250263-39-9Relevant academic research and scientific papers
Casein kinase 1 (CK1) inhibitor for plants (by machine translation)
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Paragraph 0053; 0104-0108, (2020/02/14)
[Problem] to provide various lead compounds PHA derivatives, and/or circadian rhythm control agent having stronger CK1 inhibitor activity. [Solution] a compound represented by formula I, or a salt thereof or a solvate thereof. (R1 The, H or C1 - 5 A straight-chain, branched or cyclic alkyl group, alkenyl group or alkynyl group, R2 The, H, halogen (F, Cl, Br or I), or a C1 - 4 The alkyl group, the ring A, 5 - 8 membered lactam ring showing; however, R1 And R2 Except H together. )[Drawing] no (by machine translation)
A diverse and versatile regiospecific synthesis of tetrasubstituted alkylsulfanylimidazoles as p38α mitogen-activated protein kinase inhibitors
Ansideri, Francesco,Andreev, Stanislav,Kuhn, Annette,Albrecht, Wolfgang,Laufer, Stefan A.,Koch, Pierre
, (2018/02/06)
An alternative strategy for the synthesis of 1-aryl- and 1-alkyl-2-methylsulfanyl-4-(4-fluorophenyl)-5-(pyridin-4-yl)imidazoles as potential p38α mitogen-activated protein kinase inhibitors is reported. The regioselective N-substitution of the imidazole ring was achieved by treatment of α-aminoketones with different aryl or alkyl isothiocyanates. In contrast to previously published synthesis routes starting from 2-amino-4-methylpyridine, the presented route is characterized by a higher flexibility and a lower number of steps. This strategy was also applied to access 1-alkyl-2-methylsulfanyl-5-(4-fluorophenyl)-4-(pyridin-4-yl)imidazoles in six steps starting from 2-chloro-4-methylpyridine.
Mo(CO)6 as a Solid CO Source in the Synthesis of Aryl/Heteroaryl Weinreb Amides under Microwave-Enhanced Condition
Ningegowda, Raghu,Bhaskaran, Savitha,Sajith, Ayyiliath M.,Aswathanarayanappa, Chandrashekar,Padusha, M. Syed Ali,Priya, Babu Shubha
, p. 44 - 51 (2017/01/21)
The facile transformation of aryl/heteroaryl nonaflates into corresponding amides via Pd-catalyzed aminocarbonylation using Mo(CO)6 as a solid CO source under microwave-enhanced condition is reported. The method was found to be tolerant with respect to a
18F LABELLED THIAZOLYLHYDRAZONE DERIVATIVES
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Page/Page column 10-11, (2016/07/05)
The present invention relates to compounds of Formula (I) wherein R1 and R2 are independently selected from 19F and 18F having selective binding for MAO-B as compared with MAO-A. The invention also provides radi
SUBSTITUTED 2-AMINOPYRIDINE PROTEIN KINASE INHIBITOR
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Paragraph 0105, (2015/12/19)
Disclosed are a 2-aminopyridine derivative having protein kinase inhibition activity, a preparation method and a pharmaceutical composition thereof Also disclosed are uses of the compounds and the pharmaceutical compositions thereof in the preparation of drugs for treating and/or preventing protein kinase-related diseases.
HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt
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Paragraph 0274; 0275; 0444; 0445, (2014/05/07)
The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
8-AZABICYCLO[3.2.1]OCTANE-8-CARBOXAMIDE DERIVATIVE
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Page/Page column 50, (2012/09/11)
Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof (In the formula, A represents a group that is represented by formula (A-1); R1a and R1b may be the same or different and each independently represents a C1-6 alkyl group which may be substituted by one to three halogen atoms; m and n each independently represents an integer of 0-5; X1 represents a hydroxyl group or an aminocarbonyl group; Z1 represents a single bond or the like; and R2 represents an optionally substituted C1-6 alkyl group, an optionally substituted C6-10 aryl group or the like.)
Identification of pyrimidine derivatives as hSMG-1 inhibitors
Gopalsamy, Ariamala,Shi, Mengxiao,Bennett, Eric M.,Bard, Joel,Zhang, Wei-Guo,Yu, Ker
, p. 6636 - 6641,6 (2012/12/12)
hSMG-1 kinase plays a dual role in a highly conserved RNA surveillance pathway termed nonsense-mediated RNA decay (NMD) and in cellular genotoxic stress response. Since deregulation of cellular responses to stress contributes to tumor growth and resistance to chemotherapy, hSMG-1 is a potential target for cancer treatment. From our screening efforts, we have identified pyrimidine derivatives as hSMG-1 kinase inhibitors. We report structure-based optimization of this pan-kinase scaffold to improve its biochemical profile and overall kinome selectivity, including mTOR and CDK, to generate the first reported selective hSMG-1 tool compound.
1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS
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, (2010/10/19)
The present invention relates to compounds of formula I wherein R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
CYCLIC COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
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Page 17, (2010/02/08)
The invention provides a novel class of cyclic compounds, pharmaceutical compositions comprising such cyclic compounds and methods of using such compounds to treat or prevent diseases and disorders associated with cyclin-dependent kinases (CDKs) activity,
