6880-04-2Relevant articles and documents
THERAPEUTIC COMPOUNDS
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Page/Page column 57, (2010/11/27)
This invention relates to a novel class of substituted amino-ethoxy benzene derivatives of formula (I) which are inhibitors of serine proteases and to their use in treating aberrant serine protease activity in a mammal, contraception, anti-coagulant methods and methods for treating aberrant cell proliferation, tumours, cancer, angiogenesis, angiogenesis-based retinopathies, autoimmummune disease, inflammation, skin disease, arthritis, rheutmatoid arthritis, asthma, osteoarthritis and multiple sclerosis. (I), Wherein Rm, Rn, Rp, Rq, V, W, X, Y and R8 are as defined in the claims.
De novo asymmetric synthesis of milbemycin β3 via an iterative asymmetric hydration approach
Li, Miaosheng,O'Doherty, George A.
, p. 3987 - 3990 (2007/10/03)
The enantioselective synthesis of the spiroketal/macrolide natural product milbemycin β3 has been achieved in 22 steps and 2.8% overall yield from an achiral dienoate. The spiroketal ring system was installed by three sequential asymmetric hydr
Carboxylation of anisole derivatives with CO and O2 catalyzed by Pd(OAc)2 and molybdovanadophosphates
Ohashi, Shinichiro,Sakaguchi, Satoshi,Ishii, Yasutaka
, p. 486 - 488 (2008/09/18)
Anisole and its homologues were carboxylated under the influence of CO and O2 catalyzed by Pd(OAc)2 combined with molybdovanadophosphates (HPMoV) under mild conditions to give the corresponding carboxylic acids in fair to good yields; for instance, anisole underwent the carboxylation under a mixed gas of CO (0.5 atm) and O2 (0.5 atm) in the presence of Pd(OAc)2 (5 mol%) and H5PMo 10V2O40·nH2O (2 mol%) to form an isomeric mixture of anisic acids in good yield.
Towards a total synthesis of the new anticancer agent mensacarcin: Synthesis of the carbocyclic core
Tietze, Lutz F.,Stewart, Scott G.,Polomska, Marta E.,Modi, Andrea,Zeeck, Axel
, p. 5233 - 5242 (2007/10/03)
A synthesis of the carbocyclic core associated with the new anti-cancer agent mensacarcin (1) is reported. The strategy involves the synthesis of several novel highly substituted aromatic compounds, such as 12 and 23. The lithium derivative of 12 readily
1,2-disubstituted 1,4-dihydro-4-oxoquinoline compounds
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, (2008/06/13)
The present invention relates to substituted 1,4-dihydro-4-oxoquinolines having antiviral activity. The substituents are present at positions 1, 2 and at least one of 5-8 positions of the quinoline ring.
Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists
Van Muijlwijk-Koezen,Timmerman,Vollinga,Frijtag von Drabbe Künzel,De Groote,Visser,IJzerman
, p. 749 - 762 (2007/10/03)
Novel classes of heterocyclic compounds as adenosine antagonists were developed based on a template approach. Structure-affinity relationships revealed insights for extended knowledge of the receptor-ligand interaction. We replaced the bicyclic heterocycl
Steric Enhancement of Resonance-Evidence from Kinetic Study on some Acetophenones
Pillay, M. Krishna,Palanivelu, S.
, p. 1055 - 1059 (2007/10/02)
The kinetics of oxidation of some mono-, di- and tri-substituted acetophenones by alkaline hexacyanoferrate(III) in 50percent (v/v) methanol-water mixture at constant ionic strength and at 20, 30 and 40 deg have been studied spectrophotometrically and the rate constants determined by least-squares analysis.Electron-withdrawing groups in the ring facilitate the oxidation of the acetyl function while electron-releasing groups retard the rate.The rate constant values for the oxidation of 3-substituted-4-alkoxy-acetophenones are computed based on the principle of additivity of group effects.The observed rate constants are significantly lower than the calculated values.This is attributed to the phenomenon of steric enhancement of resonance (SER). 3,5-Disubstituted-4-methoxyacetophenones have higher observed rate constant values than the calculated ones.The steric inhibition of resonance (SIR) operates in these systems.In the case of 3-halogeno-4-methoxyacetophenones, the importance of SER increases with increase in the bulkiness of the 3-substituents.The difference between the calculated and observed multiple substituent constants of 3-substituted-4-methoxyacetophenones also lends support for SER.