- NOVEL INDAZOLE COMPOUND OR SALT THEREOF
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An indazole compound represented by the following Formula (I) or a salt thereof: wherein X, R1, R2, ring A, L1, L2, L3, and R5 are as defined in this specification.
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Paragraph 0244
(2021/09/02)
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- ANTICANCER COMBINATION THERAPY WITH N-(1-ACRYLOYL-AZETIDIN-3-YL)-2-((1H-INDAZOL-3-YL)AMINO)METHYL)-1H-IMIDAZOLE-5-CARBOXAMIDE INHIBITOR OF KRAS-G12C
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A method of treating cancer comprises administering: (a) a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof; and (b) a therapeutically effective amount of an additional anti-cancer agent, to a subject in need of such treatment, the compound of Formula (I) being: where X, R1, R2, ring A, L1, L2, L3, and R5 are as defined in this disclosure.
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Page/Page column 00299
(2021/10/30)
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- KRAS G12D PROTEIN INHIBITORS
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Compounds and pharmaceutically acceptable salts thereof inhibit the G12D mutant of KRAS protein and are expected to have utility as therapeutic agents, for example, for the treatment of cancer.
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Paragraph 00113
(2021/10/30)
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- Synthesis, Characterization, and Properties of Diazapyrenes via Bischler-Napieralski Reaction
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Via Bischler-Napieralski cyclization of amide precursors as the key step, a series of diazapyrene derivatives were designed and successfully synthesized. Their crystal structures, optoelectronic properties, and acid-responsive feature were investigated, which demonstrated that the doping of nitrogen atoms to the pyrene framework remarkably modulates their physical and chemical properties.
- Han, Yi,Hu, Zhenzhu,Liu, Meifang,Li, Mengwei,Wang, Tingting,Chen, Yulan
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p. 3953 - 3959
(2019/04/10)
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- Chiral Bis(oxazoline) Ligands as C2-Symmetric Chiral Auxiliaries for the Synthesis of Enantiomerically Pure Bis-Cyclometalated Rhodium(III) Complexes
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The synthesis of enantiomerically pure bis-cyclometalated rhodium(III) complexes using chiral bis(oxazoline) ligands as C2-symmetric chiral auxiliaries is described. Bis(oxazolines) are versatile chiral ligands for asymmetric catalysis but have
- Grell, Yvonne,Demirel, Nemrud,Harms, Klaus,Meggers, Eric
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supporting information
p. 3852 - 3859
(2019/11/13)
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- MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
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Paragraph 00882
(2018/09/12)
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- Synthesis of ladder-type graphene ribbon oligomers from pyrene units
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A series of ladder-type graphene ribbon oligomers have been synthesized through DDQ/acid-mediated oxidative cyclization. The oligomers present a bright blue light emission, and the new oligomers were clearly characterized by NMR and MALDI-TOF.
- Liu, Feng,Shen, Xiaoxiao,Wu, Yonggang,Bai, Libin,Zhao, Hongchi,Ba, Xinwu
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supporting information
p. 4157 - 4161
(2016/08/24)
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- Octahedral Chiral-at-Metal Iridium Catalysts: Versatile Chiral Lewis Acids for Asymmetric Conjugate Additions
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Octahedral iridium(III) complexes containing two bidentate cyclometalating 5-tert-butyl-2-phenylbenzoxazole (IrO) or 5-tert-butyl-2-phenylbenzothiazole (IrS) ligands in addition to two labile acetonitrile ligands are demonstrated to constitute a highly versatile class of asymmetric Lewis acid catalysts. These complexes feature the metal center as the exclusive source of chirality and serve as effective asymmetric catalysts (0.5-5.0 mol % catalyst loading) for a variety of reactions with α,β-unsaturated carbonyl compounds, namely Friedel-Crafts alkylations (94-99 % ee), Michael additions with CH-acidic compounds (81-97 % ee), and a variety of cycloadditions (92-99 % ee with high d.r.). Mechanistic investigations and crystal structures of an iridium-coordinated substrates and iridium-coordinated products are consistent with a mechanistic picture in which the α,β-unsaturated carbonyl compounds are activated by two-point binding (bidentate coordination) to the chiral Lewis acid.
