reactions and manipulations described were performed in a well-ventilated fume hood. Operations and reactions under increased or reduced pressure are carried out behind explosion-proof barriers. Abbreviations: ACN, acetonitrile; AcOH, acetic acid; AIBN, azobisisobutyronitrile; BF 3 -Et 2 O, boron trifluoride diethyl etherate complex; (Boc) 2 O, di-tert-butyl dicarbonate; BuLi, butyllithium; CDI, 1,1′-carbonyldiimidazole; DBU, 1,8-diazabicyclo[5.4.0]undec-7-ene; DCE , 1,2-dichloroethane; DCM, dichloromethane or methylene chloride; DIEA, N,N-diisopropylethylamine; DMA, N,N-dimethylethylamine Amide; DMAP, 4-dimethylaminopyridine; DME, 1,2-dimethoxyethane; DMEDA-N,N'-dimethylethylenediamine; DMF, N,N-dimethylformamide ; DMSO, dimethylsulfoxide; DPPP, 1,3-bis(diphenylphosphino)propane; EDC, 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide; EDCI , 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride; ...

Embodiment 2

[0245] Activity of Compounds of the Disclosure

[0246] Inhibition of FASN by Compounds of the Disclosure

[0247] Determination of FASN biochemical activity: FASN enzyme was isolated from SKBr3 cells. SKBr3 is a human breast cancer cell line with high FASN expression levels. It is estimated that FASN accounts for approximately 25% of the cytosolic proteins in this cell line. SKBr3 cells were homogenized in a dounce homogenizer and then centrifuged at 4°C for 15 minutes to remove particulate matter. Supernatants were then analyzed for protein content, diluted to appropriate concentrations, and used to measure FASN activity. The presence of FASN was confirmed by Western blot analysis. A similar method for isolating FASN from SKBr3 cells is described in Teresa, P. et al. (Clin. Cancer Res. 2009; 15(24), 7608-7615).

[0248] FASN activity of extracts from SKBr3 cells was determined by measuring the amount of thiol-containing coenzyme A (CoA) oxidized or released by NADPH...

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Abstract

The invention discloses heterocyclic modulators of lipid synthesis for use against cancer and viral infections. According to the invention, also provided are heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and methods of treating conditions characterized by disregulation of a fatly acid synthase pathway by the administration of such compounds.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Patent Application No. 61 / 924,520 filed January 7, 2014. The foregoing applications are hereby incorporated by reference in their entirety. technical field [0003] The present disclosure generally relates to heterocyclic modulators of lipid synthesis and methods of their use. The heterocyclic modulators of lipid synthesis of the invention can be used to treat disorders characterized by dysregulation of fatty acid synthase function in a subject by modulating the fatty acid synthase pathway and / or fatty acid synthase function. Background technique [0004] Viral disease is a major health problem that threatens large numbers of people. Some of the characteristics associated with viral infection of interest to healthcare professionals include its highly infectious nature (eg, HIV, SARS, etc.) and high mutability. Some viruses are also onco...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/10C07D401/10C07D405/14A61K31/4155A61K31/454A61P31/14A61P31/16A61P31/22A61P31/20A61P31/12A61P31/18A61P35/00A61P35/02
CPCC07D401/10C07D403/10C07D405/14A61P31/12A61P31/14A61P31/16A61P31/18A61P31/20A61P31/22A61P35/00A61P35/02A61P37/02A61P43/00A61K31/337A61K2300/00A61K31/454A61K31/4155A61K45/06A61K31/704
Inventor A·S·韦格曼R·J·约翰逊C·A·扎哈里亚H·蔡L·W·胡G·杜克Y·欧豪T·霍耶尔M·欧法雷尔
Owner GANNEX PHARM CO LTD
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