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8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists

A compound, cycloalkyl technology, applied in the direction of active ingredients of heterocyclic compounds, organic chemistry, digestive system, etc., can solve problems such as increased duration

Active Publication Date: 2009-03-25
THERAVANCE BIOPHARMA R&D IP LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Also, because surgical patients are often treated with opioid analgesics during and after surgery, the duration of POI can be increased by decreased gastrointestinal motility associated with opioid use

Method used

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  • 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
  • 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
  • 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0138] The preparation of the urea compound of formula (Ib) is shown in reaction (ii) of scheme A. The reaction is usually carried out by reacting intermediate (II) with between about 1 and about 2 equivalents of a base such as N,N-diisopropylethylamine in the presence of between about 3 and about 6 equivalents of Isocyanate compound R 5 -N=C=O contact to implement. The reaction is typically carried out at ambient temperature for about 1 hour to about 16 hours, or until the reaction is substantially complete.

[0139] A general procedure for the preparation of intermediates of formula (II) is depicted in Scheme B1, where P 1 Represents an amino protecting group.

[0140] Option B1

[0141]

[0142] An intermediate of formula (III) (herein referred to as "phenyltropane") is reductively N-alkylated by reaction with an aldehyde of formula (TV) to obtain a protected intermediate (V), which is obtained by Deprotection by usual procedures affords intermediate (II).

[0143]...

example A

[0212] Formulation Example A: Hard Gelatin Capsule for Oral Administration

[0213] Compound of the invention (50 g), spray-dried lactose (200 g) and magnesium stearate (10 g) were thoroughly blended. The resulting composition was loaded into hard gelatin capsules (260 mg composition / capsule).

example B

[0214] Formulation Example B: Hard Gelatin Capsule for Oral Administration

[0215] Compound of the invention (20 mg), starch (89 mg), microcrystalline cellulose (89 mg), and magnesium stearate (2 mg) were blended thoroughly and then passed through a 45 mesh US sieve. The resulting composition was loaded into hard gelatin capsules (200 mg composition / capsule).

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Abstract

The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I) wherein R<1>, R<2>, R<3>, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Description

technical field [0001] The present invention relates to 8-azabicyclo[3.2.1]octane compounds useful as mu opioid receptor antagonists. The invention also relates to pharmaceutical compositions comprising said compounds, methods of using said compounds to treat or prevent medical conditions mediated by mu opioid receptor activity, and processes and intermediates for the preparation of said compounds. Background technique [0002] It is now generally understood that endogenous opioids play complex roles in gastrointestinal physiology. Opioid receptors are expressed throughout the body in the central nervous system and peripheral regions including the gastrointestinal (GI) tract. [0003] Compounds that act as agonists at the opioid receptor, typified by morphine, are the mainstay of analgesic therapy for the treatment of moderate to severe pain. Unfortunately, opioid analgesic use is often associated with adverse effects on the gastrointestinal tract, collectively known as op...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D451/02A61K31/46A61P1/10
Inventor 丹尼尔·朗蒂莫西·J·丘奇约翰·R·雅各布森姜岚大介·罗兰·齐藤约安娜·斯泰尔贾德斯普里西拉·范迪克肖恩·达尔齐尔莱蒂西亚·普雷萨
Owner THERAVANCE BIOPHARMA R&D IP LLC
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