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Bioorg Med Chem Lett. 2009 Aug 15;19(16):4740-2. doi: 10.1016/j.bmcl.2009.06.057. Epub 2009 Jun 17.

The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. ian_bell@merck.com

Abstract

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.

PMID:
19577468
DOI:
10.1016/j.bmcl.2009.06.057
[Indexed for MEDLINE]

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