Nitrogenated fused ring derivative, pharmaceutical composition comprising the same, and use of the same for medical purposes
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一种衍生物、稠环的技术，应用在含氮的稠环衍生物领域
Inactive Publication Date: 2010-03-03
KISSEI PHARMA
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However, in any of these documents, there is no description or suggestion that the fused tetrahydroimidazole derivatives of the present invention have GnRH antagonistic activity
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[0243] The present invention will be explained in more detail by the following reference examples, examples and test examples. However, the present invention is not limited thereto.
reference example 1
[0245] 2,3-Difluoro-6-methoxybenzyl chloride
[0246] To a solution of 2,3-difluoro-6-methoxybenzyl alcohol (6.97 g) in toluene (100 mL) was added dropwise thionyl chloride (4.4 mL) at room temperature, and the mixture was stirred at room temperature for 1 hr. The reaction mixture was poured into water, and the resulting mixture was extracted with ethyl acetate. The extract was washed twice with water and brine, and dried over anhydrous sodium sulfate. The solvent was removed under reduced pressure to give the title compound (7.65 g).
[0249] 2,3-difluoro-6-methoxybenzyl chloride (7.65g), 4-chloro-2-methoxyphenol (6.34g), potassium carbonate (8.29g) and sodium iodide (1.2g ) in N,N-dimethylformamide (20 mL) was stirred at 80° C. for 2 hours. The reaction mixture was poured into water, and the resulting mixture was extracted with diethyl ether. The extract was washed successively with 1 mol / L sodium hydroxide aqueous solution, water and brine, and dried over anhydrous magnesium sulfate, and the solvent was removed under reduced pressure. The residual solid was suspended in a mixed solvent (n-hexane / diethyl ether=5 / 1), and collected by filtration. The collected solid was washed with the same solvent, and dried under reduced pressure to obtain the title compound (8.6 g).
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Abstract
To provide a compound useful as a prophylactic or therapeutic agent for a sex hormone-dependent disease or the like. [MEANS FOR SOLVING PROBLEMS] Disclosed are: a nitrogenated fused ring derivative represented by the general formula (I), or a prodrug, salt or the like thereof, which has a GnRH antagonistic activity; a pharmaceutical composition comprising the derivative or the prodrug, salt or the like thereof; use of the the derivative or the prodrug, salt or the like thereof for medical purposes; and others. In the general formula (I), the rings A and B independently represent an aryl or a heteroaryl; R and R independently represent a halogen, a cyano, an alkyl, an alkylsulfonyl, -OW<1>, -SW<1>, -COW<2>, -NW<3>W<4>, -SO2NW<3>W<4>, an aryl or the like; R<C> represents H or an alkyl; Erepresents an oxygen atom or the like; U represetns a single bond or an alkylene; and X represents Y, -CO-Y, -SO2-Y, -S-(alkylene)-Y, -O-(alkylene)-Y, -SO2-(alkylene)-Y or the like [wherein Y represents Z, an amino or the like; and Z represents a cycloalkyl, a heterocycloalkyl, an aryl, a heteroaryl or the like].
Description
technical field [0001] The present invention relates to nitrogen-containing fused ring derivatives. [0002] More specifically, the present invention relates to the following nitrogen-containing fused ring derivatives or their prodrugs or pharmaceutically acceptable salts thereof and the nitrogen-containing fused ring derivatives or their prodrugs or pharmaceutically acceptable salts thereof, etc. The pharmaceutical composition of said nitrogen-containing fused ring derivative has antagonistic activity against gonadotropin-releasing hormone and can be used for the prevention or treatment of sex hormone-dependent diseases, such as benign prostatic hypertrophy, uterine fibroids, endometriosis, Uterine fibroids, precocious puberty, amenorrhea, premenstrual syndrome, dysmenorrhea, etc. Background technique [0003] Gonadotropin-releasing hormone (GnRH, or luteinizing hormone-releasing hormone LHRH, hereinafter referred to as "GnRH") is a peptide including 10 amino acids: pGlu-H...
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