- HETEROCYCLIC COMPOUNDS AS MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)
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The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
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Page/Page column 149-150
(2021/06/22)
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- FUNCTIONALIZED HETEROCYCLIC COMPOUNDS AS MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)
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The present invention relates to compound-linker constructs and antibody-drug-conjugates of compounds of formula (I) that are useful as modulators of STING (Stimulator of Interferon Genes).
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Page/Page column 185; 186
(2021/06/22)
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- QUINOLINE DERIVATIVES AS SMO INHIBITORS
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Disclosed are quinoline derivatives as hedgehog pathway inhibitors, especially as SMO inhibitors. Compounds of the present invention can be used in treating diseases relating to hedgehog pathway including cancer.
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Paragraph 0189; 0191
(2017/02/28)
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- A one-pot, two-step synthesis of 3-deazacanthin-4-ones via sequential Pd-catalyzed Suzuki-Miyaura and Cu-catalyzed Buchwald-Hartwig reactions
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3-Deazacanthin-4-one and nine analogues, including the 8-aza analogue, were prepared rapidly and in high yields from 8-iodoquinolones and 2-chloro(het)arylboronic acids. The strategy involves construction of the central B ring via concomitant Pd-catalyzed
- Broumidis, Emmanouil,Koutentis, Panayiotis A.
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supporting information
p. 2661 - 2664
(2017/06/14)
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- Photoreductive Removal of O-Benzyl Groups from Oxyarene N-Heterocycles Assisted by O-Pyridine-pyridone Tautomerism
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Facile photoreductive protocols have been developed to remove benzyl O-protective groups from oxyarene N-heterocycles at positions capable for 2-/4-O-pyridine-2-/4-pyridone tautomerism. Blue light irradiation, a [Ru] or [Ir] photocatalyst, and ascorbic acid in a water-acetonitrile solution debenzylates a variety of aryl N-heterocycles cleanly and selectively. Ascorbic acid has two functions in the reaction. On the one hand, it protonates the N-heterocycles that reduces their reduction potentials notably and on the other hand it acts as a sacrificial reductant. Reduction potentials and free energy barriers calculated at the CPCM-B3LYP/6-31+G? level can predict the reactivities of the studied substrates.
- Todorov, Aleksandar R.,Wirtanen, Tom,Helaja, Juho
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p. 13756 - 13767
(2017/12/26)
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- NOVEL BICYCLIC COMPOUND OR SALT THEREOF
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Provided is a novel bicyclic compound which has an HSP90 inhibitory effect and a carcinostatic effect. Also provided is a pharmaceutical agent which is based on the HSP90 inhibitory effect and is useful in the prevention and/or treatment of a disease involving HSP90, particularly, cancer. The present invention provides a compound represented by the following general formula (I) or a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are the same or different and each represent C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are the same or different and each represent CH or N;R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O;R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.;R3 represents a hydrogen atom, —CO—R5 etc.;R4 represents a hydrogen atom, —CO—R6, —N(R7)(R8) etc.;R5 represents a hydroxyl group, an amino group etc.;R6 represents a hydroxyl group etc.;R7 and R8 are the same or different and each represent a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; and R9 represents an optionally substituted cycloalkyl group having 3 to 7 carbon atoms etc.
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Paragraph 0308
(2013/11/19)
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- Direct C-3-alkenylation of quinolones via palladium-catalyzed C-H functionalization
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An unprecedented C-3-alkenylation of quinolones was reported through palladium-catalyzed C-H functionalization with 1% catalyst loading. This method provides an efficient route to a variety of new quinolone derivatives.
- Li, Mingzong,Li, Liangxi,Ge, Haibo
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supporting information; experimental part
p. 2445 - 2449
(2010/12/25)
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- Synthesis of novel halogenated 4(1H)-quinolones by thermolysis of arylaminomethylene-1,3-dioxane-4,6-diones
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A variety of novel 4(1H)-quinolone derivatives were prepared by thermolysis of aminomethylene Meldrum's acid derivatives. Georg Thieme Verlag Stuttgart.
- Rotzoll, Sven,Reinke, Helmut,Fischer, Christine,Langer, Peter
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experimental part
p. 69 - 78
(2009/06/17)
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