- ATF6 MODULATORS AND USES THEREOF
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Compounds (I) as modulators of Activating Transcription Factor 6 (ATF6) are provided. The compounds may find use as therapeutic agents for the treatment of diseases or disorders mediated by ATF6 and may find particular use in the treatment of viral infections, neurodegenerative diseases, vascular diseases, or cancer.
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Paragraph 201
(2021/04/17)
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- N,O- vs N,C-Chelation in Half-Sandwich Iridium Complexes: A Dramatic Effect on Enantioselectivity in Asymmetric Transfer Hydrogenation of Ketones
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Cyclometalation of [Cp?IrCl2]2 with methyl (S)-2-phenyl-4,5-dihydrooxazole-4-carboxylate in the presence of NaOAc selectively led to a N,C- or N,O-chelated Cp?Ir(III) complex, depending on whether or not water was present in the reaction. While derived from the same precursor, these two complexes behaved in a dramatically different manner in asymmetric transfer hydrogenation (ATH) of ketones by formic acid, with the N,O-chelated complex being much more selective and active. The sense of asymmetric induction is also different, with the N,O-complex affording S while the N,C-analogue R alcohols. Further study revealed that the nature of the base additive considerably impacts the enantioselectivity and the effective HCOOH/amine ratios. These observations show the importance of ligand coordination mode and using the right base for ATH reactions.
- Zhou, Gang,Aboo, Ahmed H.,Robertson, Craig M.,Liu, Ruixia,Li, Zhenhua,Luzyanin, Konstantin,Berry, Neil G.,Chen, Weiping,Xiao, Jianliang
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p. 8020 - 8026
(2018/09/06)
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- VINYL COMPOUNDS AS FGFR AND VEGFR INHIBITORS
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FGFR and VEGFR inhibitors are provided, and compounds represented by formula (1) or formula (II) as FGFR and VEGFR inhibitors, pharmaceutically acceptable salts or tautomers thereof are specifically disclosed.
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Paragraph 0576; 0577
(2018/06/23)
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- CYCLIC COMPOUND
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The present invention provides compounds having a Toll-like receptor 4 (TLR4) signaling inhibitory action useful as preventive and therapeutic drugs of autoimmune disease and/or inflammatory disease or diseases such as chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver injury, ischemia-reperfusion injury (IRI) and the like. The present invention relates to a compound represented by formula (I) and a salt thereof: (wherein, each symbol is explained in greater detail in the specification).
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Paragraph 0349
(2018/04/13)
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- Towards a Large-Scale Asymmetric Reduction Process with Isolated Enzymes: Expression of an (S)-Alcohol Dehydrogenase in E. coli and Studies on the Synthetic Potential of this Biocatalyst
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An NAD-dependent and widely applicable (S)-alcohol dehydrogenase is isolated and described as a novel enzyme. It is expressed in an E. coli strain with a high production potential. The application of this enzyme in asymmetric biocatalytic reduction is presented as well. This enzyme shows a broad substrate range comprising aliphatic and aromatic ketones as well as β-keto esters. The synthetic application of this new (S)-alcohol dehydrogenase led to optically active alcohols in high conversion rates accompanied by enantioselectivities of up to > 99% ee. Compared to the wild-type enzyme significant advantages are observed besides the improved availability, such as a high enantioselectivity independent of the reaction time. Furthermore, the alcohol dehydrogenase was cloned and successfully overexpressed in E. coli resulting in a biocatalyst with a potential to be available on technical scale in the future. The development of a large-scale available and widely applicable (S)-alcohol dehydrogenase is one prerequisite to use isolated enzymes for asymmetric reduction processes as a valuable tool.
- Hummel, Werner,Abokitse, Kofi,Drauz, Karlheinz,Rollmann, Claudia,Gr?ger, Harald
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p. 153 - 159
(2007/10/03)
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- Herbicidal triazolinones
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A herbicidal compound which is a Q-substituted 1-aryl-4,5-dihydro-1,2,4-triazol-5(1H)-one in which the Q-substituent is on the ring-carbon atom at the 5-position of the aryl group and in which: Q is (a) --CH(R1)ZR in which Z is O or S(O)n and n is zero, one or two; or (b) --CH(R1)N(R4)(R5); or (c) --C(R9)=NR6 ; or STR1
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- Herbicidal aryl tetrahydrophthalimides
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A herbicidal compound of the formula STR1 where X is F, Cl or Br, Y is Cl, Br, CHF2 O or CF3, R is alkyl of 1 to 6 carbon atoms or lower halo alkyl and R' is H or lower alkyl. Related compounds, including those which have --SR or --NR2 R in place of --OR are also disclosed.
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