- Synthesis and biological evaluation of pyrimidine derivatives with diverse azabicyclic ether/amine as novel GPR119 agonist
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A class of novel pyrimidine derivatives bearing diverse conformationally restricted azabicyclic ether/amine were designed, synthesized and evaluated for their GPR119 agonist activities against type 2 diabetes. Most compounds exhibited superior hEC50
- Yang, Zunhua,Fang, Yuanying,Park, Haeil
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p. 2515 - 2519
(2017/05/10)
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- TRICYCLIC GYRASE INHIBITORS FOR USE AS ANTIBACTERIAL AGENTS
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Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
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- Synthesis of novel azanorbornylpurine derivatives
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Azanorbornylpurine derivatives were prepared by Mitsunobu reaction of appropriate hydroxyazanorbornane derivative with 6-chloropurine or construction of purine base at azanorbornylamines. The prepared target compounds were evaluated for antiviral activity and effect on neuronal and muscle nicotinic acetylcholine receptors.
- H?ebabecky, Hubert,Dejmek, Milan,Dra?ínsky, Martin,?ála, Michal,Leyssen, Pieter,Neyts, Johan,Kaniaková, Martina,Kr?ek, Jan,Nencka, Radim
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experimental part
p. 1286 - 1298
(2012/02/15)
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- TRICYCLIC GYRASE INHIBITORS
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Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
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- BRIDGED BICYCLIC RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE
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The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptab
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Page/Page column 51
(2011/06/26)
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- Improved synthesis of monoprotected 5- and 6-amino-2-azanorbornanes
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(Chemical Equation Presented) An improved synthesis of Boc-monoprotected 5- and 6-amino-2-azanorbornanes is reported. The synthetic scheme consists of five steps and allows multigram quantities of the title compounds to be obtained. The regio- and stereochemistries of the products are established by two-dimensional NMR experiments. Copyright Taylor & Francis Group, LLC.
- Dacenko, Oleksandr P.,Manoylenko, Olga V.,Grygorenko, Oleksandr O.,Mykhailiuk, Pavel K.,Volochnyuk, Dmitriy M.,Shishkin, Oleg V.,Tolmachev, Andrey A.
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p. 981 - 992
(2011/04/25)
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- PIPERAZINO DERIVATIVES AS NEUROKININ ANTAGONISTS
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The invention relates to compounds of formula (I) wherein Z, Rc, y, m, u, Ar2, n, X, Rc', l and Ar2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
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Page/Page column 38
(2010/11/08)
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- Heterocyclic compounds
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The present invention provides heterocyclic 2-aza-bicyclo[2.2.1]heptane compounds which are useful for modulating a muscarinic ptor.
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