The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core

被引：7

作者：

Harrington, Paul E. ^{[1
]}

Jean, David J. St., Jr. ^{[1
]}

Clarine, Jeffrey ^{[4
]}

Coulter, Thomas S. ^{[5
]}

Croghan, Michael ^{[1
]}

Davenport, Adam ^{[5
]}

Davis, James ^{[2
]}

Ghiron, Chiara ^{[5
]}

Hutchinson, Jonathan ^{[5
]}

Kelly, Michael G. ^{[1
]}

Lott, Fred ^{[2
]}

Lu, Jenny Ying-Lin ^{[3
]}

Martin, David ^{[2
]}

Morony, Sean ^{[2
]}

Poon, Steve F. ^{[1
]}

Portero-Larragueta, Elena ^{[5
]}

Reagan, Jeff D. ^{[3
]}

Regal, Kelly A. ^{[4
]}

Tasker, Andrew ^{[1
]}

Wang, Minghan ^{[2
]}

Yang, Yuhua ^{[3
]}

Yao, Guomin ^{[1
]}

Zeng, Qingping ^{[1
]}

Henley, Charles, III ^{[2
]}

Fotsch, Christopher ^{[1
]}

机构：

[1] Amgen Inc, Chem Res & Discovery, Thousand Oaks, CA 91320 USA

[2] Amgen Inc, Metab Disorders, Thousand Oaks, CA 91320 USA

[3] Amgen Inc, Metab Disorders, San Francisco, CA 94080 USA

[4] Amgen Inc, Pharmacokinet & Drug Metab, Thousand Oaks, CA 91320 USA

[5] Evotec UK Ltd, Abingdon OX14 4SA, Oxon, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 18期

关键词：

Calcimimetic; Allosteric modulator; REDUCTIVE AMINATION; CALCIMIMETICS; HYPERPARATHYROIDISM; METABOLISM; ACTIVATORS;

D O I：

10.1016/j.bmcl.2010.07.060

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The discovery of a series of novel and orally efficacious type II calcimimetics, developed from the lead compound 1, is described herein. Compound 22 suppressed plasma PTH levels relative to vehicle when dosed orally in a rat pharmacodynamic model. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：5544 / 5547

页数：4

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