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New indole amide derivatives as potent CRTH2 receptor antagonists |
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| Authors: | Zaghdane Helmi Boyd Michael Colucci John Simard Daniel Berthelette Carl Leblanc Yves Wang Zhaoyin Houle Robert Lévesque Jean François Molinaro Carmela Hamel Martine Stocco Rino Sawyer Nicole Sillaots Susan Gervais François Gallant Michel |
| Institution: | a Medicinal Chemistry, Merck Frosst, Center of Therapeutic Research, 16711 Trans Canada Hwy, Kirkland, Quebec, Canada H9H 3L1 b DMPK, Merck Frosst, Center of Therapeutic Research, 16711 Trans Canada Hwy, Kirkland, Quebec, Canada H9H 3L1 c Process Chemistry, Merck Frosst, Center of Therapeutic Research, 16711 Trans Canada Hwy, Kirkland, Quebec, Canada H9H 3L1 d Biochemistry and Molecular Biology, Merck Frosst, Center of Therapeutic Research, 16711 Trans Canada Hwy, Kirkland, Quebec, Canada H9H 3L1 |
| Abstract: | A new series of indole amide acting as hCRTH2 receptor ligands had been explored and are described herein. Several amide derivatives displaying low nanomolar activity in hCRTH2 binding and whole blood assays were identified. They were found to behave as a full antagonists, exhibiting good selectivity over related prostaglandin receptors. Also, prototypical compounds in this novel series which displayed acceptable CYP profiles and were orally bioavailable in rats were identified. |
| Keywords: | CRTH2 receptor antagonists DP2 receptor antagonist Prostaglandin receptors MK-7246 Asthma |
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