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Urea compounds having muscarinic receptor antagonist activity

A compound and nitrogen atom technology, applied in 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: 2006-08-23
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

[0304]Preparation of compounds of formula (I)

[0305] In general, compounds of formula (I) can be prepared as illustrated and described in Reaction Scheme A.

[0306] Reaction Scheme A

[0307]

[0308] Compounds of formula (I) are prepared by the following method: 1 equivalent formula 1 Compounds and Formulas 2 Compounds are covalently linked to form intermediates of formula (II), wherein X is a linker as defined herein, FG 1 is the functional base, FG 2 is with FG 1 Complementary functional group, 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 and 1 equivalent compound 4 The reaction yields the compound of formula (I). compound 1 and 4 with compound 2 and 3 The reaction conditions used for ligation depend on the compound 1 , 2 , 3 and 4 on the nature of the functional group, which in turn depends on the type of bond required. Functional groups and...

Embodiment 1

[0368] Intermediate compounds of formula IB are prepared as described below.

[0369]

[0370] 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, 256 rnol) dissolved in 400 mL of anhydrous acetonitrile was added over a period of 5 minutes. The formation of a precipitate was immediately observed. After 15 minutes, an additional 600 mL of dry acetonitrile was added and the viscous solution was stirred at 35°C for 12 hours. The solid was filtered off, washed with cold acetonitrile and dried in vacuo to give a colorless solid (100 g, 98%). pass the substance through 1 H-NMR, 13 C-NMR and MS were used for identification.

[0371] Compound IA (20 g, 52 mmol) was dissolved in 800 mL of a 3:1 mixture of anhydrous methanol / anhydrous DMF. Aqueous HCl (0.75 mL of a 37% concentrated solution, 7.6 mmol) was ...

preparation Embodiment

[0392] Example 1

[0393] Hard gelatin capsules are prepared containing the following ingredients:

[0394] quantity

[0395] Ingredients (mg / capsule)

[0396] Active ingredient 30.0

[0397] Starch 305.0

[0398] Magnesium Stearate 5.0

[0399] The above ingredients were mixed and filled into hard gelatin capsules in an amount 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-REFERENCE 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 to one or more ligands, and the binding can have biological consequences. Receptors can exist entirely outside the cell (extracellular receptors), within the cell membrane (although some part of the receptor is exposed to the extracellular environment and the cytosol) or completely inside the cell (intracellular receptors). They can also function independently of each other as cells (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 transporting molecules and ions in and out of the cell. [0004] A ligand is a binding partner f...

Claims

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Application Information

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