99471-67-7Relevant articles and documents
MITOCHONDRIAL COMPLEX I INHIBITORS AND METHODS OF USE
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Paragraph 0123-0125, (2021/03/19)
Disclosed herein are methods of using mitochondrial complex I inhibitors in the treatment of a disease or condition that would benefit from the inhibition of mitochondrial respiration. Also described herein are methods of treating a disease or condition s
PYRROLE DERIVATIVES AS ACC INHIBITORS
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Page/Page column 43; 44, (2020/12/29)
Novel pyrrole derivatives of Formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Acetyl- CoA carboxylase (ACC).
Rapid and efficient copper-catalyzed finkelstein reaction of (hetero)aromatics under continuous-flow conditions
Chen, Mao,Ichikawa, Saki,Buchwald, Stephen L.
supporting information, p. 263 - 266 (2015/02/05)
A general, rapid, and efficient method for the copper-catalyzed Finkelstein reaction of (hetero)aromatics has been developed using continuous flow to generate a variety of aryl iodides. The described method can tolerate a broad spectrum of functional groups, including N-H and O-H groups. Additionally, in lieu of isolation, the aryl iodide solutions were used in two distinct multistep continuous-flow processes (amidation and Mg-I exchange/nucleophilic addition) to demonstrate the flexibility of this method.
High birefringence bistolane liquid crystals: Synthesis and properties
W?g?owska, Dorota,Kula, Przemys?aw,Herman, Jakub
, p. 403 - 408 (2016/01/09)
Twenty liquid crystals both symmetrical and non-symmetrical bistolanes with terminal alkyl, alkoxy and alkylsulfanyl chain and lateral methyl or ethyl group have been synthesized via Sonogashira cross-coupling and their mesomorphic properties have been studied. Most compounds exhibit an enantiotropic nematic phase in a broad temperature range (>40 °C). Optical properties of selected compounds have been investigated. They exhibit a high value of birefringence (>0.4).
Modular synthesis of triazole-containing triaryl α-helix mimetics
Ehlers, Ina,Maity, Prantik,Aube, Jeffrey,Koenig, Burkhard
scheme or table, p. 2474 - 2490 (2011/06/10)
We describe novel scaffold designs for nonpeptidic α-helix mimetics. The tricyclic scaffolds contain triazoles and reproduce amino acid side chains i, i+3, and i+7. The three different scaffolds are synthetically readily accessible, allow the introduction
Preparative fluorous mixture synthesis of diazonium-functionalized oligo(phenylene vinylene)s
Jian, Huahua,Tour, James M.
, p. 3396 - 3424 (2007/10/03)
(Chemical Equation Presented) A series of building blocks for the synthesis of oligo(phenylene vinylene)s (OPVs) and hybrid oligomers were prepared, and alternating Heck coupling and Horner-Wadswoth-Emmons (HWE) reactions were used to couple the building blocks. Model studies were carried out to optimize the reaction strategies. The products were made to bear aryl diazonium functionalities that allow them to be used as surface grafting moieties in hybrid silicon/molecule assemblies. A library of OPV and hybrid oligomer tetramers was synthesized using fluorous mixture synthesis (FMS). The fluorous tags, which are secondary amines bearing different numbers of fluorine atoms, were synthesized and used as phase tags in mixture synthesis. The tags and substrates were anchored together by triazene linkages. The mixture synthesis was monitored by analytical HPLC on a fluorous column, and isolation of final OPV and hybrid oligomer tetramers was achieved by preparative HPLC. At the end of the FMS, after demixing, the tagged products were detagged by cleaving the triazene linkage and generating a series of aryl diazonium compounds. The fluorous tags could be recovered and reused. The NMR spectra of the 1-aryl-3,3-dialkyltriazenes are discussed.
QUINOLINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
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Page 93-94, (2008/06/13)
There are provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R19, R20 and R34 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
2(1H)-Quinolinones with cardiac stimulant activity. 1. Synthesis and biological activities of (six-membered heteroaryl)-substituted derivatives
Alabaster,Bell,Campbell,Ellis,Henderson,Roberts,Ruddock,Samuels,Stefaniak
, p. 2048 - 2056 (2007/10/02)
A series of (six-membered heteroaryl)-substituted 2(1H)-quinolinones was synthesized, and structure-activity relationships for cardiac stimulant activity were determined. Most compounds were prepared by acidic hydrolyisis of a heteroaryl-2-methoxyquinoline obtained by palladium-catalyzed cross-coupling methodology. Direct reaction of a pyridinylzinc reagent with a 6-haloquinolinone also proved successful. In anesthetized dogs, 6-pyridin-3-yl-2(1H)-quinolinone (3; 50 μg/kg) displayed greater inotropic activity (percentage increase in dP/dt max) than positional isomers, and potency was maintained with either mono- or di- alkylpyridinyl substituents. Introduction of a 4- or 7- methyl group into 3 reduced inotropic activity, whereas the 8-isomer proved to be the most potent member of the series. Compound 26 and the 2,6-dimethylpyridinyl analogue (27 were approximately 6 and 3 times more potent than milrinone. Several quinolinones displayed positive inotropic activity (decrease in QA interval) in conscious dogs after oral administration (1 mg/kg), and 26, 27 were again the most potent members of the series. Compound 27 (0.25, 0.5, 1.0 mg/kg po) demonstrated dose-related cardiac stimulant activity, which was maintained for at least 4 h. No changes in heart rate were observed. Compounds 3, 4, 26, and 27 also selectively stimulated the force of contraction, rather than heart rate, in the dog heart-lung preparation. For a 50% increase in dP/dt max with 27, heart rate changed by less than 10 beats/min. In norepinephrine contracted rabbit femoral artery and saphenous vein, 27 produced dose related (5 x 10-7 to 5 x 10-4 M) vasorelaxant activity. The combined cardiac stimulant and vasodilator properties displayed by 27, coupled with a lack of effect on heart rate, should be beneficial for the treatment of congestive heart failure.
Quinolone inotropic agents
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, (2008/06/13)
A heterocyclic-substituted 2-quinolone compound of the formula: STR1 or a pharmaceutically-acceptable salt thereof, wherein "Het" is an optionally substituted 5-or 6-membered monocyclid aromatic heterocyclic group attached by a carbon atom to the 5-, 6-, 7- or 8- position of the quinolone nucleus; R, which is attached to the 5-, 6-, 7- or 8- position, is hydrogen, C1 -C4 alkyl, C1 -C4 alkoxy, C1 -C4 alkylthio, C1 -C4 alkylsulphinyl, C1 -C4 alkylsulphonyl, halo, CF3, hydroxy, hydroxymethyl, or cyano; R1 is hydrogen, cyano (C1 -C4 alkoxy)carbonyl, C1 -C4 alkyl, nitro, halo, --NR3 R4 or --CONR3 R4 where each of R3 and R4 is hydrogen or C1 -C4 alkyl or R3 and R4 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocyclic group optionally containing a further heteroatom or group selected from O, S and N--R5 where R5 is hydrogen or C 1 -C4 alkyl; R2 is hydrogen, C1 -C4 alkyl, or 2-hydroxyethyl; Y is hydrogen or C1 -C4 alkyl; and the dotted line between the 3- and 4- positions represents an optional bond. The compounds are inotropic agents useful as cardiac stimulants in the treatment of congestive heart failure.
