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Tryptophan hydroxylase inhibitors for the treatment of metastatic bone disease

A metastatic, bone disease technology that is used in the management, treatment, and/or prevention of metastatic bone disease to address issues such as damage to bone health

Inactive Publication Date: 2012-10-24
LEXICON PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, those therapies used to treat primary cancers often compromise bone health

Method used

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  • Tryptophan hydroxylase inhibitors for the treatment of metastatic bone disease
  • Tryptophan hydroxylase inhibitors for the treatment of metastatic bone disease
  • Tryptophan hydroxylase inhibitors for the treatment of metastatic bone disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0212] HPLC identification

[0213] In some of the synthetic examples below, high performance liquid chromatography (HPLC) retention times are provided. Unless otherwise stated, the various conditions used to obtain those retention times are as follows:

[0214] Method A: YMC-PACK ODS-A 3.0x50mm; Solvent A=90% water, 10% MeOH, 0.1% TFA; Solvent B=90% MeOH, 10% water, 0.1% TFA; B% from 0 to 100%; flow rate = 2ml / min; observation wavelength = 220nm.

[0215] Method B: YMC-PACK ODS-A 3.0x50mm; solvent A=90% water, 10% MeOH, 0.1% TFA; solvent B=90% MeOH, 10% water, 0.1% TFA; B% from 10 to 4 minutes 100%; flow rate = 3ml / min; observation wavelength = 220nm.

[0216] Method C: YMC-PACK ODS-A 3.0x50mm; Solvent A=90% water, 10% MeOH, 0.1% TFA; Solvent B=90% MeOH, 10% water, 0.1% TFA; B% from 0 to 100%; flow rate = 2ml / min; observation wavelength = 220nm.

[0217] Method D: Shim VP ODS 4.6x50mm; solvent A = 90% water, 10% MeOH, 0.1% TFA; solvent B = 90% MeOH, 10% water, 0.1% TFA...

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Abstract

This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and / or prevention of metastatic bone disease.

Description

technical field [0001] The present invention relates to tryptophan hydroxylase inhibitors, compositions containing them, and their application methods for treating, managing, and / or preventing metastatic bone disease. Background technique [0002] The neurotransmitter serotonin (5-hydroxytryptamine (5-HT)) is involved in several central nervous aspects of mood control and is involved in the regulation of sleep, anxiety, alcoholism, drug abuse, food intake and sexual behaviour. In peripheral tissues, serotonin is involved in the regulation of vascular tone, intestinal motility, primary hemostasis, and cell-mediated immune responses. Walther, D.J. et al., science 299:76 (2003). Some evidence also suggests that serotonin can affect bone growth. See, eg, Yadav, V.K. et al., Cell 135:825-837 (2008). [0003] Dysregulation of serotonin synthesis and metabolism is associated with various diseases. An example is carcinoid syndrome, a collection of symptoms caused by carcino...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4045A61K31/4192A61K31/497A61K31/506A61K45/06A61P35/04
CPCC07D239/42C07D403/04C07D403/12A61K31/405C07D241/20C07D249/06A61K31/4192C07D241/24A61K31/5377A61K31/197A61K31/497A61K45/06A61K31/506C07C229/16A61K31/4965C07D251/52A61K31/505A61K31/53A61K31/4045C07D239/34C07D251/18C07D239/47C07D409/10C07D401/04A61P19/08A61P35/04A61P43/00A61K2300/00
Inventor 阿瑟·托马斯·桑兹
Owner LEXICON PHARM INC
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