- (8β)-Ergoline-8-carboxylic acid cycloalkyl esters as serotonin antagonists: Structure-activity study
-
A series of (8β)-6-methyl-1-(1-methylethyl)ergoline-8-carboxylic acid cycloalkyl esters were prepared and examined for blockade of vascular 5HT2 receptors. The antagonist in this series that had the highest 5HT2 receptor affinity was
- Garbrecht,Marzoni,Whitten,Cohen
-
-
Read Online
- MICROWAVE ROTATIONAL SPECTRUM, ELECTRIC DIPOLE MOMENT AND GEOMTRY OF 2-BICYCLOHEXANONE
-
We report the microwave rotational spectrum of 2-bicyclohexanone in its vibrational ground state and in vibrationally excited states associared with the bending mode νB of the five-membered ring.Variation of the rotational constants with vb allows the conclusion that five/membered ring is effectively planar although the mode vb is governed by an asssymetric potential energy function.Measurement of the Stark effect in a number of transitions leads to the components μa=3.28+/-0.02D and μb=1.81+/-0.2D of the electric dipole moment.
- Davies, Ann P.,Legon, A. C.,Millen, D. J.,Roberts, A. J.
-
-
Read Online
- COMPOUND SERVING AS IRAK INHIBITOR
-
The present disclosure relates a compound as an IRAK inhibitor. Specifically, the present disclosure provides a compound of formula I, or a cis-trans isomer, an optical isomer, a racemate, a pharmaceutically acceptable salt, a prodrug, a deuterated derivative thereof, a hydrate or a solvate thereof. The compounds disclosed herein have potent inhibitory effects on IRAK and thus have therapeutic effect on IRAK-related diseases.
- -
-
-
- SUBSTITUTED 5-CYANOINDOLE COMPOUNDS AND USES THEREOF
-
A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for the treatment of lysine (K)-specific demethylase 1A (LSD1) - mediated diseases or disorders, Formula (I), wherein R1, R2, R3, R4, and R5 are as defined herein.
- -
-
Paragraph 00274; 00311
(2019/01/10)
-
- FUSED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTCIAL COMPOSITION, AND USES THEREOF
-
Disclosed are a fused heterocyclic compound, a preparation method therefor, a pharmaceutical composition, and uses thereof. The fused heterocyclic compound is shown in formula I, formula II, or formula III. The preparation method of the fused heterocyclic compound and/or the pharmaceutically acceptable salt thereof in the present invention comprises three synthesizing routes. The present invention also provides a pharmaceutical composition of the fused heterocyclic compound, the pharmaceutical composition containing one or more of the fused heterocyclic compound shown in formula I, formula II, or formula III, the pharmaceutically acceptable salt thereof, hydrates, solvent compounds, polymorphs and prodrugs thereof, and a pharmaceutically acceptable carrier. The present invention also relates to an application of the fused heterocyclic compound and/or the pharmaceutical composition in preparing kinase inhibitors and in preparing drugs for preventing and treating diseases related to kinase. The fused heterocyclic compound of the present invention has selective inhibition function on PI3Kδ, and can be used for preparing drugs for preventing and treating cell proliferation diseases such as cancers, infections, inflammations, or autoimmune diseases.
- -
-
Paragraph 0317; 0318; 0337; 0338
(2016/09/26)
-
- Ionic liquids based on the 7-azabicyclo[2.2.1]heptane skeleton: Synthesis and properties
-
Based on a previously developed method for the synthesis of epibatidine analogues, a series of new ionic liquids, based on the 7-azabicyclo[2.2.1] heptane skeleton, have been synthesized. The chemical and physical properties of the ionic liquids with bis(trifluoromethylsulfonyl)imide (Tf2N) and dicyanamide [N(CN)2] anions were investigated and they were found to exhibit very good electrochemical and thermal stabilities. Ionic liquids with the cationic part based on the structure of epibatidine (a 7-azabicyclo[2.2.1] skeleton) have been prepared. The chemical and physical properties of these ionic liquids with dicyanamide and bis(trifluoromethylsulfonyl)imide anions were investigated and they were found to show very good electrochemical and thermal stability. Copyright
- De Vos, Nils,Maton, Cedric,De Vreese, Peter,Brooks, Neil R.,Binnemans, Koen,Stevens, Christian V.
-
p. 3741 - 3750
(2013/07/19)
-
- Unified oxidation protocol for the synthesis of carbonyl compounds using a manganese catalyst
-
We have developed a unified protocol for the oxidation of ethers, benzylic compounds, and alcohols to carbonyl compounds. The protocol uses catalytic amounts of manganese(II) chloride tetrahydrate and tri(t-butyl)-2,2':6',2Prime;- terpyridine in combination with a stoichiometric amount of either m-chloroperbenzoic acid (MCPBA) or potassium hydrogen peroxysulfate (KHSO 5). A reagent system consisting of the Mn catalyst and MCPBA permitted the chemoselective sp3 C-H oxidation of alkyl ethers and benzylic compounds to generate the corresponding ketones. Alternatively, the water-soluble inorganic salt KHSO5 in combination with the Mn catalyst was used to oxidize alcohols to ketones or carboxylic acids. Importantly, the Mn catalyst/KHSO5 system eliminates technical difficulties associated with the isolation of carboxylic acid products. All the oxidations presented in this feature article proceed at sup-ambient temperature in an aerobic atmosphere, and can therefore be used in practical syntheses of complex organic molecules. Georg Thieme Verlag Stuttgart · New York.
- Kamijo, Shin,Amaoka, Yuuki,Inoue, Masayuki
-
experimental part
p. 2475 - 2489
(2010/09/06)
-
- Manganese-catalyzed direct oxidation of methyl ethers to ketones
-
Direct C-H oxidation of alkyl ethers into ketones was achieved using 0.1 mol % of MnCl2 and 4, 4′, 4″-tri(tert-butyl)-2, 2′:6′, 2″-terpyridine (tBu-terpy) in the presence of mCPBA. Conversion of methyl ethers into ketones was particularly efficient and chemoselective. Electron-deficient oxygen functionalities survived under the reaction conditions. The present method broadens the utility of methyl ethers as stable protective groups for hydroxy functionalities and as precursors to carbonyl compounds. (Chemical equation presented).
- Kamijo, Shin,Amaoka, Yuuki,Inoue, Masayuki
-
supporting information; experimental part
p. 486 - 489
(2010/09/04)
-
- Heterocylic antiviral compounds
-
This invention relates to piperidine derivatives of formula I wherein R1, R2, R3 and R4 are as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 re
- -
-
Page/Page column 30-31
(2008/12/08)
-