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Amido compounds and their use as pharmaceuticals

A technology of compounds and prodrugs, applied in the field of modulators of type 1 11-β hydroxysteroid dehydrogenase and/or mineralocorticoid receptors, which can solve problems such as increased blood pressure

Inactive Publication Date: 2007-11-28
INCYTE CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These may contribute to the increased blood pressure observed in aP2-11βHSD1 transgenic mice

Method used

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  • Amido compounds and their use as pharmaceuticals
  • Amido compounds and their use as pharmaceuticals
  • Amido compounds and their use as pharmaceuticals

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0393]

[0394] N-(3R)-1-[(3-Chloro-2-methylphenyl)sulfonyl]piperidin-3-ylcyclohexanecarboxamide

[0395] Step 1: N-[(3R)-piperidin-3-yl]cyclohexanecarboxamide hydrochloride

[0396] Cyclohexanecarbonyl chloride (70.0 μL, 0.515 mmol) was added to (3R)-tert-butyl 3-aminopiperidine-1-carboxylate (100.0 mg, 0.499 mmol) and potassium carbonate (150 mg, 2.1 eq.) at room temperature in a mixture in acetonitrile (3.0 mL). The reaction mixture was stirred at room temperature for 1 hour and filtered. The filtrate was concentrated under reduced pressure. The residue was treated with 4.0 M hydrochloric acid in 1,4-dioxane (2.0 mL) at room temperature for 1 hour. The solvent was evaporated under reduced pressure to give the product which was used in the next reaction without further purification.

[0397] Step 2: N-(3R)-1-[(3-Chloro-2-methylphenyl)sulfonyl]piperidin-3-ylcyclohexanecarboxamide

[0398]N-[(3R)-piperidin-3-yl]cyclohexanecarboxamide hydrochloride (12.3 mg, 50.0 mol) i...

Embodiment 2

[0400]

[0401] N-(3R)-1-[(2-nitrophenyl)sulfonyl]piperidin-3-ylcyclohexanecarboxamide

[0402] This compound was prepared by methods similar to those of Example 1. LCMS: (M+H) + = 396.0.

Embodiment 3

[0404]

[0405] N-[(3R)-1-(2-naphthalenesulfonyl)piperidin-3-yl]cyclohexanecarboxamide

[0406] This compound was prepared by methods similar to those of Example 1. LCMS: (M+H) + = 401.1.

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Abstract

The present invention relates to inhibitors of 11-Beta hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-Beta hydroxyl steroid dehydrogenase type 1 and / or diseases associated with aldosterone excess.

Description

field of invention [0001] The present invention relates to modulators of 11-beta hydroxysteroid dehydrogenase type 1 (11βHSD1) and / or mineralocorticoid receptor (MR), compositions thereof, and methods of using them. Background of the invention [0002] Glucocorticoids are steroid hormones that regulate fat metabolism, function and distribution. In vertebrates, glucocorticoids also have profound and diverse physiological effects on development, neurobiology, inflammation, blood pressure, metabolism and programmed cell death. In humans, the major endogenous glucocorticoid is cortisol. Cortisol is synthesized in the zona fascicularis of the adrenal cortex under the control of a short-term neuroendocrine feedback circuit known as the hypothalamic-pituitary-adrenal (HPA) axis. Production of cortisol by the adrenal glands is under the control of adrenocorticotropic hormone (ACTH), which is produced and secreted by the anterior pituitary gland. ACTH production within the anterio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/44C07D401/14A61K31/47C07D403/12A61K31/54C07D403/14A61K31/445C07D413/12A61K31/495C07D413/14A61K31/535C07D417/12C07D401/12C07D417/14
CPCC07D401/14C07D401/12C07D413/10C07D417/04C07D211/56C07D451/06C07D409/12C07D211/96C07D413/12C07D401/10C07D401/04A61P13/12A61P19/10A61P25/24A61P25/28A61P27/06A61P29/00A61P3/04A61P3/06A61P3/08A61P43/00A61P5/50A61P7/00A61P7/02A61P9/04A61P9/08A61P9/10A61P9/12A61P3/10A61K31/445
Inventor W·姚J·卓B·W·梅特卡夫D·-Q·钱Y·李
Owner INCYTE CORP
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