- ALPHA, BETA-UNSATURATED AMIDE COMPOUND
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An object of the present invention is to provide an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like. The α,β-unsaturated amide compound represented by the following formula (I) or a pharmaceutically acceptable salt or the like thereof has anticancer activity and the like: [wherein, "A" represents optionally substituted heterocyclic diyl, R1 represents hydrogen atom or optionally substituted lower alkyl, R2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents -O-, -S-, -SO2-, -NRX1- (wherein, RX1 represents hydrogen atom or lower alkyl), -CHRX2- (wherein, RX2 represents hydrogen atom or hydroxy), -CH=CH-, -CO- or -NH-CO-, and n1 and n2 are the same or different, and each represents 0 or 1].
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Paragraph 1073
(2020/12/10)
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- BICYCLIC DERIVATIVES
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The present invention provides compounds of formula (I): (I) which are useful in the control of endoparasites, for example heartworms, in warm-blooded animals.
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Page/Page column 31-32
(2020/07/14)
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- Compound serving as IRAK inhibitor
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The present invention relates to a compound suitable for the treatment of cancer and inflammatory diseases associated with interleukin-1 receptor associated kinase (IRAK), particularly relates to a compound serving as an IRAK4 inhibitor and a preparation
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Paragraph 0181-0184
(2020/09/01)
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- a, ? UNSATURATED AMIDE COMPOUND
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The present invention provides an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like represented by the following formula (I): [wherein, "A" represents optionally substituted heterocyclic diyl, R1 represents hydrogen atom or optionally substituted lower alkyl, R2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents -O-, -S-, -SO2-, -NRX1- (wherein, RX1 represents hydrogen atom or lower alkyl), -CHRX2- (wherein, RX2 represents hydrogen atom or hydroxy), -CH=CH-, -CO- or -NH-CO-, and n1 and n2 are the same or different, and each represents 0 or 1].
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Paragraph 0885
(2018/11/27)
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- Synthesis, molecular docking study, and evaluation of the antiproliferative action of a new group of propargylthio- and propargylselenoquinolines
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This study describes the synthesis of a new group of halogenopropargylthio- , dipropargylthio-, and halogenopropargylseleno-quinoline derivatives. The ability of all of the synthesized compounds to inhibit the proliferation of the T-47D, MCF-7, MDA-MB-231, and SNB-19 cell lines was determined with the WST-1 assay. The normal fibroblast cell line (HFF-1) was used as a control. The cytotoxic properties of these new, modified propargylquinoline derivatives were comparable to those of cisplatin. The most active compounds, 4,7-dipropargylthiquinoline (8b) and 7-chloro-4-propargylselenoquinoline (5b), were docked into the binding site of human CYP1A1 and CYP1B1. Our data indicate that these derivatives may present promising chemotherapeutic agents, possibly targeting CYP1s pathway.
- Marciniec, Krzysztof,Latocha, Ma?gorzata,Boryczka, Stanis?aw,Kurczab, Rafa?
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p. 3468 - 3477
(2014/06/24)
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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 0322
(2013/11/19)
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