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Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

JNJ 54166060

Target

P2X7 receptor

Action

modulators

Mechanism

P2X7 receptor modulators(P2X purinoceptor 7 modulators)

Therapeutic Areas

Nervous System Diseases

Active Indication-

Inactive Indication

Depressive Disorder

Originator Organization

Johnson & Johnson

Active Organization-

Inactive Organization

Johnson & Johnson

License Organization-

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC20H15ClF4N4O

InChIKeyPLIXFSPGDVKMDM-NSHDSACASA-N

CAS Registry1627900-42-8

Author: De Angelis, Meri ; Schoetens, Freddy ; Everson, Anita ; Savall, Brad M. ; Wall, Jessica ; Lord, Brian ; Skaptason, Judith ; Koudriakova, Tatiana ; Lovenberg, Timothy W. ; Rech, Jason ; Scott, Brian ; Wang, Qi ; Swanson, Devin M. ; Coe, Kevin J. ; Carruthers, Nicholas I. ; Letavic, Michael A. ; Deng, Xiahou ; Ao, Hong ; Sepassi, Kia ; Bhattacharya, Anindya

The synthesis and SAR of a series of 4,5,6,7-tetrahydro-imidazo[4,5-c]pyridine P2X7 antagonists are described. Addressing P2X7 affinity and liver microsomal stability issues encountered with this template afforded methyl substituted 4,5,6,7-tetrahydro-imidazo[4,5-c]pyridines ultimately leading to the identification of 1 (JNJ 54166060). 1 is a potent P2X7 antagonist with an ED50 = 2.3 mg/kg in rats, high oral bioavailability and low-moderate clearance in preclinical species, acceptable safety margins in rats, and a predicted human dose of 120 mg of QD. Additionally, 1 possesses a unique CYP profile and was found to be a regioselective inhibitor of midazolam CYP3A metabolism.

100 Deals associated with JNJ-54166060

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