62380-38-5Relevant academic research and scientific papers
ISOINDOLINONE COMPOUNDS
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Page/Page column 193-194, (2021/04/17)
Disclosed herein is a compound or pharmaceutically acceptable salts or stereoisomers thereof of of formula I wherein X1 is linear or branched C1-6 alkyl, C3-6 cycloalkyl, -C1-6 alkyl C3-6 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, C1-6 alkyl C6-10 aryl, C1-6 alkyl 5-10 membered heteroaryl, wherein X1 is unsubstituted or substituted with one or more of halogen, linear or branched C1-6 alkyl, linear or branched C1-6 heteroalkyl, CF3, CHF2, -O-CHF2, -O-(CH2)2-OMe, OCF3, C1-6 alkylamino, -CN, -N(H)C(O)-C1- 6alkyl, -OC(O)-C1-6alkyl, -OC(O)-C1-4alkylamino, -C(O)O-C1-6alkyl, -COOH, - CHO, -C1-6alkylC(O)OH, -C1-6alkylC(O)O-C1-6alkyl, NH2, C1-6 alkoxy or C1-6 alkylhydroxy; X2 is hydrogen, C6-10 aryl, 5-10 membered heteroaryl, -O-(5-10 membered heteroaryl), 4-8 membered heterocycloalkyl, C1-4 alkyl 4-8 membered heterocycloalkyl, -O-(4-8 membered heterocycloalkyl), -O-C1-4 alkyl-(4-8 membered heterocycloalkyl), -OC(O)-C1-4alkyl-4-8 membered heterocycloalkyl or C6 aryloxy, wherein X2 is unsubstituted or substituted with one or more of linear or branched C1-6 alkyl, NH2, NMe2 or 5-6 membered heterocycloalkyl; n is 0, 1 or 2.
KINASE INHIBITOR
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Paragraph 0214; 0215, (2021/04/16)
The present invention aims to provide a novel kinase inhibitor and the like, and a therapeutic agent for a disease, a drug discovery screening method and the like utilizing such inhibitor and the like. The compound represented by the following formula (I) and a salt thereof can inhibit plural kinases including LATS (particularly LATS2) which is the major kinase in the Hippo signal transduction pathway. In addition, diseases or tissue damage associated with failure of cellular proliferation can be treated. Therefore, the present invention is beneficial, for example, in the research field of cell functions and diseases, in which the Hippo signal transduction pathway is involved, and the like. Furthermore, it is beneficial in the medical field for the treatment of such diseases and the like. wherein each symbol is as defined in the DESCRIPTION.
ADDITIVE COMPOSITION FOR CULTURE MEDIUM, ADDITIVE COMPOUND FOR CULTURE MEDIUM, AND METHOD FOR CULTURE OF CELLS OR TISSUE USING SAME
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Paragraph 0202-0203, (2020/06/15)
The present invention provides a medium additive composition containing a compound represented by the following formula (I), or a salt thereof: {wherein each symbol is as defined in the DESCRIPTION.}
Coumarin-based fluorescent sensors for zinc(II) and hypochlorite
Aulsebrook, Margaret L.,Grace, Michael R.,Tuck, Kellie L.,Graham, Bim
, p. 798 - 806 (2015/12/24)
Two new fluorescent chemosensors have been designed and synthesised through functionalisation of a common 7-aminocoumarin precursor. One sensor features a di(2-picoyl)amine metal ion-binding moiety that allows for selective detection of Zn2+ ions over other common cations in aqueous solution, with the sensor exhibiting a 5.4-fold increase in fluorescence upon Zn2+ binding (limit of detection = 26 nM). The second sensor incorporates an aminophenyl group designed to react with highly reactive oxygen species (hROS). This sensor reacts with ClO- in preference to other ROS, exhibiting a 27-fold increase in fluorescence upon the addition of 150 equivalents of ClO- (limit of detection = 2 M).
Preparation of substituted semicarbazides from corresponding amines and hydrazines via phenyl carbamates
Hron, Rebecca,Jursic, Branko S.
supporting information, p. 1540 - 1543 (2014/03/21)
A simple synthetic procedure for the conversion of amines and hydrazines into substituted semicarbazides was developed. The initial condensation between the desired amine and phenyl chloroformate into phenyl carbamate is followed by the addition of hydrazine under basic conditions. The reaction is tolerable to a variety of functional groups, with mild conditions and high percent yields.
Synthesis, characterization and biological screening of various O-phenyl-N-aryl carbamates
Abbasi, Muhammad Athar,Sonia, Ayesha,Aziz-Ur-Rehman,Khan, Khalid Mohammed,Ashraf, Muhammad,Afzal, Iftikhar,Ambreen, Nida,Shahid, Muhammd,Abbas, Mazhar
, p. 385 - 390 (2013/07/27)
A series of O-phenyl-N-aryl carbamates (3a-i) were synthesized by the reaction of phenyl chloroformate (1) with different aromatic amines (2a-i). The compounds were characterized by IR and 1H-NMR and screened against acetylcholinesterase, butrylcholinesterase and lipoxygenase enzymes. The results revealed that O-phenyl-N-phenyl carbamate (3a) and O-phenyl-N-(3-hydroxyphenyl) carbamate (3e) were active against acetylcholinesterase while O-phenyl-N-benzyl carbamate (3b), O-phenyl-N-(4-hydroxyphenyl) carbamate (3f) and O-phenyl-N-(3-methoxyphenyl) carbamate (3h) exhibited potential inhibitory activity against 5-lipoxygenase. All these carbamates were also assayed for their antimicrobial and hemolytic activities. O-phenyl-N-(2-hydroxyphenyl) carbamate (3d), O-phenyl-N-(4-hydroxyphenyl) carbamate (3f) and O-phenyl-N-(3-methoxyphenyl) carbamate (3h) showed good antimicrobial and hemolytic activity among all the carbamates.
On-bead fluorescence assay for serine/threonine kinases
Akita, Shoji,Umezawa, Naoki,Higuchi, Tsunehiko
, p. 5565 - 5568 (2007/10/03)
(Chemical Equation Presented) A novel fluorescence-based assay for serine/threonine kinases is described. Base-mediated β-elimination of the phosphate moiety and the Michael addition of a thiol-containing fluorescent molecule allows convenient and efficie
HYDROXYLATION DIRECTE D'ESTERS DE PHENYLE ET D'ANILIDES PAR LE PEROXYDE D'HYDROGENE EN MILIEU SUPERACIDE
Berrier, Christian,Jacquesy, Jean-Claude,Jouannetaud, Marie-Paule,Morellet, Guy
, p. 158 - 164 (2007/10/02)
In SbF5-HF, hydrogen peroxide reacts on the aromatic ring of esters 1a-5a and anilides 11a-15a to give monohydroxylated derivatives in good yields.With compounds 2a, 4a and 5a, meta or para isomers are by far the major products, whereas with formate 1a and benzoate 3a, the proportion of the ortho isomer is more important.With anilides, the reaction is less selective, the three isomers being obtained in comparable amounts.Thus, the relative proportions of ortho, meta and para-hydroxylated derivatives obtained using 70 percent H2O2 with acetate 2a and acetanilide 12a are 6/51/43 and 36.5/30/33.5, respectively.The important proportion of meta hydroxylation is the result of the reaction of protonated hydrogen peroxide H3O2+ on the protonated substrate.
