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Urea compounds having muscarinic receptor antagonist activity

A compound and selective technology, applied in the direction of organic active ingredients, active ingredients of heterocyclic compounds, organic chemistry, etc., can solve problems such as blurred vision, application restrictions, dry mouth, etc.

Inactive Publication Date: 2003-04-02
THERAVANCE BIOPHARMA R&D IP LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these drugs have limited use due to side effects such as dry mouth, blurred vision and dilated pupils

Method used

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  • Urea compounds having muscarinic receptor antagonist activity
  • Urea compounds having muscarinic receptor antagonist activity
  • Urea compounds having muscarinic receptor antagonist activity

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0234] The preparation of formula (I) compound

[0235] In general, compounds of formula (I) can be prepared as illustrated and described in Reaction Scheme A. Reaction Scheme A

[0236] The compound of formula (I) is prepared by the following method: 1 equivalent of the formula 1 Compounds and Formulas 2 Compounds are covalently linked to generate intermediates of formula (II), wherein X is a linking group as defined herein, FG 1 is the functional basis, FG 2 Yes with FG 1 Complementary functional groups, PG is a protecting group, FG 2 PG is a protected functional group. The functional group on the linker is deprotected, and the resulting compound 3 with 1 equivalent of the compound 4 The reaction gives the compound of formula (I). compound 1 and 4 with compound 2 and 3 The reaction conditions used for the ligation depend on the compound 1 , 2 , 3 and 4 The nature of the functional base, which in turn depends on the type of bond required. Functional g...

Embodiment

[0277] The following preparations and examples are given so that those skilled in the art can more clearly understand and practice the present invention. They should not be considered as limiting the scope of the invention, but merely illustrative and representative examples of the invention.

[0278] In the following examples, the following abbreviations have the following meanings. All temperatures are in degrees Celsius unless otherwise stated. If an abbreviation is not defined, it has its accepted meaning.

[0279] g = gram

[0280] mg = milligram

[0281] min=minute

[0282] ml = milliliter

[0283] mmol=mmol

[0284] Synthetic example

[0285] Example 1 Intermediate compounds of formula 1B were prepared as described below.

[0286] Biphenyl-2-isocyanate (50 g, 256 mmol) was dissolved in 400 ml of anhydrous acetonitrile in a 2 L round bottom flask at room temperature. After cooling to 0° C. with an ice bath, a solution of 4-amino-N-benzylpiperidine (48.8 g,...

Embodiment 1

[0301] Example 1 Prepare hard gelatin capsules containing the following ingredients:

[0302] Quantity Ingredient (mg / capsule) Active Ingredient 30.0 Starch 305.0 Magnesium Stearate 5.0 The above ingredients are mixed and filled into hard gelatin capsules in quantities of 340 mg.

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PUM

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Abstract

This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists and antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

Description

[0001] Cross references to related applications: [0002] This application is a continuation-in-part of US Patent Application Serial No. 09 / 456,170, filed December 7,1999. Background of the invention [0003] A receptor is a biological structure containing one or more binding domains that can reversibly bind one or more ligands, and this binding can have biological consequences. Receptors can exist entirely outside the cell (extracellular receptors), within the cell membrane (although some portion of the receptor is exposed to the extracellular environment and the cytosol), or entirely within the cell (intracellular receptors). They can also perform cellular functions independently of each other (eg clot formation). Receptors within the cell membrane allow the cell to communicate with its external space (ie, signal transduction) and play a role in the transport of molecules and ions into and out of the cell. [0004] A ligand is a bind...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/08A61K31/445A61K31/4468A61K31/451A61K31/4523A61K31/4525A61K31/4535A61K31/454A61K31/4545A61K31/47A61K31/473A61K31/496A61K31/506A61K31/5377A61K31/55A61K31/551A61P1/00A61P1/02A61P1/04A61P11/00A61P11/06A61P13/02A61P13/10A61P25/00A61P25/08A61P25/28A61P27/02A61P43/00C07D211/48C07D211/52C07D211/58C07D211/60C07D211/62C07D211/64C07D211/66C07D401/06C07D401/12C07D401/14C07D405/12C07D409/12C07D413/06C07D413/12C07D417/14C07D453/02C07D471/04C07D471/08C07D471/10C07D471/14C07D487/10C07D491/08C07D491/10C07D495/08
CPCC07D401/14C07D401/12C07D471/08C07D405/12C07D409/12C07D471/14C07D211/52C07D495/08C07D401/06C07D211/48C07D471/10C07D413/06A61P1/00A61P1/02A61P1/04A61P11/00A61P11/06A61P13/02A61P13/10A61P25/00A61P25/08A61P25/28A61P27/02A61P43/00
Inventor M·曼门D·奥尔
Owner THERAVANCE BIOPHARMA R&D IP LLC
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