24941-58-0Relevant articles and documents
INHIBITORS OF TYROSINE KINASE
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Paragraph 00371, (2021/01/29)
The present disclosure provides compounds and compositions thereof which are useful as inhibitors of tyrosine kinase and which exhibit desirable characteristics for the same. Further disclosed herein are methods of treating cancer using these tyrosine kin
ANTIMICROBIAL COMPOSITIONS, METHODS OF USE, AND METHODS OF TREATMENT OF INFECTIONS
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Page/Page column 29, (2016/12/22)
The present disclosure provides compositions including a compound (e.g., compounds A-D), pharmaceutical compositions including the compound, methods of treatment of a condition (e.g., an infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.
Synthesis of the oxa-bridged octalin system of two anti-anaerobe antibiotics, luminamicin and lustromycin
Sunazuka, Toshiaki,Handa, Masaki,Hirose, Tomoyasu,Matsumaru, Takanori,Togashi, Yuko,Nakamura, Kaoru,Iwai, Yuzuru,Omura, Satoshi
, p. 5297 - 5300 (2008/02/09)
An efficient, stereocontrolled entry to the 11-oxatricyclo[5.3.1.1,703,8]undecane nucleus of luminamicin and lustromycin was afforded via intramolecular hetero-Michael addition of enone 7 followed by intramolecular aldol condensation of aldehyde 5 by way of the epimerization at the stereocenter attached by the aldehyde group.
Preorganized ligand arrays based on spirotetrahydrofuranyl motifs. Synthesis of the steyeoisomeric 1,8,14-trioxatrispiro[4.1.4.1.4.1]octadecanes and the contrasting conformational features and ionic binding capacities of these belted ionophores
Paquette,Tae,Hickey,Trego,Rogers
, p. 9160 - 9171 (2007/10/03)
The cis,trans trispiro ether 4 is accessible from several synthetic directions as a consequence of a crossover in reaction selectivity when proceeding from nucleophilic attack on the cis dispiro ketone to oxygenation of the α,β-unsaturated ester 17. Its cis,cis isomer 3 was obtained in 17 steps and 14.6% overall yield from 3,5-dimethoxybenzoic acid by making use of the alicyclic side chain in N as a "conformational lock". Although 4 shows no measurable tendency to complex with alkali metal ions, 3 binds strongly to Li+ and Na+ ions, as well as to CH3NH3+. Whereas the 3eq conformation is populated in the solid state and in solution, complex formation occurs readily. 13C NMR studies have defined slow exchange limits as the 2:1 sandwich complex with lithium ion is initially formed and transformed progressively into a 1:1 species upon the addition of more LiClO4. Only the 2:1 complex with sodium ion is formed during comparable titration with NaClO4. Association constants, molecular mechanics calculations, and X-ray crystallographic studies provide insight into the binding capacity of this belted tridentate ionophore.
Conformationally restricted butyrophenones with mixed dopaminergic (D2) and serotoninergic (5-HT(2A)) affinities. Synthesis of 5-aminoethyl-and 6- aminomethyl-4-oxotetrahydroindoles as potential atypical antipsychotics
Masaguer, Christian F.,Casariego, Isabel,Ravina, Enrique
, p. 621 - 632 (2007/10/03)
We describe the synthesis of 5-aminoethyl- and 6-aminomethyl-4- oxotetrahydroindoles as butyrophenone derivatives in the indole series, as potential atypical antipsychotics. The affinities of these compounds for serotonin (5-HT(2A)) and dopamine (D2) receptors were evaluated in vitro. The ratios of pK(i)'s for 5-HT(2A)/D2 receptors may be useful for rapid screening of new compounds and assessing potential induction of extrapyramidal symptoms; ratio values ≥1.12 (Meltzer's ratio) are predictive of an atypical antipsychotic profile. Compounds 26e (QF 0408B) and 26f (QF 0409B) showed high affinity for both D2 and 5-HT(2A) receptors, and their Meltzer's ratios were 1.32 and 1.17 respectively, while haloperidol showed a ratio of 0.93.
New cyclic butyrophenone derivatives in the indole series as potential atypical antipsychotics. A simple and practical synthesis of 6-aminomethyl-tetrahydroindol-4-ones and their affinities for D2 and 5-HT(2A) receptors
Masaguer, Christian F.,Ravina, Enrique,Loza, Isabel,Fontenla, Jose Angel
, p. 913 - 918 (2007/10/03)
A simple and efficient synthesis of novel 6-aminomethyl-tetrahydroindol-4-ones, which are butyrophenone analogues of molindone, is described. These compounds exhibit potent affinities for D2 and 5-HT(2A) receptors in vitro. The most active compounds, 6d (QF 0408B) and 6e (QF 0409B), with pK(i) (5-HT(2A)/D2) ratios of 1.32 and 1.17 respectively, show an antipsychotic profile according to Meltzer's classification.
Synthesis of 4,4-Disubstituted Cyclohexenones. Part 2. Cycloaddition of 2-Chloroacrylonitrile to 5-Substituted 1,3-Dimethoxycyclohexa-1,4-dienes
Clark, Richard S. J.,Holmes, Andrew B.,Matassa, Victor G.
, p. 1389 - 1400 (2007/10/02)
The cycloaddition of 2-chloroacrylonitrile to 1,3-dimethoxycyclohexadienes (3; R1=OMe, R2=H), derived by in situ conjugation of the Birch reduction products (12) produced from aromatic precursors (11) gave after acid work-up mainly bicyclooctanone
