InChI | InChI=1S/C29H23F6N5O3/c1-13-16(22-18(30)4-5-19(31)23(22)32)8-20(26(42)40(13)12-29(33,34)35)38-25(41)15-7-14-9-28(10-21(14)37-11-15)17-3-2-6-36-24(17)39-27(28)43/h2-7,11,13,16,20H,8-10,12H2,1H3,(H,38,41)(H,36,39,43)/t13-,16-,20+,28+/m1/s1 |
Reference | 1. Preparation of piperidinonylcarboxamideazaindane derivatives for use as CGRP receptor antagonists
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By: Bell, Ian M.; Fraley, Mark E.; Gallicchio, Steven N.; Ginnetti, Anthony; Mitchell, Helen J.; Paone, Daniel V.; Staas, Donnette D.; Wang, Cheng; Zartman, C. Blair; Stevenson, Heather E.
Assignee: Merck Sharp & Dohme Corp., USA<br>
Patent Information: May 18, 2012, WO 2012064910, A1<br>
Application: Nov 10, 2011, WO 2011-US60081<br>
Priority: Nov 12, 2010, US 2010-61413077, Dec 20, 2010, US 2010-61425034, Nov 10, 2011, WO 2011-US60081, Nov 10, 2011, EP 2011-787987, Nov 10, 2011, US 2011-13293177, Sep 12, 2014, US 2014-14485259
Source: PCT Int. Appl., 93pp., Patent, 2012, CODEN: PIXXD2
Language: English
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Abstract<br>
Title compds. I [X = CH, CF, CCN, or N; R1 = (un)substituted alkyl, cyclopropylmethyl, cyclobutylmethyl, or [1-(trifluoromethyl)cyclopropyl]methyl; R2 = H or Me; R3, R4, and R7 independently = H, F, Cl, etc.; R5 and R6 independently = H or F; with provisions], and their pharmaceutically acceptable salts, are prepd. and disclosed as CGRP receptor antagonists. Thus, e.g., II was prepd. by a multistep procedure (prepn. given). Select I were evaluated in recombinant receptor functional assays, e.g., II demonstrated a Ki value of 0.067 nM.
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