Amido compound and its application as medicine

A technology for compounds and medicinal salts, applied in the field of modulators of type 1 11-beta hydroxysteroid dehydrogenase and/or mineralocorticoid receptors, can solve problems such as increasing the risk of fractures

Active Publication Date: 2015-10-07
INCYTE HLDG & INCYTE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Continued exposure to moderate glucocorticoids can lead to osteoporosis (Cannalis (1996) J.Clin.Endocrinol.Metab.81:3441-3447), thereby increasing the risk of fractures

Method used

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  • Amido compound and its application as medicine
  • Amido compound and its application as medicine
  • Amido compound and its application as medicine

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0224] The preparation of compounds involves the protection and deprotection of various chemical groups. The selection of protection and deprotection as well as the selection of suitable protecting groups can be easily determined by those skilled in the art. Protecting group chemistry can be found in, for example, Greene, et al., Protective Groups in Organic Synthesis, Second Edition, Wiley & Sons, 1991, which is incorporated herein by reference in its entirety.

[0225] The reaction of the method described herein can be carried out in a suitable solvent, which can be easily selected by those skilled in the art of organic synthesis. At the temperature at which the reaction proceeds, that is, from the freezing temperature of the solvent to the boiling temperature of the solvent, a suitable solvent does not substantially react with the starting materials (reactants), intermediates or products. A given reaction can be carried out in one solvent or a mixture of more than one solvent...

Embodiment 1

[0338] (3S)-1-((1-(4-chlorophenyl)cyclopropyl)carbonyl)pyrrolidin-3-ol

[0339] To 1-(4-chlorophenyl) cyclopropanecarboxylic acid (50mg, 0.25mmol), (3S)-pyrrolidin-3-ol (24.4mg, 0.28mmol) and BOP (116.0mg, 0.26mmol) in 0.4mL DMF In the solution inside, add hunig base (0.066ml, 0.38mmol). The mixture was stirred at room temperature overnight, and then directly purified by preparative HPLC to obtain (3S)-1-((1-(4-chlorophenyl)cyclopropyl)carbonyl)pyrrolidin-3-ol (20 mg). LCMS: m / z266.0(M+H) + 553.1(2M+Na) + .

Embodiment 2

[0341] (3S)-1-[(1-phenylcyclopropyl)carbonyl]pyrrolidin-3-ol

[0342] This compound was prepared by a method similar to that described in Example 1. LCMS: m / z232.1(M+H) + .

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PUM

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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

Invention field [0001] The present invention relates to a modulator of type 1 11-β hydroxysteroid dehydrogenase (11βHSD1) and / or mineralocorticoid receptor (MR), a composition thereof and a method of use thereof. Background of the invention [0002] Glucocorticoids are steroid hormones that regulate fat metabolism, function and distribution. In vertebrates, glucocorticoids also have profound and various physiological effects on development, neurobiology, inflammation, blood pressure, metabolism, and programmed cell death. In humans, the main endogenously produced glucocorticoid is cortisol. Cortisol is synthesized in the fascicular zone of the adrenal cortex under the control of a short-term neuroendocrine feedback loop called the hypothalamic pituitary adrenal (HPA) axis. The adrenal gland produces cortisol under the control of adrenocorticotropic hormone (ACTH), a factor produced and secreted by the anterior pituitary gland. The production of ACTH in the anterior pituitary i...

Claims

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Application Information

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IPC IPC(8): C07D221/00C07D223/02C07D223/04C07D231/04
Inventor W·姚J·卓M·徐C·章B·梅特卡尔夫C·何D·-Q·钱
Owner INCYTE HLDG & INCYTE
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