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
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  • 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

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  • 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
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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...

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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 which have gonadotropin-releasing hormone antagonistic activity and can be used for the prevention or treatment of sex hormone-dependent diseases such as benign prostatic hypertrophy, uterine fibroids, intrauterine Memtopia, 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, wait. Background technique [0003] Gonadotropin-releasing hormone (GnRH, GnRH also known as luteinizing hormone-releasing hormone: LHRH, hereinafter 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 portal ...

Claims

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Application Information

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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
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