33142-21-1Relevant articles and documents
Thiazole derivative and synthesis method thereof
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Paragraph 0025; 0028-0029; 0044; 0047-0048; 0063; 0066-0067, (2020/11/22)
The invention belongs to the technical field of organic synthesis, particularly relates to a thiazole derivative and a synthetic method thereof, and particularly relates to a thiazole derivative (Z)-4-((2-(2-(2-(2,5-dimethoxyphenyl)-thiazole-5-yl)-ethylimino)(phenyl)methyl)-1,3-benzenediol and a synthetic method thereof. The synthesis method provided by the invention comprises the following steps:by taking 2,5-dimethoxybenzamide and ethyl 2-chloroacetate as raw materials, carrying out six reaction steps of carbonyl sulfide reaction, substitution, cyclization, substitution, chlorination, cyanidation, amidation, hydrolysis and substitution reaction to prepare the (Z)-4-((2-(2-(2-(2,5-dimethoxyphenyl)-thiazole-5-yl)-ethylimino)(phenyl)methyl)-1,3-benzenediol. According to the invention, an efficient synthesis method is provided for the synthesis of the thiazole derivative.
Benzo [d] [1, 3] oxathiol, benzo [d] [1, 3] benzo [d] [1, 3] oxathiol 3 - oxide or 3, 3 - dioxide compounds and G protein-coupled receptor 119 oxathiol action of number as method/use
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Paragraph 0768-0770, (2019/04/02)
There are provided compounds containing benzo[d][1,3]oxathiole, benzo[d][1,3]oxathiole 3-oxide, and benzo[d][1,3]oxathiole 3,3-dioxide, as well as uses/methods related thereto, including treatment of diseases and condition associated with GPR119 dysregulation, Type 2 diabetes mellitus, and related metabolic disorders.
COMPOUNDS CONTAINING POLYSUBSTITUTED BENZO[D][1,3]OXATHIOLE, BENZO[D][1,3]OXATHIOLE 3-OXIDE OR BENZO[D][1,3]OXATHIOLE 3,3-DIOXIDE AND METHODS/USES THEREOF AS AGONISTS OF G PROTEIN-COUPLED RECEPTOR 119
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Paragraph 0506-0507, (2019/07/04)
There are provided compounds having formula (I), in which: X1 and X2 are selected from certain combinations of O, S, SO and SO2; X3 is selected from CH, CF and N; X4 is selected from CH and N; X6, X6' and X6'' are selected from H, halogen, and certain alkyl, haloalkyl, alkoxy, hydroxyalkyl, and amide groups; X7 and X7' are selected from H, halogen, and certain alkyl, haloalkyl, alkoxy, hydroxyalkyl, aminoalkyl and amide groups, or both X7 and X7' together form a cycloalkyl or heterocycle; and A is selected from certain optionally substituted, alkoxy, piperazinyl and pyrrolidinyl groups. Also provided are compositions comprising these compounds, as well as uses/methods related thereto, including treatment of diseases and conditions associated with GPR119 dysregulation, Type 2 diabetes mellitus, and related metabolic disorders. (I)
CYCLIC SULFAMIDE COMPOUNDS AND METHODS OF USING SAME
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Page/Page column 278, (2018/09/21)
The present disclosure provides, in part, cyclic sulfamide compounds, and pharmaceutical compositions thereof, useful as modulators of Hepatitis B (HBV) core protein, and methods of treating Hepatitis B (HBV) infection.
FIVE-MEMBERED HETEROCYCLIC AMIDES WNT PATHWAY INHIBITOR
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Paragraph 0121-0123, (2018/10/19)
The present invention discloses a five-membered heterocyclic amide WNT pathway inhibitor, which belongs to a compound that regulates the activity of a Wnt signaling pathway, and provides a method for preparing such a compound, and the use of such a compound in preparing a medicament that antagonizes the Wnt signaling pathway. The five-membered heterocyclic amide WNT pathway inhibitor provided by the invention has a remarkable anti-tumor activity based on a target-based rational drug design of, and can be used for the development of a new generation of Wnt pathway inhibitors, and has a great clinical application value and considerable market potential.
Heteroatom-Interchanged Isomers of Lissoclinamide 5: Copper(II) Complexation, Halide Binding, and Biological Activity
Xie, Sida,Savchenko, Andrei I.,Kerscher, Marion,Grange, Rebecca L.,Krenske, Elizabeth H.,Harmer, Jeffrey R.,Bauer, Michelle J.,Broit, Natasa,Watters, Dianne J.,Boyle, Glen M.,Bernhardt, Paul V.,Parsons, Peter G.,Comba, Peter,Gahan, Lawrence R.,Williams, Craig M.
supporting information, p. 1465 - 1476 (2018/04/06)
Cyclic peptides, especially those produced by marine cyanobacteria symbionts, are considered to play an important ecological role in host defence. Chemists have long compared the cyclic peptide cavitand architecture with that of macrocyclic ligands, and proposed that they mediate metal-ion transport. The study presented herein investigated the metal chelation of non-natural heteroatom-interchanged (HI) isomers of lissoclinamide 5, by using MS, EPR, and DFT calculations. The latter identified three possible structures for the CuII complex with natural lissoclinamide 5, with the most likely determined to be that with the metal ion bound through the nitrogen donors of the thiazoles and one deprotonated amide. For HI-lissoclinamide 5 the calculations suggest that the CuII ion is bound in a bidentate manner by the oxazoline nitrogen atom and one deprotonated amide nitrogen atom, with the S donor of the thiazole not involved in coordination. Along with evidence of copper binding these systems also bound halide ions. Evaluation of the anti-cancer properties demonstrated that the biological activity of HI-lissoclinamide 5 against T24 bladder cells was eleven-fold lower as compared to natural lissoclinamide 5. Addition of a CuII salt had no effect on the activity of lissoclinamide 5. Overall, this comprehensive study of the HI concept has demonstrated that small changes propagate dramatic effects in complexation, halide binding, and biological activity.
ANTIBIOTIC COMPOUNDS
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Page/Page column 219; 220, (2018/03/25)
The present invention relates to antibiotic compounds of formula (I), to compositions containing these compounds and to methods of treating bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Gram-positive and/or Gram-negative bacteria, and in particular in the treatment of infection with, and diseases caused by, Neisseria gonorrhoeae.
HEPATITIS B CORE PROTEIN MODULATORS
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Page/Page column 108; 109, (2018/04/13)
The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound of formula:
PROCESS FOR MAKING HEPATITIS B CORE PROTEIN MODULATORS
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Page/Page column 19, (2018/10/19)
The present disclosure provides, in part, a process for preparing compounds (I) having allosteric effector properties against Hepatitis B virus Cp.
CK2 INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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Paragraph 0454; 0457, (2018/02/01)
The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. For Formula (I) compounds R1, R2, R3, Ar and Z are as defined in the specification. The inventive Formula (I) compounds are inhibitors of CK2 and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer, inflammation and immunological disorders.