Compounds > n-(1-(3,4-difluorobenzyl)piperidin-4-yl)-6-(trifluoromethyl)pyridazin-3-amine

Page last updated: 2024-11-13

n-(1-(3,4-difluorobenzyl)piperidin-4-yl)-6-(trifluoromethyl)pyridazin-3-amine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

N-(1-(3,4-difluorobenzyl)piperidin-4-yl)-6-(trifluoromethyl)pyridazin-3-amine: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	91826482
MeSH ID	M0579128

Synonyms (19)

Synonym
jnj 37822681 dihydrochloride
2108806-02-4
n-(1-(3,4-difluorobenzyl)piperidin-4-yl)-6-(trifluoromethyl)pyridazin-3-amine
unii-y3xcp46pa8
n-{1-[(3,4-difluorophenyl)methyl]piperidin-4-yl}-6-(trifluoromethyl)pyridazin-3-amine dihydrochloride
3-pyridazinamine, n-(1-((3,4-difluorophenyl)methyl)-4-piperidinyl)-6-(trifluoromethyl)-, hydrochloride (1:2)
jnj-37822681 dihydrochloride
Y3XCP46PA8 ,
CS-0099689
jnj-37822681 (dihydrochloride)
HY-111066A
MS-28021
n-[1-[(3,4-difluorophenyl)methyl]piperidin-4-yl]-6-(trifluoromethyl)pyridazin-3-amine;dihydrochloride
n-{1-[(3,4-difluorophenyl)methyl]piperidin-4-yl}-6-(trifluoromethyl)pyridazin-3-aminedihydrochloride
jnj37822681dihydrochloride
jnj-37822681 (hydrochloride)
E98972
EN300-1700042
AKOS040733501

Research Excerpts

Pharmacokinetics

Excerpt	Reference	Relevance
" The aim of the analyses was to develop a population pharmacokinetic model to describe the pharmacokinetics of JNJ-37822681 in healthy subjects and patients with schizophrenia and to identify covariates of interest."	( Population pharmacokinetics of JNJ-37822681, a selective fast-dissociating dopamine D₂-receptor antagonist, in healthy subjects and subjects with schizophrenia and dose selection based on simulated D₂-receptor occupancy. Hoeben, E; Mannaert, E; Neyens, M; Schmidt, M; Vermeulen, A, 2013)	0.39
" Nonlinear mixed effects modeling of pooled data was conducted using NONMEM(®) to estimate population pharmacokinetic parameters and the effect of covariates on these parameters."	( Population pharmacokinetics of JNJ-37822681, a selective fast-dissociating dopamine D₂-receptor antagonist, in healthy subjects and subjects with schizophrenia and dose selection based on simulated D₂-receptor occupancy. Hoeben, E; Mannaert, E; Neyens, M; Schmidt, M; Vermeulen, A, 2013)	0.39
" The estimated pharmacokinetic parameters for the phase IIb study were similar to those observed in the phase IIa study."	( Population pharmacokinetics of JNJ-37822681, a selective fast-dissociating dopamine D₂-receptor antagonist, in healthy subjects and subjects with schizophrenia and dose selection based on simulated D₂-receptor occupancy. Hoeben, E; Mannaert, E; Neyens, M; Schmidt, M; Vermeulen, A, 2013)	0.39
"The population pharmacokinetic model of JNJ-37822681 successfully described the pharmacokinetics of JNJ-37822681 and allowed the reliable determination of individual exposure parameters in a phase IIb study."	( Population pharmacokinetics of JNJ-37822681, a selective fast-dissociating dopamine D₂-receptor antagonist, in healthy subjects and subjects with schizophrenia and dose selection based on simulated D₂-receptor occupancy. Hoeben, E; Mannaert, E; Neyens, M; Schmidt, M; Vermeulen, A, 2013)	0.39

Bioavailability

Excerpt	Reference	Relevance
" Significant covariates were sex and bioavailability on apparent clearance and food intake on the absorption rate constant."	( Population pharmacokinetics of JNJ-37822681, a selective fast-dissociating dopamine D₂-receptor antagonist, in healthy subjects and subjects with schizophrenia and dose selection based on simulated D₂-receptor occupancy. Hoeben, E; Mannaert, E; Neyens, M; Schmidt, M; Vermeulen, A, 2013)	0.39

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	11 (100.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.62

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	11.62 (24.57)
Research Supply Index	2.89 (2.92)
Research Growth Index	4.51 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (11.62)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	6 (54.55%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	5 (45.45%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

Trial			Phase	Enrollment	Study Type	Start Date	Status
A Randomized, Double-Blind, Placebo- and Active-Controlled, Parallel-Group Study to Evaluate the Efficacy and Safety of 3 Fixed Doses of JNJ-37822681 Administered Twice Daily in Subjects With Schizophrenia [NCT00728195]			Phase 2	498 participants (Actual)	Interventional	2008-11-30	Completed
A Double-Blind, Multiple Dose Titration Study to Investigate the Safety, Tolerability and Pharmacokinetics of Once Daily and Twice Daily Doses of JNJ-37822681 in Male and Female Patients With Stable Schizophrenia [NCT01812642]			Phase 2	33 participants (Actual)	Interventional	2008-07-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.	2.07	1	0	aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol	antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist
apomorphine Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.	2.07	1	0	aporphine alkaloid	alpha-adrenergic drug; antidyskinesia agent; antiparkinson drug; dopamine agonist; emetic; serotonergic drug
ocaperidone ocaperidone: structure given in first source	2.07	1	0	pyridopyrimidine
raclopride Raclopride: A substituted benzamide that has antipsychotic properties. It is a dopamine D2 receptor (see RECEPTORS, DOPAMINE D2) antagonist.	4.17	3	1	salicylamides
piperidines Piperidines: A family of hexahydropyridines.	7.73	11	6
olanzapine Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.	6.21	4	3	benzodiazepine; N-arylpiperazine; N-methylpiperazine	antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor
pyrimidinones Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O.	2.07	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Dementia Praecox [description not available]	0	6.95	7	4
Schizophrenia A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.	0	6.95	7	4
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	0	3.47	1	1
Chronic Insomnia [description not available]	0	3.46	1	1
Acathisia, Drug-Induced [description not available]	0	3.46	1	1
Acute Disease Disease having a short and relatively severe course.	0	3.46	1	1
Sleep Initiation and Maintenance Disorders Disorders characterized by impairment of the ability to initiate or maintain sleep. This may occur as a primary disorder or in association with another medical or psychiatric condition.	0	3.46	1	1
Anochlesia [description not available]	0	2.07	1	0