PF-04531083

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C17H16ClN5O2
Molecular Weight	357.794
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

COC1=CC=C(Cl)C(=C1)C2=C(N)N=C(NC(=O)C3=CC=NN3C)C=C2

InChI

InChIKey=ZRJGMDIPCQOGNI-UHFFFAOYSA-N

InChI=1S/C17H16ClN5O2/c1-23-14(7-8-20-23)17(24)22-15-6-4-11(16(19)21-15)12-9-10(25-2)3-5-13(12)18/h3-9H,1-2H3,(H3,19,21,22,24)

HIDE SMILES / InChI

Molecular Formula	C17H16ClN5O2
Molecular Weight	357.794
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

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

Description

PF-04531083 is selective Nav1.8 blocker. It has been investigated for the treatment of chronic pain, heart pain, post-surgical dental pain. However, these trials were discontinued.

Originator

Approval Year

PubMed

PubMed

Title	Date	PubMed
Recent progress in sodium channel modulators for pain.	2014 Aug 15	25060923

Sample Use Guides

In Vivo Use Guide

Single dose - 1000 mg or 2000 mg

Route of Administration: Oral

Substance Class	Chemical
Record UNII	40497CY7Y3
Record Status	`Validated (UNII)`
Record Version

Show entries

Name

Type

Language

PF-04531083

Common Name

English

PF-4531083

Code

English

1H-PYRAZOLE-5-CARBOXAMIDE, N-(6-AMINO-5-(2-CHLORO-5-METHOXYPHENYL)-2-PYRIDINYL)-1-METHYL-

Systematic Name

English

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Code System

Code

Type

Description

DRUG BANK

DB12468

PRIMARY

CAS

1079400-07-9

PRIMARY

CLINICAL_TRIALS.GOV

PF-04531083

PRIMARY

6 studies found for: PF-04531083

MANUFACTURER PRODUCT INFORMATION

PF-04531083

PRIMARY

PF-04531083: Synonym: N-(6-Amino-5-(2-chloro-5-methoxyphenyl)-2-pyridinyl)-1-methyl-1H-pyrazole-5-carboxamide, N-(6-Amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide, PF 4531083

SMS_ID

300000041337

PRIMARY

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Related Record

Type

Details


					40497CY7Y3

PF-04531083

ACTIVE MOIETY

Comments:

Originator: Pfizer; Class: Analgesic; Orphan Drug Status: No; On Fast track: No; Highest Development Phases: Discontinued for Pain, Postoperative pain; Most Recent Events: 10 Jul 2012 Pfizer terminates phase II trial in Postoperative pain in USA (NCT01512160), 22 May 2012 Pfizer completes enrolment in its phase II trial for Postoperative pain in USA (NCT01512160), 10 May 2012 Discontinued - Phase-I for Pain in Belgium (PO)


					40497CY7Y3

PF-04531083

ACTIVE MOIETY

Comments:

Compound: PF-04531083; Company: Pfizer; Pharmacology: Nav1.8; Phase: I; Therapeutic indication: Neuropathic/Inflammatory pain (oral)

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