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Benzoxazines and related nitrogen-containing heterobicyclic compounds useful as mineralocorticoid receptor modulating agents

A kind of technology of compound and benzene ring, applied in the field of nitrogen-containing heterocyclic compounds, can solve the problems such as not reporting benzoxazine-sulfonamide derivatives

Active Publication Date: 2009-03-04
MITSUBISHI TANABE PHARMA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, no benzoxazine-sulfonamide derivatives with MR-modulating activity (such as MR-antagonistic activity) have been reported

Method used

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  • Benzoxazines and related nitrogen-containing heterobicyclic compounds useful as mineralocorticoid receptor modulating agents
  • Benzoxazines and related nitrogen-containing heterobicyclic compounds useful as mineralocorticoid receptor modulating agents
  • Benzoxazines and related nitrogen-containing heterobicyclic compounds useful as mineralocorticoid receptor modulating agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0485] To 7-amino-2,2-dimethyl-4-phenyl-2H-1,4-benzoxazin-3(4H)-one (obtained in reference example 1(3)) under ice-cold conditions To a solution of compound, 50 mg) in chloroform (2 mL), methanesulfonyl chloride (22 μL) and pyridine (30 μL) were successively added dropwise and the mixture was stirred at room temperature for 18 hours. To the reaction mixture was added saturated sodium bicarbonate solution, and the mixture was extracted with chloroform. The organic layer was washed sequentially with water, 10% HCl solution and brine, dried over sodium sulfate and concentrated in vacuo. The resulting residue was purified by column chromatography on NH-silica gel (solvent; n-hexane / ethyl acetate=1 / 1→ethyl acetate) to give N-(2,2-dimethyl-3-oxo-4 -Phenyl-3,4-dihydro-2H-1,4-benzoxazin-7-yl)methanesulfonamide (55 mg), a colorless powder. MS(APCI) m / z: 347[M+H] +

Embodiment 2 to 38

[0487] The corresponding materials were treated in the same manner as described in Example 1 to obtain the compounds shown in Tables 1 to 8 below.

[0488] Table 1

[0489]

[0490] Table 2

[0491]

[0492]

[0493] table 3

[0494]

[0495] Table 4

[0496]

[0497]

[0498] table 5

[0499]

[0500] Table 6

[0501]

[0502] Table 7

[0503]

[0504] Table 8

[0505]

Embodiment 39

[0507] 7-Amino-4-(4-fluorophenyl)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one (the compound obtained in Reference Example 7(4), 113 mg) was treated in the same manner as described in Example 1 to give N-[4-(4-fluorophenyl)-2,2-dimethyl -3-Oxo-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazin-7-yl]methanesulfonamide (98 mg) as colorless crystals.

[0508] MS(APCI) m / z: 366[M+H] +

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PUM

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Abstract

The present invention relates to a compound, useful as a mineralocorticoid receptor-modulating agent, of the following formula [I]: wherein Ring A is a benzene ring optionally having a substituent(s) other than R1 etc, R1 is a group of the formula: RaSO2NH- etc, Ra is an alkyl group etc, R2 and R3 are each a hydrogen atom, a phenyl group, an optionally substituted alkyl group etc, X is an oxygen atom etc, Y is a group of the formula: -C(=O)- etc, Ar is an optionally substituted aryl group or an optionally substituted heteroaryl group, Q is a single bond, an alkylene group etc, or a pharmaceutically acceptable salt thereof.

Description

technical field [0001] The present invention relates to nitrogen-containing heterocyclic compounds that have an affinity for the mineralocorticoid receptor (MR) and are useful for the prevention or treatment of various diseases or disease states associated with such receptors, and modulators comprising such compounds reagent. Background technique [0002] Physiologically active low molecular weight hydrophobic substances such as steroid hormones display their activity as ligands through their specific nuclear receptors. Nuclear steroid hormone receptors constitute a gene superfamily and receptors act as ligand-dependent transcription factors and thereby regulate (activate or repress) the expression of target genes at the transcriptional level. Such receptors include mineralocorticoid receptor (MR), glucocorticoid receptor (GR), androgen receptor (AR), estrogen receptor (ER) and progesterone receptor (PR). Ligands of the steroid hormone receptors, such as mineralocorticoids...

Claims

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Application Information

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IPC IPC(8): C07D265/36C07D279/16C07D413/04A61K31/538A61K31/5415A61P9/12
Inventor 饭岛彻山元康王赤塚英则川口隆行
Owner MITSUBISHI TANABE PHARMA CORP
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