Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Benzodiazapine compounds containing imidazole propanamido and its preparing process and application

A technology containing imidazole propionamide group and imidazole propionamide group, which is applied in the fields of benzodiazepine compounds, transferase activity, and farnesyl protein transferase inhibitors, and can solve the problem of poor selectivity of enzymes and cells, Compound activity is not high, to achieve the effect of inhibiting the growth of cancer

Inactive Publication Date: 2004-12-15
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] However, the activity of these compounds is not high, and their selectivity to enzymes and cells is poor.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Benzodiazapine compounds containing imidazole propanamido and its preparing process and application
  • Benzodiazapine compounds containing imidazole propanamido and its preparing process and application
  • Benzodiazapine compounds containing imidazole propanamido and its preparing process and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Example 1 7-nitro-1-ethoxycarbonylmethylene-5-phenylbenzodiazepine  preparation of

[0066] In the 50ml round-bottomed flask, add 7-Xoctyl-5-phenylbenzodiazepine (2.0g 7.2mmol), potassium carbonate (20g 14.4mmol), 20ml acetonitrile and ethyl bromoacetate (1.8g 10.6mmol), React at room temperature for 2 hours. After the reaction, 50ml of water was added, extracted with ethyl acetate, concentrated under reduced pressure to remove ethyl acetate, and the residue was recrystallized with absolute ethanol to obtain 1.8g of white crystals. The crystal was determined to be 7-nitro-1-ethoxycarbonylmethylene-5-phenylbenzodiazepine. mp: 141-143°C, yield 81.6%.

Embodiment 2

[0067] Example 2 7-nitro-1-(2-methoxycarbonylethyl)-5-phenylbenzodiazepine  preparation of

[0068] Proceed in the same manner as in Example 1, except that 1.8 g of methyl 3-bromopropionate is used instead of ethyl bromoacetate to obtain an oil. The oil, 7-nitro-1-(2-methoxycarbonylethyl)-5-phenylbenzodiazepine, was used in Example 5 without further purification.

Embodiment 3

[0069] Example 3 7-nitro-1-(3-ethoxycarbonylpropyl)-5-phenylbenzodiazepine  preparation of

[0070] Proceed in the same manner as in Example 1, except that 1.8 g of ethyl 4-bromobutyrate is used instead of ethyl bromoacetate to obtain an oily substance. The oil, 7-nitro-1-(3-ethoxycarbonylpropyl)-5-phenylbenzodiazepine, was used in Example 6 without further purification.

[0071] 7-Amino-1-(ω-alkoxycarbonylalkyl)-5-phenylbenzodiazepine  preparation of

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

A benzodiazapine compound containing imidazole-propanamide, its preparing process, its function of suppressing farnesyl protein transferase and the farnesylation of cancer gene Ras protein, and its application to treat the cancers relative to farnesyl protein transferase are disclosed.

Description

Background technique [0001] The present invention relates to imidazolyl-containing benzodiazepine compounds, in particular to new compounds of general formula I and preparation methods thereof, and these compounds are effective in inhibiting farnesyl protein transferase and oncogene Ras protein farnesyl role of transformation. The present invention also relates to the use of these compounds as drugs for the treatment of cancers associated with farnesyl protein transferase. [0002] [0003] Anticancer drugs are one of the important contents of current drug research and development, especially the design and development of anticancer drugs targeting specific targets has become the mainstream of anticancer drug research. [0004] Ras proto-oncogene plays an important role in the normal growth process of cells, and Ras gene mutation can make cell proliferation uncontrollable. Studies have found that Ras oncogene exists in 50% of colon cancer and 90% of pancreatic cancer. Ras...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/18A61K31/405A61K31/54A61K45/00A61P27/02A61P35/00A61P43/00C07D243/24C07D243/26C07D403/12
Inventor 郭宗儒陈晓光褚凤鸣
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com