Title of article
Nonpeptide αvβ3 antagonists. Part 10: In vitro and in vivo evaluation of a potent 7-methyl substituted tetrahydro-[1,8]naphthyridine derivative
Author/Authors
Michael J. Breslin، نويسنده , , Mark E. Duggan، نويسنده , , Wasyl Halczenko، نويسنده , , George D. Hartman، نويسنده , , Le T. Duong، نويسنده , , Carmen Fernandez-Metzler، نويسنده , , Michael A Gentile، نويسنده , , Donald B. Kimmel، نويسنده , , Chih-Tai Leu، نويسنده , , Kara Merkle، نويسنده , , Thomayant Prueksaritanont، نويسنده , , Gideon A. Rodan، نويسنده , , Sevgi B. Rodan، نويسنده , , John H Hutchinson، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
4515
To page
4518
Abstract
Subtle modifications were incorporated into the structure of clinical candidate 1. These changes were designed to maintain potency and selectivity while inducing changes in physical properties leading to improved pharmacokinetics in three species. This approach led to the identification of 4 as a potent, selective αvβ3 receptor antagonist that was selected for clinical development based on an improved PK profile and efficacy demonstrated in an in vivo model of bone turnover.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794823
Link To Document