787585-27-7Relevant articles and documents
Discovery of a potent and short-acting oral calcilytic with a pulsatile secretion of parathyroid hormone
Shinagawa, Yuko,Inoue, Teruhiko,Katsushima, Takeo,Kiguchi, Toshihiro,Ikenogami, Taku,Ogawa, Naoki,Fukuda, Kenji,Hirata, Kazuyuki,Harada, Kazuhito,Takagi, Masaki,Nakagawa, Takashi,Kimura, Shuichi,Matsuo, Yushi,Maekawa, Mariko,Hayashi, Mikio,Soejima, Yuki,Takahashi, Mitsuru,Shindo, Masanori,Hashimoto, Hiromasa
body text, p. 238 - 242 (2011/04/26)
Short-acting oral calcilytics, calcium-sensing receptor (CaSR) antagonists, have been considered as alternatives for parathyroid hormone (PTH), an injectable bone anabolic drug used in the treatment of osteoporosis. Previously, we identified aminopropandi
1,1-(Dimethyl-Ethylamino)-2-Hydroxy-Propoxy]-Ethyl}-3-Methyl-Biphenyl-4- Carboxylic Acid Derivatives As Calcium Receptor Antagonists
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Page/Page column 31-32, (2010/10/03)
The present invention is directed to novel 1,1 -(dimethyl-ethylamino)-2- hydroxy-propoxy]-ethyl}-3-methyl-biphenyl-4-carboxylic acid derivatives and pharmaceutically acceptable salts thereof of structural formula I wherein the variable R1 is as described herein. Also provided are pharmaceutical compositions comprising the compounds of formula I as well as methods of treatment employing compounds of formula I to treat a disease or disorder characterized by abnormal bone or mineral homeostasis such as hypoparathyroidism, osteoporosis, osteopenia, periodontal disease, Paget's disease, bone fracture, osteoarthritis, rheumatoid arthritis, and humoral hypercalcemia of malignancy.
Metabolism-guided design of short-acting calcium-sensing receptor antagonists
Southers, James A.,Bauman, Jonathan N.,Price, David A.,Humphries, Paul S.,Balan, Gayatri,Sagal, John F.,Maurer, Tristan S.,Zhang, Yan,Oliver, Robert,Herr, Michael,Healy, David R.,Li, Mei,Kapinos, Brendon,Fate, Gwendolyn D.,Riccardi, Keith A.,Paralkar, Vishwas M.,Brown, Thomas A.,Kalgutkar, Amit S.
scheme or table, p. 219 - 223 (2010/11/03)
As part of a strategy to deliver short-acting calcium-sensing receptor (CaSR) antagonists, the metabolically labile thiomethyl functionality was incorporated into the zwitterionic amino alcohol derivative 3 with the hope of increasing human clearance through oxidative metabolism, while delivering a pharmacologically inactive sulfoxide metabolite. The effort led to the identification of thioanisoles 22 and 23 as potent and orally active CaSR antagonists with a rapid onset of action and short pharmacokinetic half-lives, which led to a rapid and transient stimulation of parathyroid hormone in a dose-dependent fashion following oral administration to rats. On the basis of the balance between target pharmacology, safety, and human disposition profiles, 22 and 23 were advanced as clinical candidates for the treatment of osteoporosis.
CaSR ANTAGONIST
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Page/Page column 45, (2008/06/13)
The present invention provides a compound having a calcium-sensitive receptor antagonistic action, a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis. A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the description.
CaSR antagonist
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Page/Page column 39, (2010/02/10)
A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.
