- 1,3,4-OXADIAZOLE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The present invention relates to 1,3,4-oxadiazole derivative compounds having a histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, a use thereof in preparation of a medicament, a pharmaceutical composition comprising the same, a therapeutic method using the composition, and a method for preparing the same, and the 1,3,4-oxadiazole derivative compounds are represented by a following chemical formula (I).
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- An efficient synthesis of the piperidinyl dihydroquinazolinone (PDQ) fragment of olcegepant
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Olcegepant is one of the most potent and selective small molecule CGRP antagonists for the treatment of migraine headaches. Herein, we describe a new and efficient synthesis of the key piperidinyl dihydroquinazolinone (PDQ) fragment of olcegepant. PDQ plays a key role in the activity of CGRP antagonists. Primary improvements over existing methods include a high-yielding reductive amination step, greater overall yield, and operational simplicity. Coupling of PDQ to a D-tyrosine derivative effectively produced over one half of the total molecular structure of olcegepant. A unique tandem deprotection-nucleophilic addition sequence was also applied to the coupling of Fmoc-PDQ with phenyl isocyanate.
- Habay, Stephen A.,Miller, Julia M.,Bowler, Matthew M.,Manchak, Randi,Thomas, John Z.
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supporting information
p. 3389 - 3391
(2018/08/06)
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- CGRP receptor antagonists
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The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
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Page/Page column 138
(2008/06/13)
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- AMIDE-SUBSTITUTED ARYL PIPERIDINES
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Amide-substituted aryl piperidines derivatives of the following Formulas are provided:(Formulas), in which the variables are as described herein. Such compounds may be used to modulate calcitonin gene-related peptide (CGRP) receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CGRP modulation in humans, domesticated companion animals and livestock animals, including headache, such as migraine. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such compounds for receptor localization studies and various in vitro assays.
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Page/Page column 66-67
(2008/12/05)
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- BIARYL KETONE-SUBSTITUTED PIPERIDINES
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Biaryl ketone-substituted piperidines of the following Formulas are provided:, and in which the variables are as described herein. Such compounds may be used to modulate calcitonin gene-related peptide (CGRP) receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CGRP modulation in humans, domesticated companion animals and livestock animals, including headache such as migraine. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such compounds for receptor localization studies and various in vitro assays.
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Page/Page column 58
(2008/12/06)
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- Synthesis of (1-substituted piperidin-4-yl)-1H-benzimidazoles and (1-substituted piperidin-4-yl)-3,4-dihydroquinazolines as possible antihypertensive agents
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Structural modifications of 4-piperidylbenzimidazolinones (I) by replacing the benzimidazolinone group with other heterocycles (2-cyanoamino, 2-ethoxy, and 2-methylbenzimidazole and 2-cyanoamino-3,4-dihydroquinazoline) has been made and a number of new pi
- Obase,Takai,Teranishi,Nakamizo
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p. 565 - 573
(2007/10/02)
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