PF-03715455

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C35H34ClN7O3S2
Molecular Weight	700.273
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)(C)C1=NN(C(NC(=O)NCC2=CC=CC=C2SC3=CN4C(C=C3)=NN=C4C5=CC=CC=C5SCCO)=C1)C6=CC=C(O)C(Cl)=C6

InChI

InChIKey=VGEXRDWWPSGZDH-UHFFFAOYSA-N

InChI=1S/C35H34ClN7O3S2/c1-35(2,3)30-19-32(43(41-30)23-12-14-27(45)26(36)18-23)38-34(46)37-20-22-8-4-6-10-28(22)48-24-13-15-31-39-40-33(42(31)21-24)25-9-5-7-11-29(25)47-17-16-44/h4-15,18-19,21,44-45H,16-17,20H2,1-3H3,(H2,37,38,46)

HIDE SMILES / InChI

Molecular Formula	C35H34ClN7O3S2
Molecular Weight	700.273
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://adisinsight.springer.com/drugs/800028997 | https://erj.ersjournals.com/content/42/Suppl_57/1764.article-info | https://www.ncbi.nlm.nih.gov/pubmed/25599809 | https://www.ncbi.nlm.nih.gov/pubmed/26265232

PF-03715455 is a potent p38 inhibitor, showing some selectivity for p38-alpha over p38-beta. PF-03715455 inhibited IL-6, MCP-1, MIP1β, CC16 and CRP levels in plasma of healthy subjects. PF-03715455 was optimized for delivery by inhalation. PF-03715455 substantially reduced tobacco-smoke--induced lung neutrophilia and inflammatory damage to the lungs. PF-03715455 had been in phase II clinical trial for the treatment of asthma and phase I clinical trial for the treatment of chronic obstructive pulmonary disease. However, these investigations were discontinued.

Originator

Approval Year

PubMed

Title	Date	PubMed
Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease.	2011 Nov 24	21888439
Oral and inhaled p38 MAPK inhibitors: effects on inhaled LPS challenge in healthy subjects.	2015 Oct	26265232

Patents

Sample Use Guides

In Vivo Use Guide

680 ug b.i.d.

Route of Administration: Respiratory

Substance Class	Chemical Created by `admin` on `Sat Dec 16 05:41:35 GMT 2023` Edited by `admin` on `Sat Dec 16 05:41:35 GMT 2023`
Record UNII	0TJ631J0KP
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PF-03715455

Common Name

English

PF-3715455

Common Name

English

UREA, N-(1-(3-CHLORO-4-HYDROXYPHENYL)-3-(1,1-DIMETHYLETHYL)-1H-PYRAZOL-5-YL)-N'-((2-((3-(2-((2-HYDROXYETHYL)THIO)PHENYL)-1,2,4-TRIAZOLO(4,3-A)PYRIDIN-6-YL)THIO)PHENYL)METHYL)-

Systematic Name

English

Code System Code Type Description

CAS

1056164-52-3