- QUATERNARY LACTAM COMPOUND AND PHARMACEUTICAL USE THEREOF
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A quaternary lactam compound of formula (I). The compound is used in the manufacture of a medicament for the treatment and/or prevention of thrombotic or thromboembolic disorders.
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Paragraph 0143-0145
(2021/02/05)
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- Medium-Ring Nitrogen Heterocycles through Migratory Ring Expansion of Metalated Ureas
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Simple benzo-fused nitrogen heterocycles (indolines, tetrahydroquinolines, and their homologues) undergo migratory ring expansion through deprotonation of their benzylic urea derivatives with lithium diisopropylamide (LDA) in the presence of N,N′-dimethyl
- Hall, Jessica E.,Matlock, Johnathan V.,Ward, John W.,Gray, Katharine V.,Clayden, Jonathan
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supporting information
p. 11153 - 11157
(2016/10/13)
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- Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
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Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of semicarbazone-based cathepsin K inhibitors with greater solubility and better pharmacokinetic profiles than their parent aldehydes. Furthermore, a representative semicarbazone inhibitor attenuated bone resorption in an ex vivo rat calvarial bone resorption model. However, based on enzyme inhibition comparisons at neutral pH, semicarbazone hydrolysis rates, and 13C NMR experiments, these semicarbazones probably function as prodrugs of aldehydes.
- Adkison, Kim K.,Barrett, David G.,Deaton, David N.,Gampe, Robert T.,Hassell, Anne M.,Long, Stacey T.,McFadyen, Robert B.,Miller, Aaron B.,Miller, Larry R.,Payne, J. Alan,Shewchuk, Lisa M.,Wells-Knecht, Kevin J.,Willard Jr., Derril H.,Wright, Lois L.
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p. 978 - 983
(2007/10/03)
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- New linear or cyclic ureas
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Compound of formula (I): wherein: V represents a single bond or an alkylene chain, M represents a single bond or an alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group
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- Process for the preparation of 1-4-disubstituted-5 (4H)-tetrazolinones
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1,4-Disubstituted-5(4H)-tetrazolinones of the formula (I) STR1 wherein R1, R2 and R3 have the meanings given in the specification), which are known to be useful as herbicides, can be obtained in very good yields by reacting the corresponding 1-substituted-5(4H)-tetrazolinones with the corresponding carbamoyl chlorides in the presence of 4-dimethylaminopyridine.
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- Mesolimbic selective antipsychotic arylcarbamates
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4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidine has been linked to various arylcarbamates to obtain compounds having affinity for dopamine-D1 and -D2, serotonin 5HT(2A) and α1-adrenoceptors. When linkers with restricted flexibility are used, the biological activity is reduced indicating that a bended conformation is needed in this series of bioactive molecules. Compounds with a relatively low D2/5HT(2A) affinity ratio in receptor binding experiments and high affinity for the α1-adrenoceptors exhibit a pharmacological profile which suggests a preferential effect on the mesocorticolimbic dopaminergic system and an 'atypical' antipsychotic activity.
- Hansen, John Bondo,Fink-Jensen, Anders,Christensen, Birgitte V.,Gronvald, Frederick C.,Jeppesen, Lone,Mogensen, John P.,Nielsen, Erik B.,Scheideler, Mark A.,White, Francis J.,Zhang, Xu-Feng
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p. 839 - 858
(2007/10/03)
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