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2- ( arylalkoxy ) -1- phenylethylamine derivatives as nk1 antagonist and 5-serotonin reuptake inhibitors

An alkoxy, alkyl technology, applied in the field of 2-(arylalkoxy)-1-phenethylamine derivatives as NK1 antagonists and serotonin reuptake inhibitors, can solve delays, etc. question

Inactive Publication Date: 2007-05-02
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However SSRIs have a delayed onset effect, are associated with undesirable side effects such as sexual dysfunction, and are ineffective in approximately 30% of patients (M.J.Gitlin, MJ, J.Clin.Psych., 55, 406-413 , 1994)

Method used

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  • 2- ( arylalkoxy ) -1- phenylethylamine derivatives as nk1 antagonist and 5-serotonin reuptake inhibitors
  • 2- ( arylalkoxy ) -1- phenylethylamine derivatives as nk1 antagonist and 5-serotonin reuptake inhibitors
  • 2- ( arylalkoxy ) -1- phenylethylamine derivatives as nk1 antagonist and 5-serotonin reuptake inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] Example 1: 4-{[2-(3-chloro-4-fluorophenyl)-2-piperazin-1-ylethoxy]methyl}-3-methoxy-2-naphthalenecarbonitrile

[0096]4-{1-(3-chloro-4-fluorophenyl)-2-[(3-cyano-2-methoxy-1-naphthyl)methoxy]ethyl}piperazine-1-carboxy Acid tert-butyl ester (100 mg, 0.18 mmol) was dissolved in DCM (2 mL) and TFA (2 mL) was added. After 2 hours the volatiles were removed under reduced pressure. The residue was dissolved in EtOAc (20 mL) and washed with saturated aqueous sodium bicarbonate (20 mL). The organic phase was dried over sodium sulfate, filtered through a pad of celite, and the volatiles were removed under reduced pressure. The residue was chromatographed on silica gel (MeOH: 0-5% 2M NH in DCM 3 ) to afford the title compound (81.6 mg, 79%) as an off-white solid. To a solution of the title compound in methanol was added citric acid (1.0 equiv) to form the citrate salt. Concentration under reduced pressure afforded the desired salt form of the product as an off-white powder. ...

Embodiment 2-29

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PUM

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Abstract

The invention discloses compounds of the following formula (I) wherein R<1> R<2>, n, Ar<1> and A<2> are as defined in the specification, in vivo-hydrolysable precursors thereof, pharmaceutically acceptable salts thereof, the use in therapy and pharmaceutical compositions and methods of treatment using the same. The example compounds are 1-(2-(naphthylmethoxy)-1-phenylethyl)piperazine derivatives. The compounds are neurokinin 1 (NK1) receptor antagonist and / or serotonin reuptake inhibitors, with medical indications for depression and other disorders.

Description

technical field [0001] The present invention relates to the treatment of diseases involving serotonin, substance P or neurokinin A, such as the treatment of the following disorders or diseases: hypertension, depression, generalized anxiety, phobias, post-traumatic stress syndrome , Avoidant Personality Disorder, Premature Ejaculation, Irregular Eating, Obesity, Chemical Dependence, Cluster Headaches, Migraines, Pain, Alzheimer's Disease, Obsessive Compulsive Disorder, Panic Disorder, Amnesia, Parkinson's Disease, Endocrine disorders Vasospasm, Cerebellar ataxia, Gastrointestinal dysfunction, Negative symptoms of schizophrenia, Premenstrual syndrome, Fibromyalgia syndrome, Stress incontinence, Tourette's syndrome, Trichotillomania, Kleptomania , male impotence, ADHD, chronic episodic migraines and headaches. Background technique [0002] Mammalian neurokinins are peptide neurotransmitters found in the peripheral and central nervous systems. The three main neurokinins are su...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/04C07C217/48A61K31/495A61K31/137A61P25/00A61P9/00A61P1/00A61KC07D295/088
CPCA61K31/495A61K31/137C07D295/088A61P1/00A61P1/04A61P15/08A61P25/00A61P25/06A61P25/14A61P25/16A61P25/22A61P25/24A61P25/28A61P25/30A61P29/00A61P3/00A61P43/00A61P9/00
Inventor 卡西·丹茨曼
Owner ASTRAZENECA AB
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