PF-04634817

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C25H36F3N5O3
Molecular Weight	511.5802
Optical Activity	UNSPECIFIED
Defined Stereocenters	6 / 6
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CO[C@@H]1COCC[C@@H]1N[C@@H]2CC[C@](C2)(C(C)C)C(=O)N3C[C@@H]4C[C@H]3CN4C5=NC=NC(=C5)C(F)(F)F

InChI

InChIKey=MCRWZBYTLVCCJJ-DKALBXGISA-N

InChI=1S/C25H36F3N5O3/c1-15(2)24(6-4-16(10-24)31-19-5-7-36-13-20(19)35-3)23(34)33-12-17-8-18(33)11-32(17)22-9-21(25(26,27)28)29-14-30-22/h9,14-20,31H,4-8,10-13H2,1-3H3/t16-,17+,18+,19+,20-,24+/m1/s1

HIDE SMILES / InChI

Molecular Formula	C25H36F3N5O3
Molecular Weight	511.5802
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	6 / 6
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/30450458 | https://www.ncbi.nlm.nih.gov/pubmed/29847672 | https://adisinsight.springer.com/drugs/800032291

PF-04634817 is a small molecule chemokine CCR2 and CCR5 receptor dual antagonist. Treatment with PF-04634817 was associated with a modest improvement in best-corrected visual acuity, which was inferior to intravitreal ranibizumab. Analysis of the primary endpoint, Urine Albumin-to-Creatinine Ratio, indicated a modest effect of PF-04634817 in reducing albuminuria in subjects with type 2 diabetes who received angiotensin receptor blocker therapy after 12 weeks of treatment. Despite the tolerable safety profile shown by PF-04634817, clinical development was discontinued in light of the modest efficacy observed.

Originator

Approval Year

PubMed

Title	Date	PubMed

Sample Use Guides

In Vivo Use Guide

200 mg once daily

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Sat Dec 16 11:35:41 GMT 2023` Edited by `admin` on `Sat Dec 16 11:35:41 GMT 2023`
Record UNII	51M3FB9B9E
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PF-04634817

Common Name

English

1,5-ANHYDRO-2,3-DIDEOXY-4-O-METHYL-3-(((1R,3S)-3-(1-METHYLETHYL)-3-(((1S,4S)-5-(6-(TRIFLUOROMETHYL)-4-PYRIMIDINYL)-2,5-DIAZABICYCLO(2.2.1)HEPT-2-YL)CARBONYL)CYCLOPENTYL)AMINO)-D-ERYTHRO-PENTITOL

Systematic Name

English

D-ERYTHRO-PENTITOL, 1,5-ANHYDRO-2,3-DIDEOXY-4-O-METHYL-3-(((1R,3S)-3-(1-METHYLETHYL)-3-(((1S,4S)-5-(6-(TRIFLUOROMETHYL)-4-PYRIMIDINYL)-2,5-DIAZABICYCLO(2.2.1)HEPT-2-YL)CARBONYL)CYCLOPENTYL)AMINO)-

Systematic Name

English

Code System Code Type Description

SMS_ID

300000041328