Heterocyclic modulators of lipid synthesis and combinations thereof

A technology of fatty acid synthase and compounds, applied in the direction of active ingredients of heterocyclic compounds, drug combinations, medical preparations containing active ingredients, etc., can solve problems such as anemia, impaired nutrient absorption, side effects, etc.

Active Publication Date: 2016-10-26
GANNEX PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition to limited clinical success, devastating side effects accompany classic treatments
Both radiation-based therapy and cytotoxicity-based therapy result in destruction of rapidly dividing hematopoietic and intestinal epithelial cells, resulting in impaired immune function, anemia, and impaired nutrient absorption

Method used

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  • Heterocyclic modulators of lipid synthesis and combinations thereof
  • Heterocyclic modulators of lipid synthesis and combinations thereof
  • Heterocyclic modulators of lipid synthesis and combinations thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0678] Synthesis of Compounds of the Disclosure

[0679] General: All reactions and manipulations described were performed in a well-ventilated fume hood. Manipulations and reactions under high or reduced pressure are performed behind explosion-proof shields. Abbreviations: ACN: acetonitrile; AcOH: acetic acid; AIBN: azobisisobutyronitrile; BF 3 -Et 2 O: boron trifluoride diethyl ether; (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-dimethylacetamide ; 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; EtOAc: ethyl acetate;...

Embodiment 2

[2099] Activity of Compounds of the Disclosure

[2100] antiviral activity

[2101] The antiviral activity of the compounds was assessed using the HCV1b replicon system. The replicon was constructed using the ET (luc-ubi-neo / ET) cell line, a Huh7 human with a stable luciferase (Luc) reporter gene and three cell culture-adaptive mutations Liver cancer cell lines (Pietschmann et al. (2002) J. Virol. 76:4008-4021). HCV Replicon Antiviral Evaluation Assay The effect of compounds at ten triplicate dilutions was studied. Subconfluent cultures of ET cell lines were seeded into 96-well plates dedicated to analysis of cell viability (cytotoxicity) or antiviral activity, and the next day, drugs were added to the appropriate wells. After 72 hours, cells were processed while still subconfluent. Determination of EC 50 Value (concentration that suppresses 50% of HCV RNA replicons), CC 50 value (concentration that reduces cell viability by 50%) and SI value (selection index: CC 50...

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Abstract

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 fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of U.S. Provisional Patent Application No. 61 / 919,235, filed December 20, 2013, pursuant to 35 U.S.C. § 119(e). The foregoing application is incorporated herein by reference in its entirety. technical field [0003] The present disclosure generally relates to heterocyclic modulators of lipid synthesis and methods of use thereof. The heterocyclic modulators of lipid synthesis of the invention can be used to treat a condition in a subject characterized by dysfunctional fatty acid synthase by modulating the fatty acid synthase pathway and / or fatty acid synthase function. Background technique [0004] Viral diseases are a significant health problem that threatens large segments of the population. Some of the characteristics associated with viral infection that are of concern to healthcare professionals include its highly contagious (eg HIV, SARS, etc.) and highly mutagenic. Some viru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/10C07D403/10C07D403/14C07D407/14A61K31/4155A61K31/4178A61K31/4188A61K31/422A61P31/12A61P35/00
CPCA61K31/4155A61K31/422C07D401/10C07D403/10C07D403/14C07D407/14A61K31/337A61K31/4196A61K31/437A61K31/445A61K31/453A61K31/454A61K31/5377A61K31/55A61K31/4178A61K31/4525A61K31/4545A61K31/496A61P1/18A61P11/00A61P31/12A61P31/14A61P35/00A61P35/02A61P37/06A61P43/00A61K2300/00
Inventor T·S·霍耶尔J·D·奥斯洛布R·S·麦克道尔R·约翰逊H·杨M·伊万奇克C·A·扎哈里亚H·蔡L·W·胡G·杜克Y·欧豪M·欧法雷尔
Owner GANNEX PHARM CO LTD
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