14703-92-5Relevant articles and documents
DIPHENYL DERIVATIVES AND USES THEREOF
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Paragraph 1224, (2019/03/30)
The present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, and its therapeutic uses for activating a growth factor pathway, promoting wound healing, promoting tissue repair, and treating hearing loss, skeletal muscle loss, organ degeneration, tissue damage, neurodegeneration, and muscular atrophy. The disclosure further provides pharmaceutical compositions and combinations. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.
INDOLE DERIVATIVES AND USES THEREOF
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Paragraph 00653; 00654; 00655, (2019/02/13)
The present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, and its therapeutic uses for activating a growth factor pathway, promoting wound healing, promoting tissue repair, and treating hearing loss, skeleta
NEW COMPOUND
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Paragraph 0316; 0340, (2019/11/26)
PROBLEM TO BE SOLVED: To provide a new compound that does not have structural similarity to ceramide and has excellent CERT inhibitory activity. SOLUTION: The present invention provides a new compound of structural formula (I). A bond group -X- is cis-cyclopropyl-, R1, R2, R3, R4, and R5 independently represent a hydrogen atom, a halogen atom, a linear or branched C1-C8 alkyl group that may have a halogen atom, or OR6. SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2020,JPOandINPIT
INHIBITING ATAXIA TELANGIECTASIA AND RAD3-RELATED PROTEIN (ATR)
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Paragraph 0027, (2017/08/08)
Novel compounds inhibiting ATR protein kinase include compounds of formula (I) disclosed herein, as well as liposome formulations comprising ATR protein kinase inhibitor compounds. The compositions are useful for the treatment of cancer.
TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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Page/Page column 62; 63, (2016/05/02)
The present invention is directed to substituted indole compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, adisease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-(2-(4′-(3- methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916)
Semple, Graeme,Santora, Vincent J.,Smith, Jeffrey M.,Covel, Jonathan A.,Hayashi, Rena,Gallardo, Charlemagne,Ibarra, Jason B.,Schultz, Jeffrey A.,Park, Douglas M.,Estrada, Scott A.,Hofilena, Brian J.,Smith, Brian M.,Ren, Albert,Suarez, Marissa,Frazer, John,Edwards, Jeffrey E.,Hart, Ryan,Hauser, Erin K.,Lorea, Jodie,Grottick, Andrew J.
supporting information; experimental part, p. 71 - 75 (2012/02/16)
The design of a new clinical candidate histamine-H3 receptor antagonist for the potential treatment of excessive daytime sleepiness (EDS) is described. Phenethyl-R-2-methylpyrrolidine containing biphenylsulfonamide compounds were modified by re
Design, Synthesis, and Evaluation of 2-(arylsulfonyl)oxiranes as Cell-permeable Covalent Inhibitors of Protein Tyrosine Phosphatases
Dana, Dibyendu,Das, Tirtha K.,Kumar, Ish,Davalos, Anibal R.,Mark, Kevin J.,Ramai, Daryl,Chang, Emmanuel J.,Talele, Tanaji T.,Kumar, Sanjai
, p. 489 - 499 (2012/11/06)
A structure-based design approach has been applied to develop 2-(arylsulfonyl)oxiranes as potential covalent inhibitors of protein tyrosine phosphatases. A detailed kinetic analysis of inactivation by these covalent inhibitors reveals that this class of compounds inhibits a panel of protein tyrosine phosphatases in a time- and dose-dependent manner, consistent with the covalent modification of the enzyme active site. An inactivation experiment in the presence of sodium arsenate, a known competitive inhibitor of protein tyrosine phosphatase, indicated that these inhibitors were active site bound. This finding is consistent with the mass spectrometric analysis of the covalently modified protein tyrosine phosphatase enzyme. Additional experiments indicated that these compounds remained inert toward other classes of arylphosphate-hydrolyzing enzymes, and alkaline and acid phosphatases. Cell-based experiments with human A549 lung cancer cell lines indicated that 2-(phenylsulfonyl)oxirane (1) caused an increase in intracellular pTyr levels in a dose-dependent manner thereby suggesting its cell-permeable nature. Taken together, the newly identified 2-(arylsulfonyl)oxiranyl moiety could serve as a novel chemotype for the development of activity-based probes and therapeutic agents against protein tyrosine phosphatase superfamily of enzymes.
One-pot catalyst-free synthesis of β-and γ-hydroxy sulfides using diaryliodonium salts and microwave irradiation
Vaddula, Buchi Reddy,Varma, Rajender S.,Leazer, John
supporting information, p. 6852 - 6855 (2013/02/22)
A simple and rapid one-pot protocol is described for the preparation of α- and β-hydroxy sulfides. The direct solvent-free microwave irradiation of diaryliodonium salts, potassium thiocyanate, and ethylene glycol/β-propylene glycol without any catalyst or base affords the final compounds in good yields (65-95 %) in around 10-25 min. Copyright
A new approach to the synthesis of 4-hydroxyethylsulfonylstyrene
Grosjean, Christophe,Henderson, Andrew P.,Herault, Damien,Ilyashenko, Gennadiy,Knowles, Jonathan P.,Whiting, Andrew,Wright, Allen R.
experimental part, p. 434 - 441 (2010/04/22)
A new, more environmentally benign route to hydroxyethylsulfonylstyrene has been developed, starting from 4-bromobenzenethiol, involving a solventless thioether formation, water-based perborate oxidation, and Suzuki-Miyaura cross coupling with a vinylborate reagent.
Facile preparation of aryl sulfides catalyzed by PEG400 and nickel without solvent
Cao, Yu-Qing,Zhang, Zhan,Guo, Yan-Xin,Wu, Guo-Qiang
, p. 1325 - 1332 (2008/09/19)
A variety of aryl sulfides were synthesized by aryl bromides with thiols, with PEG400 and nickel as catalysts under basic conditions in the absence of solvents. This article reported an easy and convenient method for formation of aryl-sulfur bonds. Copyright Taylor & Francis Group, LLC.