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

Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof

A technology for fused heterocycles and derivatives, applied in the field of fused heterocycle derivatives, can solve the problems of no hemodynamics, no specific description and description of compounds, etc.

Active Publication Date: 2008-12-24
KISSEI PHARMA
View PDF7 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no specific statement about the compound except that the compound has a sulfonamide or amide group, and there is no specific statement about the hemodynamics of oral administration

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
  • Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof
  • Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof
  • Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0181] The present invention is further illustrated in more detail by the following Examples and Test Examples. However, the present invention is not limited thereto.

reference example 1

[0183] 2-Chloro-5-(3,4-dihydroquinolin-1(2H)-ylsulfonyl)aniline

[0184] To a suspension of 1,2,3,4-tetrahydroquinoline (3.12 g) and sodium bicarbonate (2.66 g) in tetrahydrofuran (60 mL), water (6 mL) and 4-chloro-3-nitro Benzenesulfonyl chloride (5.4 g) was dissolved in tetrahydrofuran (30 ml), and the mixture was stirred at room temperature overnight. The reaction mixture was diluted with ethyl acetate, and the resulting mixture was washed successively with water, 1 mol / L hydrochloric acid, water and brine, and dried over anhydrous magnesium sulfate. The solvent was removed under reduced pressure to give 1-[(4-chloro-3-nitrophenyl)sulfonyl]-1,2,3,4-tetrahydroquinoline (5.0 g). This material was dissolved in tetrahydrofuran (45 mL). To the solution were added methanol (45 ml), nickel(II) bromide (0.15 g) and sodium borohydride (1.61 g) under ice-cooling, and the mixture was stirred at the same temperature for 30 minutes. The mixture was then stirred at room temperature fo...

reference example 12

[0188] 2-Chloro-5-(3,4-dihydroquinolin-1(2H)-ylmethyl)aniline

[0189] Under ice-cooling, to a solution of 4-chloro-3-nitrobenzyl alcohol (1 g) in dichloromethane (10 ml) was added triethylamine (1.12 ml) and methanesulfonyl chloride (0.5 ml), and the The mixture was stirred for 10 hours. The reaction mixture was diluted with ethyl acetate, and the resulting mixture was washed successively with water and brine, and dried over anhydrous magnesium sulfate. The solvent was removed under reduced pressure to give (4-chloro-3-nitrobenzyl)methanesulfonate (1.08 g). This material was dissolved in acetonitrile (4 mL)-ethanol (4 mL). To this solution were added 1,2,3,4-tetrahydroquinoline (1.62 g) and a catalytic amount of sodium iodide, and the mixture was stirred at 60°C overnight. The reaction mixture was diluted with ethyl acetate, and the resulting mixture was washed successively with water and brine, and dried over anhydrous magnesium sulfate. The solvent was removed under red...

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

Provided is a compound useful as a preventive or therapeutic agent for sexual-hormone-dependent diseases, etc. It is a fused heterocyclic derivative represented by the following general formula (I). In the formula (I), ring A is a five-membered cyclic unsaturated hydrocarbon or five-membered heteroaryl; R is halogeno, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; ring B is aryl or heteroaryl; R is halogeno, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; E<1> and E<2> each is oxygen, etc.; U is a single bond or alkylene; and X is, e.g., a group represented by Y, -SO2-Y, -O-(alkylene)-Y-, or -O-Z (wherein Y is Z, amino, etc. and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.).

Description

Technical field [0001] The present invention relates to fused heterocyclic derivatives. [0002] More specifically, the present invention relates to fused heterocyclic derivatives that have antagonistic activity against gonadotropin-releasing hormone and can be used to prevent or treat sex hormone-dependent diseases, such as benign prostatic hypertrophy, uterine fibroids, intrauterine Trichometriosis, uterine fibroids, precocious puberty, amenorrhea, premenstrual syndrome, dysmenorrhea, etc., or their prodrugs, or their pharmaceutically acceptable salts, or their hydrates or solvates, and pharmaceutical combinations containing them Things, etc. Background technique [0003] Gonadotropin-releasing hormone (GnRH, GnRH is also called luteinizing hormone-releasing hormone: LHRH, hereafter referred to as "GnRH") is a peptide consisting of 10 amino acids: pGlu-His-Trp-Ser-Tyr-Gly-Leu- Arg-Pro-Gly-NH 2 ), which is secreted from the hypothalamus. GnRH secreted into the pituitary...

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): C07D487/04A61K31/519A61K31/55A61K45/00A61P13/08A61P15/00A61P15/18A61P17/02A61P17/10A61P17/14A61P19/00A61P25/20A61P25/28A61P35/00A61P43/00C07D495/04
Inventor 大野孝介宫城贵史小沢知永伏见信彦
Owner KISSEI PHARMA
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