ORM-12741

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C20H23NO3
Molecular Weight	325.4015
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC1=CC=CC(=C1)[C@H]2CCCN(C[C@H]3COC4=CC=CC=C4O3)C2

InChI

InChIKey=FOESNAGBEJURCI-WMZOPIPTSA-N

InChI=1S/C20H23NO3/c22-17-7-3-5-15(11-17)16-6-4-10-21(12-16)13-18-14-23-19-8-1-2-9-20(19)24-18/h1-3,5,7-9,11,16,18,22H,4,6,10,12-14H2/t16-,18-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C20H23NO3
Molecular Weight	325.4015
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://adisinsight.springer.com/drugs/800022078https://www.ncbi.nlm.nih.gov/pubmed/29067315 | https://www.ncbi.nlm.nih.gov/pubmed/24489014 | https://adisinsight.springer.com/drugs/800029247
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/16317384 | https://www.ncbi.nlm.nih.gov/pubmed/17902637

Juvantia Pharma and Orion developed ORM-12741, also known as ORM-10921, a novel selective antagonist of alpha-2C adrenoceptors for the treatment of depression and Alzheimer's disease. ORM-12741 participated in phase II clinical trial where was evaluated the safety and efficacy of the drug in patients with Alzheimer's disease. In spite of the successfully completed phase II, further study of the drug for this disease was discontinued. In addition, ORM-12741 participated in clinical trial phase II to prove the concept that this drug could prevent blood vessel spasms for Raynaud's phenomenon. Raynaud's phenomenon is a disorder of the digital blood vessels resulting in episodic impairment of blood flow. However, this study was terminated because of the recommendation by study Data and Safety Monitoring Committee to the sponsor following the interim analysis of 8 subjects.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Estrogen receptor 75 Target ID: CHEMBL2093866 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17902637	Interacts 323
Nuclear factor NF-kappa-B complex 11 Target ID: CHEMBL2094258 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17902637	Inhibitor 8297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Septic shock 21 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16317384	Primary		Preclinical	Unknown Approved Use Unknown
Rheumatoid arthritis 316 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17902637 http://adisinsight.springer.com/drugs/800022078	Primary		Phase I 428	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Estrogen receptor dependent inhibitors of NF-kappaB transcriptional activation-1 synthesis and biological evaluation of substituted 2-cyanopropanoic acid derivatives: pathway selective inhibitors of NF-kappaB, a potential treatment for rheumatoid arthritis.	2007 Nov 1	17902637

Patents

Sample Use Guides

In Vivo Use Guide

Unknown

Route of Administration: Oral

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Sat Dec 16 10:35:02 GMT 2023` Edited by `admin` on `Sat Dec 16 10:35:02 GMT 2023`
Record UNII	D26C95A960
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

ORM-12741

Code

English

DB-105

Code

English

Phenol, 3-[(3R)-1-[[(2S)-2,3-dihydro-1,4-benzodioxin-2-yl]methyl]-3-piperidinyl]-

Systematic Name

English

3-[(3R)-1-[[(2S)-2,3-Dihydro-1,4-benzodioxin-2-yl]methyl]-3-piperidinyl]phenol

Systematic Name

English

Code System Code Type Description

SMS_ID

100000184092