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Fused ring inhibitors of hepatitis c

一种杂环、环烷基的技术，应用在非结构性5A蛋白功能的化合物领域，能够解决副作用、致衰弱、治疗作出反应等问题

Inactive Publication Date: 2012-04-25
PRESIDIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The therapy is complex and sometimes has debilitating and severe side effects, and many patients do not consistently respond to treatment

Method used

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  • Fused ring inhibitors of hepatitis c
  • Fused ring inhibitors of hepatitis c
  • Fused ring inhibitors of hepatitis c

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 11-5

[0903] Example 1.1-5, (2S,2′S)-1,1′-((2S,2′S)-2,2′-(5,5′-(dibenzo[b,e][1 , 4] Dioxin-2,7-diyl)bis(1H-imidazole-5,2-diyl))bis(pyrrolidine-2,1-diyl))bis(3-methyl Of dimethyl-1-oxobutane-2,1-diyl) dicarbamate

[0904] Step 1. At -78 ℃, dibenzo-p-dioxin (1-1) (5.0g, 27.14mmol) and chloroacetyl chloride (4.5mL, 57mmol) in dichloromethane (50mL) The solution was added to a stirred suspension of aluminum chloride (14.5 g, 108.6 mmol) in dichloromethane (300 mL) over 20 minutes, and the reaction mixture was stirred at -78°C for 15 minutes and allowed to warm up over 30 minutes To room temperature. The reaction mixture was then heated at 50°C for 3 hours and stirring was continued overnight at room temperature. The reaction was cooled to 0°C and carefully quenched with ice-cold water (250 mL). The volatiles were removed in vacuo, the formed precipitate was collected by vacuum filtration, washed with diethyl ether, and dried under vacuum at 50°C to obtain the crude product 1-2 (8.85g,...

Embodiment 2

[0909] Preparation of Example 2.1-4B

[0910]

[0911] Follow the general procedure A described above for the synthesis of 1-4, and replace N-Boc-L-proline with N-Boc-L-pipecolic acid in step a to obtain the compound in a yield of 60% 1-4B (0.82g). LC-MS(ESI): m / z 681[M-H] - .

Embodiment 3

[0912] Preparation of Example 3.1-5B

[0913]

[0914] Following general procedure B, and replacing 1-4A with compound 1-4B, compound 1-5B is obtained. LC-MS(ESI): m / z 797[M+H] + .

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PUM

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Abstract

Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.

Description

[0001] Related application statement [0002] This application claims the rights of U.S. Provisional Application No. 61 / 164,342 filed on March 27, 2009 and U.S. Provisional Application No. 61 / 214,883 filed on April 28, 2009. Invention field [0003] The present invention relates to compounds suitable for inhibiting the replication of hepatitis C virus ("HCV"), especially compounds that inhibit the function of the non-structural 5A ("NS5A") protein of HCV. Background of the invention [0004] HCV is a single-stranded RNA virus and is a member of the Flaviviridae family. The virus exhibits extensive genetic heterogeneity, with currently seven confirmed genotypes and more than 50 confirmed subtypes. In HCV-infected cells, viral RNA is translated into polyproteins, which are cleaved into ten single proteins. At the amino terminus are structural proteins: core (C) protein and envelope glycoproteins, E1 and E2, and p7, which are integral membrane proteins after E1 and E2. In addition, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N37/00A61K31/21
CPCC07D417/14C07D413/14C07D405/14A61P1/16A61P29/00A61P31/12A61P31/14C07D403/14A61K31/498
Inventor L·李M·钟
Owner PRESIDIO PHARMA
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