- Shen, Xiaodong,Huo, Haohua,Wang, Chuanyong,Zhang, Bo,Harms, Klaus,Meggers, Eric
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supporting information
p. 9720 - 9726
(2015/06/30)
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- Expanding the palette of phenanthridinium cations
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5,6-Disubstituted phenanthridinium cations have a range of redox, fluorescence and biological properties. Some properties rely on phenanthridiniums intercalating into DNA, but the use of these cations as exomarkers for the reactive oxygen species (ROS), superoxide, and as inhibitors of acetylcholine esterase (AChE) do not require intercalation. A versatile modular synthesis of 5,6-disubstituted phenanthridiniums that introduces diversity by Suzuki-Miyaura coupling, imine formation and microwave-assisted cyclisation is presented. Computational modelling at the density functional theory (DFT) level reveals that the novel displacement of the aryl halide by an acyclic N-alkylimine proceeds by an SNAr mechanism rather than electrocyclisation. It is found that the displacement of halide is concerted and there is no stable Meisenheimer intermediate, provided the calculations consistently use a polarisable solvent model and a diffuse basis set.
- Cairns, Andrew G.,Senn, Hans Martin,Murphy, Michael P.,Hartley, Richard C.
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supporting information
p. 3742 - 3751
(2014/04/03)
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- Highly efficient dye-sensitized solar cells based on panchromatic ruthenium sensitizers with quinolinylbipyridine anchors
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Panchromatic RuII sensitizers TF-30-TF-33 bearing a new class of 6-quinolin-8-yl-2,2′-bipyridine anchor were synthesized and tested under AM1.5 G simulated solar irradiation. Their increased π conjugation relative to that of the traditional 2,2
- Chou, Chun-Cheng,Hu, Fa-Chun,Yeh, Hsiu-Hsuan,Wu, Hsin-Pei,Chi, Yun,Clifford, John N.,Palomares, Emilio,Liu, Shih-Hung,Chou, Pi-Tai,Lee, Gene-Hsiang
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supporting information
p. 178 - 183
(2014/01/17)
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- AMINOPYRIMIDINONES AS INTERLEUKIN RECEPTOR-ASSOCIATED KINASE INHIBITORS
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This invention relates to aminopyrimidinone compounds of Formula (I) that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment or prevention of inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease.
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Page/Page column 219
(2013/05/22)
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- An enantioselective fluorescence sensing assay for quantitative analysis of chiral carboxylic acids and amino acid derivatives
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A chiral 1,8-diacridylnaphthalene-derived fluorosensor exhibiting a C 2-symmetric cleft designed for stereoselective interactions with hydrogen bond donors has been used for the determination of both concentration and enantiomeric composition of carboxylic acids and amino acid derivatives. The Royal Society of Chemistry 2006.
- Wolf, Christian,Liu, Shuanglong,Reinhardt, Brian C.
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p. 4242 - 4244
(2007/10/03)
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- Oligoindenopyrenes: A new class of polycyclic aromatics
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(Graph Presented) A new class of polycyclic aromatic hydrocarbons - oligoindenopyrenes - has been synthesized featuring a Pd-catalyzed Suzuki - Heck coupling cascade. The oligoindenopyrenes are robust, highly colored substructures of C70 and have properties that might prove useful in new organic materials or devices. After excitation, the tetraindenopyrene derivative 3d undergoes efficient deactivation (99%) by internal conversion to the ground state. The small fluorescence quantum yield (0.004) is in accordance with the short (0.6 ns) fluorescence decay time.
- Wegner, Hermann A.,Reisch, Helge,Rauch, Karsten,Demeter, Attila,Zachariasse, Klaas A.,De Meijere, Armin,Scott, Lawrence T.
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p. 9080 - 9087
(2007/10/03)
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- HIV protease inhibitors
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The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.
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- Thiocyanation of alkylanilines. A simple and efficient synthesis of thiosulfonates containing 2-aminobenzothiazole
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Thiocyanation of anilines was used to introduce a thiol functionality and to construct the aminothiazole ring, all in a single step. A systematic study of thiocyanation of alkyl anilines was investigated to understand the regio-chemistry of the reaction. X-Ray crystal structures of two 2- aminobenzothiazoles were determined to assign the structures without any ambiguity. The intermediates obtained were further expanded to thiosulfonates containing 2-aminobenzothiazoles, which are extremely valuable intermediates to synthesize HIV protease inhibitors. (C) 2000 Elsevier Science Ltd.
- Vara Prasad,Panapoulous,Rubin, John R.
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p. 4065 - 4068
(2007/10/03)
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