Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Nitrogen-containing saturated heterocyclic compound

A technology of compound and heterocyclic group, applied in the direction of medical preparations containing active ingredients, drug combination, organic chemistry, etc., can solve problems that do not involve details of morpholine compounds, etc.

Active Publication Date: 2014-02-05
SHANGAI PHARMA GRP CO LTD +1
View PDF8 Cites 11 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, no details about morpholine compounds are involved in this publication

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
  • Nitrogen-containing saturated heterocyclic compound
  • Nitrogen-containing saturated heterocyclic compound
  • Nitrogen-containing saturated heterocyclic compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment ）

[0447] Specific examples (Examples) of synthesizing the objective compound [I] of the present invention by the methods exemplified above are shown below, but the present invention is not limited thereto.

Embodiment 1

[0450] (2R)-N-cyclopropyl-N-{1-[4-(3-methoxypropoxy)-1-benzofuran-6-yl]ethyl}morpholine-2-carboxamide[ Ex(1-1), Ex(1-2)]

[0451] [chemical formula 25]

[0452]

[0453] To (2R)-2-[(cyclopropyl{1-[4-(3-methoxypropoxy)-1-benzofuran-6-yl]ethyl}amino)carbonyl]morpholine-4 - To a solution of tert-butyl carboxylate (200mg) and 2,6-lutidine (0.142ml) in chloroform (4ml), add trimethylsilyl trifluoromethanesulfonate (0.180ml) under ice-cooling, in Stir at the same temperature for 30 minutes. Under ice-cooling, saturated aqueous sodium bicarbonate solution was added, followed by extraction with ethyl acetate. The organic phase was washed with brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The resulting residue was purified by silica gel chromatography (eluent: chloroform / methanol / ammonia = 200 / 2 / 1) to give (2R)-N-cyclopropyl-N-{(1R)-1 as a colorless oil -[4-(3-Methoxypropoxy)-1-benzofuran-6-yl]ethyl}morpholine-2-carboxamide [Ex(1-1)] (1...

Embodiment 2

[0456] (2R)-N-{(1R)-1-[3-chloro-1-(3-methoxypropoxy)-1H-indolyl-6-yl]ethyl}-N-cyclopropyl Piperazine-2-carboxamide[Ex(2-1)]

[0457] [chemical formula 26]

[0458]

[0459] To (2R)-2-{[{(1R)-1-[3-chloro-1-(3-methoxypropyl)-1H-indolyl-6-yl]ethyl}(cyclopropyl )amino]carbonyl}piperazine-1,4-dicarboxylic acid tert-dibutyl ester (44.0mg) and 2,6-lutidine (0.050ml) in dichloromethane (1.0ml) solution, under ice cooling Trimethylsilyl trifluoromethanesulfonate (0.051 ml) was added, followed by stirring at the same temperature for 1 hour. Under ice-cooling, saturated aqueous sodium bicarbonate solution and methanol (2.0 ml) were added, extracted with chloroform, the organic phase was washed with brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The resulting residue was purified by NH-silica gel chromatography (eluent: ethyl acetate→ethyl acetate / methanol=5 / 1) to give (2R)-N-{(1R)-1-[ 3-Chloro-1-(3-methoxypropyl)-1H-indolyl-6-yl]ethyl}-N-cy...

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

The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R 1 is a cycloalkyl group and the like, R 22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is -O- and the like, and R 3 to R 6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.

Description

technical field [0001] The present invention relates to a medicine, especially a nitrogen-containing saturated heterocyclic compound effective as a renin inhibitor or a pharmacologically acceptable salt thereof, as well as their use, preparation method and intermediate. Background technique [0002] The development of renin inhibitor drugs is expected as a drug for the prevention and treatment of hypertension, cardiac insufficiency, diabetic nephropathy, and the like, and for example, 3,4-substituted piperidine compounds are disclosed (Patent Document 1). However, no details about morpholine compounds are mentioned in this publication. In addition, although the morpholine compound is disclosed in International Publication No. 2008 / 153182, only the compound in which R in the formula I of the present invention is hydrogen is disclosed (Patent Document 2). [0003] prior art literature [0004] patent documents [0005] Patent Document 1: International Publication No. 06 / 069...

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 Applications(China)
IPC IPC(8): C07D265/30A61K31/4025A61K31/416A61K31/437A61K31/496A61K31/5375A61K31/5377A61P9/00A61P9/12A61P13/12C07D403/12C07D405/12C07D413/12C07D413/14C07D471/04
CPCC07D471/04C07D231/56C07D413/14C07D265/30C07D403/12C07D405/12C07D413/12A61P9/00A61P9/04A61P9/12A61P13/12A61K31/5377
Inventor 饭嶋彻须釜宽川口隆行沈竞康夏广新谢建树
Owner SHANGAI PHARMA GRP CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
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