The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists

Ian M. Bell,Rodney A. Bednar,Halea A. Corcoran,John F. Fay,Steven N. Gallicchio,Victor K. Johnston,James C. Hershey,Cynthia M. Miller-Stein,Eric L. Moore,Scott D. Mosser,Shane A. Roller,Christopher A. Salvatore,Cory R. Theberge,Bradley K. Wong,C. Blair Zartman,Stefanie A. Kane,Theresa M. Williams,Samuel L. Graham,Joseph P. Vacca

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

A series of tricyclic CGRP receptor antagonists was optimized in order to improve oral bioavailability. Attenuation of polar surface area and incorporation of a weakly basic indoline nitrogen led to compound 5, a potent antagonist with good oral bioavailability in three species.

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关键词

CGRP receptor antagonists,CGRP,Migraine,Orally bioavailable

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