- Design and synthesis of a novel series of 4-heteroarylamino-1′-azaspiro[oxazole-5,3′-bicyclo[2.2.2]octanes as α7 nicotinic receptor agonists 2. Development of 4-heteroaryl SAR
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Quinuclidine-containing spirooxazolines, as described in the previous report in this series, were demonstrated to have utility as α7 nicotinic acetylcholine receptor (α7 nAChR) partial agonists. In this work, the SAR of this chemotype was expanded to include an array of diazine heterocyclic substitutions. Many of the heterocyclic analogs were potent partial agonists of the α7 receptor, selective against other nicotinic receptors and the serotinergic 5HT3A receptor. (1′S,3′R,4′S)-N-(6-phenylpyrimidin-4-yl)-4H-1′-azaspiro[oxazole-5,3′-bicyclo[2.2.2]octan]-2-amine, a potent and selective α7 nAChR partial agonist, was demonstrated to improve cognition in the mouse novel object recognition (NOR) model of episodic memory.
- Iwuagwu, Christiana,King, Dalton,McDonald, Ivar M.,Cook, James,Zusi, F. Christopher,Hill, Matthew D.,Mate, Robert A.,Fang, Haiquan,Knox, Ronald,Gallagher, Lizbeth,Post-Munson Amy Easton, Debra,Miller, Regina,Benitex, Yulia,Siuciak, Judy,Lodge, Nicholas,Zaczek, Robert,Morgan, Daniel,Bristow, Linda,Macor, John E.,Olson, Richard E.
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supporting information
p. 1261 - 1266
(2017/06/19)
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- Hydantoin and thiohydantoin derivatives as antiviral drugs
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The present invention relates to a compound of the following formula (I), or a salt, solvate, tautomer, enantiomer, diastereoisomer or racemic mixture thereof: as well as its use as a drug, notably in the treatment of hepatitis C, its preparation process, and the pharmaceutical compositions containing such a compound.
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Paragraph 0207-0208
(2013/12/03)
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- HYDANTOIN AND THIOHYDANTOIN DERIVATIVES AS ANTIVIRAL DRUGS
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The present invention relates to a compound of the following formula (I), or a salt, solvate, tautomer, enantiomer, diastereoisomer or racemic mixture thereof: as well as its use as a drug, notably in the treatment of hepatitis C, its preparation process, and the pharmaceutical compositions containing such a compound.
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Page/Page column 109-110
(2013/12/03)
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- Multifunctional Compounds and Methods of Use Thereof
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Compositions comprising multifunctional agents and methods of use thereof are provided.
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Page/Page column 10
(2009/05/29)
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- IMIDAZOL [1,2-A] PYRIDINES AND RELATED COMPOUNDS WITH ACTIVITY AT CANNABINOID CB2 RECEPTORS
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Disclosed are compounds of Formula (I) or Formula (II) or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof; and methods of modulating the activity of a cannabinoid CB2 receptor comprising contacting a compound of Formula (I) or Formula (II) with the cannabinoid CB2 receptor. Said compounds are useful in the treatment of various condition and disorders such as pain, and neurodegenerative disorders.
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Page/Page column 54
(2009/01/20)
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- COMPOUNDS AND THERAPEUTICAL USE THEREOF
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Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
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Page 136; 233-234
(2008/06/13)
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- Compounds and uses thereof for decreasing activity of hormone-sensitive lipase
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Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.
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- The use of high pressure liquid chromatography in stability studies of sulfonamides. 3. Sulfamethoxydiazine. Isolation and identification of hydrolytic decomposition products
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The stability of sulphamethoxydiazine (1) in HCl (1 mol/l) under elevated temperature was investigated. Isolated decomposition products further served as standards for the selection of HPLC conditions. Three types of stationary phases were tested: Pragosil 5, MicroPak CN-10, MicroPak CH-10. The selection of mobile phases was made in such a way as to be able to inject 1 hydrolysate in HCl (1 mol/l) directly or after simple dilution. Detection was performed with an UV detector at the wavelength of 226 nm. A column packed with MicroPak CN-10 was selected to investigate the process of 1 decomposition. The method made it possible to quantify 1 in the course of hydrolysis and to illustrate the process of decomposition. On the basis of continuous examination of the development of decomposition products during the stability study it was possible to consider the chemism of the decomposition reaction.
- Klimes,Zahradnicek
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p. 511 - 513
(2007/10/02)
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